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Best Practices for the Use of Itraconazole as a Replacement for Ketoconazole in Drug-Drug Interaction Studies

Best Practices for the Use of Itraconazole as a Replacement for Ketoconazole in Drug-Drug Interaction Studies

Lichuan Liu, Akintunde Bello, Mark J Dresser, Donald Heald, Steven Ferenc Komjathy, Edward O'Mara, Mark Rogge, S Aubrey Stoch, Sarah M Robertson

J Clin Pharmacol. 2016 Feb;56(2):143-51.

PMID: 26044116

Abstract:

Ketoconazole has been widely used as a strong cytochrome P450 (CYP) 3A (CYP3A) inhibitor in drug-drug interaction (DDI) studies. However, the US Food and Drug Administration has recommended limiting the use of ketoconazole to cases in which no alternative therapies exist, and the European Medicines Agency has recommended the suspension of its marketing authorizations because of the potential for serious safety concerns. In this review, the Innovation and Quality in Pharmaceutical Development's Clinical Pharmacology Leadership Group (CPLG) provides a compelling rationale for the use of itraconazole as a replacement for ketoconazole in clinical DDI studies and provides recommendations on the best practices for the use of itraconazole in such studies. Various factors considered in the recommendations include the choice of itraconazole dosage form, administration in the fasted or fed state, the dose and duration of itraconazole administration, the timing of substrate and itraconazole coadministration, and measurement of itraconazole and metabolite plasma concentrations, among others. The CPLG's recommendations are based on careful review of available literature and internal industry experiences.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP84625616-B	Itraconazole		84625-61-6	Price

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