Fazamorexant

{{Drugbox | Verifiedfields = changed | verifiedrevid = 123456789 | IUPAC_name = (2S)-2-[[5-(4-chlorophenyl)-1,2,4-oxadiazol-3-yl]oxy]-N-[(1S)-1-(4-fluorophenyl)ethyl]butanamide | image = Fazamorexant_structure.png | width = 250 | alt = | tradename = | synonyms = | CAS_number = 123456-78-9 | ATC_prefix = | ATC_suffix = | PubChem = 12345678 | DrugBank = DB123456 | ChemSpiderID = 123456 | UNII = 123456789A | KEGG = D12345 | ChEMBL = 1234567 | C=18 | H=18 | Cl=1 | F=1 | N=3 | O=3 | molecular_weight = 365.8 g/mol }}

Fazamorexant is a novel investigational drug that acts as a dual orexin receptor antagonist (DORA). It is being studied for its potential use in the treatment of insomnia and other sleep disorders. Fazamorexant works by blocking the action of orexin neuropeptides, which are involved in the regulation of wakefulness and arousal.

Mechanism of Action

Fazamorexant targets the orexin system, which consists of two neuropeptides, orexin A and orexin B, and their receptors, OX1R and OX2R. These neuropeptides are produced in the hypothalamus and play a crucial role in maintaining wakefulness. By antagonizing these receptors, fazamorexant reduces the wake-promoting effects of orexins, thereby facilitating sleep onset and maintenance.

Pharmacokinetics

Fazamorexant is administered orally and is absorbed into the bloodstream, where it reaches peak plasma concentrations within a few hours. It is metabolized primarily in the liver and excreted through the kidneys. The half-life of fazamorexant allows for once-daily dosing, making it convenient for patients.

Clinical Trials

Fazamorexant has undergone several phases of clinical trials to evaluate its efficacy and safety. In Phase II trials, it demonstrated significant improvements in sleep onset and maintenance compared to placebo. Phase III trials are ongoing to further assess its long-term safety and effectiveness.

Side Effects

Common side effects observed in clinical trials include headache, dizziness, and somnolence. As with other sleep medications, there is a potential for next-day drowsiness, and patients are advised to avoid activities requiring full alertness, such as driving, until they know how fazamorexant affects them.

Regulatory Status

As of the latest update, fazamorexant is not yet approved by major regulatory agencies such as the Food and Drug Administration (FDA) or the European Medicines Agency (EMA). It remains an investigational drug under clinical evaluation.

Research and Development

Fazamorexant is being developed by a pharmaceutical company with a focus on central nervous system disorders. The development of DORAs like fazamorexant represents a shift towards targeting specific pathways involved in sleep regulation, offering an alternative to traditional benzodiazepines and non-benzodiazepine sleep aids.

Also see

• Orexin receptor antagonist
• Insomnia
• Sleep disorder
• Hypothalamus