ISM0387

ISM0387 is a small molecule, MTA-cooperative PRMT5 (Protein Arginine Methyltransferase 5) inhibitor developed by Insilico Medicine in collaboration with the Emirates Drug Establishment (EDE). It utilizes a synthetic lethality mechanism by selectively targeting cancer cells with MTAP (Methylthioadenosine phosphorylase) gene deletions, which leads to the accumulation of methylthioadenosine (MTA). ISM0387 is designed to bind to the PRMT5-MTA complex, thereby inhibiting the enzyme's activity specifically in tumor cells while sparing healthy tissue. The candidate has demonstrated significant blood-brain barrier penetration and dose-dependent tumor suppression in preclinical models, making it a promising candidate for aggressive, treatment-resistant brain cancers such as glioblastoma. It was discovered using Insilico Medicine's Chemistry42 generative AI platform and represents the first drug candidate fully discovered and developed within the UAE, with its preclinical candidate nomination announced in April 2026.

Other names

ISM0387ISM-0387ISM 0387