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Lenalidomide: in vitro evaluation of the metabolism and assessment of cytochrome P450 inhibition and induction.

Abstract：

PURPOSE:To assess the potential for drug-drug interactions between lenalidomide and substrates and inhibitors of cytochrome P450 (CYP) isozymes. METHODS:In vitro metabolism of lenalidomide by human liver microsomes, recombinant human CYPs and human hepatocytes was evaluated. The inhibitory and inductive effects of lenalidomide on the CYP activities were evaluated in human liver microsomes and cultured human hepatocytes, respectively. RESULTS:In vitro incubation of lenalidomide with human liver microsomes, recombinant-CYP isozymes, and human hepatocytes did not result in Phase I or Phase II metabolism, confirming the low propensity of lenalidomide for metabolism in vivo in humans. In vitro, lenalidomide did not inhibit CYP isozymes in human liver microsomes and did not induce CYP activities in cultured human hepatocytes. CONCLUSIONS:Lenalidomide is not a substrate, inhibitor, or inducer of CYP group of enzymes; clinically relevant pharmacokinetic drug-drug interactions are unlikely to occur between lenalidomide and co-administered CYP substrates or inhibitors.

journal_name

Cancer Chemother Pharmacol

journal_title

Cancer chemotherapy and pharmacology

authors

Kumar G,Lau H,Laskin O

doi

10.1007/s00280-008-0867-7

subject

Has Abstract

pub_date

2009-05-01 00:00:00

pages

1171-5

issue

6

eissn

0344-5704

issn

1432-0843

journal_volume

63

pub_type

杂志文章

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