RMC-7977

RMC-7977 is an orally active, potent, reversible small molecule inhibitor that targets both wild-type and mutant forms of RAS proteins (KRAS, HRAS, NRAS) in their active (GTP-bound) state. It functions as a tri-complex inhibitor by simultaneously binding to cyclophilin A (CYPA) and RAS proteins, thereby inhibiting the active state of both mutant and wild-type RAS. Preclinical studies have demonstrated robust anti-tumor activity across a range of RAS-mutated cancers—including non-small cell lung cancer (NSCLC), pancreatic cancer, and neurofibromatosis type 1 (NF1)-related tumors—at well-tolerated doses. Tumor cells appear uniquely sensitive to this inhibitor compared to normal cells. The drug is being developed by Revolution Medicines[2][3][4][5][6].