The world's third BTK-PROTAC starts clinical trial

Article source: Medical Rubik's Cube Info

Author: Shi Bei

On August 16, BeiGene registered the US Phase I study of BTK protein degradation agent (BTK-PROTAC) BGB-16673 on the American Clinical Network to treat B-cell malignancies.

The international patent WO 2021018018 A1 of BGB-16673 has been published

In April of this year, Haisco HSK29116 powder was approved for clinical use in China for the treatment of B-cell malignancies.

Medicine Rubik's Cube NextPharma

At present, BTK small molecule inhibitors have been successfully applied to the treatment of B-cell lymphoma, but the existing marketed BTK inhibitors mainly produce enzyme inhibition by forming a covalent bond with the cysteine ​​residues in the active site of BTK, which has great side effects.

PROTAC is a hot topic in medical research and development in recent years.

Schematic diagram of the mode of action of PROTAC (Source: Royal Society of Chemistry)

PROTAC domestic and foreign pharmaceutical companies have been competing to become the layout of the track, as many as 136 in research projects involving targets including: BTK, AR, ER, CDK , KRAS , and so on

Domestic companies Haisco, pioneering pharmaceuticals, Hejing Pharmaceuticals, Nuocheng Jianhua, Wuyuan Biology, Meizhi Pharmaceuticals, Yasheng Pharmaceuticals, Kelun Pharmaceuticals, Hengrui, CSPC, Jiaxing Youbo, Haichuang Pharmaceuticals , Xingkang Yuan Biology, Shanghai Ruiyin, Fendi Technology, Lingtai Biology, Multidomain Biology, Tongtongkang, BeiGene and other companies have all deployed