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Lesinurad sodium. Solute carrier family 22 member 12 (URAT1) inhibitor, uricosuric, treatment of gout

机译:Lesinurad钠。溶质载体家族22成员12(URAT1)抑制剂,尿酸,痛风的治疗

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摘要

(Chemical Equation Presented). Gout is the most common form of inflammatory arthritis in men over 40 years of age. Available drugs target various steps to lower serum urate levels and include the xanthine oxidase inhibitors allopurinol and febuxostat, as well as the uricosuric agents probenecid, sulfinpyrazone and benzbromarone. Current treatment options are limited, associated with adverse events and often have an inadequate response. These factors have driven the need for the development of new and alternative agents to lower uric acid levels. In this context, lesinurad sodium (RDEA-594), an active metabolite of RDEA-806, was noted to have significant uricosuric effects by inhibiting solute carrier family 22 member 12 (urate anion exchanger 1, URAT1). URAT1 is a primary transporter of uric acid. In clinical trials, lesinurad sodium has been well tolerated, with dose-dependent reductions in serum uric acid. Moreover, co-administration of xanthine oxidase inhibitors and lesinurad sodium can safely accelerate urate reduction in gout patients.
机译:(呈现化学方程式)。痛风是40岁以上男性最常见的炎症性关节炎形式。可用的药物针对降低血清尿酸盐水平的各种步骤,包括黄嘌呤氧化酶抑制剂别嘌醇和非布索坦,以及尿酸排泄剂丙磺舒,亚砜吡嗪和苄溴马隆。当前的治疗选择是有限的,与不良事件有关,并且通常反应不足。这些因素驱使开发新的替代药物以降低尿酸水平的需求。在这种情况下,通过抑制溶质载体家族22成员12(尿酸阴离子交换剂1,URAT1),莱斯诺拉钠(RDEA-594)(一种RDEA-806的活性代谢物)具有显着的尿尿排尿作用。 URAT1是尿酸的主要转运蛋白。在临床试验中,对lesinurad钠的耐受性良好,血清尿酸呈剂量依赖性降低。此外,将黄嘌呤氧化酶抑制剂和来那度钠合用可以安全地加速痛风患者的尿酸盐减少。

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  • 来源
    《Drugs of the Future》 |2011年第12期|共6页
  • 作者

    PemaK.M.;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 药学;
  • 关键词

  • 入库时间 2022-08-18 22:45:11

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