lesinuard sodium是一种新型的痛风治疗药物，于2008年由Ardea Biosciences公司研发。该药物主要通过抑制尿酸盐转运蛋白1（URAT1）增加尿酸的排泄来治疗痛风。URAT1被认为是存在于肾脏中用于转运尿酸盐的主要蛋白，能够将尿酸从管腔转入近曲小管上皮细胞并转化为单羧酸盐。临床研究显示，lesinuard sodium可被良好耐受，且能剂量相关性地降低血浆中的尿酸水平。主要介绍lesinuard sodium的药物概况、相关背景、合成路线、药理作用、临床前及临床试验的研究、安全性评价等方面。

Lesinuard sodium is a new drug used for the treatment of gout. It was discovered fortuitously by Ardea Biosciences in 2008. Lesinuard sodium could increase the excretion of uric acid by inhibiting the uric acid salt transport protein 1 (URAT1) to treat gout mainly. URAT1 is considered to be the main protein existing in kidney used to transport the uric acid salt, which is able to transfer the uric acid from the lumen proximal to tubule epithelial cells and translate into single carboxylic acid salt. In clinical trials, lesinuard sodium has been well tolerated with dose-dependent reductions in serum uric acid. The drug situation, background, route of synthesis, pharmacological action, preclinical and clinical trials research, safety evaluation of lesinuard sodium are reviewed in this paper.

天津市应用基础与前沿技术研究计划（13JCZDJC28500）