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 | Â |
EMD-1214063 (EMD Serono) | Selective small-molecule inhibitor, ATP competitive | Met | Phase 1 | Â |
INCB-028060 (Incyte) | Selective small-molecule inhibitor, ATP competitive | Met | Phase 1 | Â |
MK-8033 (Merck) | Selective small-molecule inhibitor, ATP competitive | Met, Ron (10-fold less active) | Phase 1 | Â |
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 | Â |
MK-2461 | Broad-spectrum kinase inhibitor, ATP competitive | Met, KDR, FGFR1 to FGFR3, Flt-1, Flt-3, Flt-4 | Phase 1 completed | Â |