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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。
Uric Acid Reuptake Transporter (URAT1) is an anion transporter located in the proximal tubule of the proximal tubule, which determines uric acid reabsorption and is often used as a target for the treatment of hyperuricemia and gout. Lesinurad, a URAT1 selective inhibitor developed by AstraZeneca Pharmaceuticals, was approved by the FDA in late 2015 to be used in combination with xanthine oxidase inhibitors for the relief of hyperuricemia and gout symptoms. It mainly introduces the research situation of Lesinuard’s drug, research background, synthesis route, pharmacology, pharmacokinetics, clinical trials and so on, which provides the basis for the popularization and application of this drug and the research and development of similar new drugs.