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Drug Metabolism Letters

Editor-in-Chief

ISSN (Print): 1872-3128
ISSN (Online): 1874-0758

Application of Modern Drug Metabolism Structure Determination Tools and Assays to the In Vitro Metabolism of Imiloxan

Author(s): William L. Fitch, Yuan Chen, Liling Liu, Axel Paehler and May Young

Volume 4 , Issue 2 , 2010

Page: [77 - 87] Pages: 11

DOI: 10.2174/187231210791292753

Price: $65

Sekisui-XenoTech-DML
Abstract

Imiloxan is an alpha2 adrenoceptor antagonist and was developed for depression in the 1980s. In Phase 1 clinical trials imiloxan dosing led to hypersensitivity reactions; the molecules development was discontinued. The present study revisits the in vitro metabolism of imiloxan using modern analytical methods. Human and rat liver microsomes convert imiloxan into a variety of metabolites many of which are unstable and or reactive. Imiloxan also yields high protein covalent binding in microsomal assays. Imiloxan is a useful test molecule for defining the relationship between liver covalent binding and idiosyncratic toxicity.

Keywords: Imiloxan, metabolism, mass spectrometry, reactive metabolite


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