尿酸鹽重吸收轉(zhuǎn)運(yùn)因子(URAT1)是一種陰離子轉(zhuǎn)運(yùn)體,它位于腎小管近端小管頂部細(xì)胞中,決定尿酸的重吸收,常作為治療高尿酸血癥及痛風(fēng)藥物的靶點(diǎn)。Lesinurad是一種URAT1選擇性抑制劑,由阿斯利康制藥公司研發(fā),并于2015年底被FDA批準(zhǔn)與黃嘌呤氧化酶抑制劑聯(lián)合用于高尿酸血癥及痛風(fēng)癥狀的緩解治療。主要介紹Lesinuard的藥物概況、相關(guān)研發(fā)背景、合成路線、藥理作用、藥動學(xué)、臨床試驗等方面研究情況,為該藥的推廣應(yīng)用以及同類新藥研發(fā)提供依據(jù)。

Urate transporter 1(URAT1) is an anion transporter, which localizes to the apical side of the renal proximal tubular cells and is an important determinant of urate reabsorption and often as a target for the treatment of hyperuricemia and gout. It was developed by AstraZeneca, and approved by the FDA in the end of 2015 with a xanthine oxidase inhibitor used to relieve joint treating hyperuricemia and gout symptoms. This paper describes Lesinurad's drug profiles, background, synthetic route, pharmacology, pharmacokinetics, and clinical trial research. It provides a basis for the promotion and application of the drug and similar drug research and development.