TABLE 1.
Summary table (include Drug name, Mechanism of action, Combination therapy, Clinical trial stage, Clinical effect, Trial ID).
| Mechanism of action | Combination therapy | Clinical trial stage | Clinical effect | Trial ID | |
|---|---|---|---|---|---|
| ARS-853 | Selective binding with RAS in GDP-bound state | — | — | — | — |
| ARS-1620 | Selective binding with RAS in GDP-bound state | Triple therapy of ARS-1620, an mTOR inhibitor and the IGF1R inhibitor linsitinib | — | — | — |
| AMG-510 | Binds with His95 with nanomolar-level affinity | ①AMG-510 combined with a MEK inhibitor | Phase I/II | Half of the assessable patients achieved objective partial responses | NCT03600883 |
| ②AMG-510 combined with a PD-1 inhibitor | |||||
| MRTX849 | Selective binding with RAS-GDP, maintaining it in an inactive state | ①MRTX849 combined with the HER family inhibitor afatinib | Phase I/II | — | NCT03785249 |
| ②MRTX849 combined with an SHP2 inhibitor | |||||
| ③MRTX849 combined with the mTOR inhibitor vistusertib | |||||
| BI-2852 | Binds with the switch II pocket regardless of GTP or GDP status | — | — | — | — |
| ARS-3248 | Based on ARS-1620 | — | Phase I | — | NCT04006301 |
| LY3499446 | — | — | — | — | NCT04165031 |
| US 2019/0248767A1 | — | — | — | — | — |
| WO 2019/110751 A1 | — | — | — | — | — |