Metabolic profiling of a novel antithrombotic compound, S002-333 and enantiomers: metabolic stability, species comparison and in vitro-in vivo extrapolation

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• 作者：Amrita Saxena ; Guru R. Valicherla ; Girish K. Jain ; Rabi S. Bhatta ; Anil K. Saxena and Jiaur R. Gayen
• 刊名：Biopharmaceutics & Drug Disposition
• 出版年：2016
• 出版时间：May 2016
• 年：2016
• 卷：37
• 期：4
• 页码：185-199
• 全文大小：760K
• ISSN：1099-081X

文摘

The aim of this research work was to characterize the metabolism of S002-333, (2-(4'-methoxy-benzenesulfonyl)-2,3,4,9-tetrahydro-1H-pyrido (3,4-b) indole-3-carboxylic acid amide) and its enantiomers, S004-1032 (R-form) and S007-1558 (S-form) in pooled human liver microsomes (PHLM) and pooled liver microsomes (LM) of rat (RLM), rabbit (RABLM), dog (DLM) and monkey (MLM). Another objective of this study was to identify suitable surrogate species to humans for further development of lead candidates.