HS-10587

HS-10587 is an orally bioavailable, small molecule inhibitor of Protein Arginine Methyltransferase 5 (PRMT5) developed by Jiangsu Hansoh Pharmaceutical. It is specifically designed as an MTA-cooperative inhibitor to target tumors characterized by Methylthioadenosine Phosphorylase (MTAP) deletion. In MTAP-deficient cells, the metabolite methylthioadenosine (MTA) accumulates and binds to PRMT5, creating a unique conformational state. HS-10587 selectively binds to this PRMT5-MTA complex, inducing synthetic lethality in cancer cells while sparing normal cells that do not accumulate MTA. This selective approach is intended to provide a superior safety profile compared to first-generation, non-selective PRMT5 inhibitors, which are often limited by hematological toxicities. HS-10587 is currently being evaluated in Phase I clinical trials for patients with MTAP-deleted advanced solid tumors.