tasimelteon + ketoconazole

This is a **combination of tasimelteon, a dual melatonin receptor agonist**, and **ketoconazole, a triazole antifungal and strong CYP3A4 inhibitor**. Tasimelteon is indicated for treating Non-24-Hour Sleep-Wake Disorder (Non-24) and Smith-Magenis Syndrome, working by agonism of the MT1 and MT2 melatonin receptors to regulate circadian rhythms. When co-administered with ketoconazole, plasma exposure of tasimelteon increases by approximately 50%, as ketoconazole inhibits the CYP3A4-mediated metabolism of tasimelteon[1][2][3][4]. The drug interaction is primarily of pharmacokinetic significance and may increase the risk of dose-dependent adverse effects of tasimelteon.

Other names

BMS 214778BMS214778BMS-214778VEC 162VEC162VEC-162N-{[(1R,2R)-2-(2,3-dihydro-1-benzofuran-4-yl)cyclopropyl]methyl}propanamide