[1][5][6] Generally, the introduction of β3 adrenergic receptors agonists such as vibegron has improved overactive bladder (OAB) management by minimizing anticholinergic-related adverse effects.

Vibegron was generally effective, safe and well tolerated, thus represents a valuable treatment option for patients with OAB.

[1] Vibegron is, in contrast to other OAB drugs, very selective and leads to a lesser degree of unwanted side effects.

Vibegron is found to be a substrate for CYP3A4 in vivo, but does not actually induce or inhibit any of the cytochrome P450 enzymes and is thus less likely to take part in drug–drug interactions (DDI).

Here vibegron differs from the previous overactive bladder drug mirabegron, which was known to be associated in various drug–drug interactions by inhibiting CYP2D6 or inducing CYP3A4, CYP2D6 and CYP2C9 in the liver.

[18] Additionally, co-administration with imidafenacin shows an increase in bladder capacity and voided volume in comparison to monotherapy.

Maximal concentrations and systemic exposure (Cmax and area under the curve (AUC)) of digoxin are both increased as a result of DDI.

[19][1] Apart from the no to little DDIs, vibegron has an additional safety quality in that it does not cross the blood-brain barrier and therefore does not induce cognitive impairment.

[21] A phase IIb global trial completed in 2013 of 1395 patients, of which 89.7% were women and 63.3% had not been treated previously, demonstrated a significant decrease in daily micturitions and urgent urinary incontinence episodes upon administration of vibegron.

[22][13] An international phase III trial of 506 participants completed in 2019 found statistically significant efficacy of vibegron after two weeks of daily administration.

A large active-controlled study, called Empower, showed the beneficial effects of the drug to treat the condition and UUI.

[26] Pregnant rats were given very high daily oral doses of vibegron during the period of organogenesis and showed no embryo-fetal developmental toxicity up to 300 mg/kg/day.