lesinuard sodium是一種新型的痛風(fēng)治療藥物，于2008年由Ardea Biosciences公司研發(fā)。該藥物主要通過(guò)抑制尿酸鹽轉(zhuǎn)運(yùn)蛋白1（URAT1）增加尿酸的排泄來(lái)治療痛風(fēng)。URAT1被認(rèn)為是存在于腎臟中用于轉(zhuǎn)運(yùn)尿酸鹽的主要蛋白，能夠?qū)⒛蛩釓墓芮晦D(zhuǎn)入近曲小管上皮細(xì)胞并轉(zhuǎn)化為單羧酸鹽。臨床研究顯示，lesinuard sodium可被良好耐受，且能劑量相關(guān)性地降低血漿中的尿酸水平。主要介紹lesinuard sodium的藥物概況、相關(guān)背景、合成路線(xiàn)、藥理作用、臨床前及臨床試驗(yàn)的研究、安全性評(píng)價(jià)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.

天津市應(yīng)用基礎(chǔ)與前沿技術(shù)研究計(jì)劃（13JCZDJC28500）