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DRUG CLASS:

KRAS Q61H inhibitor

1year
RM-046, a first-in-class, mutant-selective, and oral KRASQ61H(ON) inhibitor that drives tumor regression in preclinical models and validates KRASQ61H as a therapeutic target (AACR 2023)
As far as we are aware, RM-046 is the first oral and mutant-selective inhibitor of KRASQ61H(ON). It also represents an example of a non-covalent, mutant-selective tri-complex inhibitor of a KRAS oncogenic driver mutation.
Preclinical
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KRAS (KRAS proto-oncogene GTPase)
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KRAS mutation • KRAS wild-type • RAS mutation • RAS wild-type • NRAS Q61 • KRAS Q61H
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RMC-0708