Peringatan Keamanan

There is limited clinical information on overdose from vibegron. In the case of a suspected drug overdose, supportive and symptomatic treatment should be initiated.L28305

Vibegron

DB14895

small molecule approved investigational

Deskripsi

Vibegron is a potent, selective beta-3 adrenergic receptor (?3) agonist that relaxes the detrusor smooth muscle of the bladder, thereby increasing bladder capacity.L28305 Vibegron was first approved in Japan in September 2018 for the treatment of overactive bladder,A226050 a condition associated with distressing symptoms of urge urinary incontinence, urgency, and urinary frequency, and reduced quality of life of patients. On December 23, 2020, vibegron was approved for the same indication in adults. It is available as oral tablets under the market name GEMTESA.L28310

Vibegron is the second beta-3 adrenergic agonist approved for the treatment of overactive bladder following mirabegron, which was approved in 2012. Unlike mirabegron, vibegron is less likely to be associated with drug-drug interactions involving the CYP3A4, 2D6, or 2C9 enzymes.A226065

Struktur Molekul 2D

Berat 444.535
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal plasma half-life ranges from 60 to 70 hours.[A226065] The effective half-life is 30.8 hours.[L28305]
Volume Distribusi The mean apparent volume of distribution is 6304 L. The average blood-to-plasma concentration ratio is 0.9.[L28305] According to tissue distribution studies in animals, vibegron does not penetrate the blood-brain barrier, suggesting limited potential for CNS toxicity in humans.[A226065]
Klirens (Clearance) There is limited information on the clearance rate of vibegron.

Absorpsi

The mean Tmax is 1-3 hours. Steady-state concentrations are achieved within 7 days of once-daily dosing.L28305

Metabolisme

In vitro, CYP3A4 is the main enzyme responsible for the metabolism of vibegron, which plays a minor role in the elimination of vibegron.L28305 Two predominant metabolic pathways are oxidation and glucuronidation to form two oxidative metabolites and three glucuronide metabolites.A226065 Metabolites have not been fully characterized.

Rute Eliminasi

In a radiolabeled drug study, approximately 59% of the radiolabeled dose was recovered in feces, in which 54% of that amount was in the unchanged parent drug form. About 20% of the radioactivity was recovered in urine, in which 19% of the amount was in the unchanged form.L28305

Interaksi Makanan

1 Data
  • 1. Take with or without food. A high-fat meal had no clinically significant effects on vibegron plasma concentrations.

Interaksi Obat

165 Data
Digoxin The serum concentration of Digoxin can be increased when it is combined with Vibegron.
Metildigoxin The serum concentration of Metildigoxin can be increased when it is combined with Vibegron.
Acetyldigoxin The serum concentration of Acetyldigoxin can be increased when it is combined with Vibegron.
Trospium Trospium may increase the smooth muscle relaxing activities of Vibegron.
Darifenacin Darifenacin may increase the smooth muscle relaxing activities of Vibegron.
Tolterodine Tolterodine may increase the smooth muscle relaxing activities of Vibegron.
Oxybutynin Oxybutynin may increase the smooth muscle relaxing activities of Vibegron.
Flavoxate Flavoxate may increase the smooth muscle relaxing activities of Vibegron.
Solifenacin Solifenacin may increase the smooth muscle relaxing activities of Vibegron.
Solabegron Solabegron may increase the smooth muscle relaxing activities of Vibegron.
Fesoterodine Fesoterodine may increase the smooth muscle relaxing activities of Vibegron.
Mirabegron Mirabegron may increase the smooth muscle relaxing activities of Vibegron.
Ritobegron Ritobegron may increase the smooth muscle relaxing activities of Vibegron.
Propiverine Propiverine may increase the smooth muscle relaxing activities of Vibegron.
Meladrazine Meladrazine may increase the smooth muscle relaxing activities of Vibegron.
Emepronium Emepronium may increase the smooth muscle relaxing activities of Vibegron.
Terodiline Terodiline may increase the smooth muscle relaxing activities of Vibegron.
Benzylpenicilloyl polylysine Vibegron may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
Spironolactone The therapeutic efficacy of Vibegron can be decreased when used in combination with Spironolactone.
Methysergide Methysergide may increase the hypertensive and vasoconstricting activities of Vibegron.
Cabergoline Cabergoline may increase the hypertensive and vasoconstricting activities of Vibegron.
Dihydroergotamine Dihydroergotamine may increase the hypertensive and vasoconstricting activities of Vibegron.
Methylergometrine Methylergometrine may increase the hypertensive and vasoconstricting activities of Vibegron.
Lisuride Lisuride may increase the hypertensive and vasoconstricting activities of Vibegron.
Ergotamine Ergotamine may increase the hypertensive and vasoconstricting activities of Vibegron.
Nicergoline Nicergoline may increase the hypertensive and vasoconstricting activities of Vibegron.
Ergoloid mesylate Ergoloid mesylate may increase the hypertensive and vasoconstricting activities of Vibegron.
Pergolide Pergolide may increase the hypertensive and vasoconstricting activities of Vibegron.
Bromocriptine Bromocriptine may increase the hypertensive and vasoconstricting activities of Vibegron.
Ergometrine Ergometrine may increase the hypertensive and vasoconstricting activities of Vibegron.
Lysergic acid diethylamide Lysergic acid diethylamide may increase the hypertensive and vasoconstricting activities of Vibegron.
Dihydroergocornine Dihydroergocornine may increase the hypertensive and vasoconstricting activities of Vibegron.
Dihydroergocristine Dihydroergocristine may increase the hypertensive and vasoconstricting activities of Vibegron.
Dihydroergocryptine Dihydroergocryptine may increase the hypertensive and vasoconstricting activities of Vibegron.
Terguride Terguride may increase the hypertensive and vasoconstricting activities of Vibegron.
Metergoline Metergoline may increase the hypertensive and vasoconstricting activities of Vibegron.
Venlafaxine Venlafaxine may increase the tachycardic activities of Vibegron.
Duloxetine Duloxetine may increase the tachycardic activities of Vibegron.
Sibutramine Sibutramine may increase the tachycardic activities of Vibegron.
Nefazodone Nefazodone may increase the tachycardic activities of Vibegron.
Milnacipran Milnacipran may increase the tachycardic activities of Vibegron.
Desvenlafaxine Desvenlafaxine may increase the tachycardic activities of Vibegron.
Levomilnacipran Levomilnacipran may increase the tachycardic activities of Vibegron.
Ziprasidone The therapeutic efficacy of Vibegron can be decreased when used in combination with Ziprasidone.
Amitriptyline The therapeutic efficacy of Vibegron can be decreased when used in combination with Amitriptyline.
Olanzapine The therapeutic efficacy of Vibegron can be decreased when used in combination with Olanzapine.
Alfuzosin The therapeutic efficacy of Vibegron can be decreased when used in combination with Alfuzosin.
Clozapine The therapeutic efficacy of Vibegron can be decreased when used in combination with Clozapine.
Promazine The therapeutic efficacy of Vibegron can be decreased when used in combination with Promazine.
Droperidol The therapeutic efficacy of Vibegron can be decreased when used in combination with Droperidol.
Prazosin The therapeutic efficacy of Vibegron can be decreased when used in combination with Prazosin.
Imipramine The therapeutic efficacy of Vibegron can be decreased when used in combination with Imipramine.
Chlorpromazine The therapeutic efficacy of Vibegron can be decreased when used in combination with Chlorpromazine.
Nortriptyline The therapeutic efficacy of Vibegron can be decreased when used in combination with Nortriptyline.
Amoxapine The therapeutic efficacy of Vibegron can be decreased when used in combination with Amoxapine.
Doxazosin The therapeutic efficacy of Vibegron can be decreased when used in combination with Doxazosin.
Labetalol The therapeutic efficacy of Vibegron can be decreased when used in combination with Labetalol.
Nicardipine The therapeutic efficacy of Vibegron can be decreased when used in combination with Nicardipine.
Trazodone The therapeutic efficacy of Vibegron can be decreased when used in combination with Trazodone.
Verapamil The therapeutic efficacy of Vibegron can be decreased when used in combination with Verapamil.
Thioridazine The therapeutic efficacy of Vibegron can be decreased when used in combination with Thioridazine.
Phentolamine The therapeutic efficacy of Vibegron can be decreased when used in combination with Phentolamine.
Tamsulosin The therapeutic efficacy of Vibegron can be decreased when used in combination with Tamsulosin.
Trimipramine The therapeutic efficacy of Vibegron can be decreased when used in combination with Trimipramine.
Risperidone The therapeutic efficacy of Vibegron can be decreased when used in combination with Risperidone.
Propiomazine The therapeutic efficacy of Vibegron can be decreased when used in combination with Propiomazine.
Tolazoline The therapeutic efficacy of Vibegron can be decreased when used in combination with Tolazoline.
Trifluoperazine The therapeutic efficacy of Vibegron can be decreased when used in combination with Trifluoperazine.
Flupentixol The therapeutic efficacy of Vibegron can be decreased when used in combination with Flupentixol.
Quinidine The therapeutic efficacy of Vibegron can be decreased when used in combination with Quinidine.
Phenoxybenzamine The therapeutic efficacy of Vibegron can be decreased when used in combination with Phenoxybenzamine.
Carvedilol The therapeutic efficacy of Vibegron can be decreased when used in combination with Carvedilol.
Doxepin The therapeutic efficacy of Vibegron can be decreased when used in combination with Doxepin.
Terazosin The therapeutic efficacy of Vibegron can be decreased when used in combination with Terazosin.
Quetiapine The therapeutic efficacy of Vibegron can be decreased when used in combination with Quetiapine.
Aripiprazole The therapeutic efficacy of Vibegron can be decreased when used in combination with Aripiprazole.
Paliperidone The therapeutic efficacy of Vibegron can be decreased when used in combination with Paliperidone.
Bevantolol The therapeutic efficacy of Vibegron can be decreased when used in combination with Bevantolol.
Methotrimeprazine The therapeutic efficacy of Vibegron can be decreased when used in combination with Methotrimeprazine.
Periciazine The therapeutic efficacy of Vibegron can be decreased when used in combination with Periciazine.
Acepromazine The therapeutic efficacy of Vibegron can be decreased when used in combination with Acepromazine.
Thioproperazine The therapeutic efficacy of Vibegron can be decreased when used in combination with Thioproperazine.
Zuclopenthixol The therapeutic efficacy of Vibegron can be decreased when used in combination with Zuclopenthixol.
Dronedarone The therapeutic efficacy of Vibegron can be decreased when used in combination with Dronedarone.
Iloperidone The therapeutic efficacy of Vibegron can be decreased when used in combination with Iloperidone.
Pizotifen The therapeutic efficacy of Vibegron can be decreased when used in combination with Pizotifen.
Silodosin The therapeutic efficacy of Vibegron can be decreased when used in combination with Silodosin.
Asenapine The therapeutic efficacy of Vibegron can be decreased when used in combination with Asenapine.
Indoramin The therapeutic efficacy of Vibegron can be decreased when used in combination with Indoramin.
Brexpiprazole The therapeutic efficacy of Vibegron can be decreased when used in combination with Brexpiprazole.
Trimazosin The therapeutic efficacy of Vibegron can be decreased when used in combination with Trimazosin.
Niguldipine The therapeutic efficacy of Vibegron can be decreased when used in combination with Niguldipine.
Bunazosin The therapeutic efficacy of Vibegron can be decreased when used in combination with Bunazosin.
Urapidil The therapeutic efficacy of Vibegron can be decreased when used in combination with Urapidil.
Bucindolol The therapeutic efficacy of Vibegron can be decreased when used in combination with Bucindolol.
Aripiprazole lauroxil The therapeutic efficacy of Vibegron can be decreased when used in combination with Aripiprazole lauroxil.
Protriptyline The risk or severity of hypertension can be increased when Protriptyline is combined with Vibegron.
Desipramine The risk or severity of hypertension can be increased when Desipramine is combined with Vibegron.
Clomipramine The risk or severity of hypertension can be increased when Clomipramine is combined with Vibegron.
Amineptine The risk or severity of hypertension can be increased when Amineptine is combined with Vibegron.

Target Protein

Beta-3 adrenergic receptor ADRB3

Referensi & Sumber

Artikel (PubMed)
  • PMID: 30411311
    Keam SJ: Vibegron: First Global Approval. Drugs. 2018 Nov;78(17):1835-1839. doi: 10.1007/s40265-018-1006-3.
  • PMID: 31991511
    Yoshida M, Takeda M, Gotoh M, Yokoyama O, Kakizaki H, Takahashi S, Masumori N, Nagai S, Minemura K: Efficacy of vibegron, a novel beta3-adrenoreceptor agonist, on severe urgency urinary incontinence related to overactive bladder: post hoc analysis of a randomized, placebo-controlled, double-blind, comparative phase 3 study. BJU Int. 2020 May;125(5):709-717. doi: 10.1111/bju.15020. Epub 2020 Feb 23.
  • PMID: 27965369
    Di Salvo J, Nagabukuro H, Wickham LA, Abbadie C, DeMartino JA, Fitzmaurice A, Gichuru L, Kulick A, Donnelly MJ, Jochnowitz N, Hurley AL, Pereira A, Sanfiz A, Veronin G, Villa K, Woods J, Zamlynny B, Zycband E, Salituro GM, Frenkl T, Weber AE, Edmondson SD, Struthers M: Pharmacological Characterization of a Novel Beta 3 Adrenergic Agonist, Vibegron: Evaluation of Antimuscarinic Receptor Selectivity for Combination Therapy for Overactive Bladder. J Pharmacol Exp Ther. 2017 Feb;360(2):346-355. doi: 10.1124/jpet.116.237313. Epub 2016 Dec 13.
  • PMID: 32993398
    Rechberger T, Wrobel A: Evaluating vibegron for the treatment of overactive bladder. Expert Opin Pharmacother. 2020 Sep 29:1-9. doi: 10.1080/14656566.2020.1809652.
  • PMID: 30995798
    Schena G, Caplan MJ: Everything You Always Wanted to Know about beta3-AR * (* But Were Afraid to Ask). Cells. 2019 Apr 16;8(4). pii: cells8040357. doi: 10.3390/cells8040357.

Contoh Produk & Brand

Produk: 1 • International brands: 1
Produk
  • Gemtesa
    Tablet, film coated • 75 mg/1 • Oral • US • Approved
International Brands
  • Beova — Kyorin Pharmaceutical Co., Ltd

Sekuens Gen/Protein (FASTA)

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