tasimelteon + rifampin

Tasimelteon + rifampin refers to the concomitant use of two pharmaceutical agents: **tasimelteon**, a selective dual melatonin receptor agonist (MT1 and MT2), and **rifampin**, a broad-spectrum antibiotic and strong inducer of cytochrome P450 enzymes (notably CYP3A4). Tasimelteon acts as a circadian regulator, primarily used to treat Non-24-Hour Sleep-Wake Disorder by synchronizing circadian rhythms through non-photic mechanisms. Rifampin induces hepatic metabolic enzymes, leading to increased metabolism and markedly decreased systemic exposure of tasimelteon, reducing its efficacy. Clinical data have demonstrated approximately 89–90% decrease in tasimelteon exposure when coadministered with rifampin; thus, such combination is not recommended due to loss of therapeutic effect[1][2][3].

Brand names

HetliozRifadin

Other names

tasimeltéontasimelteóntasimelteonum