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molecules of the year

MRTX849

covalent KRASG12C inhibitor

in clinical development for KRASG12C+ cancers

from optimization of known starting point

J. Med. Chem., Apr. 6, 2020

Array / Mirati Therapeutics

MRTX849
1 min read

April’s molecule, the Mirati KRAS G12C inhibitor MRTX849, has been a hotly followed compound in development as it is the closest clinical KRAS inhibitor to the likely soon-to-be approved AMG-510 (sotorasib). The KRAS clinical race easily would have been the most followed development story of 2020 had it not been for COVID, due to the significant disease burden of KRAS-mutant-driven tumors in large indications including lung cancer. That Mirati’s KRAS clinical data has led to a nearly $10B appreciation in its equity value prior to an approval says everything about expectations for KRAS inhibitors in cancer. The recent successes of covalent inhibitors in cancer for targets like BTK, FGFR, and KRAS G12C are driving a major resurgence in interest for…


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