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Updated: May 6, 2026

Mass Spectrometry and Luminogenic-based Approaches to Characterize Phase I Metabolic Competency of In Vitro Cell Cultures
Published on: March 28, 2017
An evaluation of the latest in vitro tools for drug metabolism studies
Ana Costa1, Bruno Sarmento, Vítor Seabra
1IINFACTS - Instituto de Investigaçãoe Formação Avançada em Ciênciase Tecnologias da Saude, Instituto Superior de Ciências da Saude-Norte, Department of Pharmaceutical Sciences , CESPU, Gandra-PRD , Portugal +351 22 415 71 89 ; Bruno.Sarmento@ineb.up.pt.
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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