4.5 Review

An evaluation of the latest in vitro tools for drug metabolism studies

Journal

EXPERT OPINION ON DRUG METABOLISM & TOXICOLOGY
Volume 10, Issue 1, Pages 103-119

Publisher

TAYLOR & FRANCIS LTD
DOI: 10.1517/17425255.2014.857402

Keywords

hepatic metabolism; in vitro models; intestinal metabolism; pulmonary metabolism; renal metabolism

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Introduction: Drugs are indispensable for human welfare nevertheless there is a lack of safe drugs. Obtaining pharmacokinetics information, especially metabolism, is a requirement during preclinical and clinical drug development so that in vitro tools represent a simple path where it is possible to assess drug toxicity and predict drug safety in humans. Areas covered: This review covers the latest in vitro tools developed for assessing drug toxicity in different organs. A special focus is given to hepatic models, as it is the main organ responsible for drug metabolism and consequently bioactivation and detoxification reactions. Three-dimensional culture models have been widely developed, resembling in vivo-like conditions, and are also discussed in this review. Expert opinion: Several in vitro tools to assess hepatic drug metabolism have been developed, however, novel in vitro methods to investigate extra-hepatic drug metabolism still need to be improved. These methods are able to reduce the number of animal used in preclinical experiments, but in vivo tests are mandatory for drug approval and commercialization.

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