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。

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.