Research and Development of Solifenacin for the Treatment of Overactive Bladder(OAB)

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  • Naito Ryo
    Chemistry Research Labs., Drug Discovery Research, Astellas Pharma Inc.

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  • 過活動膀胱（OAB）治療剤ソリフェナシンの研究開発と工業化
  • カカツドウ ボウコウ(OAB)チリョウザイ ソリフェナシン ノ ケンキュウ カイハツ ト コウギョウカ

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Abstract

Solifenacin succinate (Vesicare®), a novel muscarinic receptor antagonist for the treatment of overactive bladder (OAB) with symptoms of urge urinary incontinence, urgency, and urinary frequency, has been approved in more than 60 countries. In the course of continuing efforts to develop potent and bladder-selective muscarinic M3 receptor antagonists, solifenacin was designed as one of conformationally restricted analogues of quinuclidin-3-yl benzhydrylcarbamate with little selectivity among muscarinic receptor subtypes. In preclinical studies, solifenacin exhibited a highly bladder-selective profile compared with other antimuscarinic agents. Clinically, solifenacin ameliorates all symptoms in OAB patients; and, in particular, it produces a significant decrease in urgency episodes, which is the principal symptom of OAB with good tolerability. In this article, the drug discovery and the process development of solifenacin succinate are described.

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