Home > Oncology > ESMO 2021 > Gastrointestinal Cancer > Adagrasib shows promising clinical activity in heavily pretreated KRAS-mutated CRC

Adagrasib shows promising clinical activity in heavily pretreated KRAS-mutated CRC

Presented By
Dr Jared Weiss, University of North Carolina at Chapel Hill, NC, USA
Conference
ESMO 2021
Trial
Phase 1/2, KRYSTAL-1
The selective KRASG12C inhibitor adagrasib, as monotherapy or combined with cetuximab, was well tolerated and demonstrated promising clinical activity in heavily pretreated patients with KRAS-mutant colorectal cancer (CRC), first results of the KRYSTAL-1 trial showed. KRASG12C mutations, which occur in 3–4% of CRC, act as oncogenic drivers and are a negative predictor of cetuximab efficacy. Adagrasib is a KRASG12C inhibitor that irreversibly and selectively binds KRASG12C, locking it in its inactive state. Durable inhibition of KRASG12C may be particularly important in CRC due to signalling pathways which create a susceptibility to feedback reactivation of KRAS. EGFR signalling is implicated in this reactivation, providing a rational co-targeting strategy for KRAS-mutant CRC. KRYSTAL-1 (


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