RM-046 is an orally active, selective ternary complex inhibitor of KRAS Q61H (active form). RM-046 forms a ternary complex with cyclophilin A, binds to active KRAS Q61H in a non-covalent manner, blocks effector binding via steric hindrance and inhibits downstream signal transduction. RM-046 inhibits ERK phosphorylation and cancer cell proliferation, and induces sustained RAS pathway signal inhibition, anti-tumor activity and tumor regression in preclinical xenograft models. RM-046 can be used for the research of KRAS Q61H mutant cancers [1].
In Vivo, Oral administration of RM-041 enables profound, sustained inhibition of RAS pathway activity in human KRASQ61H xenograft tumor models (including NSCLC and PDAC), and induces in vivo tumor regression at tolerated doses[1].
References:
[1]. Yang Y C, Thompson S, Montgomery D, et al. 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[J]. Cancer Research, 2023, 83(7_Supplement): 1598-1598.
In Vivo, Oral administration of RM-041 enables profound, sustained inhibition of RAS pathway activity in human KRASQ61H xenograft tumor models (including NSCLC and PDAC), and induces in vivo tumor regression at tolerated doses[1].
References:
[1]. Yang Y C, Thompson S, Montgomery D, et al. 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[J]. Cancer Research, 2023, 83(7_Supplement): 1598-1598.