articleNew England Journal of MedicineAug 23, 2023GREEN OA

Single-Agent Divarasib (GDC-6036) in Solid Tumors with a KRAS G12C Mutation

University of Toronto · Princess Margaret Cancer Centre · +25 more institutions

PubMed
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Abstract

Divarasib (GDC-6036) is a covalent KRAS G12C inhibitor that was designed to have high potency and selectivity. In a phase 1 study, we evaluated divarasib administered orally once daily (at doses ranging from 50 to 400 mg) in patients who had advanced or metastatic solid tumors that harbor a KRAS G12C mutation. The primary objective was an assessment of safety; pharmacokinetics, investigator-evaluated antitumor activity, and biomarkers of response and resistance were also assessed. A total of 137 patients (60 with non–small-cell lung cancer [NSCLC], 55 with colorectal cancer, and 22 with other solid tumors) received divarasib. No dose-limiting toxic effects or treatment-related deaths were reported.…

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