Due to this muscle relaxation, bladder capacity increases and symptoms of overactive bladder are relieved. Metabolism
The two main metabolic pathways are the oxidation and glucuronidation of vibegron. Two oxidative metabolites and three glucuronide metabolites can be formed. The exact structure of these metabolites have not been studied yet. In vitro, CYP3A4 is the enzyme responsible for the metabolism of vibegron, facilitating oxidative metabolism. Eventually, still a large part of the unmodified drug is excreted through feces and urine. Indications
Vibegron is indicated for people with OAB. Urgency urinary incontinence (UUI), urgency and urinary frequency in adults are the most common symptoms for this condition.The drug is contraindicated in patients with known hypersensitivity to Vibegron itself or single components of the drug. The inactive components of the drug for which allergic reactions can occur are sodium croscarmellose, hydroxypropyl cellulose, magnesium stearate, mannitol and microcrystalline cellulose. The thin coating of the drug with green color contains FD&C Blue No.2.Vibegron treatment should be discontinued if urinary retention occurs. Use with nonselective muscarinic antagonists may increase the risk of urinary retention. The manufacturer suggests discontinuing vibegron if an elevated digoxin concentration occurs. Efficacy and side effects
Efficacy
Vibegron was evaluated in patients with overactive bladder (OAB) in several clinical studies. A large active-controlled study, called Empower, showed the beneficial effects of the drug to treat the condition and UUI. Primary outcomes of different clinical trials showed there was an overall increase in efficacy.
Vibegron, sold under the brand name Gemtesa, is a medication for the treatment of overactive bladder.Vibegron (other names: RVT-901; MK4618; KRP114V; URO-901) is a selective beta 3 adrenergic receptor agonist. The most common side effects include headache, urinary tract infection, common cold, diarrhea, nausea, and upper respiratory tract infection.It was approved for medical use in the United States in December 2020. Medical uses
Vibegron is indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency in adults. History and Discovery
The beta 3 adrenergic receptor was discovered in the late 1980s and initially beta3AR agonists were investigated as treatment for obesity and diabetes. A number of compounds were tested in clinical trials but didnt show sufficient benefits in these areas.Since the 2000s there is evidence that there are beta3AR on the detrusor muscle of the bladder. The detrusor muscle contracts during urination and remains relaxed to allow the bladder to store urine. Mirabegron was the first FDA approved selective agonist approved to treat overactive bladder (OAB).Vibegron is a selective beta3AR agonist that is developed in Japan by Kyorin Pharmaceutical Co., Ltd and Kissei Pharmaceutical Co.,Ltd and Urovant Sciences to treat overactive bladders  and pain caused by irritable bowel syndrome.