Lesinurad:一种选择性尿酸再吸收抑制剂

发布时间：2018-01-25 19:45

本文关键词： Lesinurad 高血尿酸痛风 URAT选择性抑制　出处：《药物评价研究》2016年02期 　论文类型：期刊论文

【摘要】：尿酸盐重吸收转运因子(URAT1)是一种阴离子转运体,它位于肾小管近端小管顶部细胞中,决定尿酸的重吸收,常作为治疗高尿酸血症及痛风药物的靶点。Lesinurad是一种URAT1选择性抑制剂,由阿斯利康制药公司研发,并于2015年底被FDA批准与黄嘌呤氧化酶抑制剂联合用于高尿酸血症及痛风症状的缓解治疗。主要介绍Lesinuard的药物概况、相关研发背景、合成路线、药理作用、药动学、临床试验等方面研究情况,为该药的推广应用以及同类新药研发提供依据。
[Abstract]:Uric acid reabsorption transporter (urat 1) is an anion transporter located in the apical cells of proximal tubule of renal tubules which determines the reabsorption of uric acid. Lesinurad is a selective inhibitor of URAT1 developed by AstraZeneca Pharmaceutical Company as a target for treatment of hyperuricemia and gout. In end of 2015, the combination of xanthine oxidase inhibitor and xanthine oxidase inhibitor was approved by FDA for the treatment of hyperuricemia and gout. The synthetic route, pharmacological action, pharmacokinetics, clinical trials and so on provide the basis for the popularization and application of the drug and the research and development of similar new drugs.
【作者单位】：天津市医药集团技术发展有限公司;
【分类号】：R971.1
【正文快照】： 1药物概况通用名:Lesinurad商品名:Zurampic#174;化学名:2-[[5-bromo-4-(4-cyclopropyl-1-naphthalenyl)-4H-1,2,4-triazol-3-yl]thio]-acetic acidCAS:878672-00-5分子式:C17H14Br N3O2S结构式:见图1相对分子质量:404.28原研公司:阿斯利康(Astra Zeneca)适应症:痛风,高尿酸

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