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Drug intelligence / Profile preview
FMC-242 + FMC-376
- Development stage
- Unknown
- Lead developer
- Frontier Medicines
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
FMC-242 + FMC-376 is an investigational combination of two oral, covalent small-molecule targeted cancer therapies developed by Frontier Medicines. FMC-242 is a novel, covalent allosteric breaker of the PI3Kα-RAS interaction that disrupts downstream AKT signaling in tumors without affecting normal PI3Kα functions such as glucose homeostasis. FMC-376 is a highly selective, irreversible, covalent inhibitor that targets both the active (ON) and inactive (OFF) states of the mutant KRAS G12C protein. The combination is designed to enhance anti-tumor activity and overcome resistance mechanisms in KRAS G12C-mutant cancers. A Phase 1/2 clinical trial is planned to evaluate the combination in patients with KRAS G12C-mutant colorectal cancer or non-small cell lung cancer (NSCLC).
- Other names
- FMC-242 + FMC-376FMC-242 and FMC-376FMC242 and FMC-376FMC 242 and FMC-376FMC-242/FMC-376FMC-376 + FMC-242
02
Targets
KRASG12C (Kirsten rat sarcoma viral oncogene homolog G12C)Phosphoinositide 3-kinase alpha – RAS interaction interfacePIK3CA (Phosphoinositide 3-kinase alpha)
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