JM118

JM118 is a platinum(II)-based small molecule and the primary active metabolite of the oral platinum(IV) prodrug satraplatin (JM216). As a platinum analog, JM118 exerts its cytotoxic effects by binding covalently to DNA, forming intra-strand and inter-strand crosslinks that disrupt DNA replication and transcription, leading to cell cycle arrest and apoptosis. Unlike cisplatin, the cellular uptake of JM118 is independent of the CTR1 copper transporter, allowing it to partially circumvent certain mechanisms of platinum resistance. However, its intracellular levels are still regulated by the efflux transporters ATP7A and ATP7B. JM118 has been extensively studied in the context of satraplatin's clinical development for various malignancies, including hormone-refractory prostate cancer, ovarian cancer, and small cell lung cancer, often demonstrating synergistic activity when combined with agents like docetaxel or erlotinib.

Other names

cis-amminedichloro(cyclohexylamine)platinum(II)cis-amminedichloro(cyclohexylamine)platinum