Format

Send to

Choose Destination
Clin Pharmacol Ther. 2014 May;95(5):473-6. doi: 10.1038/clpt.2014.41.

Itraconazole and clarithromycin as ketoconazole alternatives for clinical CYP3A inhibition studies.

Author information

1
Drug Disposition, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana, USA.

Abstract

High-dose ketoconazole (400 mg q.d. for ≥5 days) has been the gold-standard strong cytochrome P450 3A (CYP3A) inhibitor in drug development drug-drug interaction (DDI) studies. In 2013, the US Food and Drug Administration (FDA) and the European Medicines Agency (EMA) advised against using this ketoconazole regimen following review of clinical safety reports. We systematically evaluated 19 strong CYP3A inhibitors from regulatory guidances and a literature database to identify itraconazole (200 mg b.i.d. on day 1, q.d. on days 2-6) and clarithromycin (500 mg b.i.d. for 7 days) as acceptable ketoconazole alternatives.

PMID:
24747234
DOI:
10.1038/clpt.2014.41
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Wiley
Loading ...
Support Center