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Listed below are over 400+ promising drugs currently in pre-clinical or clinical trials for advanced or metastatic breast cancer. The majority of the drugs listed are targeted therapies which target ONLY cancer cells. In order to receive targeted therapy, a patient needs to provide a tumor sample for genomic testing. If the tumor carries certain mutations (e.g. HER2+ or Androgen Receptor+), these targeted drugs can exploit those mutations and stop the spread of cancer.

Unlike targeted therapies, chemotherapy and some immunotherapies are less precise and attack both normal cells AND cancer cells. When a drug attacks normal cells, it can lead to potentially worse side effects. However, a combination of therapies may result in a better outcome for the patient. Any patient can receive non-targeted drugs (marked with an asterisk (*) in the table below) regardless of the mutations carried by their tumor.

*When you see a word or acronym with a dotted line underneath, hover over the word to display the full name*

Table of Promising Drugs for Breast Cancer
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Generic
Name
Code
Name
Brand
Name
Specific
Target
Mechanism of Action & Additional NotesNews Articles & Other Publications
AbemaciclibLY2835219VerzenioCDK 4/6Binds to CDK 4/6 which may suppress DNA synthesis of tumor cells & inhibit tumor cell growth; Part of the MONARCH study; May cross BBB; FDA approved in Sept 2017 for HR+/HER2-Neg MBCOncLive; Dana-Farber News
Adenovirus/MAGE-A3AdMA3MAGE-A3Engineered cold virus (Adenovirus) binds to MAGE-A3 & inhibits growth of MAGE-A3-overexpressing tumor cellsCTV News
Ad-RTS-hIL-12IL-12Virus that produces IL-12 which increases immune response
AfatinibBIBW
2992 MA2
GilotrifEGFR,
HER 1/2/4
Binds to EGFR & HER 1/2/4 which may result in inhibition of tumor growth & vascularization of blood vessels (angiogenesis) in tumor cells overexpressing RTKs
AldesleukinProleukinIL-2Binds to & activates IL-2 expressed on the surface of activated T-lymphocytes which may induce a T-cell mediated tumor regression in certain tumor types
AlectinibRO5424802,
RG7853,
CH542482,
AF802
AlecensaALKBinds to & inhibits the ALK which stops tumor cell growth of ALK-overexpressing tumor cells; Approved for ALK+ metastatic NSCLC in Nov 2017
AlisertibMLN8237Aurora ABinds to Aurora A kinase which inhibits cell division & proliferation & may induce cell death in Aurora A-overexpressing tumor cellsScience Daily
AlpelisibBYL719PI3KPI3K inhibitor which may result in apoptosis (cell death) & growth inhibition in tumor cells
AnakinraKineretIL-1Binds to & blocks IL-1 which may inhibit the cascade downstream of VEGF, TNF, & IL-6 resulting in inhibition of the growth & maintenance of tumor blood vessels
AnastrozoleArimidexAromataseInhibits aromatase which converts androgen into estrogen creating an environment with less estrogen available to stimulate the growth of HR+ breast cancer cells; FDA approved to treat post menopausal patients with HR+ breast cancer
AndecaliximabGS-5745MMP-9Binds to MMP-9 & inhibits extracellular matrix protein degradation which could potentially inhibit tumor blood vessel growth as well as proliferation & metastasis of MMP-9-overexpressing tumor cells
Anetumab ravtansine (DM4)BAY 94-9343MesothelinADC composed of the anti-mesothelin antibody (anetumab) & a cytotoxic agent (ravtansine or DM4); Anetumab Ravtansine binds to the tumor associated antigen, mesothelin, & is internalized by the cancer cell where DM4 is released which can inhibit division & growth of mesothelin-overexpressed tumor cells
ApatinibYN968D1AitanVEGFR-2Binds to VEGFR-2 which can inhibit tumor cell proliferation & vascularization (angiogenesis) of tumor cells that overexpress VEGFR-2; Granted orphan-drug designation for the treatment of gastric cancer in June 2017LSK BioPharma News
ApitolisibGDC-0980,
RG7422
PI3K/
mTOR
Inhibits both PI3K & mTOR which may result in tumor cell death & growth inhibition of cancer cells
AtezolizumabMPDL3280ATecentriqPD-L1Immune checkpoint inhibitor that blocks PD-L1 from turning off the function of T-cells & activates the immune system to kill PD-L1-expressing tumor cells; Showing improved efficacy when combined with other immunotherapies; FDA approved in May 2016 for most common type of bladder cancer (urothelial carcinoma) & Oct 2016 for lung cancers Breastcancer-news; SABCS17 Abstract
AtorvastatinHMG-CoA ReductaseBlocks the HMG-CoA enzyme that helps make cholesterol in the body & may inhibit proliferation, invasion, & metastasis of breast cancer cells
AvelumabMSB0010718CBavencioPD-L1Immune checkpoint inhibitor that blocks PD-L1 from turning off the function of T-cells & activates the immune system to kill PD-L1-expressing tumor cells; Showing improved efficacy when combined with other immunotherapies; Received accelerated approval in March 2017 to treat metastatic carcinoma & breakthrough therapy in combination with a VEGF inhibitor in Dec 2017 for advanced RCCFDA News; OncLive
AxitinibAG-013736InlytaVEGFR/PDGFRBinds to VEGFR & PDGFR which inhibits maintenance of tumor blood vessels, & stops tumor cell growth & proliferation in VEGFR/PDGFR-overexpressing tumor cells; FDA approved in 2012 for advanced RCC
BalixafortidePOL6326CXCR4Binds to CXCR4 which may inhibit tumor cell growth & proliferation in CXCR4-overexpressing tumor cells; Received fast track designation in combination with eribulin as 3rd line therapy for HER2-Neg MBCImmuno Oncology News; Breastcancer-news
BasilixumabSDZ-CHI-621SimulectIL-2RaImmunosuppressant that binds to & blocks IL-2Ra, expressed on the surface of activated T-lymphocytes, thereby inhibiting the activation of these lymphocytes
BazedoxifeneWAY 140424,
TSE-424
DuaveeERSERM that inhibits tumor cell proliferation in ER+ breast cells; Used to treat ER+ breast cancer
BevacizumabAvastinVEGFR-ABinds to VEGFR-A which inhibits the growth & maintenance of tumor blood vessels; FDA approved for metastatic colorectal cancer; Not shown to be effective in US for breast cancer
BicalutamideICI 176,334CasodexARInhibits the AR found on surface of cancer cells which can lead to a decrease in tumor cell proliferation; Showing promise for AR+ TNBC
BinimetinibARRY-162,
ARRY438162,
MEK162
MEK 1/2Binds to MEK 1/2 & inhibits cellular proliferation in MEK-expressing tumor cells
*Bi-shRNA-furin/GM-CSF-expressing VaccineFANG VaccineVigilTM-The expressed GM-CSF protein of the vaccine is a potent stimulator of the immune system; the Bi-shRNA blocks furin protein production which reduces immunosuppressive cytokines and may cause a CTL response against tumor cells
BortezomibPS-341VelcadeProteasomeInhibits the activity of the 26S proteasome which plays central role in regulation of proteins that control cell-cycle progression & cell death; Showing promise in TNBC patients with TP53 mutationNIH News
*BriaVaxTM-Immunomodulator; Vaccine of whole cells genetically engineered to release a protein, called GM-CSF, that activates the immune systemBreastcancer-news 11/8/17;
Breastcancer-news 11/2/17
BrigatinibAP26113AlunbrigALK/EGFRDual kinase inhibitor that binds to ALK/EGFR which inhibits tumor cell growth & proliferation; FDA approved in April 2017 for metastatic ALK+ NSCLC
BuparlisibBKM120Pan-PI3KPan-PI3K inhibitor which may result in inhibition of tumor cell growth
CAB-AXL-ADCBA3011AXLADC composed of an anti-AXL antibody & a cytotoxic agent; CAB-AXL-ADC binds to AXL & releases the cytotoxic agent into the cancer cell which may inhibit the metastasis of AXL-overexpressing tumor cells
CabiralizumabBMS-986227/FPA-008CSF1Monoclonal antibody that binds to CSF1 receptors & enhances antitumor T-cell immune responses, which inhibits the proliferation of tumor cells
CabozantinibBMS-907351,
XL184
Cometriq, CabometyxMultipleBinds to several RTKs which may result in inhibition of tumor growth; Treats brain metastases; FDA approved in Dec 2017 as first-line treatment for advanced RCC
CanakinumabACZ885IlarisIL-1bAntibody that binds to IL-1b & inhibits an inflammatory response in the tumor microenvironment which may lead to tumor regression
*CapecitabineXeloda-Antimetabolite that prevents division of cancer cells (Chemotherapy)
CarfilzomibPR-171KyprolisProteasomeInhibits the activity of the 20s proteasome which may lead to tumor cell cycle arrest, induction of tumor cell death, & inhibition of tumor growth
CAR T-cell Therapyc-MET, NKG2D,
Mesothelin
A form of immunotherapy called ACT that involves genetically reengineering T-cells (immune cells), taken from a blood sample, to have CARs on the surface of the T-cell. When the altered T-cells are infused back into the patient, they target & kill cancer cells that overexpress the targeted protein; FDA approved for ALL (Aug 2017) & large B-cell lymphomas (Oct 2017)Forbes News; Fact Sheet
CediranibAZD-2171RecentinVEGFR 1/2/3,
c-Kit
Binds to VEGFR 1/2/3 & c-Kit which inhibits the formation of blood vessels in tumor cells that overexpress VEGFR
CelecoxibSC-58635CelebrexCOX-2Binds to & inhibits COX-2 which may result in tumor cell death, & reduction in the tumor 's ability to form new blood vessels & metastasize
Cergutuzumab amunaleukinRO6895882, RG7813, CEA-IL2vCEA Recombinant fusion protein comprised of an anti-CEA antibody (cergutuzumab) which is linked to an engineered IL-2v; The IL-2v moiety activates both NK cells & cytotoxic T-cells for a local immune response which inhibits tumor cell proliferation & induces tumor cell death of CEA-overexpressing tumor cells
CetuximabC225ErbituxEGFRBinds to the EGFR which inhibits tumor growth & metastasis in EGFR-dependent tumors
CirmtuzumabUC-961ROR1Binds to ROR1 & inhibits tumor cell proliferation in ROR1-overexpressed tumor cells
CobimetinibGDC-0973,
XL518
CotellicMEK 1/2Binds to MEK 1/2 which inhibits cellular proliferation in MEK-expressing tumors; FDA approved in 2015 to treat advanced melanoma
CopanlisibBAY80-6946AliquopaPI3KPI3K inhibitor which may result in apoptosis (cell death) & growth inhibition in tumor cells; FDA approved for follicular lymphoma in Oct 2017
CrenigacestatLY3039478N1ICDThe Notch signaling pathway plays an important role in cell survival & proliferation; LY3039478 may inhibit cell growth & induce cell death in tumor cells in which Notch signaling pathway is over activated
CrizotinibPF-2341066XalkoriALK/c-METBinds to ALK & c-MET which inhibits tumor cell growth of ALK & c-MET-overexpressing tumor cells; Approved in 2011 for patients with metastatic NSCLC that are ALK+ (2011) & ROS1+ (2016)
DabrafenibGSK2118436TafinlarBRAFBinds to & inhibits the BRAF kinase which may inhibit tumor cell proliferation in BRAF-expressing tumor cells; Approved in June 2017 for metastatic NSCLC with BRAF V600E mutation
DacomitinibPF-00299804Pan-EGFRBinds to EGFR subtypes which inhibits tumor cell proliferation & tumor vascularization in tumor cells that overexpress EGFR
DaratumumabJNJ-54767414DarzalexCD38IgGk antibody that binds to glycoprotein CD38 which triggers ADCC in order to recruit & activate immune cells to directly kill tumor cells; FDA approved for multiple myeloma
DarolutamideODM 201/
BAY 1841788
ARInhibits the AR found on surface of cancer cells which can lead to a decrease in tumor cell proliferation; Showing promise for AR+ TNBC
DasatinibBMS-354825SprycelPDGFRBinds to the Src family kinases including PDGFRs which may inhibit tumor cell proliferation; FDA approved for various types of leukemia & in Nov 2017 for pediatric patients with Ph+ CMLScience Daily
DecitabineDacogenChemotherapy drug that inhibits tumor DNA replication & cell proliferation, & triggers tumor cell death; FDA approved for myelodysplastic syndrome, but may be able to treat TNBCMayo Clinic News; Breast-cancer News
DefactinibPF-04554878, VS-6063FAKBinds to FAK which may inhibit tumor cell migration, proliferation, survival, & tumor blood vessel formation
Denileukin diftitoxOntakIL-2Immunomodulator; Engineered protein that combines a bacterial toxin (Diphtheria) with IL-2 which can introduce the toxin to, & kill IL-2-expressing tumor cells; FDA approved for cutaneous T-cell lymphoma
DenosumabXgevaRANKLA human monoclonal antibody that binds to the RANKL on bone cells for the treatment of osteoporosis, metastases to bone, etc
Depatuxizumab mafodotinABT-414EGFRADC composed of an anti-EGFR antibody & a cytotoxic agent; ABT-414 binds to the EGFR on tumor cell surface & is internalized by the tumor cell where the cytotoxic agent is released which induces cell death & inhibits the proliferation of EGFR-expressing tumor cells
DinaciclibSCH 727965CDK 1/2/5/9Binds to & inhibits CDK 1/2/5/9 which may result in tumor cell cycle repression & apoptosis (cell death)
*DisulfiramAntabuseProteasomeInhibits the activity of the proteasome which can lead to inhibition of tumor cell growth; Anti-tumor activity of disulfiram is highly dependent upon binding to copper (Cu), a metal that selectively accumulates in cancer cellsScience Mag
DM-CHOC-PEN-Chemotherapy drug composed of a cholesterol carbonate derivative of DM-PENÊwhich inhibits tumor DNA replication & cell proliferation, & triggers tumor cell death; Crosses the BBB
DovitinibTKI258,
CHIR-258
FGFR3Binds to & inhibits FGFR3, which may inhibit tumor cell proliferation & induce tumor cell death in FGFR3-overexpressing tumor cells; May inhibit other members of the RTK superfamily (i.e.. VEGF, c-Kit, CSF1) which may result in an additional reduction in proliferation & blood vessel formation by tumor cells
DurvalumabMEDI4736ImfinziPD-L1Immune checkpoint inhibitor that blocks the PD-L1 from turning off the function of T-cells & activates the immune system to kill PD-L1-expressing tumor cells; Showing improved efficacy when combined with other immunotherapies; Received accelerated approval in May 2017 for urothelial carcinoma
EdelfosineAkt, MAPK/ERKBinds to & inhibits the activity of Akt & ERK, which may result in inhibition of the PI3K/Akt & MAPK/ERK pathways which may inhibit tumor cell proliferation & may lead to tumor cell death; FDA-approved as investigational leukemia treatment & prevented TNBC stem cells from spreading to the brain in miceScience Daily
ElacestrantRAD1901ERSERD that binds to & inhibits estrogen receptors thereby making less estrogen available to stimulate the growth of HR+ breast cancer cells; FDA granted fast track designation for the treatment of ER+/HER2-Neg MBCFDA News
EmactuzumabRO5509554CSF1Monoclonal antibody that binds to CSF1 receptors & improves anti-tumor cell responses
EndostatinEndostarFGFR/VEGFRDual kinase inhibitor that binds to FGFR & VEGFR which may result in inhibition of tumor blood vessel formation & cell proliferation & may also induce tumor cell death
EnobosarmGTx-024OstarineARSARM that mimics the action of testosterone & can block the use of androgen by tumor cells
EnsituximabNEO-102, NPC-1CCPAABinds to CPAA & activates a CTL & ADCC response to directly kill CPAA-overexpressing tumor cells
EntrectinibRXDX-101NTRK; ROS1; ALKMulti-kinase Inhibitor; Binds to TRKs-A/B/C, ROS1, & ALK which can lead to inhibition of tumor cell proliferation & cell death in cells that express these kinases
EnzalutamideASP9785,
MDV3100
XtandiARInhibits the AR found on surface of cancer cells which can lead to a decrease in tumor cell proliferation; FDA approved for advanced prostate cancer; Showing promise for AR+ TNBCOncLive
EpacadostatINCB024360IDO1IDO1 protein inhibitor & immunomodulator which can increase & restore proliferation & activation of various immune cells; Showing promise in clinical trials that combine IDO inhibitors with antibodies that target the PD-1/PD-L1 pathwayOncLive 11/17;
OncLive 08/17
ErdafitinibJNJ-42756493FGFRBinds to & inhibits the FGFR, which may inhibit tumor cell proliferation & induce tumor cell death in FGFR-overexpressing tumor cells
*Eribulin mesylateER-086526,
E7389, B1939
Halaven-Microtubule inhibitor that prevents division of cancer cells (Chemotherapy)
ErlotinibCP358774,
OSI774
TarcevaEGFRBinds to the EGFR which may result in inhibition of tumor growth & vascularization of blood vessels (angiogenesis) in tumor cells overexpressing EGFR
EtinostatSNDX-275,
MS-275
HDACBinds to & inhibits HDACs which can arrest the tumor cell cycle & induce tumor cell death; Designated as a breakthrough therapy in 2013 for ER+ MBCBreastcancer-news
*Etirinotecan pegolNKTR 102OnzealdTopo ITopo I inhibition that causes tumor DNA damage (Chemotherapy); In phase 3 clinical trials for MBC patients with brain metastases
EverolimusRAD001AfinitormTORImmunosuppressant that binds to mTOR which may result in inhibition of tumor cell growth & proliferation; FDA approved in Feb 2016 for NETs of GI or lung origin & in July 2012 for HR+/HER2-Neg breast cancer; Proven to be effective for overcoming endocrine resistance in postmenopausal women with ER+/HER2-Neg MBC that have become resistant to AI therapyTargeted Oncology
ExemestaneAromasinAromataseInhibits aromatase which converts androgen into estrogen creating an environment with less estrogen available to stimulate the growth of HR+ breast cancer cells; FDA approved to treat post menopausal patients with HR+ breast cancer
Farletuzumab eribulinMORAb-202FRAADC composed of a G1 antibody & a cytotoxic agent (eribulin); Farletuzumab eribulin binds to FRA & is internalized by the cancer cell where the eribulin is released which can stop the division, and hence the growth of tumor cells
FilgrastimHSP-130Neupogen/ZarxioG-CSFBinds to & activates a natural protein, G-CSF, which boosts the production of white blood cells (neutrophils) in the bone marrow
FruquintinibHMPL-013VEGFR 1/2/3Binds to VEGFR 1/2/3 which inhibits tumor cell proliferation, migration & the formation of blood vessels in VEGFR 1/2/3-overexpressing tumor cells
FulvestrantFaslodexERSERD that binds to & inhibits estrogen receptors thereby making less estrogen available to stimulate the growth of HR+ breast cancer cells; FDA approved in combination with Palbociclib (Ibrance) in May 2016 & with Abemaciclib (Verzenio) in Aug 2017 to treat patients with HR+/HER2-Neg MBC who have progressed after endocrine therapyOncLive;
Breast cancer-news
GalunisertibLY2157299TGFBRBinds to the TGFBR which may inhibit the proliferation of TGFBR-overexpressing tumor cells
GedatolisibPKI-587,
PF-05212384
PI3K/
mTOR
Inhibits both PI3K & mTOR which may result in tumor cell death & growth inhibition of cancer cells
Glembatumumab vedotinCDX-011gpNMBADC composed of an anti-gpNMB antibody & cytotoxic agent (MMAE); CDX-011 binds to gpNMB on surface of tumor cell & is internalized by the tumor cell where it releases MMAE which inhibits cell growth & induces cell death; In development for the treatment of Stage III & IV melanoma & TNBC
*Globo H-CRM197OBI-833-Immunomodulator; Vaccine comprised of the hexasaccharide 1 (Globo H) antigen that may stimulate a T-lymphocyte response
GlumetinibSCC244c-METBinds to & inhibits c-MET phosphorylation which disrupts c-MET's signal transduction pathways; this may induce cell death & inhibit the proliferation of c-MET-expressing tumor cells
GoserelinZoladexERSERD used to treat pre-menopausal patients with HR+ breast cancer
High Intensity Focused Ultrasound (HIFU)-Using a HIFU beam to "pop" oxygen-filled microbubbles within tumors may make tumors more sensitive & more permeable to both chemotherapy and radiation therapy Science Daily
IbrutinibPCI-32765,
CRA-032765
ImbruvicaBTKBinds to the BTK & inhibits the growth & activation of malignant B cells that overexpress BTK; FDA approved in Jan 2017 for certain types of lymphoma
iCasp9M28z T-cell infusionsMesothelinA form of immunotherapy called ACT that involves genetically reengineering T-cells (immune cells), taken from a blood sample, to have anti-mesothelin CARs on the surface of the T-cell. When the altered T-cells are infused back into the patient, they target & kill mesothelin-overexpressing tumor cells; If the CAR t-cell infusion has unacceptable side effects, a binding agent can be administered which will result in the cell death of the previously infused T-cells
IcotinibBPI-2009ConmanaEGFRBinds to the EGFR which may result in inhibition of cell proliferation in tumors overexpressing EGFR
IGF-Methotrexate765IGF-MTXIGFRDrug conjugate composed of a cytotoxic agent (methotrexate) & IGF; IGF-Methotrexate binds to the IGFR on the surface of a tumor cell & is internalized by the tumor cell; Methotrexate is then released which inhibits DNA & RNA synthesis & can lead to tumor cell death
ImatinibGleevecABL; c-Kit; PDGFR A/BBinds to the intracellular pocket of TKs encoded by various oncogenes which results in decreased proliferation & enhanced apoptosis (cell death) in tumor cells; FDA approved for CML
*Imprime PGG-Enhances the efficacy of anti-PD-1 & anti-PD-L1 immune checkpoint inhibitors by instructing T-cells to ignore the tumor
IniparibBSI-201PARP 1/2Binds to PARP 1/2 & inhibits the tumor cell's ability to repair DNA, which enhances DNA strand breaks, promotes instability, & results in tumor cell death; A phase 3 trial for metastatic TNBC demonstrated that iniparib does not inhibit PARP in vitro
*Interferon alpha-2bSch 30500Intron A-Alpha interferons bind to specific cell-surface receptors and have antiviral, antiproliferative, anticancer, & immune-modulating effects
*Interferon-gammaActimmune-Immunomodulator that binds to Interferon-gamma & may activate certain components of the immune system including natural killer cells & T-cells
IpatasertibGDC-0068,
RG-7440
AktBinds to Akt (key node in the PI3K/Akt signaling network) thereby inhibiting tumor cell growth & proliferation in tumors with hyper activated Akt; Early clinical support for use with TNBC
IpilimumabMDX-010,
BMS-734016
YervoyCTLA4Immune checkpoint inhibitor; Binds to & blocks the CTLA4 protein on the surface of T-cells which leaves the T-cells free to stay active & attack cancer cells
IsomangiferinVEGFR-2Binds to VEGFR-2 which can inhibit tumor cell proliferation & vascularization (angiogenesis)Journal of Breast Cancer
ItacitinibINCB039110JAK1Binds & inhibits JAK1 which may result in programmed cell death and/or reduction of cell proliferation in JAK1-expressing tumor cells
*IT-pIL12-EPIL-12IT-pIL12-EP is an injection of plasmid IL-12 into the tumor delivered via an electric current (electroporation) which facilitates uptake & sustained expression of IL-12, increases TILs & stimulates an immune response
IxazomibMLN9708NinlaroProteasomeInhibits the activity of the proteasome which plays central role in regulation of proteins that control cell-cycle progression & cell death
L-NMMANOSNOS inhibitors have been shown to reduce tumor volume in TNBC mouse models BC-News
Ladiratuzumab vedotinSGN-LIV1ALIV-1ADC composed of the anti-LIV-1 antibody & a cytotoxic agent (MMAE); SGN-LIV1A binds to LIV-1 & is internalized by the tumor cell where MMAE is released which inhibits tumor cell growth & induces tumor cell death in LIV-1+ cancer cells; In clinical trials for TNBCOncLive
LapatinibGW-572016TykerbEGFR,
HER2
Dual kinase inhibitor that binds to ATP-binding pocket of EGFR/HER2 which inhibits tumor cell growth & proliferation; Can cross the BBB; FDA approved in 2010 for post-menopausal women with HER2+ breast cancerScience Daily
LarotrectinibLOXO-101TRKBinds to TRK & inhibits the Neurotrophic-TRK interaction which may result in apoptosis (cell death) & growth inhibition of cancer cells that overexpress TRKNCI News
LenvatinibE7080LenvimaVEGFR-2Binds to VEGFR-2 which can inhibit tumor cell proliferation & vascularization (angiogenesis); FDA approved for metastatic thyroid cancer (2015) & in combination with everolimus for advanced RCC (2016)
LetrozoleFemaraAromataseInhibits aromatase which converts androgen into estrogen creating an environment with less estrogen available to stimulate the growth of HR+ breast cancer cells; FDA approved to treat post menopausal patients with HR+ breast cancer
LeuprolideLupronERSERD that binds to & activates GnRH receptors which leads to decreased estradiol production; FDA approved to treat pre-menopausal patients with HR+ breast cancer
LirilumabBMS-986015, IPH2102KIRBinds to & inhibits the KIR expressed by NK cells & T-cells which "unblinds" these immune cells & results in an enhanced immune response against tumor cells, decreasing tumor cell proliferation & inducing tumor cell death
LucitanibE-3810,
AL3810
VEGFR 1/2/3,
FGFR 1/2
Dual kinase inhibitor that binds to VEGFR 1/2/3 & FGFR 1/2 which may result in inhibition of tumor blood vessel formation & cell proliferation & may also induce tumor cell death
177Lu-DOTA-EB-TATESSTRRadioconjugate that binds to the SSTR present on many types of NET cells; Upon binding & internalization by NET cells, a cytotoxic dose of beta radiation to SSTR+ cells is delivered
*LurbinectedinPM01183Pol IITranscription inhibitor that induces DNA double-strand breaks which may result in delayed tumor cell progression & cell death; Data shows activity in platinum-resistant breast cancers
Maraba/MAGE-A3 virusMG1MA3MAGE-A3Engineered Maraba virus from the Brazilian sandfly binds to MAGE-A3 & is internalized by the tumor cell where the virus can replicate and kill MAGE-A3-overexpressing tumor cells directlyCTV News
MargetuximabMGAH22HER2Binds to HER2 which may induce ADCC response to recruit & activate immune cells to directly kill HER2-overexpressed tumor cells; Part of the SOPHIA study OncLive
MerestinibLY2801653c-METBinds to & inhibits c-MET phosphorylation which disrupts c-MET's signal transduction pathways; this may induce cell death & inhibit the proliferation of c-MET-expressing tumor cells
Metformin HCLRiomet/Glumetza/Glucophage/FortametmTORC1Metformin inhibits mTORC1 which may prevent tumor cell growth & proliferation of mTORC1-overexpressed tumor cells
MifepristoneRU 486,
RU-38486
MifeprexPRBinds to the PR resulting in inhibition of the effects of progesterone; also exhibits antiglucocorticoid & weak antiandrogenic activities
Mirvetuximab soravtansine (DM4)IMGN853FOLR1ADC composed of an anti-FOLR1 antibody (mirvetuximab) & a cytotoxic agent (soravtansine or DM4); Mirvetuximab Soravtansine binds to FOLR1 & is internalized by the cancer cell where DM4 is released which can inhibit division & growth of FOLR1-overexpressed tumor cells
MivebresibABBV-075BETBinds to BET proteins (BRD 2/3/4/T) which can inhibit tumor cell growth
MocetinostatMGCD0103HDACBinds to & inhibits HDACs which can arrest the tumor cell cycle & induce tumor cell death
MogamulizumabKW-0761CCR4Binds to CCR4 which is expressed on the surface of certain T-cells & may inhibit tumor cell proliferation & trigger ADCC against CCR4-overexpressed T-cells
MolibresibGSK525762, I-BET-762BETBinds to BET proteins which prevents interaction with peptides & disrupts gene expression which can lead to inhibition of cell growth in BET-overexpressing tumor cellsScience Daily
MVA/FPV-Brachyury VaccineN/AN/ABrachyuryA vaccine composed of two viruses (MVA & FPV) that harnesses the immune system against the brachyury protein which is overexpressed in some cancersGlobe Newswire
NeratinibHKI-272NerlynxHER 1/2/4Binds to the cysteine residue in the ATP-binding pockets of both HER2 & EGFR which can inhibit tumor cell proliferation & vascularization & induces tumor cell cycle arrest & death; Can cross the BBB; FDA approved in July 2017 for early stage HER2+ breast cancer
NilotinibAMN 107TasignaBCR-ABL, c-Kit, PDGFRBinds to the intracellular pocket of TKs encoded by various oncogenes which results in decreased proliferation & enhanced apoptosis (cell death) in tumor cells; FDA approved for imatinib-resistant CML
NintedanibBIBF1120OfevVEGFR,
FGFR
, PDGFR
Angiogenesis inhibitor that binds to VEGF,
FGF
, & PDGF receptors which can inhibit tumor vasculature & tumor cell proliferation
NiraparibZejulaPARP 1/2Binds to PARP 1/2 & inhibits the tumor cell's ability to repair DNA, which enhances DNA strand breaks, promotes instability, & results in tumor cell death; FDA approved in March 2017 for maintenance therapy for recurrent ovarian & peritoneal cancer
NivolumabBMS-936558, MDX-1106, ONO-4538OpdivoPD-L1Immune checkpoint inhibitor that blocks PD-L1 from turning off the function of T-cells & activates the immune system to kill PD-L1-expressing tumor cells; Showing improved efficacy when combined with other immunotherapies; FDA approved for lung, melanoma, bladder, head/neck cancers, Hodgkin lymphoma, & in Oct 2017 it was approved for advanced liver cancerOncLive
OlaparibAZD2281,
KU-0059436
LynparzaPARP 1/2/3Binds to PARP 1/2/3 & inhibits the tumor cell's ability to repair DNA, which enhances DNA strand breaks, promotes instability, & results in tumor cell death; OlympiAD trial showed Olaparib prolonged PFS vs. standard therapy in patients with HER2-Neg BRCA+ MBC; FDA approved in Jan 2018 for HER2-Neg BRCA 1/2+ MBC patientsFDA News; Targeted Oncology
OnalespibAT13387HSP90HSP90 is a chaperone protein upregulated in a variety of tumor cells & regulates the folding, stability & degradation of many oncogenic signaling proteins; Onalespib binds to HSP90 which may inhibit tumor cell proliferation
OrteronelTAK-700ARAndrogen synthesis inhibitor may decrease growth signaling & inhibit cell proliferation of androgen-dependent tumor cells; In phase 3 trials for prostate cancer
OsimertinibMereletinib, AZD9291TagrissoEGFRBinds to EGFR which may inhibit tumor cell proliferation & vascularization in EGFR-overexpressing tumor cells; Approved in March 2017 for metastatic EGFR+ NSCLC
PalbociclibPD0332991IbranceCDK 4/6Binds to CDK 4/6 which may suppress DNA synthesis of tumor cells & inhibit tumor cell growth; FDA approved in March 2017 for HR+/HER2-Neg MBC EMB Mol Med Pub; ICR News
PanitumumabABX-EGFVectibixEGFRBinds to EGFR which inhibits tumor cell proliferation in EGFR-dependent tumors
PanobinostatLBH589FarydakHDACBinds to & inhibits HDACs which can arrest the tumor cell cycle & induce tumor cell death
PatritumabAMG 888,
U3-1287
HER3Binds to HER3 & blocks the PI3K signaling pathway which may result in inhibition of tumor cell growth
PazopanibGW786034BVotrientVEGFR 1/2/3,
c-Kit, PDGFR
Binds to VEGFR 1/2/3, c-Kit & PDGFR which inhibits tumor cell proliferation & the formation of blood vessels in tumor cells that overexpress these proteins
*Pegylated liposomal doxorubicinTLC D-99LipoDox, Doxil, Caelyx-Liposome-encapsulated form of the hydrochloride salt of the antibiotic doxorubicin which prevents DNA replication & inhibits protein synthesis; Liposomal delivery of doxorubicin HCL has cardio-preserving properties & improves drug penetration into tumors & the duration of therapeutic drug effects (Chemotherapy)
Pegylated PH20HalozymeHADegrades the hyaluronic acid that coats tumor cells which may result in the inhibition of tumor cell growth
*PEG-rHuIL-10AM0010IL-10A conjugate of IL-10 & PEG with immunomodulating activities that may activate immunity against cancer cells by stimulating tumor specific cytotoxic CD8+ T-cells
PembrolizumabMK-3475KeytrudaPD-L1Immune checkpoint inhibitor that blocks PD-L1 from turning off the function of T-cells & activates the immune system to kill PD-L1-expressing tumor cells; Showing improved efficacy when combined with other immunotherapies; FDA approved for several other cancers; I-SPY2 trial showed Keytruda increased pCR rate nearly threefold in TNBC & in patients with HR+/HER2-Neg patients vs. standard therapy
PertuzumabRO4368451PerjetaHER2Inhibits the pairing (dimerization) of HER2 proteins which results in an inhibition of cell growth & proliferation in HER2-expressing tumor cells; FDA approved in 2012 as standard of care 1st line treatment in combo w/ trastuzumab for HER2+ breast cancer
PevonedistatMLN4924NAEBinds to & inhibits NAE which may result in inhibition of tumor cell proliferation & survival in NAE-overexpressed tumor cells
PictilisibGDC-0941PI3KBinds to PI3K & inhibits the activation of the PI3K/Akt signaling pathway which may result in apoptosis (cell death) & growth inhibition of cancer cells
PilaralisibSAR245408,
XL147
PI3KPI3K inhibitor which may result in apoptosis (cell death) & growth inhibition of cancer cells
Plasmodium vivax vaccine-Vaccine composed of the malaria parasite, plasmodium vivax, which can stimulate a CTL response against tumor cells
PonatinibAP24534IclusigVEGFR, FGFR, TIE-2, FLT-3Inhibits multiple tyrosine kinases; Binds to VEGFR, FGFR, TIE-2, & FLT-3 which may result in the inhibition of tumor blood vessel formation & tumor cell proliferation, & may induce tumor cell death
PoziotinibHM781-36B,
NOV120101
HER 1/2/4Pan-HER inhibitor that binds to HER1, HER2, & HER4 receptors inhibiting the proliferation of tumor cells that overexpress these receptors
PrexasertibLY2606368CHK1Binds to CHK1 which inhibits the repair of damaged DNA in cancerous cells
PyrotinibHTI-1001EGFR,
HER2
Binds to both EGFR & HER2 which may result in inhibition of tumor growth & formation of blood vessels (angiogenesis) in EGFR/HER2-expressing tumor cells ASCO News
QuarfloxacinCX-3543Pol ITranscription inhibitor that binds to & inhibits Pol I which prevents ribosomal RNA synthesis- a process that plays a key role in cell proliferation & survival
Radioiodide131-INISRadiation from 131-I may help kill cancer cells or show where they are in the body
RamucirumabLY3009806CyramzaVEGFR-2Binds to VEGFR-2 which can inhibit tumor vascularization (angiogenesis) & decrease the tumor nutrient supply; FDA approved for adenocarcinoma, colorectal cancer, & NSCLC
RebastinibDCC-2036TIE-2,
VEGFR-2
Inhibits multiple tyrosine kinases; Binds to TIE-2 & VEGFR-2 which may inhibit the formation of blood vessels (angiogenesis) in TIE-2- & VEGFR-2-expressing tumor cells
RegorafenibBAY 73-4506StivargaVEGFR 2/3, c-Kit, PDGFR, RAFBinds to VEGFR 2/3, c-Kit, PDGFR, & RAF which inhibits tumor cell growth, proliferation & the formation of new blood vessels in tumor cells that overexpress these proteins
RelatlimabBMS-986016LAG3Immune checkpoint inhibitor that binds to LAG3 expressed on TILs which activates a T-cell mediated response against tumor cells leading to a reduction in tumor growth; Showing improved efficacy when combined with other immunotherapiesImmuno-Oncology News
ReparixinDF 1681YCXCR 1/2Binds to CXCR 1/2 which may inhibit tumor cell proliferation in CXCR2-overexpressing tumor cells
RibociclibLEE011KisqaliCDK 4/6Binds to CDK 4/6 which may suppress DNA synthesis of tumor cells & inhibit tumor cell growth; Ribociclib is showing a lot of progress for T-DM1-resistant breast cancers; FDA approved for postmenopausal (March 2017) & premenopausal (Jan 2018) HR+/HER2-Neg MBC patients based on the results of the MONALEESA trialsFDA News 01/18

FDA News 03/17
RicolinostatACY-1215HDAC6Binds to & inhibits HDAC6 which can arrest the tumor cell cycle & induce tumor cell death
Rovalpituzumab tesirineSC16LD6.5DLL3ADC composed of anti DLL3-antibody & a cytotoxic agent (tesirine); Rovalpituzumab tesirine binds to DLL3 & is internalized by the cancer cell where tesirine is released which can lead to inhibition of blood vessel growth & tumor cell death; Received orphan drug designation from FDA for treatment of SCLC
RucaparibAG014699RubracaPARPBinds to PARP proteins & interferes with the cells' ability to replicate; Received accelerated approval for advanced ovarian cancer with BRCA 1/2 mutations; FDA approved as maintenance therapy for recurrent ovarian, fallopian, & peritoneal cancer in April 2018NCI News
RuxolitinibINCB18424JakafiJAK 1/2Binds & inhibits JAK 1/2 which may result in programmed cell death & a reduction of cell proliferation in JAK 1/2-expressing tumor cells
Sacituzumab govitecanIMMU-132TROP2ADC composed of an anti-TROP2 antibody & a cytotoxic agent (SN-38); Sacituzumab govitecant binds to TROP2 & releases SN-38 into the cancer cell which may inhibit the metastasis of tumor cells; Received breakthrough status in Feb 2016; In clinical trials for TNBCCancer Network; ASCO News
SapanisertibTAK-228,
MLN0128
mTORC 1/2TORC inhibitor; Binds to mTORC1 & mTORC2 which can result in cell death & a decrease in tumor cell proliferationScience Daily
SapitinibAZD8931pan-EGFR, HER2Binds to EGFR & HER2 & inhibits tumor cell proliferation & blood vessel formation in EGFR & HER2-dependent tumors
SargramostimDRG-0012-Similar to the GM-CSF protein, sargramostim binds to specific cell surface receptors that stimulate leukocyte (white cell) production & promote an anti-tumor & ADCC response
SelinexorKPT-330CRM1Inactivates the CRM1-mediated export of tumor suppressor proteins which inhibits tumor cell proliferation & migration in CRM1-overexpressed tumor cells
SelumetinibAZD6244MEK 1/2Binds to MEK 1/2 & inhibits tumor cellular proliferation; In clinical trials for advanced melanoma & pancreatic cancer
SerabelisibTAK-117,
MLN1117,
INK1117
PI3K PI3K inhibitor which may result in apoptosis (cell death) & growth inhibition of cancer cells
SeribantumabMM-121HRGMonoclonal antibody that blocks HRG from binding to HER3 thereby inhibiting tumor resistance to anti-hormonal therapies; May result in cell death & growth inhibition of cancer cells expressing HRG which is widely expressed in ER+/HER2-Neg breast cancer Detroit Public Radio
SeviteronelVT-464ARAndrogen synthesis inhibitor which may decrease growth signaling & inhibit cell proliferation of androgen-dependent tumor cells
SimmiparibSMOCL-9112PARP 1/2Binds to PARP 1/2 & inhibits the tumor cell's ability to repair DNA which enhances DNA strand breaks, promotes instability, & results in tumor cell death
SimvastatinZocorHMG-CoA ReductaseDrug used to reduce the levels of triglyceride & "bad" cholesterol or LDLs in the blood, while increasing levels of "good" cholesterol or HDLs
siRNA-EphA2-DOPCEphA2Liposomal formulation composed of siRNAs encapsulated into liposomes that target & bind to EphA2-expressing cells (found in 50-100% of major tumor types) which interferes with both the transcription & translation of EphA2 thus inhibiting tumor cell growth
Sodium seleniteSp1Inorganic form of the trace element selenium which inhibits the expression & activity of the transcription factor Sp1; Inhibiting Sp1 may in turn, block AR signaling & inhibit tumor cell proliferation of AR-expressing tumor cells
SorafenibBAY 54-9085NexavarRAF, VEGFR2, PDGFRBlocks the RAF kinase which inhibits tumor cell division & binds to VEGFR2/PDGFR which may prevent growth of new blood vessels (angiogenesis) that tumors need to proliferate
SpartalizumabPDR001PD-L 1/2Immune checkpoint inhibitor that blocks PD-L 1/2 from turning off the function of T-cells & activates the immune system to kill PD-L1-expressing tumor cells; Showing improved efficacy when combined with other immunotherapies
*STEMVACEP-101CD105/Yb-1/SOX2/CDH3/MDM2Multi-antigen DNA plasmid-based vaccine that targets immunogenic proteins expressed in breast cancer stem cells which can be resistant to chemotherapy & can stimulate a CTL response against CD105/Yb-1/SOX2/CDH3/MDM2-expressing tumor cells
SunitinibSU11248PDGFR, VEGFR,
c-Kit
Binds to PDGFR, VEGFR & c-Kit which can inhibit the formation of blood vessels by tumors & tumor cell proliferation; FDA approved for RCC & imatinib-resistant GISTs
SupinoxinRX-5902P-p68Inhibits the RNA helicase P-p68 which is overexpressed in various types of solid tumors but absent in normal tissues, & plays a role in tumor progression and metastasisGlobe Newswire
TaladegibLY2940680SMOBinds to SMO & inhibits the signaling of Shh-SMO which plays an important role in tissue growth & repair & may lead to inhibition of tumor cell proliferation
TalazoparibBMN-673PARPBinds to PARP proteins & "traps" tumor DNA which interferes with the cells' ability to replicate; Showing promise for TNBC & BRCA 1/2 mutationsASCO News 12/17;

ASCO News 07/17
*Talimogene Laherparepvec (T-VEC)Imlygic-Genetically modified oncolytic virus that infects & breaks down cancer cells without harming normal cells; FDA approved for melanoma recurrencesNCI News
TamoxifenSoltamoxERInhibits the binding of estradiol to the ER on breast cancer cells via structural changes in the receptor which block the signal to the cell to divide & grow; Tamoxifen inhibits cell proliferation in ER+ tumor cells & can promote estrogen-like activities in other organs (e.g. bone, uterus). It is therefore classified as a SERM; FDA approved to treat ER+ breast cancer
Targeted Liposomal Doxorubicin (TLD-1)Talidox-Chemotherapy drug that uses a liposome to selectively deliver the hydrochloride salt of the antibiotic doxorubicin, which prevents DNA replication & inhibits protein synthesis; Liposomal delivery of doxorubicin HCL improves drug penetration into tumors & the duration of therapeutic drug effects; TLD-1 combines the cardio-preserving properties of the liposomal delivery system with shorter blood circulation time in order to reduce the risk of hand-foot-syndrome
TaselisibGDC-0032PI3KPI3K inhibitor which may result in cell death & growth inhibition of cancer cells
*TemozolomideSCH 52365Temodar-Chemotherapy drug that penetrates well into the central nervous system; In clinical trials for HER2+ breast cancer patients with brain metastases; FDA approved to treat brain cancers
TemsirolimusCCI-779ToriselmTORBinds to mTOR which may result in inhibition of tumor cell growth & proliferation; FDA approved for advanced RCC & kidney cancer
*TinostamustineEDO-2101-Chemotherapy drug that combines an alkylating agent with an HDAC inhibitor to damage tumor DNA & block damage repair; Slowed disease progression in hematological malignancies; Clinical trials for TNBC expected
TocilizumabR-1569ActemraIL-6Immunosuppressive IgG1 antibody that binds to IL-6 & is used to treat rheumatoid arthritis; May get Herceptin-resistant HER2+ tumors to start responding again
*TrabectedinET 743YondelisPol IITranscription inhibitor that induces DNA double-strand breaks which may result in delayed tumor cell progression & cell death; Data shows activity in platinum-resistant breast cancers
TrametinibGSK1120212,
JTP-74057,
TMT212
MekinistMEK 1/2Binds to MEK 1/2 & inhibits tumor cell proliferation; FDA approved in 2013 for metastatic BRAF+ melanoma patients; Approved in June 2017 for metastatic NSCLC with BRAF V600E mutation
TrastuzumabRO0452317,
PF-05280014
HerceptinHER2Binds to HER2 & inhibits tumor cell growth in HER2+ cancer cells; FDA approved in 1998 as standard of care 1st line treatment for HER2+ breast cancer
Trastuzumab deruxtecanDS-8201aHER2ADC composed of the anti-HER2 antibody & a cytotoxic agent (Topo I inhibitor); DS-8201a binds to HER2 & is internalized by the cancer cell where Topo I is released which can stop tumor cell growth & induce tumor cell death; Designated as breakthrough therapy in Aug 2017 for Herceptin/Perjeta/Kadcyla-resistant HER2+ breast cancerOncLive; ADC Review
Trastuzumab-dkst (Herceptin biosimilar)MYL-1401OÊOgivriHER2Binds to HER2 & inhibits tumor cell growth in HER2+ cancer cells; FDA approved in 1998 as standard of care 1st line treatment for HER2+ breast cancerOncLive; Targeted Oncology
Trastuzumab duocarmazineSYD 985HER2ADC composed of an anti-HER2 antibody & cytotoxic agent (duocarmycin); SYD985 binds to HER2 receptors & is internalized by the cancer cell where duocarmycin is released which can induce cell death of HER2-overexpressing tumor cells
Trastuzumab emtansine (T-DM1)RO5304020,
PRO132365
KadcylaHER2ADC composed of the trastuzumab (Herceptin) antibody & a cytotoxic agent (emtansine or DM1); T-DM1 binds to HER2 & is internalized by the cancer cell where DM1 is released which can inhibit proliferation of HER2-overexpressed tumor cells; FDA approved in 2013 for HER2+ breast cancers that are resistant to Herceptin or Perjeta
TrebananibAMG386Ang 1/2Binds to Ang 1/2 & may inhibit tumor blood vessel formation & may eventually lead to an inhibition of tumor cell proliferation
TremelimumabCP-675, 206CTLA4Immune checkpoint inhibitor; Binds to & blocks the CTLA4 protein on the surface of T-cells which leaves the T-cells free to stay active & attack cancer cells
Triciribine Phosphate Monohydrate (TCN-PM)Akt 1/2/3 Binds to Akt 1/2/3 (key nodes in the PI3K/Akt signaling network) thereby inhibiting tumor cell growth & proliferation in tumors with hyper activated Akt
TrilaciclibG1T28CDK 4/6Binds to & inhibits CDK 4/6 which may suppress DNA synthesis of tumor cells & inhibit tumor cell growth
TucatinibONT-380,
ARRY-380
HER2Binds to HER2 & inhibits tumor cell proliferation & induces tumor cell death in HER2-expressing tumor cells; Can cross the BBB; Part of the HER2CLIMB studyASCO News
UlixertinibBVD-523ERK 1/2Binds to the ERK 1/2 & inhibits ERK-dependent tumor cell proliferation & may lead to tumor cell death; FDA granted fast track designation in Oct 2017 to patients with metastatic BRAF V600-mutant melanomaTargetedOnc
*UrelumabBMS-663513CD137Binds to & activates CD137-expressing immune cells, stimulating an immune response against tumor cells
UtomilumabPF-05082566TNFIgG2 antibody that targets the TNF receptor to stimulate a more intense immune system attack on cancers
VanctictumabOMP-18R5WntBinds to & blocks Wnt signaling pathway which may result in inhibition of cancer stem cell activity
VandetanibAZD6474CaprelsaEGFR,
VEGFR2
Binds to EGFR & VEGFR2 & inhibits tumor cell proliferation & the formation of blood vessels (angiogenesis) in EGFR- & VEGFR-dependent tumors
VeliparibABT-888PARPBinds to PARP proteins which interfere with the cells' ability to replicate
VemurafenibRO5185426,
RG7204,
PLX4032
ZelborafBRAF Binds to & inhibits the BRAF kinase which may inhibit tumor cell proliferation in BRAF-expressing tumor cells; Approved for metastatic melanoma in 2011
VenetoclaxABT-199BCL-2Small molecule inhibitor that binds to BCL-2 which restores apoptotic (cell death) processes to tumor cells; Approved in April 2016 for CLL
VismodegibGDC-0449ErivedgePTCH,
SMO
Binds to PTCH & SMO & inhibits the signaling of Shh-SMO which plays an important role in tissue growth & repair & may lead to inhibition of tumor cell proliferation
VistusertibAZD2014mTORC 1/2TORC inhibitor; Binds to mTORC1 & mTORC2 which can result in cell death
VorinostatZolinzaHDACHDAC inhibitor which may induce programmed cell death in tumor cells
XentuzumabBI 836845IGF 1/2Antibody that binds to IGF 1/2 which can inhibit cancer cell proliferation
Ziv-afliberceptVEGF Trap R1R2ZaltrapVEGFRBinds to VEGFR which inhibits the growth & maintenance of tumor blood vessels & tumor cell proliferation; FDA approved for metastatic colorectal cancer
Zoledronic acidZOL 446, CGP 42446ZometaFPPSBones are continually broken down by cells called osteoclasts & rebuilt by osteoblasts; Zometa reduces the turnover of bone by binding to the bone tissue & inhibiting FPPS which prevents osteoclasts from removing calcium & protects bones from cancers that can cause excessive bone breakdownScience Daily
N/AABBV-085LRRC15ADC composed of the anti-LRRC15 antibody & a cytotoxic agent; ABBV-085 binds to LRCC15 & is internalized by the cancer cell where the cytotoxic agent is released which induces cell death & inhibits the proliferation of LRCC15-expressing tumor cells
N/AABBV-176PRLRADC composed of the anti-PRLR antibody & a cytotoxic agent; ABBV-176 binds to PRLR & is internalized by the cancer cell where the cytotoxic agent is released which induces cell death & inhibits the proliferation of PRLR-expressing tumor cells
N/AABBV-181PD-L1Immune checkpoint inhibitor that blocks PD-L1 from turning off the function of T-cells & activates the immune system to kill PD-L1-expressing tumor cells; Showing improved efficacy when combined with other immunotherapies
N/AABBV-221EGFRADC composed of anti EGFR-antibody & a cytotoxic agent; ABBV-221 binds to EGFR & is internalized by the cancer cell where the cytotoxic agent is released which induces cell death & inhibits the proliferation of EGFR-expressing tumor cells
N/A*ABBV-368-Immunomodulator which can increase & restore proliferation & activation of various immune cells
N/AABBV-399c-METADC composed of anti-c-MET antibody & a cytotoxic agent; ABBV-399 binds to c-MET & is internalized by the cancer cell where the cytotoxic agent is released which induces cell death & inhibits the proliferation of c-MET-expressing tumor cells
N/AABT-165DLL4,
VEGF
Two monoclonal antibodies are combined to create an Ig dual-targeting agent that binds to DLL4 & VEGF & prevents the growth of blood vessels by tumor cells (angiogenesis)
N/AABT-767PARPBinds to PARP proteins & that interferes with the cells' ability to replicate
N/AADCT-502HER2ADC composed of a trastuzumab (Herceptin) antibody & the PBD-based drug, tesirine; ADCT-502 binds to HER2 & is internalized by the cancer cell where tesirine is released which can inhibit tumor DNA replication & proliferation of HER2-overexpressing tumor cells; Development of drug was halted in April 2018 because anti-cancer responses were only seen at doses not well tolerated by patients & thus failed to meet its primary objectiveBreastcancer News
N/AADI-PEG 20ArginineADI-PEG 20 20 breaks down the amino acid arginine & may inhibit the growth of cancers that have a high degree of arginine-dependency while leaving normal cells unharmed
N/AAK-104PD-1, CTLA4Immune checkpoint inhibitor that binds to & blocks PD-1 & CTLA4 on the surface of immune cells which leaves the immune cells free to stay active & attack tumor cells; Showing improved efficacy when combined with other immunotherapies
N/AAK-105PD-1Immune checkpoint inhibitor that binds to & blocks PD-1 which leaves the immune cells free to stay active & attack tumor cells; Showing improved efficacy when combined with other immunotherapies
N/AALRN-6924MDM2, MDMXBinds to both MDM2 & MDMX & interferes with the activation domain of tumor suppressor protein p53; By preventing the MDM2-p53 & MDMX-p53 interactions, the degradation of p53 is inhibited which restores p53 signaling & may lead to cell cycle arrest & programed cell death in MDM2- & MDMX-overexpressing tumor cells
N/AALT-803IL-2/IL-15Fusion protein that binds to IL-2/IL-15 expressed on immune cells which activates NK cells & T-cells for an enhanced immune response against tumor cells, decreasing tumor cell proliferation & inducing tumor cell deathSABCS17 Poster
N/AALT-P7HER2ADC composed of an anti-HER2 specific antibody & a cytotoxic agent (MMAE); ALT-P7 binds to HER2 & is internalized by the tumor cell where MMAE is released which inhibits tumor cell growth & induces tumor cell death in HER2+ cancer cells
N/AAPG-1252Bcl-2Small molecule inhibitor that binds to Bcl-2 which restores apoptotic (cell death) processes to tumor cells
N/AAPG-1387SM-1387IAPBinds to cIAP 1/2 & XIAP & promotes the rapid degradation of these proteins which results in tumor cell death & has an antitumor effect in certain cancers
N/AAPR-246, PRIMA-1p53 cysteine residueBinds to the cysteines of a mutated form of tumor suppressor (P53) which modifies the core domain, & activates & restores p53 signaling leading to tumor cell cycle arrest & programed cell death; Showing strong synergy when combined with DNA-damaging (chemotherapeutic) drugs Science Daily
N/AAPX3330, E-3330REF-1Binds to & inhibits REF-1 which may have detrimental effects on the viability of tumor cells by disrupting DNA damage repair and redox regulation mechanisms
N/AARQ 751Pan-Akt Binds to Akt (key node in the PI3K/Akt signaling network) thereby inhibiting tumor cell growth & proliferation in Akt-expressing tumors
N/AARRY-382CSF1Binds to CSF1 & prevents tumor cell proliferation of CSF1-overexpressing tumor cells & improves anti-tumor cell responses
N/AARX788HER2ADC composed of a HER2 specific antibody & a cytotoxic agent (MMAF); ARX788 binds to HER2 receptors & is internalized by the cancer cell where MMAF is released which can inhibit tumor cell division & induce tumor cell death
N/AASN007ERKBinds to the ERK & inhibits ERK-dependent tumor cell proliferation & may lead to tumor cell death
N/AASP8374/PTZ-201TIGITImmune checkpoint inhibitor that blocks the interaction of TIGIT with its ligands which activates a T-cell-mediated immune response against tumor cells
N/AAZD1775,
MK1775
Wee1Binds to & inhibits Wee1 which may result in tumor cell cycle repression & apoptosis (cell death)
N/AAZD4547FGFRBinds to FGFR which may result in the inhibition of tumor blood vessel formation & tumor cell proliferation, & may induce tumor cell death in FGFR-overexpressing tumor cells
N/AAZD5069CXCR2Binds to CXCR2 which may inhibit tumor cell proliferation in CXCR2-overexpressing tumor cells
N/AAZD5363AktBinds to Akt (key node in the PI3K/Akt signaling network) thereby inhibiting tumor cell growth & proliferation in tumors with hyper activated Akt; Early clinical support for use with TNBC
N/AAZD6738ATRBinds to & inhibits ATR which disrupts tumor DNA damage repair & induces cell death; In clinical trials for TNBC
N/AAZD8186PI3KB PI3K-Beta inhibitor that interrupts the PI3K /Akt/mTOR (PAM) signaling pathway which may result in cell death & growth inhibition of cancer cells
N/AAZD9150ISIS-STAT3rxSTAT3Binds to & inhibits the phosphorylation of STAT3 which prevents binding of STAT3 to DNA sequences which may result in the inhibition of tumor cell proliferation
N/AAZD9496ERSERD that binds to & degrades the estrogen receptor
N/ABAY 1217389Mps1Binds to Mps1 which can interfere with the tumor cell's ability to divide & replicate & can induce tumor cell death in Mps1-overexpressing cancer cells
N/ABCD-115CDK 8/19Binds to & inhibits CDK 8/19 which may suppress estrogen-induced transcription which inhibits tumor growth in ER+ breast cancer cells
N/ABDB001TLRBinds to & activates TLR which initiates the innate immune system, stimulates immune cells (e.g. dendritic cells), & enhances CTL responses against cancer cells
N/ABGB-290PARPBinds to PARP proteins & that interferes with the cells' ability to replicate
N/ABGB-324AXLBinds to AXL & inhibits tumor cell proliferation, survival, & migration in AXL-overexpressing tumor cells
N/ABGB-A317PD-1Immune checkpoint inhibitor that blocks the binding of PD-1 (expressed on activated immune cells) to PD-L 1/2 (overexpressed on certain cancer cells) which restores immune responses against tumor cells; Showing improved efficacy when combined with other immunotherapies Immuno-Oncology News
N/ABGB-A333PD-L1Immune checkpoint inhibitor that blocks PD-L1 from turning off the function of T-cells & activates the immune system to kill PD-L1-expressing tumor cells; Showing improved efficacy when combined with other immunotherapies
N/ABGJ398Pan-FGFRBinds to FGFRs which may result in the inhibition of tumor blood vessel formation & tumor cell proliferation & may induce tumor cell death
N/ABI-754091PD-1Immune checkpoint inhibitor that binds to & blocks the binding of PD-1 (expressed on activated immune cells) to PD-L 1/2 (overexpressed on certain cancer cells) which activates a T-cell mediated immune response against tumor cells; Showing improved efficacy when combined with other immunotherapies
N/ABI-754111LAG3Immune checkpoint inhibitor that binds to LAG3 expressed on TILs which activates a T-cell mediated response against tumor cells leading to a reduction in tumor growth; Showing improved efficacy when combined with other immunotherapies
N/ABI-CON-02HER2ADC composed of a trastuzumab (Herceptin) antibody & a cytotoxic agent; BI-CON-02 binds to HER2 & is internalized by the cancer cell where the cytotoxic agent is released which can inhibit tumor cell division & induce tumor cell death in HER2-overexpressed cells
N/ABLU-9931FGFR4Binds to FGFR4 which may result in the inhibition of tumor blood vessel formation & tumor cell proliferation & may induce tumor cell death
N/ABLZ945CSF1Binds to CSF1 receptors & prevents tumor cell proliferation of CSF1-overexpressing tumor cells & improves anti-tumor cell responses
N/ABMS-986156GITRBinds to & activates the GITR expressed on T-cells which stimulates the immune system & can lead to tumor cell eradication
N/ABMS-986158BETBinds to & inhibits BET proteins (BRD 2/3/4/T) which can prevent tumor cell growth
N/ABMS-986205IDO1IDO1 protein inhibitor & immunomodulator which can increase & restore proliferation & activation of various immune cells; Showing promise in clinical trials that combine IDO inhibitors with antibodies that target the PD-1/PD-L1 pathwayImmuno-Oncology News
N/ABMS-986218CTLA4Binds to CTLA4 expressed on the surface of T-cells which leaves the T-cells free to stay active & cause a CTL-mediated immune attack against tumor cells
N/ABMS-986226ICOSImmune checkpoint inhibitor that binds to ICOS expressed on certain T-cells & activates an immune response against tumor cells; Showing improved efficacy when combined with other immunotherapies
N/ABMS-986249CTLA4Probody & immune checkpoint inhibitor that binds to & blocks the CTLA4 protein on the surface of T-cells which leaves the T-cells free to stay active & attack cancer cells
N/ABMS-986253, MDX-018HuMax-IL8IL-8Antibody that binds to IL-8 thereby inhibiting the binding of IL-8 to its receptors (CXCR 1/2) which decreases proliferation of CXCR 1/2-overexpressing tumor cells
N/ABOS172722ÊMps1Binds to Mps1 which can interfere with the tumor cell's ability to divide & replicate & can induce tumor cell death in Mps1-overexpressing cancer cells
N/ABT1718MT1-MMPBDC composed of an anti-MT1-MMP bicyclic peptide & a cytotoxic agent (DM1); BT1718 binds to MT1-MMP & is internalized by the cancer cell where the cytotoxic agent is released which induces cell death & inhibits the proliferation of MT1-MMP-expressing tumor cells
N/AC188-9STAT3Binds to & inhibits the phosphorylation of STAT3 which prevents binding of STAT3 to DNA sequences which may result in the inhibition of tumor cell proliferation
N/ACAN04IL1RAPBinds to & activates IL1RAP which initiates the innate immune system, stimulates immune cells (e.g. dendritic & NK cells), & results in an enhanced ADCC
N/ACB-103NICDThe Notch signaling pathway plays an important role in cell survival & proliferation; CB-103 may inhibit cell growth & induce cell death in tumor cells in which the Notch signaling pathway is over activated; Exhibits anti-tumor efficacy in a xenograft (tissue) model of human TNBC resistant to other therapies
N/ACB-839GlutaminaseGlutaminase converts glutamine into glutamate; CB-839 inhibits glutaminase which can halt the proliferation & induce cell death of glutamine-dependent tumors which rely on the conversion of glutamine into glutamate for cell growth & survival; Granted Fast Track designation by the FDA in combination with cabozantinib (Cabometyx) for the treatment of metastatic RCC
N/ACDX-1140CD40Monoclonal antibody that may activate a consistent & controlled immune response when it binds to the CD40 receptor
N/ACJM112IL-17aAntibody that binds to IL-17a & inhibits an inflammatory response in the tumor microenvironment which may lead to tumor regression
N/ACORT-125134GRBinds to & blocks the GR which inhibits the proliferation of GR-overexpressing cancer cells
N/A*CPI-006CD73Inhibits CD73 which prevents the degradation of ATP into adenosine. When ATP is available, it promotes immune cell-mediated killing of cancer cells & prevents tumor blood vessel formation and proliferation
N/A*CPI-444Adenosine A2aImmune checkpoint inhibitor that binds to adenosine A2a receptors expressed on surface of immune cells which stimulates anti-tumor immune responses resulting in tumor regression; Showing improved efficacy when combined with other immunotherapies
N/ACPX-POMNICDThe Notch signaling pathway plays an important role in cell survival & proliferation; CPX-POM may inhibit cell growth & induce cell death in tumor cells in which the Notch signaling pathway is over activated
N/ACS1001PD-L1Immune checkpoint inhibitor that blocks PD-L1 from turning off the function of T-cells & activates the immune system to kill PD-L1-expressing tumor cells; Showing improved efficacy when combined with other immunotherapiesPR Newswire
N/ACS1003PD-1Binds to & blocks the binding of PD-1 (expressed on activated immune cells) to PD-L 1/2 (overexpressed on certain cancer cells) which restores immune responses against tumor cells; Showing improved efficacy when combined with other immunotherapies PR Newswire
N/ACS3006MEK 1/2Binds to MEK 1/2 & inhibits cellular proliferation in MEK-expressing tumor cellsPR Newswire
N/ACT7001, ICEC0942CDK7Binds to CDK7 which may inhibit tumor cell growth & proliferation; Inhibiting CDK7 may also help control the estrogen receptor & is showing promise for ER+ breast cancerMedical News Today
N/ACUDC-907PI3K, HDACDual inhibitor which shows an increased inhibition of tumor cell growth & induction of cell death when compared to inhibitors that only target either PI3K or HDAC
N/ACX-2009CD166PDC composed of a cytotoxic agent & recombinant antibody targeting CD166, which is masked by a cleavable peptide; Normal cells cannot cleave the peptide & are therefore protected, but tumor proteases cleave the peptide enabling CX-2009 to bind to, be internalized by, & deliver the cytotoxic agent to CD166-expressing tumor cells
N/ACX5461Pol ITranscription inhibitor that binds to & inhibits Pol I which prevents ribosomal RNA synthesis- a process that plays a key role in cell proliferation & survival
N/ADebio 1347,
FF284,
CH5183284
FGFR 1/2/3Binds to & inhibits FGFR 1/2/3 which halts both tumor cell proliferation & blood vessel formation & can cause cell death in FGFR-overexpressing tumor cellsPR Newswire
N/ADHES0815AHER2ADC composed of the anti-HER2 antibody & a cytotoxic agent (PBD-MA); DHES0815A binds to HER2 & is internalized by the cancer cell where PBD-MA is released which can stop tumor cell growth & induce tumor cell death
N/ADS-3032bMDM2Inhibits the binding of MDM2 to the activation domain of tumor suppressor protein p53; By preventing the MDM2-p53 interaction, the degradation of p53 is inhibited which restores p53 signaling & may lead to cell cycle arrest & programed cell death in MDM2-overexpressing tumor cells
N/A*DSP-0509TLR7Binds to & activates TLR7 which initiates the innate immune system, stimulates immune cells (e.g. dendritic & NK cells), & results in an enhanced ADCC
N/AE7386-CREB/beta-catenin modulator which induces infiltration of T-cells into the tumor & enhances antitumor activity of anti-PD-1 immunotherapies
N/AeFT508MNK 1/2Binds to MNK 1/2 & inhibits tumor cell proliferation of MNK 1/2-overexpressing tumor cells
N/AEGF816EGFRSelectively binds to mutated forms of EGFR which may induce tumor cell death & inhibit tumor growth in EGFR-overexpressing tumor cells; Toxicity profile may be reduced compared to non-selective EGFR inhibitors which inhibit all EGFR-expressing cells
N/AENMD-2076Aurora A,
VEGFR, FGFR, c-Kit, FLT-3, CSFR1
Binds to Aurora A, angiogenic kinases (VEGFR, FGFR), & growth factor kinases (c-Kit, FLT-3, CSFR1) which inhibit cell division, cell proliferation, growth of blood vessels, & induce cell death in tumor cells overexpressing these kinases
N/AETBX-011CEAVaccine that elicits a targeted immune response against CEA-overexpressed tumor cells resulting in inhibition of tumor cell proliferation & induces tumor cell death
N/AETBX-021HER2Vaccine that elicits a targeted immune response against HER2-overexpressed tumor cells resulting in tumor cell deathImmuno-Oncology News
N/AETBX-051BrachyuryTherapeutic cancer vaccine that elicits a targeted CTL immune response against brachyury-overexpressed tumor cells
N/AETBX-061MUC1Therapeutic cancer vaccine that elicits a targeted CTL immune response against MUC1-overexpressed tumor cells
N/AFAZ 053PD-L1Immune checkpoint inhibitor that blocks PD-L1 from turning off the function of T-cells & activates the immune system to kill PD-L1-expressing tumor cells; Showing improved efficacy when combined with other immunotherapies
N/AFF-10832-Chemotherapy drug that uses a liposome to selectively deliver the anti-cancer agent (gemcitabine) which prevents DNA replication & growth; Liposomal delivery of FF-10832 improves drug penetration into tumors & the duration of therapeutic drug effects
N/AFoxy-5Wnt-5aFoxy-5 binds to & activates the Wnt-5a receptors which may inhibit endothelial tumor cell migration & invasion, thereby decreasing metastasis of susceptible tumor cells
N/AFS118LAG3, PD-L1 Immune checkpoint inhibitor that binds to LAG3 expressed on TILs & PD-L1, which activates a T-cell mediated response against tumor cells leading to a reduction in tumor growth; Showing improved efficacy when combined with other immunotherapies
N/AG1T38CDK 4/6Binds to & inhibits CDK 4/6 which may suppress DNA synthesis of tumor cells & inhibit tumor cell growth
N/AG1T48ERSERD that binds to & degrades the estrogen receptor
N/AGBR 1302-101CD3, HER2Redirects cytotoxic T-cells through its CD3 binding arm onto HER2-expressing cancer cells & inhibits tumor cell proliferation & induces tumor cell death
N/AGDC-0077,
RO7113755,
RG6114
PI3K PI3K inhibitor which may result in cell death & growth inhibition in PI3K-overexpressing tumor cells
N/AGDC-0927ERSERD that binds to & degrades the estrogen receptor; In phase 1 clinical trials for ER+/HER2-Neg breast cancer
N/AGDC-9545ERSERD that binds to the ER & induces degradation of the receptor
N/AGI-4000RasYeast-based vaccine that elicits a targeted CTL immune response against Ras-overexpressed tumor cellsNCI News
N/AGI-6207CEAYeast-based vaccine that elicits a targeted CTL immune response against CEA-overexpressed tumor cells
N/AGI-6301BrachyuryVaccine composed of genetically modified yeast that elicits a targeted immune response against brachyury-overexpressed tumor cells
N/AGS-5829BETBinds to BET proteins which prevents interaction with peptides & disrupts gene expression which can lead to inhibition of cell growth in BET-overexpressing tumor cells
N/AGSK1795091TLR4Binds to & activates TLR4 which initiates the innate immune system, stimulates immune cells (e.g. dendritic & NK cells), & results in an activated CTL response against tumor cells
N/AGSK2636771PI3K-betaBinds to PI3K-beta & inhibits activity in the PI3K /Akt/mTOR (PAM) pathway which may result in tumor cell death & growth inhibition in PI3K-beta-expressing and/or PTEN-driven tumor cells
N/AGSK3174998OX40Binds to & activates OX40 to induce proliferation & killing ability of T-cells; Showing promise in clinical trials that combine OX40 agonists (that enhance T-cells' ability) with PD-1 inhibitors (that limit T-cells' ability)NCI News
N/AGWN323GITRBinds to & activates the GITR receptor found on T-cells which stimulates the immune system & can lead to tumor cell eradication
N/AH2EH3EGFR,
HER 2/3
Binds to EGFR & HER 2/3 which may result in inhibition of tumor growth & vascularization of blood vessels (angiogenesis) in tumor cells that overexpress these receptorsGEN News
N/AH3B-6545ERSERCA that inactivates the estrogen receptor by targeting a cysteine not present in other nuclear hormone receptors
N/AHDM201HDM2Inhibits the binding of HDM2 to the activation domain of tumor suppressor protein p53; By preventing the HDM2-p53 interaction, the degradation of p53 is inhibited which may result in restoration of p53 signaling and prevent tumor cell proliferationASH Clinical News
N/AHemay022EGFRBinds to EGFR which may result in inhibition of tumor growth & vascularization of blood vessels (angiogenesis) in EGFR-overexpressing tumor cells
N/AHLX02HER2Trastuzumab (Herceptin) Biosimilar; Binds to HER2 & inhibits tumor cell growth in HER2+ cancer cells
N/AHLX10PD-1Binds to & blocks the binding of PD-1 (expressed on activated immune cells) to PD-L 1/2 (overexpressed on certain cancer cells) which restores immune responses against tumor cells; Showing improved efficacy when combined with other immunotherapies
N/AHM95573RAFBinds to RAF proteins & inhibits proliferation & survival of RAF-overexpressing tumor cells
N/AHS-10241c-METBinds to c-MET which inhibits tumor cell growth & may induce tumor cell death in c-MET-overexpressing tumor cells
N/AHTI-1066c-METADC composed of anti-c-MET antibody & a cytotoxic agent; HTI-1066 binds to c-MET & is internalized by the cancer cell where the cytotoxic agent is released which induces cell death & inhibits the proliferation of c-MET-expressing tumor cells
N/AHu5F9-G4CD47 Antibody that binds to CD47 (expressed on the surface of tumor cells) & prevents the binding of CD47 to its ligand, SIRPa, (expressed on phagocytic cells) which results in phagocytosis of the tumor cell & a T-cell immune response against CD-47-overexpressing tumor cells
N/AIACS-010759OxPhosBinds to & inhibits complex I of the electron transport chain, thereby selectively depriving tumor cells of nutrients & energy, & inhibiting nucleotide & amino acid production, which causes tumor cell death & inhibits cell proliferation
N/AIM156OxPhosBinds to & inhibits complex I of the electron transport chain, thereby selectively depriving tumor cells of nutrients & energy, & inhibiting nucleotide & amino acid production, which causes tumor cell death & inhibits cell proliferation
N/A*IMP321DCBinds to DCs which may result in DC maturation, DC migration to lymph nodes & a cytotoxic T-cell response against tumor cells
N/AIMX-110STAT3, NF-KB1, poly-TKIÊNanoparticle composed of STAT3, NF-KB1, & TKIsÊas well as a low-dose chemotherapy agent (doxorubicin) which may result in the inhibition of tumor cell proliferation & may induce tumor cell death
N/AINCAGN01876GITRBinds to & activates the GITR found on T-cells which stimulates the immune system & can lead to tumor cell eradication
N/AINCAGN01949OX40Binds to & activates OX40 to induce proliferation & killing ability of T-cells; Showing promise in clinical trials that combine OX40 agonists that enhance T-cells' ability with PD-1 inhibitors that limit T-cells' abilityNCI News
N/A*INCB001158ArginaseBinds to & inhibits the breakdown of arginine by arginase which induces the proliferation & activation of T-cells may cause a CTL response against tumor cells
N/AINCB050465PI3K-deltaPI3K inhibitor which decreases proliferation & induces cell death in PI3K-delta-overexpressing tumor cells; PI3K-delta is designed to preserve PI3K signaling in normal cells
N/AINCB052793JAK1Binds to JAK1 and may inhibit tumor cell proliferation in JAK1-expressing tumor cells
N/AINCB054828FGFR2Binds to FGFR2 which may result in the inhibition of tumor blood vessel formation & tumor cell proliferation & may induce tumor cell death
N/AINCB057643BETBinds to BET proteins which prevents interaction with peptides & disrupts gene expression which can lead to inhibition of cell growth in BET-overexpressing tumor cells
N/AINCB062079FGFR4Binds to FGFR4 which may result in the inhibition of tumor blood vessel formation & tumor cell proliferation & may induce tumor cell death
N/AIPI-549PI3K-gammaBinds to & inhibits PI3K-gamma which may result in cell cycle arrest & cell death in PI3K-gamma-expressing tumor cells
N/AJS001PD-1Binds to & blocks the binding of PD-1 (expressed on activated immune cells) to PD-L 1/2 (overexpressed on certain cancer cells) which restores immune responses against tumor cells; Showing improved efficacy when combined with other immunotherapies
N/AJTX-2011ICOSImmune checkpoint inhibitor that binds to ICOS expressed on certain T-cells & activates a CTL immune response against tumor cells; Showing improved efficacy when combined with other immunotherapies
N/AKITE718MAGE-A3/A6A form of immunotherapy called ACT that involves genetically reengineering T-cells (immune cells), taken from a blood sample, to express a specific receptor on the surface of the T-cell. When the altered T-cells are infused back into the patient, they bind to & inhibit the growth of MAGE-A3/A6-overexpressing tumor cells
N/AKN035PD-L1 Immune checkpoint inhibitor that blocks PD-L1 from turning off the function of T-cells & activates the immune system to kill PD-L1 expressing tumor cells; Showing improved efficacy when combined with other immunotherapies
N/ALAG525, IMP701LAG3Immune checkpoint inhibitor that binds to LAG3 expressed on TILs which activates a T-cell mediated response against tumor cells leading to a reduction in tumor growth; Showing improved efficacy when combined with other immunotherapiesImmuno-Oncology News
N/ALCL161IAPBinds to cIAP 1/2 & XIAP & promotes the rapid degradation of these proteins which results in tumor cell death & has an antitumor effect in certain cancers
N/ALHC165TLR7Binds to & activates TLR7 which initiates the innate immune system, stimulates immune cells (e.g. dendritic & NK cells), & results in an enhanced ADCC
N/ALJM716HER3Binds to HER3 & blocks the PI3K signaling pathway which decreases proliferation & induces cell death in HER2-overexpressing tumor cells
N/ALOXO-195TRKBinds to TRK & inhibits the neurotrophin-TRK interaction which may result in apoptosis (cell death) & growth inhibition of cancer cells that overexpress TRK
N/ALOXO-292RETBinds to RET which may inhibit cell growth in RET-overexpressing tumor cells
N/ALSZ102ERSERD that binds to the ER & induces degradation of the receptor
N/ALTT462ERKBinds to the ERK & inhibits ERK-dependent tumor cell proliferation & may lead to tumor cell death
N/ALXH254pan-RAFBinds to RAF proteins & inhibits proliferation & survival of RAF-overexpressing tumor cells
N/ALY2780301AktBinds to & inhibits the activity of Akt, which may result in inhibition of the PI3K/Akt pathways which may stop tumor cell proliferation & lead to tumor cell death
N/ALY2875358c-META humanized IgG4 monoclonal antibody that binds to c-MET which may result in cell death of c-Met-expressing tumor cells
N/ALY3023414PI3K/
mTOR
Dual inhibitor which may result in cell death & growth inhibition of tumor cells overexpressing PI3K and/or mTOR; LY3023414 may also inhibit DNA-PK, thereby inhibiting the ability of tumor cells to repair damaged DNA
N/ALY3300054PD-L1Immune checkpoint inhibitor that blocks PD-L1 from turning off the function of T-cells & activates the immune system to kill PD-L1-expressing tumor cells; Showing improved efficacy when combined with other immunotherapies
N/A*LY3321367TIM3Immune checkpoint inhibitor that binds to TIM3 expressed on certain T cells, which enhances cytotoxic T-cell-mediated tumor cell disintegration & results in a reduction in tumor growth
N/ALY500307ER-betaBinds to & activates ER-beta which elicits tumor suppressive effects in ER-beta-expressing TNBC; Clinical trials at the Mayo Clinic are being developed & should be recruiting in late 2018 Medical Xpress;
Oncotarget
N/ALZM009PD-1Binds to & blocks the binding of PD-1 (expressed on activated immune cells) to PD-L 1/2 (overexpressed on certain cancer cells) which restores immune responses against tumor cells; Showing improved efficacy when combined with other immunotherapies
N/AM6620,
VX-970
ATR Binds to & inhibits ATR which disrupts tumor DNA damage repair & induces cell death; In clinical trials for TNBC
N/AMBG453TIM3Immune checkpoint inhibitor that binds to TIM3 expressed on certain T cells, which enhances cytotoxic T-cell-mediated tumor cell disintegration & results in a reduction in tumor growth
N/AMCLA-128HER 2/3Antibody that binds to & inhibits cell growth & survival in HER 2/3-overexpressing tumor cells; MCLA-128 is engineered for enhanced ADCC in order to recruit & activate immune cells to directly kill tumor cellsOncoTimes;
BC-news;
GlobeNewswire; BC-news
N/AMCS110CSF1Antibody that binds to & blocks CSF1 which allows the immune system to target & destroy tumor cells
N/AMEDI-573IGF 1/2Binds to IGF 1/2 which may result in inhibition of tumor cell proliferation & induction of tumor cell death
N/AMEDI4276HER2ADC composed of a trastuzumab (Herceptin) antibody & a cytotoxic agent (tubulysin); MEDI4276 binds to HER2 & is internalized by the cancer cell where tubulysin is released which can inhibit tumor cell division & proliferation & induce cell death in HER2-overexpressing tumor cells
N/AMEDI6383OX40Binds to & activates OX40 to induce proliferation & killing ability of T-cells; Showing promise in clinical trials that combine OX40 agonists that enhance T-cells' ability with PD-1 inhibitors that limit T-cells' abilityNCI News
N/AMEDI6469OX40Binds to & activates OX40 to induce proliferation & killing ability of T-cells; Showing promise in clinical trials that combine OX40 agonists that enhance T-cells' ability with PD-1 inhibitors that limit T-cells' abilityNCI News
N/AMGA012PD-1Binds to & blocks the binding of PD-1 (expressed on activated immune cells) to PD-L 1/2 (overexpressed on certain cancer cells) which restores immune responses against tumor cells; Showing improved efficacy when combined with other immunotherapies
N/AMGD009CD3DART molecule that redirects T cells, via their CD3 component, to kill B7-H3-expressing cells on a wide variety of solid tumor types
N/AMK-2206AktBinds to Akt (key node in the PI3K/Akt signaling network) thereby inhibiting tumor cell growth & proliferation of Akt-expressing tumors
N/AMK-8353ERKBinds to the ERK & inhibits ERK-dependent tumor cell proliferation & may lead to tumor cell death
N/AMM-302HER2ADC composed of anti-HER2 antibody & a cytotoxic agent (liposomal doxorubicin); MM-302 binds to HER2 receptors & is internalized by the cancer cell where the liposomal doxorubicin is released which can inhibit DNA replication & stop tumor cell growth; In Dec 2016 the phase II HERMIONE trial was halted when MM-302 failed to improve PFS when compared to chemo + trastuzumab (Herceptin) in heavily pretreated HER2+ MBCOncLive
N/AMM-310EphA2ADN composed of anti-EphA2 antibody & docetaxel; MM-310 targets & binds to EphA2-expressing cells (found in 50-100% of major tumor types) which allows for docetaxel to accumulate at the tumor site, inhibit tumor cell growth, & induce tumor cell death
N/A*MM-398,
PEP02,
BAX2398
Onivyde-Chemotherapy drug FDA approved for metastatic pancreatic cancer
N/AmRNA-2416OX40mRNA-2416 is encoded to produce OX40L proteins on the surface of cells which binds to the OX40 receptor expressed on activated T-cells; OX40L/OX40 binding induces proliferation & killing ability of T-cells for an enhanced immune response against tumor cells
N/AMSB0011359C, M7824TGFBR, PD-L1 Fusion protein composed of an antibody (avelumab) fused to the TGFBR which serves as an enhanced immune checkpoint inhibitor. MSB0011359C blocks PD-L1 from turning off the function of T-cells, activates the immune system to kill PD-L1 expressing tumor cells, & "traps" the TGFBR protein rendering it useless which may inhibit the proliferation & migration of TGFBR-overexpressing tumor cellsNCI News
N/AMSB2311PD-L1 Immune checkpoint inhibitor that blocks PD-L1 from turning off the function of T-cells & activates the immune system to kill PD-L1 expressing tumor cells; Showing improved efficacy when combined with other immunotherapies
N/AMSC-1LIFBinds to LIF which blocks the STAT3 signaling pathway & may result in the inhibition of growth & proliferation of LIF-overexpressing tumor cellsNorthern Biologics
N/AMSC2363318A,
M2698
p70S6K, AktBinds to & inhibits the activity of p70S6K & Akt which prevents activation of the PI3K /Akt/mTOR (PAM) signaling pathway & inhibits tumor cell proliferation
N/ANHS-IL12Necrotic tumor cell DNANHS-IL12 is a fusion protein composed of a human antibody (NHS76) & cytokine (IL-12); NHS-IL12 binds to DNA released from necrotic tumor cells & delivers IL12 which stimulates an immune response against tumor cells & inhibits tumor growth
N/ANIS793TGFBRBinds to TGFBR which may inhibit the proliferation & migration of TGFBR-overexpressing tumor cells
N/ANK-92HANK-HANK cells recognize & bind to tumor cells which results in cancer cell disintegration & death as well as an enhanced ADCC
N/ANKTR-214IL-2-betaBinds to & activates IL-2-beta expressed on immune cells which activates NK cells & T-cells for an enhanced immune response against tumor cells, decreasing tumor cell proliferation & inducing tumor cell death
N/ANKTR-262TLRBinds to & activates TLR which initiates the innate immune system, stimulates immune cells (e.g. dendritic cells), & enhances CTL responses against cancer cells
N/ANOV140101, IDX1197HClPARP 1/2Binds to PARP 1/2 & inhibits the tumor cell's ability to repair DNA which enhances DNA strand breaks, promotes instability, & results in tumor cell death
N/ANOV1501, ABL001DLL4,
VEGF
Dual-targeting antibody that binds to DLL4 & VEGF & prevents the growth of blood vessels by tumor cells (angiogenesis)
N/AOBI-821-A purified, natural saponin isolated from the soapbark tree that when co-administered with a vaccine may increase antibody & CTL responses against cancer cells
N/AONC201,
TIC10
Akt, ERKBinds to & inhibits the activity of Akt & ERK, which may result in inhibition of the PI3K/Akt & MAPK/ERK pathways which may inhibit tumor cell proliferation & may lead to tumor cell deathScience Daily
N/AOTS167POMELKBinds to MELK which may lead to inhibition of cell proliferation & survival in MELK-expressing tumor cells
N/APD-0360324CSF1Monoclonal antibody that binds to CSF1 receptors & enhances antitumor T-cell immune responses, which inhibits the proliferation of tumor cells
N/APEN-866HSP90Comprised of HSP90 ligands & a cytotoxic agent (irinotecan); In contrast to ADCs that require binding to cell surface, PEN-866 is an MDC so it is much smaller & can penetrate into the tumor cell by diffusion where it binds to the HSP90 target. Once bound, PEN-866 releases irinotecan which can lead to prolonged DNA damage of the tumor cell
N/APF-04518600OX40Binds to & activates OX40 to induce proliferation & killing ability of T-cells; Showing promise in clinical trials that combine OX40 agonists that enhance T-cells' ability with PD-1 inhibitors that limit T-cells' abilityNCI News
N/APF-06647020PTK7ADC composed of an anti-PTK7 antibody & a cytotoxic agent (auristatin); PF-06647020 binds to PTK7 & is internalized by the cancer cell where the auristatin is released which can induce cell death of PTK7-overexpressing tumor cells; In phase 1 clinical trials for mTNBC
N/APF-06671008CDH3CDH3 & inhibits the proliferation of CDH3-expressing tumor cells; FDA approved in 2012Science Daily
N/APF-06804103HER2ADC composed of an anti-HER2 specific antibody & a cytotoxic agent (Auristatin-0101); PF-06804103 binds to HER2 & is internalized by the tumor cell where Auristatin-0101 is released which inhibits tumor cell growth & induces tumor cell death in HER2+ cancer cells
N/APLX8394BRAFBinds to & inhibits the BRAF kinase which may inhibit tumor cell proliferation in BRAF-expressing tumor cells & in tumors that are resistant to other BRAF inhibitor therapies
N/APQR 309Pan-PI3K/
mTOR
Dual inhibitor which may result in cell death & growth inhibition of tumor cells overexpressing PI3K and/or mTOR
N/APRS-343HER2, CD137Bispecific fusion protein that targets HER2 & CD137; PRS-343 activates CD137-expressing immune cells to form clusters which stimulate an immune response against HER2+ tumor cellsMechanism of Action Video
N/APT-112-Novel chemotherapeutic agent designed to avoid the toxicity & drug resistance mechanisms of conventional chemotherapy
N/APU-H71HSP90HSP90 is a chaperone protein upregulated in a variety of tumor cells & regulates the folding, stability & degradation of many oncogenic signaling proteins; PU-H71 binds to HSP90 which may inhibit tumor cell proliferation & survival
N/APVX-410XBP1-US, XBP1-SP, CD138, CS1Multipeptide cancer vaccine that targets tumor-associated antigens overexpressed on the surface of MM cells & stimulates a CTL anti-tumoral response
N/ARiMO-301IDO1Nanosized MOF that can be used in combination with radiation therapy to deliver an IDO1 inhibitor immunotherapy drug Chemical & Engineering News
N/ARG6058, MTIG7192ATIGITImmune checkpoint inhibitor that blocks the interaction of TIGIT with the PVR which activates a T-cell-mediated immune response against tumor cells
N/A*RGX-104LXRTargets & activates the LXR resulting in improved ability of T-cells to attack tumors; Obtained FDA orphan drug designation in several solid tumor types
N/ARO6870810BETBinds to BET proteins (BRD 2/3/4/T) which can inhibit tumor cell growth & development
N/ARO6874281FAP-alphaRecombinant fusion protein comprised of an antibody linked to an engineered IL-2v that binds to FAP-alpha which activates NK cells & cytotoxic T-cells for an enhanced immune response against tumor cells, decreasing tumor cell proliferation & inducing tumor cell death
N/ARO6958688CEA, CD3Bispecific antibody that targets the CEA (expressed on tumor cells) & CD3 (expressed on T-cells); RO6958688 binds to both T-cells & CEA-expressing tumor cells resulting in a potent CTL response against CEA-expressing tumor cells
N/ARO7009789CD40Monoclonal antibody that may activate B cells & T cells (an immune response) when it binds to the CD40 receptor
N/ARO7198457-Personalized cancer vaccine that targets tumor-associated antigens & stimulates a CTL anti-tumoral response
N/ARXC004PORCNPORCN is a key enzyme in the Wnt signaling pathway; RXC004 binds to PORCN which suppresses the Wnt signaling pathway and may inhibit tumor cell growth
N/ARXDX-106Pan-TAM Binds to TAM kinases (TYRO3, AXL, & MER) & works in synergy with immune checkpoint inhibitors to restore the body's immune-system response against tumors & eliminate tumor cellsImmuno-Oncology News
N/AS81695Mps1Binds to Mps1 which can interfere with the tumor cell's ability to divide & replicate & can induce tumor cell death in Mps1-overexpressing cancer cells
N/ASAR408701CEACAM5ADC composed of anti-CEACAM5 antibody & a cytotoxic agent; SAR408701 binds to CEACAM5 receptors & is internalized by the cancer cell where the cytotoxic agent is released which can inhibit tumor cell growth, migration, & invasion
N/ASAR439859ERSERD that binds to & degrades the estrogen receptor
N/ASC10914PARP 1/2Binds to PARP 1/2 & inhibits the tumor cell's ability to repair DNA which enhances DNA strand breaks, promotes instability, & results in tumor cell death
N/ASD-101TLR9Binds to & activates TLR9 which stimulates T-helper cells against a specific pathogen
N/ASFX-01SulforadexWntSuppresses the Wnt signaling pathway which may inhibit tumor cell growth; In phase 2 clinical trials in combination with hormone therapies for ER+ MBC
N/ASGN-2FFFucosylationFucosylation is the process of adding fucose sugar units to a molecule & is essential for tumor progression; Inhibition of fucosylation may stimulate the immune system to slow the growth & spread of cancer cells
N/ASHR-1210PD-1Immune checkpoint inhibitor that binds to & blocks the binding of PD-1 (expressed on activated immune cells) to PD-L 1/2 (overexpressed on certain cancer cells) which restores immune responses against tumor cells; Showing improved efficacy when combined with other immunotherapies
N/ASHR-1316PD-L1 Immune checkpoint inhibitor that blocks PD-L1 from turning off the function of T-cells & activates the immune system to kill PD-L1 expressing tumor cells; Showing improved efficacy when combined with other immunotherapies
N/ASHR-6390CDK 4/6Binds to CDK 4/6 which may suppress DNA synthesis of tumor cells & inhibit tumor cell growth
SHR-9146IDO1IDO1 protein inhibitor & immunomodulator which can increase & restore proliferation & activation of various immune cells; Showing promise in clinical trials that combine IDO inhibitors with antibodies that target the PD-1/PD-L1 pathway
N/ASM08502WntBlocks Wnt signaling pathway which may inhibit the proliferation of cancer cells in which the Wnt signaling pathway is overactivated
N/ASV-BR-1-GMBria-IMT-The expressed GM-CSF protein of this breast cancer vaccine is a potent stimulator of the immune system; SV-BR-1-GM secretes GM-CSF which may cause a CTL response against breast cancer cells Cancer Immunity & Immunotherapy
N/ASY-1365CDK7SY-1365 binds to CDK7 which may inhibit tumor cell proliferation
N/ASym021PD-1Binds to & blocks the binding of PD-1 (expressed on activated immune cells) to PD-L 1/2 (overexpressed on certain cancer cells) which restores immune responses against tumor cells; Showing improved efficacy when combined with other immunotherapies
N/ASym022LAG3Immune checkpoint inhibitor that binds to LAG3 expressed on TILs which activates a T-cell mediated response against tumor cells leading to a reduction in tumor growth; Showing improved efficacy when combined with other immunotherapies
N/ASym023TIM3Immune checkpoint inhibitor that binds to TIM3 expressed on certain T cells, which enhances cytotoxic T-cell-mediated tumor cell disintegration & results in a reduction in tumor growth
N/ASYN001EGFRAntibody fusion molecule in pre-clinical trials that inhibits both the development & arrangement of blood vessels in tumors; Showing promise for TNBCBreastcancer-news
N/AT-1101HEC1-Nek2Binds to HEC1-Nek2 & disrupts mitosis which inhibits tumor cell proliferation & may induce tumor cell death; Most drugs that target the mitotic machinery of cells have severe pathological side effects, but targeting the HEC1/Nek2 pathway shows no apparent side effects
N/ATAK-659SYKBinds to & inhibits the activity of SYK which can limit tumor cell proliferation
N/ATAS-0728, TPC107HER2Binds to HER2 & blocks the signaling pathway for both HER2 & HER3 which inhibits tumor cell proliferation & blood vessel growth in HER2/3-overexpressing cancer cells
N/ATAS-117Pan-AktBinds to Akt (key node in the PI3K/Akt signaling network) thereby inhibiting tumor cell growth & proliferation in Akt-expressing tumors
N/ATAS-119, TAS-2104Aurora ABinds to Aurora A kinase which inhibits cell division, proliferation & may induce cell death in Aurora A-overexpressing tumor cells
N/ATHZ1CDK7Binds to CDK7 which may inhibit tumor cell growth & proliferation; Inhibiting CDK7 may also help control the estrogen receptor & is showing promise for ER+ breast cancer that has become resistant to standard therapiesScience Daily
N/ATK006 (Denosumab biosimilar)RANKLA human monoclonal antibody that binds to the RANKL on bone cells for the treatment of osteoporosis, metastases to bone, etc
N/ATNO155SHP2Binds to SHP2 & prevents MAPK signaling which may inhibit growth & proliferation of SHP2-expressing tumor cells
N/ATP-0184ALK2Binds to ALK2 which inhibits tumor cell proliferation of ALK2-overexpressing tumor cells
N/ATPX-0005NTRK; ROS1;
ALK; Src; FAK
Multi-kinase Inhibitor; Binds to NTRK 1/2/3, ROS1, ALK, the Src proto-oncogene, & FAK which can lead to inhibition of growth & proliferation in tumor cells that express these kinases; Granted orphan drug designation by FDA for NSCLC in June 2017
N/ATSR-022TIM3Immune checkpoint inhibitor that binds to TIM3 expressed on certain T cells, which enhances cytotoxic T-cell-mediated tumor cell disintegration & results in a reduction in tumor growth
N/ATSR-033LAG3Immune checkpoint inhibitor that binds to LAG3 expressed on TILs which activates a T-cell mediated response against tumor cells leading to a reduction in tumor growth; Showing improved efficacy when combined with other immunotherapies
N/ATSR-042PD-1Binds to & blocks the binding of PD-1 (expressed on activated immune cells) to PD-L 1/2 (overexpressed on certain cancer cells) which restores immune responses against tumor cells; Showing improved efficacy when combined with other immunotherapies
N/ATTC-352ER-alphaSHERPA that binds to & activates ER-alpha, which elicits tumor suppressive effects in ER-alpha-expressing breast cancers; SHERPAs are showing promise for heavily treated breast cancers resistant to standard hormone therapies, while having less gynecological adverse side effects
N/ATVB-2640FASNBinds to & blocks FASN preventing the synthesis of palmitate needed for tumor cell growth & survival
N/AU3-1402HER3ADC composed of an anti-HER3 antibody (patritumab) & cytotoxic agent (DX 8951); U3-1402 binds to HER3 receptors & is internalized by the cancer cell where DX 8951 is released which can inhibit DNA replication & induce cell death of HER3-overexpressing tumor cells
N/AW0101IGFR-1ADC composed of an anti-IGFR-1 antibody & cytotoxic agent (auristatin derivative); W0101 binds to IGFR-1 & is internalized by the cancer cell where the auristatin derivative is released which can inhibit DNA replication & induce cell death of IGFR-1-overexpressing tumor cells
N/AWX-0593ALKBinds to & inhibits the ALK which stops tumor cell growth of ALK-overexpressing tumor cells
N/AXMT-1522HER2ADC composed of an anti-HER2 antibody & cytotoxic agent (auristatin); XMT-1522 binds to HER2 receptors & is internalized by the cancer cell where auristatin is released which can inhibit proliferation & induce cell death of HER2-overexpressing tumor cells; The attachment of multiple auristatin molecules means XMT-1522 can effectively kill tumors expressing low amounts of the HER2 protein
N/AZW25HER2Dual HER2 signal blockade that binds to HER2 receptors to 1) inhibit tumor cell proliferation & 2) induce a CTL & ADCC response to recruit & activate immune cells to directly kill HER2-overexpressed tumor cells


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