Table 2. Selective Small Molecule Tyrosine Kinase Inhibitors Specific to c-MET and RON*.
| Compound | Manufacturer | Targeted RTKs | Status | Descriptions in clinical trials | Ref |
|---|---|---|---|---|---|
| ARQ197 | ArQule/Daiichi Sankyo | c-MET | Phase II | Advanced solid (prostate) tumor; HCC; locally advanced, inoperable or metastatic primary solid tumors; advanced HCC, RCC, BC, NSCLC and melanoma | 38 |
| XL184 | Exelixis | c-MET | Phase I/II/III | MTC, PCAC, PSC, HCC, GE(GE)JC; Melanoma, SCLC, OC, PFTC, BC, NSCLC, and GM | 74 |
| PF-02341066 (crizotinib) | Pfizer | c-MET/ALK | Phase I/II | Advanced NSCLC; anaplastic LCL; relapsed/refractory solid tumors, primary CNS Tumors | 44 |
| EMD 1214063/EMD 1204831 | EMD Serono | c-MET | Phase I/II | Advanced, refractory solid tumors | 71 |
| GSK1363089 (Foretinib) | GlaxoSmithKline | c-MET/KDR/RON | Phase I/II | PRCC, AMCC, DEAGC; GE(GE)JC | 72 |
| MGCD265 | MethylGene Inc | c-MET/VEGFR/ RON/Tie-2 | Phase I/II | Advanced metastatic/ unresectable malignancies | 73 |
| JNJ-38877605 | Johnson & Johnson | c-MET | Phase I | Advanced/refractory solid tumors | 13 |
| PHA665752 | Pfizer | c-MET/RON | Preclinical | N/A | 13 |
| Compound I | Amgen | c-MET/RON | Preclinical | N/A | 51 |
*All information about individual inhibitors in clinical trials are derived from the website: http://clinicaltrials.gov, a service of the US National Institutes of Health. AMCC, advanced/metastatic gastric carcinoma; BC, breast cancer; DEAGC, distal esophageal adenocarcinoma gastric cancer; GE(GE)JC, gastro esophageal (GE) junction cancer; GM, glioblastoma multiforme; HCC, hepatocellular carcinoma, LCL, large-cell lymphoma; MTC, medullary thyroid cancer; NSCLC, non-small cell lung cancer; PFTC, peritoneal or fallopian tube carcinoma; PRCC, papillary renal-cell carcinoma; and RCC, renal cell carcinoma.