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Tasimelteon

Tasimelteon, also known by its brand name Hetlioz, is a melatonin receptor agonist that has been investigated in several clinical trials for its potential in treating various sleep-wake disorders. These trials have focused on evaluating the drug’s efficacy, safety, and pharmacokinetics in different patient populations, including those with Non-24-Hour Sleep-Wake Disorder, REM Behavior Disorder, and other circadian rhythm sleep disorders. The studies have also examined the effects of factors such as renal impairment, hepatic impairment, and drug interactions on tasimelteon’s performance in the body.

Table of Contents

What is Tasimelteon?

Tasimelteon is a medication used to treat certain sleep disorders. It is also known by its brand name Hetlioz™ and was previously referred to as VEC-162 or BMS-214778 during its development[1]. Tasimelteon belongs to a class of drugs called melatonin receptor agonists, which means it works similarly to the natural sleep hormone melatonin in your body[2].

What Conditions Does Tasimelteon Treat?

Tasimelteon is primarily used to treat the following conditions:

  • Non-24-Hour Sleep-Wake Disorder (Non-24): This is a condition common in totally blind people where their internal sleep-wake cycle is out of sync with the 24-hour day-night cycle. It causes nighttime sleep problems and daytime difficulties, including an overwhelming urge to nap[1].
  • REM Behavior Disorder (RBD): This is a sleep disorder characterized by abnormal behaviors during REM sleep, which can lead to injury and disturbed sleep[3].
  • Circadian Rhythm Sleep Disorders: These are disorders where a person’s internal body clock is misaligned with the external environment[4].
  • Sleep disturbances in Autism Spectrum Disorder (ASD): Tasimelteon is being studied for its potential to improve sleep in individuals with ASD[5].

How Does Tasimelteon Work?

Tasimelteon works by mimicking the effects of melatonin, a hormone naturally produced by your body that helps regulate sleep. It activates melatonin receptors in the brain, specifically the MT1 and MT2 receptors. This activation helps to reset your body’s internal clock (circadian rhythm) and promote sleep at the appropriate time[3].

In conditions like Non-24, where the internal body clock is not synchronized with the 24-hour day, tasimelteon can help align the sleep-wake cycle with the external environment. This can lead to improved nighttime sleep and reduced daytime sleepiness[6].

Dosage and Administration

Tasimelteon is typically taken as a single daily dose, usually about 1 hour before bedtime. The most common dosage studied is 20 mg, which comes in capsule form[7]. However, the exact dosage may vary depending on the condition being treated and individual patient factors. Always follow your doctor’s instructions regarding dosage and timing.

For children and adolescents, a liquid suspension form of tasimelteon may be available, allowing for more precise dosing based on body weight[5].

Efficacy Studies

Several clinical trials have been conducted to evaluate the effectiveness of tasimelteon:

  • In studies of Non-24 in blind individuals, tasimelteon has shown to improve nighttime sleep, reduce daytime napping, and help synchronize the internal body clock with the 24-hour day[6].
  • Research is ongoing to assess its effectiveness in treating REM Behavior Disorder, with potential improvements in dream enactment events and overall sleep quality[3].
  • Studies are also underway to evaluate tasimelteon’s efficacy in treating sleep disturbances in individuals with Autism Spectrum Disorder[5].

Safety and Side Effects

Tasimelteon has generally been well-tolerated in clinical trials. However, like all medications, it can cause side effects. Common side effects may include:

  • Headache
  • Increased liver enzymes
  • Nightmares or unusual dreams
  • Drowsiness or sleepiness

Safety is continuously monitored in clinical trials through various measures, including blood tests, electrocardiograms (ECGs), and assessments for suicidal thoughts or behaviors[7][1].

Use in Special Populations

Research has been conducted to understand how tasimelteon affects different groups of people:

  • Kidney Impairment: Studies have looked at how tasimelteon is processed in people with various levels of kidney function, including those with severe kidney impairment and those on dialysis[8].
  • Liver Impairment: The effects of mild to moderate liver disease on tasimelteon processing have been studied[2].
  • Children and Adolescents: Research is ongoing to determine appropriate dosing and safety in younger populations, particularly those with sleep disorders related to conditions like autism[4][5].
  • Elderly: Studies have included older adults to assess any age-related differences in how the body processes tasimelteon[9].

Drug Interactions

Tasimelteon can interact with other medications, particularly those that affect liver enzymes. Two important interactions that have been studied are:

  • Strong CYP3A4 Inhibitors (e.g., ketoconazole): These may increase the levels of tasimelteon in your body.
  • Strong CYP3A4 Inducers (e.g., rifampin): These may decrease the levels of tasimelteon in your body[10].

Always inform your healthcare provider about all medications, supplements, and herbal products you are taking to avoid potential interactions.

Aspect Details
Primary Uses Treatment of Non-24-Hour Sleep-Wake Disorder, potential for other circadian rhythm sleep disorders
Mechanism of Action Melatonin receptor agonist
Common Dosage 20 mg oral capsule, taken daily
Trial Populations Blind individuals, patients with renal or hepatic impairment, healthy volunteers
Key Outcomes Measured Pharmacokinetics, safety, tolerability, efficacy in treating sleep disorders
Trial Durations Single-dose studies to long-term trials lasting up to 24 months or more
Special Considerations Effects of renal/hepatic impairment, drug interactions, age, smoking status, and body size on tasimelteon’s performance

FAQ

  • What is tasimelteon used for? Tasimelteon is primarily used for treating Non-24-Hour Sleep-Wake Disorder in blind individuals with no light perception. It has also been studied for potential use in other sleep disorders such as REM Behavior Disorder and circadian rhythm sleep disorders.
  • How does tasimelteon work? Tasimelteon is a melatonin receptor agonist. It works by activating melatonin receptors in the brain, which helps regulate the body's internal clock and sleep-wake cycles.
  • What dosage of tasimelteon is typically used in clinical trials? In most clinical trials, tasimelteon is administered as a 20 mg oral capsule taken daily, usually before bedtime. However, some studies have explored different dosages and administration methods, including intravenous administration.
  • Are there any known side effects of tasimelteon? While specific side effects are not detailed in the provided trial information, the studies consistently monitored for adverse events, changes in laboratory parameters, vital signs, and ECG readings. Safety and tolerability were key aspects evaluated in these clinical trials.
  • How long do tasimelteon clinical trials typically last? The duration of tasimelteon clinical trials varies widely. Some studies involve single-dose administration, while others last for extended periods, ranging from 4 weeks to 24 months, with some even including optional extensions of up to 3 additional years.

Ongoing Clinical Trials on Tasimelteon

  • Study of tasimelteon compared to placebo for treating insomnia in children

    Recruiting

    1 1
    Investigated drugs:
    Germany Poland

  • Study on the Effects of Tasimelteon for Patients with Delayed Sleep-Wake Phase Disorder

    Recruiting

    1 1 1
    Investigated drugs:
    Austria Germany

  • Safety Study of Tasimelteon for Treating Non-24-Hour Sleep-Wake Disorder in Blind Individuals Without Light Perception

    Not yet recruiting

    1 1 1 1
    Investigated drugs:
    France

Glossary

  • Pharmacokinetics (PK): The study of how a drug is absorbed, distributed, metabolized, and eliminated by the body. It describes what the body does to the drug.
  • Non-24-Hour Sleep-Wake Disorder (N24HSWD): A circadian rhythm sleep disorder that occurs when individuals, often those who are totally blind, are unable to synchronize their internal body clock with the 24-hour day-night cycle.
  • REM Behavior Disorder (RBD): A sleep disorder characterized by abnormal behaviors emerging during REM sleep, potentially leading to injury and disturbed sleep.
  • Circadian Rhythm Sleep Disorders: A group of sleep disorders that occur when the internal body clock is out of sync with external time cues, leading to problems with the timing of sleep.
  • Melatonin Receptor Agonist: A type of drug that activates melatonin receptors in the brain, mimicking the effects of the natural hormone melatonin, which regulates sleep-wake cycles.
  • Area Under the Curve (AUC): A measure used in pharmacokinetics to represent the total drug exposure over time.
  • Maximum Concentration (Cmax): The peak concentration of a drug in the blood after administration.
  • Half-life (T1/2): The time it takes for the concentration of a drug in the body to reduce by half.
  • Bioavailability: The proportion of a drug that enters the circulation when introduced into the body and is able to have an active effect.
  • Cytochrome P450 3A4 (CYP3A4): An important enzyme in the body responsible for breaking down many medications.

References

  1. https://clinicaltrials.gov/study/NCT02130999
  2. https://clinicaltrials.gov/study/NCT01271387
  3. https://clinicaltrials.gov/study/NCT05922995
  4. https://clinicaltrials.gov/study/NCT02776215
  5. https://clinicaltrials.gov/study/NCT05361707
  6. https://clinicaltrials.gov/study/NCT01429116
  7. https://clinicaltrials.eu/trial/safety-study-of-tasimelteon-for-treating-non-24-hour-sleep-wake-disorder-in-blind-individuals-without-light-perception/
  8. https://clinicaltrials.gov/study/NCT01526746
  9. https://clinicaltrials.gov/study/NCT01477619
  10. https://clinicaltrials.gov/study/NCT01637636