Tasimelteon

The mechanism by which tasimelteon exerts its therapeutic effect in patients with Non­-24 is unclear. However, tasimelteon is an agonist at melatonin MT 1 and MT 2 receptors which are thought to be involved in the control of circadian rhythms.

• Tasimelteon capsules are a melatonin receptor agonist. Tasimelteon capsules are indicated for the treatment of Non ­24-Hour Sleep-Wake Disorder (Non-24) in adults ( 1 ) 1.1 Non-24-Hour Sleep-Wake Disorder (Non-24) Tasimelteon capsules are indicated for the treatment of Non-24 in adults.

• None.contraindicated

Indicated Population Dosage Form Body Weight Recommended Dosage Non-24 ( 2.2 ) Adults Capsules Not applicable 20 mg one hour prior to bedtime Tasimelteon capsules and tasimelteon oral suspension are not substitutable ( 2.1 ) Administer at the same time every night ( 2.2 ) Take without food ( 2.4 ) 2.1 Non-Interchangeability between Tasimelteon Capsules and Tasimelteon Oral Suspension Tasimelteon capsules and tasimelteon oral suspension are not substitutable [see Clinical Pharmacology ( 12.3 )]. 2.2 Recommended Dosage for Tasimelteon Capsules for Non-24 Adults The recommended dosage of tasimelteon capsules in adults is 20 mg one hour before bedtime, at the same time every night. Because of individual differences in circadian rhythms, drug effect may not occur for weeks or months. 2.4 Important Administration Information Administer tasimelteon capsules without food [see Clinical Pharmacology ( 12.3 )]. If a patient is unable to take tasimelteon capsules at approximately the same time on a given night, they should skip that dose and take the next dose as scheduled.

May cause somnolence: After taking tasimelteon capsules, patients should limit their activity to preparing for going to bed, because tasimelteon capsules can impair the performance of activities requiring complete mental alertness ( 5.1 ) 5.1 Somnolence After taking tasimelteon capsules, patients should limit their activity to preparing for going to bed. Tasimelteon capsules can potentially impair the performance of activities requiring complete mental alertness.

The most common adverse reactions (incidence >5% and at least twice as high on tasimelteon than on placebo) were headache, increased alanine aminotransferase, nightmares or unusual dreams, and upper respiratory or urinary tract infection ( 6.1) To report SUSPECTED ADVERSE REACTIONS, contact Apotex Corp. at 1-800-706-5575 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. More than 2080 subjects have been treated with at least one dose of tasimelteon, of which more than 380 have been treated for > 26 weeks and more than 170 have been treated for > 1 year. Non-24-Hour Sleep-Wake Disorder (Non-24) A 26-week, parallel-arm placebo-controlled study (Study 1) evaluated tasimelteon (n=42) compared to placebo (n=42) in patients with Non-24. A randomized-withdrawal, placebo-controlled study of 8 weeks duration (Study 2) also evaluated tasimelteon (n=10), compared to placebo (n=10), in patients with Non-24. In placebo-controlled studies, 6% of patients exposed to tasimelteon discontinued treatment due to an adverse event, compared with 4% of patients who received placebo. Table 2 shows the incidence of adverse reactions from Study 1.

Hepatic impairment: Tasimelteon has not been studied in patients with severe hepatic impairment and is not recommended in these patients ( 8.6 ) 8.1 Pregnancy Risk Summary Available postmarketing case reports with tasimelteon use in pregnant women are not sufficient to evaluate drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes. In pregnant rats, no embryofetal developmental toxicity was observed at exposures of 50 mg/kg/day, or up to 24 times higher than the human exposure at the maximum recommended human dose (MRHD) (see Data). The estimated background risk of major birth defects and miscarriage for the indicated populations are unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data In pregnant rats administered tasimelteon at oral doses of 5, 50, or 500 mg/kg/day during the period of organogenesis, there were no effects on embryofetal development. The highest dose tested is approximately 240 times the MRHD of 20 mg/day, based on mg/m 2 body surface area.

Metabolism

The pharmacokinetics of tasimelteon is linear over doses ranging from 3 to 300 mg (0.15 to 15 times the recommended daily dosage). The pharmacokinetics of tasimelteon and its metabolites did not change with repeated daily dosing.

There is limited premarketing clinical experience with the effects of an overdosage of tasimelteon. As with the management of any overdose, general symptomatic and supportive measures should be used, along with immediate gastric lavage where appropriate. Intravenous fluids should be administered as needed. Respiration, pulse, blood pressure, and other appropriate vital signs should be monitored, and general supportive measures employed. While hemodialysis was effective at clearing tasimelteon and the majority of its major metabolites in patients with renal impairment, it is not known if hemodialysis will effectively reduce exposure in the case of overdose. As with the management of any overdose, the possibility of multiple drug ingestion should be considered. Contact a poison control center for current information on the management of overdose.

• Jan 31, 2014NDANDA205677Vanda Pharms Inc
• Dec 1, 2020NDANDA214517Vanda Pharms Inc
• Dec 12, 2022ANDAANDA211601Teva Pharms Usa Inc
• Dec 20, 2022ANDAANDA211607Apotex
• Jan 12, 2023ANDAANDA211654Msn

1. 1Drug Ineffective1,63528%
2. 2Insomnia72813%
3. 3Product Dose Omission Issue4808.3%
4. 4Middle Insomnia4127.1%
5. 5Somnolence4087.1%
6. 6Headache3846.7%
7. 7Nightmare2684.6%
8. 8Abnormal Dreams2233.9%
9. 9Fatigue2223.9%
10. 10Therapeutic Product Effect Decreased1963.4%
11. 11Sleep Disorder1883.3%
12. 12Inappropriate Schedule Of Product Administration1793.1%
13. 13Incorrect Product Administration Duration1652.9%
14. 14Poor Quality Sleep1542.7%
15. 15Initial Insomnia1532.7%

The 10 most recently updated of 25 ClinicalTrials.gov registrations naming Tasimelteon as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Evaluating the Effects of Tasimelteon vs. Placebo in Treating Pediatric Insomnia
  Recruiting · Phase 3 · Interventional · 420 enrolled · Vanda Pharmaceuticals
  NCT06953869updated 2026-06-05
• Evaluating the Effects of Tasimelteon vs. Placebo in Delayed Sleep-Wake Phase Disorder (DSWPD)
  Recruiting · Phase 3 · Interventional · 70 enrolled · Vanda Pharmaceuticals
  NCT04652882updated 2025-12-02
• The Effects of Tasimelteon in Participants With REM Behavior Disorder (RBD)
  Terminated · Early phase 1 · Interventional · 20 enrolled · Brigham and Women's Hospital
  NCT05922995updated 2025-10-09
• Evaluating the Effects of Tasimelteon Vs. Placebo in Delayed Sleep-Wake Phase Disorder (DSWPD) and the CRY1Δ11 Variant
  Recruiting · Phase 3 · Interventional · 60 enrolled · Vanda Pharmaceuticals
  NCT06701396updated 2024-11-22
• Safety Study of Tasimelteon for Treatment of Non-24-Hour-Sleep-Wake Disorder in Blind Individuals With No Light Perception
  Unknown · Phase 3 · Interventional · 140 enrolled · Vanda Pharmaceuticals
  NCT01218789updated 2024-04-03
• Evaluating the Effects of Tasimelteon in Individuals With Autism Spectrum Disorder (ASD) and Sleep Disturbances
  Unknown · Phase 3 · Interventional · 100 enrolled · Vanda Pharmaceuticals
  NCT05361707updated 2024-03-21
• Evaluation of Next-Day Residual Effects of Tasimelteon Compared With Placebo and Active Control in Healthy Subjects
  Completed · Phase 1 · Interventional · 48 enrolled · Vanda Pharmaceuticals
  NCT06323655updated 2024-03-21
• Bioequivalence Study Between Tasimelteon Capsule Formulation and Liquid Suspension Formulation in Healthy Volunteers
  Completed · Phase 1 · Interventional · 36 enrolled · Vanda Pharmaceuticals
  NCT05572281updated 2024-03-21
• Study of the Pharmacokinetics and Safety of Tasimelteon in Children and Adolescents
  Completed · Phase 1 · Interventional · 24 enrolled · Vanda Pharmaceuticals
  NCT02776215updated 2024-03-21
• Evaluating the Effects of Tasimelteon vs. Placebo on Jet Lag Type Insomnia
  Completed · Phase 3 · Interventional · 320 enrolled · Vanda Pharmaceuticals
  NCT03373201updated 2023-09-15

Frequently asked questions

How does Tasimelteon work?

The mechanism by which tasimelteon exerts its therapeutic effect in patients with Non­-24 is unclear. However, tasimelteon is an agonist at melatonin MT 1 and MT 2 receptors which are thought to be involved in the control of circadian rhythms.

What is Tasimelteon used for?

According to FDA labeling, Tasimelteon carries indications including: Tasimelteon capsules are a melatonin receptor agonist. Tasimelteon capsules are indicated for the treatment of Non ­24-Hour Sleep-Wake Disorder (Non-24) in adults ( 1 ) 1.1 Non-24-Hour Sleep-Wake Disorder (Non-24) Tasimelteon capsules are indicated for the treatment of Non-24 in adults.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Tasimelteon?

Tasimelteon is classified as Melatonin receptor agonists, Melatonin Receptor Agonist, Melatonin Receptor Agonists, Increased Melatonin Activity.

What are the brand names for Tasimelteon?

Tasimelteon is marketed under brand names including Hetlioz.

What are the contraindications for Tasimelteon?

Tasimelteon labeling lists contraindications including: None.. Always consult the full prescribing information and a clinician.