molecules of the month


oral drug, covalent inhibitor of KRASG12C

effective in KRASG12C-mutated cancer models

SBDD utilizing KRAS proto-oncogene, GTPase

British Journal of Cancer

Astellas Pharma Inc.

Chemical structure of molecule ASP2453 Astellas KRASG12C covalent inhibitor
1 min read

3.      The Astellas KRASG12C covalent inhibitor, ASP2453, is an oral molecule with activity in preclinical mouse models of KRASG12C-mutated cancer at lower doses than sotorasib (AMG 510). Several KRAS inhibitors have been highlighted recently. ASP2453 possesses an interesting spirocyclic azetidine-containing acrylamide warhead, and the authors note that ASP2453 is likely more reactive than piperazine-bearing AMG 510. ASP2453 does not appear to have entered clinical development yet.

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