Drug Class Detail

Drug Class MET Inhibitor

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Drug Name Trade Name Synonyms Drug Classes Drug Description
AMG 337 MET Inhibitor 50 AMG 337 inhibits c-MET and may induce cell death in tumors overexpressing c-MET or expressing constitutively activated c-MET (NCI Drug Dictionary).
LCRF-0004 MET Inhibitor 50 RON Inhibitor 10 LCRF-0004 inhibits MST1R (RON) and MET, which may result in decreased tumor cell proliferation (PMID: 25953155).
PF-0461903 MET Inhibitor 50 PF-0461903 is a kinase inhibitor of c-Met, which may result in inhibition of the Mapk signaling pathway (PMID: 22745804).
Foretinib GSK1363089G|XL880|EXEL-2880 MET Inhibitor 50 ROS1 Inhibitor 14 TrkA Receptor Inhibitor 7 VEGFR2 Inhibitor 34 Foretinib (GSK1363089) is a multi-kinase inhibitor with activity against several receptor tyrosine kinases, including MET, KDR (VEGFR2), as well as ROS1 and NTRK fusions, which may result in decreased tumor angiogenesis and growth (PMID: 19808973, PMID: 26372962, PMID: 29463555).
BPI-9016M AXL Inhibitor 24 MET Inhibitor 50 BPI-9016M is a small molecule that inhibits MET and AXL and has potential anti-tumor activity (PMID: 29028616, J Clin Oncol 2018 36:15_suppl, e21108-e21108).
MK2461 MET Inhibitor 50 PDGFR Inhibitor (Pan) 27 RON Inhibitor 10 VEGFR1 Inhibitor 4 MK2461 inhibits wild-type and activated forms of MET, and also has activity against VEGFR1 (FLT1), MST1R (RON), and PDGFR resulting in inhibition of downstream signaling and decreased tumor growth (PMID: 20145145).
OSI-296 MET Inhibitor 50 RON Inhibitor 10 OSI-296 selectively inhibits MET and MST1R (RON), potentially resulting in decreased tumor cell proliferation (PMID: 23773865).
cMet RNA CAR T cells cMet CAR-mRNA electroporated autologous T lymphocytes MET Inhibitor 50 cMet RNA CAR T cells are autologous T-cells transfected with RNA that codes for a chimeric antigen receptor comprised of a portion of anti-Met and CD3-zeta chain linked to CD-137, which targets T-cells to c-MET expressing tumor cells, resulting in selective toxicity (NCI Drug Dictionary).
Ningetinib CT053PTSA AXL Inhibitor 24 MET Inhibitor 50 VEGFR2 Inhibitor 34 Ningetinib inhibits cMet, Vegfr2, and Axl, which may synergistically inhibits tumor cell growth (Cancer Res 2014;74(19 Suppl):Abstract nr 1755).
RXDX-106 AXL Inhibitor 24 MET Inhibitor 50 RXDX-106 is a small molecule inhibitor of TAM family kinases (Axl, Mer, and Tyro3) and cMet that promotes anti-tumor immune response, resulting in tumor growth inhibition (Eur J Cancer, Vol 69, Supplement 1, December 2016, Page S31).
NVP-BVU972 MET Inhibitor 50 NVP-BVU972 inhibits MET, potentially resulting in decreased growth of MET-driven tumor cells (PMID: 21697284).
SGX523 MET Inhibitor 50 SGX523 is a highly selective, ATP-competitive inhibitor of MET that blocks Met signaling, resulting in cell death in tumor cells (PMID: 19934279).
Capmatinib INC280 MET Inhibitor 50 Capmatinib (INC280) inhibits c-MET and may induce cell death in tumors over expressing c-MET or expressing constitutively activated c-MET (NCI Drug Dictionary).
S-49076 S49076 AXL Inhibitor 24 FGFR1 Inhibitor 21 FGFR2 Inhibitor 15 FGFR3 Inhibitor 12 MET Inhibitor 50 S-49076 is a multi-kinase inhibitor that inhibits wild-type and mutant forms of MET and FGFR1/2, as well as FGFR3, AXL, and MER, resulting in decreased downstream signaling, and potentially resulting in decreased tumor growth (PMID: 23804704).
Glesatinib MGCD265 AXL Inhibitor 24 MET Inhibitor 50 RON Inhibitor 10 VEGFR Inhibitor (Pan) 30 Glesatinib (MGCD265) inhibits several tyrosine kinases including MET, MST1R (RON), and AXL, as well as VEGFR1-3, and TIE2, which may result in decreased tumor growth (PMID: 25806189, PMID: 26555154).
Savolitinib HMPL-504|AZD6094|Volitinib MET Inhibitor 50 Savolitinib (AZD6094) is a selective MET inhibitor, which inhibits MET kinase activity, resulting in decreased downstream signaling, and may inhibit growth of MET-expressing tumors (PMID: 25248999).
INCB028060 MET Inhibitor 50 INCB028060 is a MET inhibitor, which may induce cell death in cells overexpressing c-MET (NCI Drug Dictionary).
Tepotinib MSC2156119J MET Inhibitor 50 Tepotinib (MSC2156119J) selectively binds to the proto-oncogene hepatocyte growth factor receptor (HGFR or c-Met), which inhibits c-Met phosphorylation and disrupts c-Met-mediated signaling pathways, thereby suppressing tumor growth in tumor cells with activated or overexpression of c-Met protein (NCI Drug Dictionary).
SU11274 MET Inhibitor 50 RON Inhibitor 10 SU11274 is an inhibitor of MET and MST1R (RON), which prevents activation of downstream signaling, and decreases tumor cell proliferation and migration (PMID: 14617781, PMID: 21543897).
CBT-101 MET Inhibitor 50 CBT-101 is a Met inhibitor that prevents Met phosphorylation and signal transduction to block tumor cell proliferation (NCI Drug Dictionary).
Tivantinib ARQ197|ARQ 197|ARQ-197 MET Inhibitor 50 Tivantinib (ARQ197) is a selective MET inhibitor, which may induce cell death in tumor cells overexpressing MET, although the antimitotic effect may be more responsible for the anti-tumor activity (PMID: 28246274).
MGCD516 Sitravatinib AXL Inhibitor 24 DDR1 Inhibitor 8 DDR2 inhibitor 7 KIT Inhibitor 48 MET Inhibitor 50 RET Inhibitor 36 Trk Receptor Inhibitor (Pan) 23 VEGFR Inhibitor (Pan) 30 MGCD516 (Sitravatinib) inhibits several receptor tyrosine kinases including AXL, MET, KIT, VEGFR1-3, RET family members, TRK family members, DDR, and Eph family members, resulting in abrogation of downstream signaling and decreased cell proliferation in tumors overexpressing the target proteins (PMID: 26675259).
SAR125844 MET Inhibitor 50 SAR125844 is a selective inhibitor of MET, which inhibits MET activation and downstream pathway signaling, and potentially results in decreased growth of MET-driven tumors (PMID: 25504634).
SIM-89 MET Inhibitor 50 TrkA Receptor Inhibitor 7 SIM-89 is an inhibitor of c-MET, TRKA, and AMPK, which may result in antitumor activity including inhibition of cell proliferation and suppression of cell migration (PMID: 28332364).
EMD 1204831 MET Inhibitor 50 EMD 1204831 is a selective inhibitor of MET, which inhibits MET signaling, potentially resulting in increased cell death in MET-expressing tumors (NCI Drug Dictionary).
KRC-00715 MET Inhibitor 50 KRC-00715 is a selective small molecule inhibitor of Met, which reduces Met activation potentially leading to decreased growth of Met-expressing tumor cells (PMID: 26801760).
Crizotinib Xalkori PF-02341066 ALK Inhibitor 19 MET Inhibitor 50 RON Inhibitor 10 ROS1 Inhibitor 14 Xalkori (crizotinib), inhibits ALK kinase, ALK fusion proteins, c-Met, ROS1 fusion proteins, and MST1R (RON), resulting in growth inhibition of tumor cells (PMID: 26951079, PMID: 22617245). Xalkori (crizotinib) is FDA approved for use in patients with ALK or ROS1 positive non-small cell lung cancer (FDA.gov).
Golvatinib E7050 EPHB4 Inhibitor 6 MET Inhibitor 50 VEGFR2 Inhibitor 34 Golvatinib (E7050) is a dual kinase inhibitor of c-Met and KDR (VEGFR2), which inhibits cell growth and proliferation (PMID: 25458359).
KTN0073-IgG2 MET Antibody 13 MET Inhibitor 50 KTN0073-IgG2 is a MET targeted antibody engineered to an IgG2 isotype, which inhibits ligand binding and induces degradation of both wild-type and mutant forms of MET, resulting in decreased tumor cell proliferation, including tumor cells harboring MET mutations and/or amplification (PMID: 27550450).
BMS-754807 ALK Inhibitor 19 Aurka Inhibitors 23 Aurkb Inhibitors 17 IGF-1R Inhibitor 17 MET Inhibitor 50 TrkA Receptor Inhibitor 7 BMS-754807 is a multi-kinase inhibitor with activity against IGF-1R, insulin receptor, MET, ALK, TRKA, TRKB, AURKA, and AURKB, potentially resulting in decreased tumor cell proliferation (PMID: 25748921).
Bozitinib PLB1001|PLB-1001 MET Inhibitor 50 Bozitinib (PLB-1001) is an ATP-competitive, small molecule inhibitor of MET, which is able to permeate the blood brain barrier and may inhibit downstream signaling and block tumor growth (PMID: 30343896).
MRX34 BCL2 inhibitor 15 c-MYC Inhibitor 9 MET Inhibitor 50 MRX34 is a liposomal formulation containing a nucleotide that mimics the human tumor suppressor microRNA (miRNA) miR-34, with potential antineoplastic activity through inhibition of MYC, MET, BCL2, CCND1 and CTNNB1 (NCI Drug Dictionary; PMID: 24657911).
PHA-665752 MET Inhibitor 50 PHA-665752 is a small molecule inhibitor of MET, which inhibits MET kinase activity and downstream signaling, potentially resulting in increased apoptosis and decreased proliferation and migration of tumor cells (PMID: 14612533).
Cabozantinib Cometriq Cabometyx|Cabozantinib-s-malate|XL184 AXL Inhibitor 24 FLT3 Inhibitor 48 KIT Inhibitor 48 MET Inhibitor 50 RET Inhibitor 36 ROS1 Inhibitor 14 VEGFR2 Inhibitor 34 Cometriq (Cabometyx, cabozantinib) inhibits several receptor tyrosine kinases, including VEGFR2, FLT3, AXL, MET, RET, ROS1 fusions, and c-KIT (PMID: 27370605, PMID: 21926191). Cometriq (cabozantinib) is FDA approved for medullary thyroid cancer and Cabometyx (cabozantinib) is FDA approved for advanced renal cell carcinoma and in sorafenib previously treated hepatocellular carcinoma (FDA.gov).
TAS-115 MET Inhibitor 50 VEGFR2 Inhibitor 34 TAS-115 is a small molecule inhibitor of MET and KDR (VEGFR2), which may lead to angiogenesis blockade and tumor regression (PMID: 24140932).
BMS-777607 ASLAN002 AXL Inhibitor 24 MET Inhibitor 50 RON Inhibitor 10 BMS-777607 (ASLAN002) is a small molecule that inhibits c-MET, MST1R (RON), and AXL, resulting in decreased downstream pathway activation, potentially resulting in decreased tumor cell growth and metastasis (PMID: 20515943, PMID: 24233399, PMID: 26555154).
AMG208 MET Inhibitor 50 AMG 208 is a small molecule inhibitor of c-MET, which blocks c-MET activation, resulting in inhibition of downstream signaling and potentially resulting in decreased growth of c-MET expressing tumor cells (NCI Drug Dictionary).
KRC-00509 MET Inhibitor 50 KRC-00509 is a selective small molecule inhibitor of Met, which reduces Met activation potentially leading to decreased growth of Met-expressing tumor cells (PMID: 26801760).
EMD 1214063 MET Inhibitor 50 EMD 1214063 selectively binds to MET tyrosine kinase and disrupts MET signal transduction pathways, which may induce apoptosis in tumor cells over expressing this kinase (NCI Drug Dictionary).
PF-04217903 MET Inhibitor 50 PF-04217903 binds to MET and inhibits its activation, resulting in decreased activation of downstream signaling, and potentially resulting in decreased tumor cell growth and migration and increased tumor cell death (NCI Drug Dictionary).
KTN0073-IgG1 MET Antibody 13 MET Inhibitor 50 KTN0073-IgG1 is a chimeric anti-MET antibody comprised of a rodent variable region and human IgG1 region, which inhibits phosphorylation of MET and induces MET degradation, potentially resulting in decreased proliferation of tumor cells harboring wild-type or mutant MET (PMID: 27550450).
Altiratinib DCC-2701 MET Inhibitor 50 Trk Receptor Inhibitor (Pan) 23 Altiratinib (DCC-2701) is an inhibitor of MET, VEGFR2, TIE2, and Trk that decreases endothelial cell survival and may inhibit cell proliferation and increase cell death in tumors expressing these factors (NCI Drug Dictionary).
AMG 458 MET Inhibitor 50 RON Inhibitor 10 AMG 458 inhibits wild-type and mutant forms of MET and has additional activity against MST1R (RON), resulting in decreased tumor growth (PMID: 20015007).
JNJ 38877605 MET Inhibitor 50 JNJ 38877605 binds to MET and prevents its activation, resulting in decreased downstream signaling and potentially resulting in increased cell death of MET-overexpressing tumor cells (NCI Drug Dictionary).
Amuvatinib MP470|HPK56 AXL Inhibitor 24 FLT3 Inhibitor 48 KIT Inhibitor 48 MET Inhibitor 50 PDGFR-alpha Inhibitor 7 RET Inhibitor 36 Amuvatinib (MP470) is a multi-kinase inhibitor, with activity against KIT, MET, AXL, RET, FLT3, and PDGFR-alpha, that also inhibits Rad51 induction, which may enhance the efficacy of chemotherapeutic agents (PMID: 17325667, PMID: 21903282, PMID: 20563581).
NPS-1034 AXL Inhibitor 24 MET Inhibitor 50 NPS-1034 inhibits AXL and MET, including mutant forms of MET, as well as other kinases, which potentially results in decreased tumor cell growth and may overcome MET or AXL mediated drug resistance (PMID: 24173966, PMID: 24165158).
BAY-853474 MET Inhibitor 50 BAY-853474 inhibits MET, resulting in decreased proliferation of MET-dependent tumor cells (PMID: 24959084).
MK8033 MET Inhibitor 50 RON Inhibitor 10 MK8033 inhibits MET and MST1R (RON), potentially resulting in decreased downstream signaling and reduced tumor growth (PMID: 23379595, PMID: 23792360).
Emibetuzumab LY2875358 MET Antibody 13 MET Inhibitor 50 Emibetuzumab (LY2875358) is MET-targeted antibody, which inhibits binding of the MET ligand HGF and promotes internalization and downregulation of MET, resulting in decreased HGF-dependent and HGF-independent signaling and potentially leading to decreased growth of MET-expressing tumors (PMID: 27803065, PMID: 25231402).
Merestinib LY2801653 AXL Inhibitor 24 DDR1 Inhibitor 8 DDR2 inhibitor 7 FLT3 Inhibitor 48 MET Inhibitor 50 RON Inhibitor 10 ROS1 Inhibitor 14 Trk Receptor Inhibitor (Pan) 23 Merestinib (LY2801653) inhibits several receptor tyrosine kinases including MET, MST1R (RON), AXL, MERTK, TYRO3, ROS1 fusions, PDGFRA, FLT3, TEK, DDR1/2, MKNK1/2, and NTRK1/2/3 with greatest activity against NTRK1, and may result in decreased tumor growth (PMID: 23275061, PMID: 24305878, PMID: 29568395).
Molecular Profile Protein Effect Treatment Approaches
MET over exp no effect HGF Antibody MET Antibody MET Inhibitor
MET D1228N gain of function MET Inhibitor
MET M1131T gain of function - predicted MET Inhibitor
MET L1213V gain of function MET Inhibitor
MET E168D unknown MET Inhibitor
MET amp no effect HGF Antibody MET Antibody MET Inhibitor
MET Y1248H gain of function MET Inhibitor
MET M1268T gain of function MET Inhibitor
MET V1238I gain of function MET Inhibitor
MET R1184Q gain of function - predicted MET Inhibitor
MET H1124D gain of function MET Inhibitor
MET Y1003fs gain of function - predicted MET Antibody MET Inhibitor
MET Y1230D gain of function MET Inhibitor
MET T1010I unknown MET Inhibitor
MET L1195V gain of function MET Inhibitor
MET H1112L gain of function MET Inhibitor
MET M1149T gain of function - predicted MET Inhibitor
MET Y1230H gain of function MET Inhibitor
MET Y1003* gain of function MET Antibody MET Inhibitor
MET H1112R gain of function - predicted MET Inhibitor
MET act mut gain of function MET Inhibitor
MET H1112Y gain of function MET Inhibitor
MET M1250T gain of function MET Inhibitor
MET N1118Y gain of function MET Inhibitor
MET D1228H gain of function MET Inhibitor
MET D1246H gain of function MET Inhibitor
MET V1206L gain of function MET Inhibitor
MET R988C gain of function MET Inhibitor
MET Y1235D gain of function MET Inhibitor
MET Y1230C gain of function MET Inhibitor
MET V1110I gain of function MET Inhibitor
MET del exon14 gain of function MET Antibody MET Inhibitor
MET F1200I gain of function - predicted MET Inhibitor