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A Phase I Study to Evaluate the Safety, Tolerability, Pharmacokinetics of BGT-002, a Novel ATP-Citrate Lyase Inhibitor, in Healthy Chinese Subjects

文献类型：期刊论文

作者Liu, Yun1,2; Yu, Chengyin1,3; Zhang, Yifan3; Xie, Zhifu3; Wang, Yating1,2; Qian, Hongjie1,2; Liang, Liyu1,2; Liu, Yanmei1,2; Chen, Qian1,2; Jia, Jingying1,2
刊名DRUG DESIGN DEVELOPMENT AND THERAPY
出版日期2025
卷号19页码:1783-1794
关键词safety tolerability pharmacokinetics pharmacodynamics BGT-002 novel ACLY inhibitor
ISSN号1177-8881
DOI10.2147/DDDT.S504814
英文摘要Objective: This Phase I study evaluated the safety, tolerability, pharmacokinetics (PK) and pharmacodynamics (PD) of BGT-002, a novel ATP-citrate lyase (ACLY) inhibitor, in healthy Chinese adults. Methods: This study included three parts: Part I (single-ascending-dose study), Part II (multiple-ascending-dose study), and Part III (food effect study). A total of 104 healthy subjects were enrolled in the study and were given BGT-002 tablet or placebo per protocol requirements. Blood samples were collected for pharmacokinetic and pharmacodynamic analysis. Safety was assessed by clinical examinations and adverse events. Results: In Part I, BGT-002 demonstrated rapid absorption with a Tmax of 0.67 to 1.75 hours, and slow elimination with a T1/2 of 24.53 to 72.86 hours, prolonged with increased dosages. Cmax and AUC0-infinity ranged from 1.55 to 48.39 mu g/mL, and 31.09 to 2930.69 hmu g/mL, respectively. In Part II, the accumulation index (Rac) of Cmax and AUCtau following 14 days of consecutive administration were 3.53 to 3.62 and 5.29 to 5.59, respectively, with a dose-proportionality PK profile. The levels of total cholesterol (TC), non-high-density lipoprotein cholesterol (non-HDL-C), and low-density lipoprotein cholesterol (LDL-C) were maximally decreased by 15.80%, 18.50%, and 22.37%, respectively. In Part III, the geometric mean ratio (90% CI) of fed to fasting condition in Cmax and AUC0-infinity of BGT-002 were 73.11% and 98.36%, respectively, indicating a minor food effect on the absorption rate. Across the study, two cases of Grade 3 adverse events (elevated blood triglycerides) were reported, both of which were assessed as not related to BGT-002. No serious adverse events were observed. Conclusion: BGT-002 demonstrated favorable safety, tolerability, and lipid-lowering effects, supporting its potential for further clinical development.
WOS关键词BEMPEDOIC ACID ; ETC-1002 ; HYPERLIPIDEMIA ; CHOLESTEROL
资助项目Burgeon Therapeutics Co., Ltd.
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:001444759400001
出版者DOVE MEDICAL PRESS LTD
源URL[http://119.78.100.183/handle/2S10ELR8/316551]  
专题新药研究国家重点实验室
通讯作者Nan, Fajun; Yu, Chen
作者单位1.Fudan Univ, Shanghai Xuhui Cent Hosp, Zhongshan Xuhui Hosp, Zhongshan, Shanghai, Peoples R China
2.Shanghai Engn Res Ctr, Phase Clin Res & Qual Consistency Evaluat Drugs 1, Shanghai, Peoples R China
3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai, Peoples R China
4.Burgeon Therapeut Co Ltd, Shanghai, Peoples R China
推荐引用方式
GB/T 7714		 Liu, Yun,Yu, Chengyin,Zhang, Yifan,et al. A Phase I Study to Evaluate the Safety, Tolerability, Pharmacokinetics of BGT-002, a Novel ATP-Citrate Lyase Inhibitor, in Healthy Chinese Subjects[J]. DRUG DESIGN DEVELOPMENT AND THERAPY,2025,19:1783-1794.
APA Liu, Yun.,Yu, Chengyin.,Zhang, Yifan.,Xie, Zhifu.,Wang, Yating.,...&Yu, Chen.(2025).A Phase I Study to Evaluate the Safety, Tolerability, Pharmacokinetics of BGT-002, a Novel ATP-Citrate Lyase Inhibitor, in Healthy Chinese Subjects.DRUG DESIGN DEVELOPMENT AND THERAPY,19,1783-1794.
MLA Liu, Yun,et al."A Phase I Study to Evaluate the Safety, Tolerability, Pharmacokinetics of BGT-002, a Novel ATP-Citrate Lyase Inhibitor, in Healthy Chinese Subjects".DRUG DESIGN DEVELOPMENT AND THERAPY 19(2025):1783-1794.

入库方式： OAI收割

来源：上海药物研究所

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