Evaluation of the CYP3A and CYP2B6 Drug-Drug Interaction Potential of Lemborexant.

ABSTRACT: Lemborexant is approved for treating insomnia and is under investigation for treating irregular sleep-wake rhythm disorder. Based on in vitro drug-drug interaction (DDI) characteristics, phase 1, open-label DDI studies were conducted to evaluate lemborexant's cytochrome P450 3A (CYP3A) and CYP2B6 interaction potential. Interactions between lemborexant 10 mg and strong and moderate CYP3A inhibitors (itraconazole and fluconazole), a strong CYP3A inducer (rifampin), and CYP3A (midazolam) and CYP2B6 substrates (bupropion) were evaluated. Coadministration of lemborexant with itraconazole or fluconazole resulted in 1.4- to 1.6-fold and 3.7- to 4-fold increases in lemborexant maximum observed concentration (C_max ) and area under the concentration-time curve from zero time extrapolated

SUBMITTER: Landry I 

PROVIDER: S-EPMC8248323 | biostudies-literature | 2021 Jun

REPOSITORIES: biostudies-literature