AMG 510 First to Inhibit "Undruggable" KRAS

Abstract

Amgen's novel small-molecule inhibitor AMG 510 has become the first drug to successfully target a KRAS mutation in patients, according to findings presented at the 2019 American Society of Clinical Oncology Annual Meeting. In a phase I trial, AMG 510 elicited partial responses in half of evaluable patients with KRAS ^G12C-mutant non-small cell lung cancer, and led to stable disease in most evaluable patients with colorectal or appendix cancer.