GEMTESA (vibegron) is not an anticholinergic treatment—it works differently by selectively targeting beta-3 adrenergic receptors to reduce OAB symptoms1

Bladder relaxation is predominantly mediated by beta-3 adrenergic receptors1,2

M3 (muscarinic) receptorActivating the muscarinic receptors contracts the bladder detrusor muscle to mediate bladder emptying2

Beta-3 receptorActivating the beta-3 adrenergic receptors relaxes the bladder detrusor muscle to increase capacity1-3

Diagram of a bladder. GEMTESA® activates the beta-3 adrenergic receptor, relaxing the bladder detrusor muscle.

GEMTESA is a selective beta-3 adrenergic agonist1,4

Beta-adrenergic receptor subtype GEMTESA (% activity)
Beta-1 0
Beta-2 2.0
Beta-3 104.0

*Clinical relevance of this in vitro receptor binding assay data is unknown.

At 10 µM (exceeds mean human Cmax values of GEMTESA by ~30x).1,4,5

Cmax=maximum serum concentration.

Take a look at the use of GEMTESA with other prescribed medications

Drug interactions

References: 1. GEMTESA [prescribing information]. Irvine, CA: Urovant Sciences; 2020. 2. Yamaguchi O, Chapple CR. β3-adrenoceptors in urinary bladder. Neurourol Urodyn. 2007;26(6):752-756. doi:10.1002/nau.20420 3. Edmondson SD, Zhu C, Kar NF, et al. Discovery of vibegron: a potent and selective β3 adrenergic receptor agonist for the treatment of overactive bladder. J Med Chem. 2016;59(2):609-623. doi:10.1021/acs.jmedchem.5b01372 4. Brucker BM, King J, Mudd PN, McHale K. Selectivity and maximum response of vibegron and mirabegron for β3-adrenergic receptors. Curr Ther Res Clin Exp. 2022;96:100674. doi:10.1016/j.curtheres.2022.100674 5. Data on file. Urovant Sciences.