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Table 2 Summary of HGF/Met inhibitors currently in clinical trials

From: The Met oncogene and basal-like breast cancer: another culprit to watch out for?

Agent Type Targets Phase of development Comments
AMG102 (Amgen) Antibody Human HGF Phase 1/2 Tested in small-cell lung cancer, metastatic colorectal carcinoma, malignant glioma, prostate cancer, renal cell carcinoma, gastric or esophagogastric junction cancer, mesothelioma, ovarian cancer or peritoneal cancer
SCH900105 (Aveo Pharmaceuticals) Antibody Human HGF Phase 1/2 Tested in nonsmall-cell lung cancer
MetMab (Genentech) Monovalent antibody Human Met Phase 1/2 Tested in nonsmall-cell lung cancer
ARQ197 (ArQule) Selective small-molecule inhibitor, non-ATP competitive Met Phase 1/2 Tested in nonsmall-cell lung cancer, metastatic colorectal carcinoma, pancreatic adenocarcinoma, hepatocellular carcinoma, gastric carcinoma, germ cell tumors, renal cell carcinoma, alveolar soft part sarcoma, clear cell sarcoma
JNJ-38877605 (Johnson and Johnson) Selective small-molecule inhibitor, ATP competitive Met Phase 1  
EMD-1214063 (EMD Serono) Selective small-molecule inhibitor, ATP competitive Met Phase 1  
INCB-028060 (Incyte) Selective small-molecule inhibitor, ATP competitive Met Phase 1  
MK-8033 (Merck) Selective small-molecule inhibitor, ATP competitive Met, Ron (10-fold less active) Phase 1  
PF-02341066 (Pfizer) Multikinase inhibitor, ATP competitive Met, ALK Phase 1/2 Tested in nonsmall-cell lung cancer
GSK-1363089/XL880 (Exelixis) Broad-spectrum kinase inhibitor, ATP competitive Met, Ron, VEGFR1 to VEGFR3, PDGFR, Kit, Flt-3, Tie-2 Phase 1/2 Tested in gastric cancer, nonsmall-cell lung cancer, papillary renal-cell carcinoma
BMS-907351/XL184 (Exelixis) Broad-spectrum kinase inhibitor, ATP competitive Met, VEGFR2, Ret, Kit, Flt-3, Tie-2 Phase 1/2/3 Tested in medullary thyroid cancer, nonsmall-cell lung carcinoma, glioblastoma, astrocytic tumors
MP470 (SuperGen) Broad-spectrum kinase inhibitor, ATP competitive Met, Ret, Rad51, mutant forms of Kit, PDGFR, Flt-3 Phase 1b Tested in neuroendocrine tumors, lung cancer, triple-negative breast cancer
MGCD265 (Methylgene) Broad-spectrum Kinase inhibitor, ATP competitive Met, Ron, VEGFR1 to VEGFR3, Kit, Flt-3, Tie-2 Phase 1  
MK-2461 Broad-spectrum kinase inhibitor, ATP competitive Met, KDR, FGFR1 to FGFR3, Flt-1, Flt-3, Flt-4 Phase 1 completed  
  1. FGFR, fibroblast growth factor receptor; HGF, hepatocyte growth factor; PDGFR, platelet-derived growth factor receptor; VEGFR, vascular endothelial growth factor receptor.