Agomelatine

DB06594

small molecule approved investigational

Deskripsi

Agomelatine is structurally closely related to melatonin. Agomelatine is a potent agonist at melatonin receptors and an antagonist at serotonin-2C (5-HT2C) receptors, tested in an animal model of depression. Agomelatine was developed in Europe by Servier Laboratories Ltd. and submitted to the European Medicines Agency (EMA) in 2005. The Committee for Medical Products for Human Use (CHMP) recommended refusal of marketing authorization on 27 July 2006. The major concern was that efficacy had not been sufficiently shown. In 2006 Servier sold the rights to develop Agomelatine in the US to Novartis.

The development for the US market was discontinued in October 2011. It is currently sold in Australia under the Valdoxan trade name.

Struktur Molekul 2D

Berat 243.301
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) <2 hours
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Bioavailability is less than 5%.

Metabolisme

Hepatic (90% CYP1A2 and 10% CYP2C9).

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

1030 Data
Deferasirox The serum concentration of Agomelatine can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Agomelatine can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Agomelatine can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Agomelatine can be decreased when it is combined with Teriflunomide.
Buprenorphine Agomelatine 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 Agomelatine.
Dronabinol The serum concentration of Dronabinol can be increased when it is combined with Agomelatine.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Agomelatine.
Hydrocodone Agomelatine 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 Agomelatine.
Magnesium sulfate The therapeutic efficacy of Agomelatine can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Agomelatine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Agomelatine may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Agomelatine.
Mirtazapine Agomelatine 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 Agomelatine.
Orphenadrine Agomelatine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Agomelatine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Agomelatine.
Pramipexole Agomelatine may increase the sedative activities of Pramipexole.
Ropinirole Agomelatine may increase the sedative activities of Ropinirole.
Rotigotine Agomelatine may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Agomelatine.
Sodium oxybate Agomelatine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Agomelatine 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 Agomelatine.
Thalidomide Agomelatine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Agomelatine 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 Agomelatine.
Phenindione The risk or severity of adverse effects can be increased when Agomelatine is combined with Phenindione.
4-hydroxycoumarin The risk or severity of adverse effects can be increased when Agomelatine is combined with 4-hydroxycoumarin.
Ethyl biscoumacetate The risk or severity of adverse effects can be increased when Agomelatine is combined with Ethyl biscoumacetate.
Clorindione The risk or severity of adverse effects can be increased when Agomelatine is combined with Clorindione.
Diphenadione The risk or severity of adverse effects can be increased when Agomelatine is combined with Diphenadione.
Tioclomarol The risk or severity of adverse effects can be increased when Agomelatine is combined with Tioclomarol.
Caffeine The serum concentration of Agomelatine can be increased when it is combined with Caffeine.
Moxifloxacin The serum concentration of Agomelatine can be increased when it is combined with Moxifloxacin.
Lidocaine The serum concentration of Agomelatine can be increased when it is combined with Lidocaine.
Mexiletine The serum concentration of Agomelatine can be increased when it is combined with Mexiletine.
Imipramine The serum concentration of Agomelatine can be increased when it is combined with Imipramine.
Alosetron The serum concentration of Agomelatine can be increased when it is combined with Alosetron.
Ketoconazole The serum concentration of Agomelatine can be increased when it is combined with Ketoconazole.
Gatifloxacin The serum concentration of Agomelatine can be increased when it is combined with Gatifloxacin.
Simeprevir The serum concentration of Agomelatine can be increased when it is combined with Simeprevir.
Dosulepin The risk or severity of CNS depression can be increased when Agomelatine is combined with Dosulepin.
Lobeglitazone The serum concentration of Agomelatine can be increased when it is combined with Lobeglitazone.
Pazufloxacin The serum concentration of Agomelatine can be increased when it is combined with Pazufloxacin.
Osilodrostat The serum concentration of Agomelatine can be increased when it is combined with Osilodrostat.
Cyproterone acetate The metabolism of Agomelatine can be increased when combined with Cyproterone acetate.
Ethanol Agomelatine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Agomelatine 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 Agomelatine.
Citalopram The risk or severity of adverse effects can be increased when Agomelatine is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Agomelatine is combined with Duloxetine.
Trazodone The risk or severity of adverse effects can be increased when Agomelatine is combined with Trazodone.
Paroxetine The risk or severity of adverse effects can be increased when Agomelatine is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Agomelatine is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Agomelatine is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Agomelatine is combined with Nefazodone.
Escitalopram The risk or severity of adverse effects can be increased when Agomelatine is combined with Escitalopram.
Zimelidine The risk or severity of adverse effects can be increased when Agomelatine is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Agomelatine is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Agomelatine is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Agomelatine is combined with Desvenlafaxine.
Seproxetine The risk or severity of adverse effects can be increased when Agomelatine is combined with Seproxetine.
Indalpine The risk or severity of adverse effects can be increased when Agomelatine is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Agomelatine is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Agomelatine is combined with Alaproclate.
Nortriptyline The risk or severity of CNS depression can be increased when Nortriptyline is combined with Agomelatine.
Desipramine The risk or severity of CNS depression can be increased when Desipramine is combined with Agomelatine.
Carbamazepine The metabolism of Agomelatine can be increased when combined with Carbamazepine.
Primidone The metabolism of Agomelatine can be increased when combined with Primidone.
Rifampin The metabolism of Agomelatine can be increased when combined with Rifampicin.
Albendazole The metabolism of Agomelatine can be increased when combined with Albendazole.
Botulinum toxin type B The risk or severity of CNS depression can be increased when Botulinum toxin type B is combined with Agomelatine.
Botulinum toxin type A The risk or severity of CNS depression can be increased when Botulinum toxin type A is combined with Agomelatine.
Tryptophan The risk or severity of CNS depression can be increased when Tryptophan is combined with Agomelatine.
Baclofen Baclofen may increase the central nervous system depressant (CNS depressant) activities of Agomelatine.
Lorazepam The risk or severity of CNS depression can be increased when Lorazepam is combined with Agomelatine.
Ethchlorvynol The risk or severity of CNS depression can be increased when Ethchlorvynol is combined with Agomelatine.
Succinylcholine The risk or severity of CNS depression can be increased when Succinylcholine is combined with Agomelatine.
Reserpine The risk or severity of CNS depression can be increased when Reserpine is combined with Agomelatine.
Enflurane The risk or severity of CNS depression can be increased when Enflurane is combined with Agomelatine.
Reboxetine The risk or severity of CNS depression can be increased when Reboxetine is combined with Agomelatine.
Butabarbital The risk or severity of CNS depression can be increased when Butabarbital is combined with Agomelatine.
Butalbital The risk or severity of CNS depression can be increased when Butalbital is combined with Agomelatine.
Methysergide The risk or severity of CNS depression can be increased when Methysergide is combined with Agomelatine.
Cabergoline The risk or severity of CNS depression can be increased when Cabergoline is combined with Agomelatine.
Topiramate The risk or severity of CNS depression can be increased when Topiramate is combined with Agomelatine.
Clemastine The risk or severity of CNS depression can be increased when Clemastine is combined with Agomelatine.
Venlafaxine The risk or severity of CNS depression can be increased when Venlafaxine is combined with Agomelatine.
Etomidate The risk or severity of CNS depression can be increased when Etomidate is combined with Agomelatine.
Morphine The risk or severity of CNS depression can be increased when Morphine is combined with Agomelatine.
Talbutal The risk or severity of CNS depression can be increased when Talbutal is combined with Agomelatine.
Pentobarbital The risk or severity of CNS depression can be increased when Pentobarbital is combined with Agomelatine.
Codeine The risk or severity of CNS depression can be increased when Codeine is combined with Agomelatine.
Dihydroergotamine The risk or severity of CNS depression can be increased when Dihydroergotamine is combined with Agomelatine.
Tolcapone The risk or severity of CNS depression can be increased when Tolcapone is combined with Agomelatine.
Cetirizine The risk or severity of CNS depression can be increased when Cetirizine is combined with Agomelatine.
Protriptyline The risk or severity of CNS depression can be increased when Protriptyline is combined with Agomelatine.

Target Protein

5-hydroxytryptamine receptor 2C HTR2C
Melatonin receptor type 1A MTNR1A
Melatonin receptor type 1B MTNR1B

Referensi & Sumber

Synthesis reference: Jean-Claude Souvie, Isaac Gonzalez Blanco, Gilles Thominot, Genevieve Chapuis, Stephane Horvath, Gerard Damien, "Process for the synthesis and crystalline form of agomelatine." U.S. Patent US20050182276, issued August 18, 2005.
Artikel (PubMed)
  • PMID: 15289999
    Millan MJ, Brocco M, Gobert A, Dekeyne A: Anxiolytic properties of agomelatine, an antidepressant with melatoninergic and serotonergic properties: role of 5-HT2C receptor blockade. Psychopharmacology (Berl). 2005 Feb;177(4):448-58. Epub 2004 Jul 31.
  • PMID: 18368944
    Hardeland R, Poeggeler B, Srinivasan V, Trakht I, Pandi-Perumal SR, Cardinali DP: Melatonergic drugs in clinical practice. Arzneimittelforschung. 2008;58(1):1-10. doi: 10.1055/s-0031-1296459.
  • PMID: 17917564
    Racagni G, Riva MA, Popoli M: The interaction between the internal clock and antidepressant efficacy. Int Clin Psychopharmacol. 2007 Oct;22 Suppl 2:S9-S14.

Contoh Produk & Brand

Produk: 12 • International brands: 2
Produk
  • Thymanax
    Tablet • 25 mg • Oral • EU
  • Thymanax
    Tablet • 25 mg • Oral • EU
  • Thymanax
    Tablet • 25 mg • Oral • EU
  • Thymanax
    Tablet • 25 mg • Oral • EU
  • Thymanax
    Tablet • 25 mg • Oral • EU
  • Thymanax
    Tablet • 25 mg • Oral • EU
  • Valdoxan
    Tablet • 25 mg • Oral • EU • Approved
  • Valdoxan
    Tablet • 25 mg • Oral • EU • Approved
Menampilkan 8 dari 12 produk.
International Brands
  • Melitor — Servier Laboratories Ltd.
  • Valdoxan — Servier Laboratories Ltd.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul