BGT-002, a new anti-hypercholesterolemia chemical class 1 drug jointly developed by Nan Fajun’s research group and Li Jingya’s research group, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, on February 17, 2022 Obtained the acquiescence of clinical trials from the State Drug Administration and was allowed to conduct clinical trials.
ATP-dependent citrate lyase (ACLY) in the cytoplasm mediates the production of acetyl-CoA and is a key hub connecting the mitochondrial tricarboxylic acid cycle and de novo lipid synthesis; inhibition of ACLY activity can Significantly reduces cytoplasmic acetyl-CoA supply and cholesterol de novo synthesis, thereby improving hypercholesterolemia.
Nan Fajun’s research group carried out systematic structure-activity relationship research on targets, Li Jingya’s research group carried out in vitro ACLY activity test and functional evaluation, hyperlipidemia and hypercholesterolemia and atherosclerosis In the preclinical pharmacodynamics study, it was finally found that BGT-002, a liver-targeted candidate drug with independent intellectual property rights and good drug prospects, has better efficacy in multiple animal models than the only marketed drug with the same target, bepiedic acid; It has good pharmacokinetic properties and safety in mice and beagle dogs.
The clinical trial approval of this product will provide a new safe and effective treatment option for patients with hypercholesterolemia, especially those with statin intolerance.
The BGT-002 project has successively won the General Project of the National Natural Science Foundation of China, the Strategic Pilot Science and Technology Project of the Chinese Academy of Sciences (Class A), the Science and Technology Support Project of the Shanghai Municipal Science and Technology Commission in the field of biomedicine, and the Shanghai Municipal Science and Technology Commission. Funded by the Natural Science Foundation of the “Science and Technology Innovation Action Plan” and the Open Project of the State Key Laboratory of New Drug Research.
The research and development of BGT-002 was also supported by researcher Li Jia from the Metabolic Disease Research Center of Shanghai Institute of Materia Medica, Zhong Dafang and Chen Xiaoyan from the Drug Metabolism Research Center, Li Yaping from the Pharmaceutical Preparation Research Center, Strong support from researcher Chen Dongying and researcher Mei Xuefeng of the Drug Quality Control and Solid Chemistry Research Center, and researcher Gao Zhaobing of the Neuropsychiatric Disease Research Center.
At present, the project has reached a cooperation agreement with Bojiyuan (Shanghai) Biopharmaceutical Co., Ltd., and has realized the transformation of the results. Preparations for clinical phase I research are being carried out.
Contributing Department | Shanghai Institute of Materia Medica Nan Fajun Research Group, Li Jingya Research Group, Research and New Drug Promotion Office