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

• 内藤 良

  アステラス製薬株式会社研究本部化学研究所

書誌事項

タイトル別名

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

抄録

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.

収録刊行物

• 有機合成化学協会誌

  有機合成化学協会誌 70 (10), 1011-1017, 2012

  公益社団法人 有機合成化学協会

キーワード

• solifenacin
• muscarinic receptor antagonist
• overactive bladder
• absolute configuration
• process chemistry

詳細情報

• CRID: 1390282680316661248
• NII論文ID: 10031124006
• NII書誌ID: AN0024521X
• DOI: 10.5059/yukigoseikyokaishi.70.1011
• COI: 1:CAS:528:DC%2BC38XhsF2qtr7P
• ISSN: 18836526
• ISSN: 00379980
• NDL書誌ID: 024031111
• Web Site: https://ndlsearch.ndl.go.jp/books/R000000004-I024031111
• 本文言語コード: ja
• データソース種別:
  • JaLC
  • NDL
  • Crossref
  • CiNii Articles
• 抄録ライセンスフラグ: 使用不可