Table 2

Summary of HGF/Met inhibitors currently in clinical trials

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


FGFR, fibroblast growth factor receptor; HGF, hepatocyte growth factor; PDGFR, platelet-derived growth factor receptor; VEGFR, vascular endothelial growth factor receptor.

Gastaldi et al. Breast Cancer Research 2010 12:208   doi:10.1186/bcr2617