Table 1.
Representative c-Met Inhibitors with Clinical Significance
| Name | Type | Mechanism | Clinical Trials of c-Met Cancer Types | Other Targets |
|---|---|---|---|---|
| Cabozantinib | Nonselective TKI | ATP competitive | RCC (Phase 2), HCC (Phase 4), Cervical Cancer (Phase 2), CRC (Phase 1), NSCLC (Phase 2), PSCC (Phase 2), Neuroendocrine Tumors (Phase 1), UC (Phase 2), Prostate Cancer (Phase 2), Breast Cancer (Phase 2), Esophageal Cancer (Phase 2), Melanoma (Phase 2), Thyroid Cancer (Phase 3), AML (Phase 1), HNSCC (Phase 2), Pancreatic Cancer (Phase 2), BCa (Phase 2) | VEGFR2, FLT3, KIT, AXL, RET |
| Crizotinib | Nonselective TKI | ATP competitive | Gastric Cancer (Phase 2), NSCLC (Phase 4), Prostate Cancer (Phase 1), Lymphoma (Phase 2) | ALK, ROS1 |
| Foretinib | Nonselective TKI | ATP competitive | HCC (Phase 1), Breast Cancer (Phase 2), NHSCC (Phase 2), RCC (Phase 2), NSCLC (Phase 1) | KDR |
| Golvatinib | Nonselective TKI | ATP competitive | Gastric Cancer (Phase 1), Solid Tumors (Phase 1) | VEGFR2 |
| Tivantinib | Nonselective TKI | Non-ATP competitive | HCC (Phase 3), NSCLC (Phase 2), CRC (Phase 2), Solid Tumors (Phase 1), Pancreatic Neoplasms (Phase 2) | - |
| Savolitinib | Selecitve TKI | ATP competitive | NSCLC (Phase 3), Prostate Cancer (Phase 2), Solid Tumors (Phase 1), RCC (Phase 3), CRC (Phase 2), Gastric Adenocarcinoma (Phase 2) | - |
| Capmatinib | Selecitve TKI | ATP competitive | HCC (Phase 2), Solid Tumors (Phase 2), Oesophageal Adenocarcinoma (Phase 2), NSCLC (Phase 3), | - |
| Tepotinib | Selecitve TKI | ATP competitive | NSCLC (Phase 2), Solid Tumors (Phase 2), Brain Tumor (Phase 1), HCC (Phase 1) | - |
| Rilotumumab | Monoclonal antibody | HGF | Gastric Cancer (Phase 3), Solid Tumors (Phase 1), NSCLC (Phase 2), Malignant Glioma (Phase 2), Prostate Cancer (Phase 1), RCC (Phase 2) | - |
| Ficlatuzumab | Monoclonal antibody | HGF | NHSCC (Phase 1), Pancreatic cancer (Phase 1), AML (Phase 1), NSCLC (Phase 2) | - |
| Onartuzumab | Monoclonal antibody | c-Met | Solid Tumors (Phase 3), HCC (Phase 1), Glioblastoma (Phase 2), Solid Tumors (Phase 1), NSCLC (Phase 3), Gastric Cancer (Phase 3), Breast Cancer (Phase 2), CRC (Phase 2) | - |
Abbreviations: TKI, tyrosine kinase inhibitor; ATP, adenosine-triphosphate; RCC, renal cell carcinoma; HCC, hepatocellular carcinoma; UC, urothelial carcinoma; PSCC, penile squamous cell carcinoma; NSCLC, non-small cell lung cancer; AML, acute myeloid leukemia; HNSCC, Head and neck squamous cell carcinomas; BCa, bladder cancer; HGF, Hepatocyte growth factor; CRC, colorectal cancer; VEGFR2, vascular endothelial growth factor receptor-2; FLT3, FMS-like tyrosine kinase 3; KIT, tyrosine protein kinase kit; AXL, AXL receptor tyrosine kinase; RET, rearranged during transfection; ALK, anaplastic lymphoma kinase; ROS1, proto-oncogene 1, receptor tyrosine kinase; c-Met, mesenchymal-epithelial transition factor.