BGB-58067

BGB-58067 is an oral, highly potent, brain-penetrant small molecule inhibitor of protein arginine methyltransferase 5 (PRMT5), developed by BeiGene for the treatment of advanced solid tumors with methylthioadenosine phosphorylase (MTAP) deficiency. MTAP loss occurs in approximately 15% of all tumor types and leads to accumulation of methylthioadenosine (MTA), which partially inhibits PRMT5 and sensitizes tumor cells to further PRMT5 inhibition. BGB-58067 is designed as an MTA-cooperative PRMT5 inhibitor that selectively targets tumors with MTAP deletion. Preclinical studies have shown its effectiveness in inhibiting PRMT5-mediated signaling and antitumor activity across several cancer types including lung, colon, pancreas, bladder cancer, and glioblastoma multiforme. The drug is currently being evaluated as monotherapy in a first-in-human phase 1a/b clinical trial for patients with advanced or metastatic solid tumors who have lost MTAP expression[3][4][6][10].

Other names

PRMT5 inhibitor (BeiGene)