Tebideutorexant

A dual orexin receptor antagonist

{{Drugbox | verifiedfields = changed | verifiedrevid = 123456789 | IUPAC_name = (2S)-2-[[4-(5-chloro-2-methylphenyl)piperazin-1-yl]methyl]-N-[(2S)-1-oxo-3-phenyl-1,2,3,4-tetrahydroisoquinolin-2-yl]butanamide | image = JNJ-61393215.svg | image2 = | width = 200 | alt = | caption = Chemical structure of Tebideutorexant }}

Tebideutorexant is a dual orexin receptor antagonist (DORA) that is being investigated for its potential use in the treatment of insomnia and other sleep disorders. It is known by its developmental code name JNJ-61393215.

Mechanism of Action

Tebideutorexant functions by selectively blocking the activity of the orexin neuropeptides, which are involved in the regulation of the sleep-wake cycle. Orexins, also known as hypocretins, are produced in the hypothalamus and promote wakefulness. By antagonizing the orexin receptors OX1 and OX2, tebideutorexant reduces wakefulness and facilitates the onset and maintenance of sleep.

Pharmacokinetics

Tebideutorexant is designed to have a favorable pharmacokinetic profile, with a rapid onset of action and a duration that supports sleep throughout the night without causing residual sedation the following day. The drug is metabolized primarily in the liver and excreted via the kidneys.

Clinical Development

Tebideutorexant is currently undergoing clinical trials to evaluate its efficacy and safety in patients with insomnia. Preliminary studies have shown promising results, with improvements in sleep onset and maintenance compared to placebo.

Potential Benefits

As a dual orexin receptor antagonist, tebideutorexant offers a novel approach to treating insomnia, particularly for patients who do not respond well to traditional benzodiazepine or non-benzodiazepine hypnotics. Its mechanism of action allows for a more natural sleep architecture, potentially reducing the risk of dependence and other side effects associated with other sleep medications.

Related pages

• Orexin receptor antagonist
• Insomnia
• Sleep disorder