TABLE II. Current Status of Ras/MAPK Small Molecules for Clinical Trials.
| Agent | Target | Company/partner | Status |
|---|---|---|---|
| RAS modulation | |||
| Lonafarnib (Sarasar) | Farnesyl transferase | Merck/Schering-Plough | Phase II |
| Tipifarnib (Zarnestra) | Farnesyl transferase | Johnson & Johnson | Phase I/II |
| Salirasib | RAS antagonist | Concordia | Phase I/II |
| RAF inhibition | |||
| Sorafenib (Nexavar) | RAF/multi-targeted | Onyx/Bayer Pharmaceuticals | Approved |
| RAF265 | RAF/multi-targeted | Novartis | Phase I/II |
| PLX4032 | BRAF | Plexxikon/Roche | Phase III |
| PLX5568 | BRAF | Plexxikon/Roche | Phase I/II |
| GSK2118436 | BRAF | GlaxoSmithKline | Phase I/II |
| XL281 (BMS908662) | BRAF | Exelixis/Bristol-Myers Squibb | Phase I/II |
| MEK inhibition | |||
| CI-1040 | MEK | Pfizer | Terminated |
| PD0325901 | MEK | Pfizer | On Hold |
| AZD6244 (ARRY-886) | MEK | Array/AstraZeneca | Phase I/II |
| AZD8330 (ARRY-704) | MEK | Array/AstraZeneca | Phase I/II |
| ARRY-162 | MEK | Array/Novartis | Phase I/II |
| ARRY-300 | MEK | Array/Novartis | Phase I/II |
| RDEA119 | MEK | Ardea/Bayer | Phase I/II |
| RDEA436 | MEK | Ardea/Bayer | Phase I/II |
| E6201 | MEK | Eisai | Phase I/II |
| GSK1120212 | MEK | GlaxoSmithKline | Phase I/II |
| WX554 | MEK | Wilex AG | Phase I/II |
| GDC-0973 | MEK | Genentech | Phase I/II |
| AS703026 | MEK | EMD Serono | Phase I/II |
| RG7168 (CH4987655) | MEK | Chugai/Roche | Phase I/II |
| TAK-733 | MEK | Takeda/Millenium | Phase I/II |