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Oct. 17, 2023

Divarasib: Great Timing for Positive Data Makes This KRAS Inhibitor a Big Deal


oral selective covalent KRASG12C inhibitor Ph. III for NSCLC from disulfide-tether fragment screen N. Engl. J. Med., August 2023 Genentech, So. San Francisco, CA

Drug Hunter Team

Genentech’s divarasib (GDC-6036) is a covalent inhibitor of KRASG12C in Ph. III in patients with non-small cell lung cancer (NSCLC) (NCT03178552), making it the third most advanced KRASG12C inhibitor after the accelerated approvals of Amgen’s sotorasib and Mirati’s adagrasib (Figure 1). Recently, efficacy data from divarasib’s Ph. I study in 137 cancer patients showed surprisingly strong efficacy, with 53.4% of patients having a confirmed response in NSCLC (median PFS = 13.1 mo, DOR = 14 months, n = 60) and 29.1% of CRC patients having a confirmed response (median PFS = 5.6 mo, DOR = 7.1 months, n = 55).



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