MRTX1133 was nominated as December 2021’s cover molecule by reviewers Joachim Rudolph and Julien Lefranc . MRTX1133 is a non-covalent inhibitor of KRAS G12D 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 says, “The discovery of MRTX1133 [...]
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Jan. 17, 2022
MRTX1133: A First-in-Class Oral KRAS(G12D) Inhibitor
MRTX1133
reversible KRASG12D inhibitor preclinical efficacy in cancer model from SBDD around KRASG12C inhibitor Journal of Medicinal Chemistry Mirati Therapeutics, San Diego, CA
Reviewer: