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Cancer Chemotherapy and Pharmacology
Published in: Cancer Chemotherapy and Pharmacology 6/2009

01-05-2009 | Short Communication

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

Authors: Gondi Kumar, Henry Lau, Oscar Laskin

Published in: Cancer Chemotherapy and Pharmacology | Issue 6/2009

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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.
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Metadata
Title
Lenalidomide: in vitro evaluation of the metabolism and assessment of cytochrome P450 inhibition and induction
Authors
Gondi Kumar
Henry Lau
Oscar Laskin
Publication date
01-05-2009
Publisher
Springer-Verlag
Published in
Cancer Chemotherapy and Pharmacology / Issue 6/2009
Print ISSN: 0344-5704
Electronic ISSN: 1432-0843
DOI
https://doi.org/10.1007/s00280-008-0867-7

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