rifampin and suvorexant

Suvorexant is an orexin receptor antagonist indicated for the treatment of insomnia, characterized by difficulties with sleep onset and/or sleep maintenance. As suvorexant is metabolized primarily by Cytochrome P450 3A (CYP3A), and its pharmacokinetics may be affected by CYP3A modulators, the effects of CYP3A inhibitors (ketoconazole or diltiazem) or an inducer (rifampin [rifampicin]) on the pharmacokinetics, safety, and tolerability of suvorexant were investigated.. Co-administration with ketoconazole resulted in increased exposure to suvorexant [AUC. These results are consistent with expectations that strong CYP3A inhibitors and inducers exert marked effects on suvorexant pharmacokinetics. In the context of a limited sample size, single suvorexant doses were generally well tolerated in healthy subjects when co-administered with/without a CYP3A inhibitor/inducer.

Topics: Administration, Oral; Adult; Azepines; Cytochrome P-450 CYP3A Inducers; Cytochrome P-450 CYP3A Inhibitors; Diltiazem; Drug Interactions; Healthy Volunteers; Humans; Ketoconazole; Male; Middle Aged; Orexin Receptor Antagonists; Rifampin; Triazoles; Young Adult