JMKX001899 + itraconazole

JMKX001899 + itraconazole is a combination of two small molecule drugs: JMKX001899, a novel, selective, irreversible oral inhibitor of KRAS G12C, and itraconazole, an established triazole antifungal. JMKX001899 covalently binds and locks KRAS G12C in its inactive state, exhibiting significant activity in preclinical models of KRAS G12C-mutant non-small cell lung cancer (NSCLC), including brain metastasis, with evidence for central nervous system penetration[1][3][7]. Itraconazole is commonly used for fungal infections and also acts as an inhibitor of CYP3A4, often used in drug-drug interaction studies to boost exposure of investigational drugs metabolized by CYP3A4. The combination is likely being independently evaluated to understand pharmacokinetics, safety, and possibly drug-drug interactions, or to address antifungal prophylaxis during JMKX001899 treatment.