This review discusses the role of the human flavin-containing monooxygenase in drug metabolism and drug development. The literature covered includes comprehensive reviews, as well as recent work that illustrates: (i) the role of flavin-containing monooxygenase in drug metabolism; (ii) its use for enhancing drug candidate selection and lead optimization, and improving pharmaceutical properties; (iii) its use to avoid drug-drug interactions; and (iv) its application to animal models. Using optimal procedures for drug metabolism evaluation, understanding the chemical complexity of metabolites, using recombinant technologies and applying new methods that are successful in other fields will help advance this field of drug metabolism and development.
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