Peringatan Keamanan

Clinical experience with lemborexant overdose is limited. In clinical studies, healthy patients receiving doses up to 10x the recommended maximum dose experienced dose-dependent increases in the frequency of adverse effects such as somnolence - it is likely, then, that symptoms of overdose will be consistent with lemborexant's adverse effect profile.L10863 In the event of an overdosage, implement supportive measures and consult the nearest poison control center for the most up to date management strategies. As lemborexant is highly protein-bound, hemodialysis is likely to be of little use in overdose situations.L10863

Lemborexant

DB11951

small molecule approved investigational

Deskripsi

Lemborexant is a novel dual orexin receptor antagonist used in the treatment of insomnia characterized by difficulties with sleep onset and/or sleep maintenance.L10863 Recent research in the field of sleep disorders has revealed that insomnia is likely driven not by the inability of the brain to "switch on" sleep-related circuits, but rather an inability to "switch-off" wake-promoting circuits.A189006,A189030 Whereas historically popular pharmacologic treatments for insomnia (e.g. zopiclone, zolpidem, benzodiazepines) focus on enhancing sleep drive via modulation of GABA and melatonin receptors, lemborexant and other orexin antagonists (e.g. suvorexant) act to counteract inappropriate wakefulness.A189006 This novel mechanism of action offers potential advantages over classic hypnotic agents, including a more favorable adverse effect profile and potentially greater efficacy, and may signal the beginning of a new wave of treatment options for patients suffering from insomnia.A189006

Struktur Molekul 2D

Berat 410.425
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life for lemborexant at doses of 5mg and 10mg is 17 and 19 hours, respectively.[L10863]
Volume Distribusi The volume of distribution of lemborexant is 1970 L, indicating extensive tissue distribution.[L10863]
Klirens (Clearance) -

Absorpsi

Animal models of lemborexant disposition have demonstrated rapid absorption following oral administration.A189003 The Tmax of lemborexant is approximately 1-3 hours, or 3-5 hours following administration of a high-fat, high-calorie meal.L10863 Cmax and AUC0-24h increase at a rate slightly less than proportionate to the given dose. Following administration of a high-fat, high-calorie meal, Cmax is decreased by 23% and AUC0-inf is increased by 18%.L10863 AUC, Cmax, and terminal half-life are increased in the presence of moderate hepatic impairment, and AUC (but not half-life) is increased in the presence of mild hepatic impairment.L10863

Metabolisme

Given that less than 1% of an administered dose is recovered unchanged in the urine,L10863 it is likely that lemborexant is extensively metabolized - this has been confirmed in rat and monkey models,A189003 but its metabolism in humans has not been fully characterized. Prescribing information states that it is predominantly metabolized by CYP3A4, with a smaller contribution by CYP3A5. The major circulating metabolite is lemborexant's M10 metabolite, which is pharmacologically active and binds to orexin receptors with a similar affinity to the parent drug. The M10 metabolite has the potential to induce CYP3A and CYP2B6 enzymes, weakly inhibit CYP3A enzymes, and is a substrate of P-gp transporters.L10863

Rute Eliminasi

Following oral administration, 57.4% of the dose is found in the feces and 29.1% in the urine. Less than 1% of the dose recovered in the urine exists as unchanged parent drug, suggesting extensive metabolism.L10863

Interaksi Makanan

1 Data
  • 1. Take on an empty stomach. Co-administration with food delays absorption and sleep onset.

Interaksi Obat

1151 Data
Ranolazine The serum concentration of Lemborexant can be increased when it is combined with Ranolazine.
Buprenorphine Lemborexant may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Lemborexant.
Dronabinol The serum concentration of Lemborexant can be increased when it is combined with Dronabinol.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Lemborexant.
Hydrocodone Lemborexant may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Lemborexant.
Magnesium sulfate The therapeutic efficacy of Lemborexant can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Lemborexant may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Lemborexant may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Lemborexant.
Mirtazapine Lemborexant may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Lemborexant.
Orphenadrine Lemborexant may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Lemborexant may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Pramipexole Lemborexant may increase the sedative activities of Pramipexole.
Ropinirole Lemborexant may increase the sedative activities of Ropinirole.
Rotigotine Lemborexant may increase the sedative activities of Rotigotine.
Sodium oxybate Lemborexant may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Lemborexant may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Lemborexant.
Thalidomide Lemborexant may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Lemborexant may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Lemborexant.
Azelastine Lemborexant may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Lemborexant.
Trazodone The risk or severity of adverse effects can be increased when Lemborexant is combined with Trazodone.
Citalopram The risk or severity of adverse effects can be increased when Lemborexant is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Lemborexant is combined with Duloxetine.
Sibutramine The risk or severity of adverse effects can be increased when Lemborexant is combined with Sibutramine.
Escitalopram The risk or severity of adverse effects can be increased when Lemborexant is combined with Escitalopram.
Zimelidine The risk or severity of adverse effects can be increased when Lemborexant is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Lemborexant is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Lemborexant is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Lemborexant is combined with Desvenlafaxine.
Indalpine The risk or severity of adverse effects can be increased when Lemborexant is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Lemborexant is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Lemborexant is combined with Alaproclate.
Sertraline The risk or severity of adverse effects can be increased when Lemborexant is combined with Sertraline.
Oxybutynin The metabolism of Lemborexant can be decreased when combined with Oxybutynin.
Quetiapine The risk or severity of CNS depression can be increased when Quetiapine is combined with Lemborexant.
Aripiprazole The risk or severity of CNS depression can be increased when Aripiprazole is combined with Lemborexant.
Olanzapine The risk or severity of CNS depression can be increased when Olanzapine is combined with Lemborexant.
Promazine The risk or severity of CNS depression can be increased when Promazine is combined with Lemborexant.
Cyproheptadine The risk or severity of CNS depression can be increased when Cyproheptadine is combined with Lemborexant.
Chlorpromazine The risk or severity of CNS depression can be increased when Chlorpromazine is combined with Lemborexant.
Gallamine triethiodide The risk or severity of CNS depression can be increased when Gallamine triethiodide is combined with Lemborexant.
Triflupromazine The risk or severity of CNS depression can be increased when Triflupromazine is combined with Lemborexant.
Amoxapine The risk or severity of CNS depression can be increased when Amoxapine is combined with Lemborexant.
Lamotrigine The risk or severity of CNS depression can be increased when Lamotrigine is combined with Lemborexant.
Rocuronium The risk or severity of CNS depression can be increased when Rocuronium is combined with Lemborexant.
Scopolamine The risk or severity of CNS depression can be increased when Scopolamine is combined with Lemborexant.
Clidinium The risk or severity of CNS depression can be increased when Clidinium is combined with Lemborexant.
Propiomazine The risk or severity of CNS depression can be increased when Propiomazine is combined with Lemborexant.
Flupentixol Flupentixol may increase the sedative activities of Lemborexant.
Maprotiline The risk or severity of CNS depression can be increased when Maprotiline is combined with Lemborexant.
Diphenhydramine The risk or severity of CNS depression can be increased when Diphenhydramine is combined with Lemborexant.
Doxacurium The risk or severity of CNS depression can be increased when Doxacurium is combined with Lemborexant.
Doxepin The risk or severity of CNS depression can be increased when Doxepin is combined with Lemborexant.
Mivacurium The risk or severity of CNS depression can be increased when Mivacurium is combined with Lemborexant.
Chlorprothixene The risk or severity of CNS depression can be increased when Chlorprothixene is combined with Lemborexant.
Metocurine The risk or severity of CNS depression can be increased when Metocurine is combined with Lemborexant.
Pancuronium The risk or severity of CNS depression can be increased when Pancuronium is combined with Lemborexant.
Pipecuronium The risk or severity of CNS depression can be increased when Pipecuronium is combined with Lemborexant.
Rapacuronium The risk or severity of CNS depression can be increased when Rapacuronium is combined with Lemborexant.
Pizotifen The risk or severity of CNS depression can be increased when Pizotifen is combined with Lemborexant.
Benactyzine The risk or severity of CNS depression can be increased when Benactyzine is combined with Lemborexant.
Umeclidinium The serum concentration of Lemborexant can be increased when it is combined with Umeclidinium.
Revefenacin The serum concentration of Lemborexant can be increased when it is combined with Revefenacin.
Emepronium The risk or severity of CNS depression can be increased when Lemborexant is combined with Emepronium.
Nortriptyline The risk or severity of CNS depression can be increased when Nortriptyline is combined with Lemborexant.
Desipramine The risk or severity of CNS depression can be increased when Desipramine is combined with Lemborexant.
Zopiclone The risk or severity of adverse effects can be increased when Lemborexant is combined with Zopiclone.
Lidocaine The risk or severity of CNS depression can be increased when Lidocaine is combined with Lemborexant.
Alprazolam The risk or severity of CNS depression can be increased when Alprazolam is combined with Lemborexant.
Buspirone The risk or severity of CNS depression can be increased when Buspirone is combined with Lemborexant.
Oxycodone The risk or severity of CNS depression can be increased when Oxycodone is combined with Lemborexant.
Dextromethorphan The risk or severity of CNS depression can be increased when Dextromethorphan is combined with Lemborexant.
Midazolam The risk or severity of sedation and CNS depression can be increased when Midazolam is combined with Lemborexant.
Risperidone The risk or severity of CNS depression can be increased when Risperidone is combined with Lemborexant.
Diazepam The risk or severity of CNS depression can be increased when Diazepam is combined with Lemborexant.
Triazolam The risk or severity of CNS depression can be increased when Triazolam is combined with Lemborexant.
Ondansetron The risk or severity of CNS depression can be increased when Ondansetron is combined with Lemborexant.
Zonisamide The risk or severity of CNS depression can be increased when Zonisamide is combined with Lemborexant.
Zaleplon The risk or severity of CNS depression can be increased when Zaleplon is combined with Lemborexant.
Chlorpheniramine The risk or severity of CNS depression can be increased when Chlorpheniramine is combined with Lemborexant.
Levacetylmethadol The risk or severity of CNS depression can be increased when Levacetylmethadol is combined with Lemborexant.
Paliperidone The risk or severity of CNS depression can be increased when Paliperidone is combined with Lemborexant.
Iloperidone The risk or severity of CNS depression can be increased when Iloperidone is combined with Lemborexant.
Aripiprazole lauroxil The risk or severity of CNS depression can be increased when Lemborexant is combined with Aripiprazole lauroxil.
Botulinum toxin type B The risk or severity of CNS depression can be increased when Botulinum toxin type B is combined with Lemborexant.
Botulinum toxin type A The risk or severity of CNS depression can be increased when Botulinum toxin type A is combined with Lemborexant.
Tryptophan The risk or severity of CNS depression can be increased when Tryptophan is combined with Lemborexant.
Baclofen Baclofen may increase the central nervous system depressant (CNS depressant) activities of Lemborexant.
Lorazepam The risk or severity of CNS depression can be increased when Lorazepam is combined with Lemborexant.
Ethchlorvynol The risk or severity of CNS depression can be increased when Ethchlorvynol is combined with Lemborexant.
Succinylcholine The risk or severity of CNS depression can be increased when Succinylcholine is combined with Lemborexant.
Enflurane The risk or severity of CNS depression can be increased when Enflurane is combined with Lemborexant.
Temazepam The risk or severity of CNS depression can be increased when Temazepam is combined with Lemborexant.
Reboxetine The risk or severity of CNS depression can be increased when Reboxetine is combined with Lemborexant.

Target Protein

Orexin/Hypocretin receptor type 1 HCRTR1
Orexin receptor type 2 HCRTR2

Referensi & Sumber

Synthesis reference: Yoshida, Y. et. al. "Discovery of (1R,2S)-2-{(2,4-Dimethylpyrimidin-5-yl)oxymethyl}-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropanecarboxamide (E2006): A Potent and Efficacious Oral Orexin Receptor Antagonist," J. Med. Chem. 2015, 58, 11, 4648-4664.
Artikel (PubMed)
  • PMID: 31830270
    Mahoney CE, Mochizuki T, Scammell TE: Dual orexin receptor antagonists increase sleep and cataplexy in wild type mice. Sleep. 2019 Dec 13. pii: 5674930. doi: 10.1093/sleep/zsz302.
  • PMID: 29806508
    Ueno T, Ishida T, Kusano K: Disposition and metabolism of (14)Clemborexant, a novel dual orexin receptor antagonist, in rats and monkeys. Xenobiotica. 2019 Jun;49(6):688-697. doi: 10.1080/00498254.2018.1482509. Epub 2018 Jul 5.
  • PMID: 28559480
    Beuckmann CT, Suzuki M, Ueno T, Nagaoka K, Arai T, Higashiyama H: In Vitro and In Silico Characterization of Lemborexant (E2006), a Novel Dual Orexin Receptor Antagonist. J Pharmacol Exp Ther. 2017 Aug;362(2):287-295. doi: 10.1124/jpet.117.241422. Epub 2017 May 30.
  • PMID: 30923834
    Beuckmann CT, Ueno T, Nakagawa M, Suzuki M, Akasofu S: Preclinical in vivo characterization of lemborexant (E2006), a novel dual orexin receptor antagonist for sleep/wake regulation. Sleep. 2019 Jun 11;42(6). pii: 5421821. doi: 10.1093/sleep/zsz076.

Contoh Produk & Brand

Produk: 5 • International brands: 0
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Sekuens Gen/Protein (FASTA)

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