DC50292

DC50292 is an orally administered small molecule inhibitor of Protein Arginine Methyltransferase 5 (PRMT5), specifically developed to treat advanced or metastatic solid tumors characterized by the deletion of the methylthioadenosine phosphorylase (MTAP) gene. In tumors with MTAP deletion, the metabolite methylthioadenosine (MTA) accumulates and binds to PRMT5, creating a unique therapeutic vulnerability. DC50292 acts as an MTA-cooperative inhibitor, selectively binding to the PRMT5-MTA complex to inhibit its enzymatic activity, thereby inducing synthetic lethality in MTAP-deficient cancer cells while minimizing effects on normal tissues. The drug is currently being evaluated in Phase I clinical trials by Beijing Double-Crane Run-Chuang Technology, a subsidiary of China Resources Double-Crane Pharmaceutical.