FMC-242 + olomorasib

FMC-242 + olomorasib is an investigational, preclinical combination of two oral, small-molecule targeted oncology agents: FMC-242, developed by Frontier Medicines, and olomorasib (LY3537982), developed by Eli Lilly. FMC-242 is a first-in-class, covalent allosteric breaker of the PI3Kα–RAS interaction that selectively binds cysteine 242 in the RAS-binding domain of PI3Kα, disrupting downstream AKT signaling in tumors while sparing normal PI3Kα metabolic functions like glucose homeostasis. Olomorasib is a potent, highly selective, next-generation covalent inhibitor of the KRAS G12C mutant protein. By simultaneously targeting the PI3Kα–RAS interaction and KRAS G12C, this combination is designed to synergistically inhibit oncogenic signaling and overcome resistance mechanisms in KRAS G12C-mutant and receptor tyrosine kinase (RTK)-driven solid tumors, such as non-small cell lung cancer (NSCLC), colorectal cancer, and breast cancer.

Other names

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