What is it about?

Drug transporters and drug-metabolizing enzymes influence the pharmacokinetics and pharmacodynamics of a drugs. In vitro assays allow researchers to evaluate whether a drug is a substrate, inducer and/or inhibitor of importers drug enzymes and transporters.

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Why is it important?

The understanding of a new drugs' potential as a substrate, inhibitor or inducer of a drug-metabolizing enzyme or transporter is an important element of risk assessment during drug discovery, development and regulatory review.

Perspectives

Not only does the article provide a brief overview of the different transporter and metabolism assays, we indicated the importance of LC/MS analysis in these assays.

Donna Volpe
U.S. Food and Drug Administration

Read the Original

This page is a summary of: Application of in vitro CYP and transporter assays to predict clinical drug–drug interactions, Bioanalysis, May 2018, Future Science,
DOI: 10.4155/bio-2017-0266.
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