Amgen Submits IND Application for KRAS G12C Inhibitor AMG 510 in China

Text | Baihuawen

On March 9, the Center for Drug Evaluation (CDE) accepted Amgen’s clinical trial application for AMG 510. AMG 510 is the first oral, selective, reversible inhibitor targeting KRAS G12C.

The Phase I clinical results of AMG 510 for the treatment of solid tumors, presented by Amgen at the ESMO 2019 Congress, showed:

Among 12 patients with colorectal cancer treated with AMG 510 (960 mg/day), one patient achieved a partial response, 10 achieved stable disease, and the disease control rate was 92%.

Among 13 patients with non-small cell lung cancer treated with AMG510 (960 mg/day), 7 achieved partial response and 6 achieved stable disease, resulting in a disease control rate of 100%.

Among the 2 patients with appendiceal cancer, 1 achieved partial response and 1 achieved stable disease.

RAS was the first oncogene identified in human tumors and remains one of the most prevalent oncogenic mutation genes, with over 30 years since its discovery. The RAS gene family currently includes three known members: KRAS, NRAS, and HRAS, among which KRAS mutations are the most common, accounting for approximately 85%. KRAS G12C mutations account for approximately 13% of non-small cell lung cancer (NSCLC) cases, 3%–5% of colorectal cancer cases, and 1%–2% of other solid tumors. In the United States, approximately 30,000 new cases of KRAS G12C-mutant cancers are diagnosed annually.