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Is Amgen's AMG 510 effective against KRASG12C?

Amgen's novel small-molecule inhibitor AMG 510 has become the first drug to show activity in patients with KRASG12C -mutant solid tumors. In a phase I trial, AMG 510 elicited partial responses in half of patients with non–small cell lung cancer (NSCLC) and led to stable disease in patients with colorectal or appendix cancer.

What's new in AMG 510?

AMG 510 is the first drug to successfully target KRAS (pictured above), which has long been considered undruggable. Researchers enrolled 35 patients with KRASG12C -mutant solid tumors who had received at least two prior therapies in the trial: 14 patients with NSCLC, 19 with colorectal cancer, and two with appendix cancer.

What is Amgen’s KRAS G12C inhibitor?

Amgen has taken on one of the toughest challenges of the last 40 years in cancer research by developing sotorasib, an investigational KRAS G12C inhibitor. 7 Sotorasib was the first KRAS G12C inhibitor to enter the clinic and is being studied in the broadest clinical program exploring 10 combinations with global sites spanning five continents.

When will enrollment into Phase 2 of AMG 510 be opened?

Enrollment into phase 2 will be opened after confirmation of the recommended phase 2 dose Separate cohort of part 1 dose expansion subjects to evaluate the safety and clinical activity of AMG 510 administered orally once daily in subjects with previously untreated advanced non-small cell lung cancer (NSCLC).


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