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Vibegron: Mechanism of Action, Adverse Effects, Contraindications, and Dosing

Mechanism of Action of Vibegron

Vibegron is a β3-adrenergic receptor agonist. In the urinary bladder, vibegron increases intracellular cAMP and relaxes detrusor smooth muscle during the filling phase, thereby increasing functional bladder capacity.

Urologic Indications for Vibegron:

Vibegron provides symptomatic treatment of urgency symptoms associated with overactive bladder (OAB) in adults. In the pivotal phase III EMPOWUR trial (randomized, double-blind, 12 weeks; vibegron 75 mg vs placebo vs tolterodine; n=1518), vibegron improved mean daily micturition frequency, urgency urinary incontinence episodes, and increased mean voided volume compared with placebo. Adverse events led to treatment discontinuation in 1.7% of patients (compared with 3.3% with tolterodine).

Pharmacokinetics of Vibegron

Oral bioavailability is approximately 57%, and patients may take vibegron with or without food. The liver metabolizes vibegron only to a limited extent, and a substantial fraction is eliminated unchanged in urine. The half-life is approximately 31 hours, and patients generally reach steady state after seven days.

Adverse Effects of Vibegron

Vibegron appears to have fewer cardiovascular adverse effects in the pivotal trials compared to mirabegron.

• Common (<10%): urinary tract infections, headache, constipation, diarrhea, nausea, and an increase in postvoid residual urine volume.
• Uncommon (<1%): hot flashes, rash, and urinary retention.

Drug Interactions:

Vibegron can increase exposure to P-glycoprotein (P-gp) substrates, consider increased exposure for other sensitive P-gp substrates, including digoxin, dabigatran, apixaban, or rivaroxaban.

Combination therapy with antimuscarinics can improve symptom control, but it can increase the risk of urinary retention, especially in patients with clinically significant bladder outlet obstruction.

Contraindications of Vibegron

Hypersensitivity to the active ingredient. Vibegron is not recommended during pregnancy, breastfeeding, severe hepatic impairment (Child-Pugh C), and end-stage renal disease (GFR <15 ml/min) because of limited data.

Dosing of Vibegron

• Adults: 75 mg p.o. once daily.
• No dose adjustment is necessary in mild to severe renal impairment (15 ml/min < GFR < 90 ml/min) or in mild to moderate hepatic impairment (Child-Pugh A or B).

References

D. Staskin, J. Frankel, S. Varano, D. Shortino, R. Jankowich, and P. N. Mudd, “International Phase III, Randomized, Double-Blind, Placebo and Active Controlled Study to Evaluate the Safety and Efficacy of Vibegron in Patients with Symptoms of Overactive Bladder: EMPOWUR.,” J Urol, vol. 204, no. 2, pp. 316–324, 2020, doi: 10.1097/JU.0000000000000807.

J. Frankel, D. Staskin, S. Varano, M. J. Kennelly, R. A. Jankowich, and C. Haag-Molkenteller, “An Evaluation of the Efficacy and Safety of Vibegron in the Treatment of Overactive Bladder.,” Ther Clin Risk Manag, vol. 18, pp. 171–182, 2022, doi: 10.2147/TCRM.S310371.

  Deutsche Version: Mechanismus, Nebenwirkungen und Kontraindikationen von Vibegron

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