Vibegron (Monograph)

Brand name: Gemtesa
Drug class: Selective beta-3 Adrenergic Agonists

Medically reviewed by Drugs.com on Dec 17, 2023. Written by ASHP.

Introduction

Selective beta-3 adrenergic agonist.

Uses for Vibegron

Overactive Bladder

Treatment of overactive bladder (OAB) with symptoms of urge urinary incontinence, urgency, and urinary frequency in adults.

Current guidelines include the beta-3 agonist class among pharmacologic management options recommended for patients with OAB who have not met treatment goals with initial behavioral therapy.

Vibegron Dosage and Administration

General

<C> Pretreatment Screening

Evaluate for bladder outlet obstruction prior to starting treatment with vibegron.

<C> Patient Monitoring

Monitor for signs and symptoms of urinary retention, particularly in patients with bladder outlet obstruction and patients taking muscarinic antagonists for the treatment of overactive bladder (OAB).

Administration

Oral Administration

Administer orally.

Take once daily without regard to meals.

Swallow tablets whole with a glass of water. Alternatively, tablets may be crushed, mixed with approximately 15 mL of applesauce, and taken immediately with a glass of water.

Dosage

Adults

OAB

Oral

75 mg once daily.

Special Populations

Hepatic Impairment

No dosage adjustment required in mild to moderate hepatic impairment (Child-Pugh classes A and B).

Not studied in severe hepatic impairment (Child-Pugh class C); use not recommended.

Renal Impairment

No dosage adjustment required in mild, moderate, or severe renal impairment (eGFR 15 to <90 mL/min/1.73 m²).

Not studied in eGFR <15 mL/min/1.73 m² (with or without hemodialysis); use not recommended.

Geriatric Use

No specific dosage recommendations.

Cautions for Vibegron

Contraindications

Known hypersensitivity to vibegron or to any ingredient in the formulation.

Warnings/Precautions

Urinary Retention

Urinary retention reported in patients taking vibegron. Risk may be increased in patients with bladder outlet obstruction and patients taking muscarinic antagonists for overactive bladder (OAB).

Monitor for signs and symptoms of urinary retention, particularly in patients with bladder outlet obstruction and patients taking muscarinic antagonists. Discontinue vibegron in patients who develop urinary retention.

Specific Populations

Pregnancy

No available data on vibegron use in pregnant females to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes.

In rat and rabbit studies, no effects on embryofetal development observed following administration of vibegron during organogenesis at exposures approximately 275- and 285-fold greater than clinical exposure at the recommended daily dose of vibegron.

Lactation

No data on the presence of vibegron in human milk, the effects of vibegron on the breast-fed infant, or the effects of vibegron on milk production. Radioactivity from radiolabeled vibegron has been observed in rat milk.

Consider the developmental and health benefits of breastfeeding along with the mother's clinical need for vibegron and any potential adverse effects on the breast-fed infant from vibegron or from the underlying maternal condition.

Pediatric Use

Safety and effectiveness not established in pediatric patients.

Geriatric Use

No overall differences in safety or effectiveness observed between patients ≥65 years of age and younger adult patients.

Hepatic Impairment

No clinically significant differences in pharmacokinetics of vibegron observed in patients with mild to moderate hepatic impairment (Child-Pugh classes A and B). Effect of severe hepatic impairment (Child-Pugh class C) on vibegron pharmacokinetics has not been studied.

Renal Impairment

No clinically significant differences in pharmacokinetics of vibegron observed in patients with mild, moderate, or severe renal impairment (eGFR ≥15 mL/min/1.73 m²). Effect of more severe renal impairment (eGFR <15 mL/min/1.73 m²) with or without hemodialysis has not been studied.

Common Adverse Effects

Most common adverse reactions (≥2%) include headache, urinary tract infection, nasopharyngitis, diarrhea, nausea, upper respiratory tract infection.

Drug Interactions

CYP3A4 and P-glycoprotein (P-gp) substrate.

Does not inhibit CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, or CYP3A4.

Does not induce CYP1A2, CYP2B6, or CYP3A4.

Does not inhibit P-gp, breast cancer resistance protein (BCRP), organic anion transporting polypeptide (OATP) 1B1, OATP1B3, organic anion transporter (OAT) 1, OAT3, organic cation transporter (OCT) 1, OCT2, multidrug and toxin extrusion protein (MATE) 1, or MATE2K.

Specific Drugs

Drug	Interaction	Comments
Digoxin	Maximum plasma concentrations and AUC of digoxin increased by 21% and 11%, respectively	Monitor serum digoxin concentrations before initiating and during vibegron treatment to titrate digoxin dose to desired effects Upon discontinuation of vibegron, monitor digoxin concentrations and adjust digoxin dose as needed
Diltiazem	No impact on vibegron concentrations with concomitant use
Hormonal contraceptives (ethinyl estradiol, levonorgestrel)	No impact on combined oral contraceptive concentrations with concomitant use
Ketoconazole	No impact on vibegron concentrations with concomitant use
Metoprolol	No impact on metoprolol concentrations with concomitant use
Rifampin	No impact on vibegron concentrations with concomitant use
Tolterodine	No impact on vibegron or tolterodine concentrations with concomitant use
Warfarin	No impact on warfarin concentrations with concomitant use

Vibegron Pharmacokinetics

Absorption

Bioavailability

Time to maximum concentration: 1–3 hours.

Steady-state achieved within 7 days.

Food

No impact when administered with a high-fat meal.

Distribution

Plasma Protein Binding

50%.

Elimination

Metabolism

Minimally metabolized.

Metabolized by CYP3A4 in vitro.

Elimination Route

Fecal excretion: 59% (54% unchanged).

Urinary excretion: 20% (19% unchanged).

Half-life

30.8 hours

Stability

Storage

Oral

Tablets, film-coated

20–25°C (excursions permitted between 15–30°C).

Actions

Selectively activates beta-3 adrenergic receptors.
Relaxes detrusor smooth muscle during bladder filling, thereby increasing bladder capacity.

Advice to Patients

Inform patients that vibegron has been associated with urinary retention. Inform patients that the risk of urinary retention may be increased in patients taking muscarinic antagonist medications for the treatment of overactive bladder (OAB). Instruct patients to contact their healthcare provider if they experience symptoms consistent with urinary retention while taking vibegron.
Advise patients that vibegron tablets can be swallowed whole with a glass of water or may be crushed, mixed with a tablespoon of applesauce, and taken immediately with a glass of water.
Advise females to inform their clinician if they are or plan to become pregnant or plan to breast-feed.
Advise patients to inform their clinician of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary and herbal supplements, as well as any concomitant illnesses.
Inform patients of other important precautionary information.

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.