General Information

Gemtesa (vibegron) is a small-molecule β3 agonist which helps relax the detrusor bladder muscle, allowing the bladder to hold more urine, thereby reducing symptoms of overactive bladder (OAB).

Gemtesa is specifically indicated for the treatment of OAB with symptoms of urge urinary incontinence, urgency, and urinary frequency in adults.

Gemtesa is supplied as a tablet for oral administration. The recommended dosage is one 75 mg tablet orally, once daily with or without food. The tablets should be swallowed whole with a glass of water. In adults, Gemtesa tablets also may be crushed, mixed with a tablespoon (approximately 15 mL) of applesauce and taken immediately with a glass of water.

Mechanism of Action

Gemtesa (vibegron) is a selective human beta-3 adrenergic receptor agonist. Activation of the beta-3 adrenergic receptor increases bladder capacity by relaxing the detrusor smooth muscle during bladder filling.

Side Effects

Adverse effects associated with the use of Gemtesa may include, but are not limited to, the following:

• headache
• urinary tract infection
• nasopharyngitis
• diarrhea
• nausea
• upper respiratory tract infection

Clinical Trial Results

The FDA approval of Gemtesa was based on a12-week, double-blind, randomized, placebo-controlled, and active-controlled trial in 1,515 patients with OAB (urge urinary incontinence, urgency, and urinary frequency). Patients were randomized to receive either Gemtesa 75 mg, placebo, or active control  (tolterodine) orally, once daily for 12 weeks. For study entry, patients had to have symptoms of OAB for at least 3 months with an average of 8 or more micturitions per day and at least 1 urge urinary incontinence (UUI) per day, or an average of 8 or more micturitions per day and an average of at least 3 urgency episodes per day. Urge urinary incontinence was defined as leakage of urine of any amount because the patient felt an urge or need to urinate immediately.

The co-primary endpoints were change from baseline in average daily number of micturitions and average daily number of UUI episodes at week 12. Additional endpoints included change from baseline in average daily number of “need to urinate immediately” (urgency) episodes and average volume voided per micturition. At 12 weeks micturitions decreased by an adjusted mean of 1.8 episodes per day for Gemtesa versus 1.3 for placebo and 1.6 for tolterodine. Among incontinent patients urge incontinence episodes decreased by an adjusted mean 2.0 episodes per day for Gemtesa versus 1.4 for placebo and 1.8 for tolterodine. Gemtesa was also statistically significantly superior to placebo for key secondary measures of number of urgency episodes, volume per micturition and proportion of incontinent patients with a 75% or greater reduction in urge incontinence episode.