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molecules of the year

Mirati KRASG12D Inhibitor

reversible KRASG12D inhibitor

preclinical efficacy in cancer model

from SBDD around KRASG12C inhibitor

MRTX1133

Mirati Therapeutics, San Diego, CA

MRTX1133 Mirati G12D inhibitor chemical structure drug hunter molecules of the year kras
2 mins read

MRTX1133 was nominated as December 2021’s cover molecule by reviewers Joachim Rudolph and Julien Lefranc. MRTX1133 is a non-covalent inhibitor of KRASG12D that demonstrated tumor regression in a mouse xenograft model when dosed IP (maximum efficacy at 10-30 mg/kg, activity as low as 3 mg/kg). Joachim said, “The discovery of MRTX1133 deserves major credit as the first reported potent and selective non-covalent mutant-specific KRAS inhibitor especially as the targeted G12D mutant is the most prevalent KRAS mutant (33% among KRAS mutant tumors). The paper represents a successful continuation of the work on KRAS G12C inhibitors demonstrating suitability of the same binding site (switch II pocket) for mutants outside of G12C.” “This reflects, in retrospect, the power of covalent screening as…


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