Nivasorexant

{{Drugbox | Verifiedfields = changed | verifiedrevid = 123456789 | IUPAC_name = (2R)-2-[[4-[(5-chloro-2-pyridinyl)oxy]phenyl]methyl]-N-[[3-(trifluoromethyl)phenyl]methyl]butanamide | image = Nivasorexant_structure.png | width = 250 | alt = | tradename = | synonyms = | CAS_number = 123456-78-9 | ATC_prefix = | ATC_suffix = | PubChem = 12345678 | DrugBank = DB12345 | ChemSpiderID = 123456 | UNII = 123456789A | KEGG = D12345 | ChEBI = 12345 | ChEMBL = 1234567 | C=20 | H=19 | Cl=1 | F=3 | N=2 | O=2 | molecular_weight = 408.83 }}

Nivasorexant is a novel pharmaceutical compound under investigation for its potential use as a treatment for insomnia and other sleep disorders. It belongs to a class of drugs known as orexin receptor antagonists, which function by inhibiting the action of orexin, a neuropeptide that regulates wakefulness.

Mechanism of Action

Nivasorexant acts as a selective antagonist of the orexin receptors, specifically targeting the OX1 and OX2 receptors. Orexins, also known as hypocretins, are neuropeptides produced in the hypothalamus that play a crucial role in maintaining wakefulness and regulating the sleep-wake cycle. By blocking these receptors, nivasorexant reduces the activity of orexin, thereby promoting sleep.

Pharmacokinetics

The pharmacokinetic profile of nivasorexant includes rapid absorption with peak plasma concentrations occurring approximately 1-2 hours post-administration. It is metabolized primarily in the liver via the cytochrome P450 enzyme system, with CYP3A4 being the major isoform involved. The elimination half-life of nivasorexant is approximately 8-10 hours, allowing for once-daily dosing.

Clinical Trials

Nivasorexant is currently undergoing clinical trials to evaluate its efficacy and safety in treating insomnia. Preliminary results from Phase II trials have shown promising improvements in sleep onset and maintenance, with a favorable safety profile. Common side effects reported include mild headache and dizziness.

Potential Benefits

The development of nivasorexant offers a potential alternative to traditional benzodiazepines and non-benzodiazepine hypnotics, which are associated with various side effects and dependency issues. As an orexin receptor antagonist, nivasorexant may provide a more targeted approach to treating sleep disorders with fewer adverse effects.

Regulatory Status

As of the latest update, nivasorexant has not yet received approval from major regulatory bodies such as the U.S. Food and Drug Administration (FDA) or the European Medicines Agency (EMA). Ongoing studies aim to provide the necessary data to support its approval for clinical use.

Also see

• Orexin receptor antagonist
• Insomnia
• Sleep disorder
• Hypothalamus
• Cytochrome P450

Receptor Antagonists
Receptor Type	Example Antagonists
Adrenergic receptor	Propranolol, Prazosin
Cholinergic receptor	Atropine, Scopolamine
Dopamine receptor	Haloperidol, Clozapine
Histamine receptor	Ranitidine, Diphenhydramine
Serotonin receptor	Ondansetron, Risperidone
Glutamate receptor	Memantine, Ketamine
GABA receptor	Flumazenil, Bicuculline
Opioid receptor	Naloxone, Naltrexone
Angiotensin receptor	Losartan, Valsartan