On November 19, the official website of the Center for Drug Evaluation (CDE) of the China State Food and Drug Administration announced that BGB-58067, a Class 1 new drug submitted by BeiGene, has received implicit approval for clinical trials and is planned to be developed to treat patients with advanced solid tumors.

According to BeiGene’s public information, BGB-58067 is a PRMT5 inhibitor and one of BeiGene’s future core projects. According to the CDE official website, this is the first time this product has been approved for clinical use in China.

PRMT5 is a new target in the field of "synthetic lethality". Research has found that the gene that constitutes "synthetic lethality" with PRMT5 is MTAP, which is a tumor suppressor gene that is often deleted in tumors. Loss of MTAP will cause the accumulation of its reaction substrate methylthioadenosine (MTA), and MTA will combine with PRMT5 to form a PRMT5-MTA complex, significantly inhibiting the activity of PRMT5.

These studies indicate that inhibiting PRMT5 activity in MTAP-deficient tumors is expected to kill cancer cells and become a new strategy for treating cancer. MTAP gene deletion occurs in about 10% of cancers, including pancreatic cancer, lung cancer, and bladder cancer.

According to BeiGene’s public information, BGB-58067 developed by the company is a second-generation MTA synergistic PRMT5 inhibitor that can selectively kill MTAP-deficient tumor cells while avoiding affecting normal blood cells.

Studies have shown that it is extremely active and selective in MTAP-deficient cells, has good blood-brain barrier penetration and intracranial efficacy, has an ideal half-life, and can be administered daily.

https://mp.weixin.qq.com/