Comparative Pharmacology
Head-to-head clinical analysis: HETLIOZ versus TASIMELTEON.
Peer-Reviewed Evidence
Head-to-head clinical analysis: HETLIOZ versus TASIMELTEON.
HETLIOZ vs TASIMELTEON
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Melatonin receptor agonist; selective agonist at MT1 and MT2 receptors in the suprachiasmatic nucleus, regulating circadian rhythms.
Tasimelteon is a selective melatonin MT1 and MT2 receptor agonist that mimics the natural sleep-promoting effects of melatonin by modulating circadian rhythms. It binds to MT1 receptors to promote sleep onset and to MT2 receptors to phase-shift the circadian clock.
20 mg orally once daily at bedtime, take within 30 minutes of bedtime, with or without food.
20 mg orally once daily at bedtime, taken within 30 minutes of retiring and at the same time each night. Not to be taken with or immediately after a high-fat meal.
None Documented
None Documented
Clinical Note
moderateTasimelteon + Ketoconazole
"The serum concentration of Ketoconazole can be increased when it is combined with Tasimelteon."
Clinical Note
moderateTasimelteon + Venlafaxine
"The risk or severity of adverse effects can be increased when Tasimelteon is combined with Venlafaxine."
Clinical Note
moderateTasimelteon + Atazanavir
"The serum concentration of Atazanavir can be increased when it is combined with Tasimelteon."
Clinical Note
moderateTasimelteon + Clarithromycin
Terminal elimination half-life is approximately 1.3-1.5 hours. No clinically relevant accumulation with daily dosing.
1.3 hours (range 0.5–2.0 h); short half-life consistent with use for sleep initiation without residual sedation.
Primarily hepatic metabolism; 77-88% excreted in feces as metabolites, 13-23% in urine as metabolites. <1% excreted unchanged.
Primarily hepatic metabolism via CYP1A2 and CYP3A4; <0.1% excreted unchanged in urine; fecal excretion accounts for ~80% of total clearance as metabolites.
Category C
Category C
Melatonin Receptor Agonist
Melatonin Receptor Agonist
"The serum concentration of Clarithromycin can be increased when it is combined with Tasimelteon."