Liver via (direct) glucuronidation, amide hydrolysis, and minimal oxidative metabolismin vivo byCYP2D6 andCYP3A4. Some involvement of butylcholinesterase[4]
Mirabegron is the first clinically availablebeta-3 agonist with approval for use in adults withoveractive bladder. Mirabegron was approved for medical use in the United States and in the European Union in 2012.[8][9][3] In 2023, it was the 214th most commonly prescribed medication in the United States, with more than 2million prescriptions.[10][11] It is available as ageneric medication.[12]
In the United Kingdom it is less preferred to antimuscarinic medication such asoxybutynin.[7]
Mirabegron is also indicated to treat neurogenic detrusor overactivity (NDO), a bladder dysfunction related to neurological impairment, in children ages three years and older.[13]
As a selective beta-3adrenergic agonist, mirabegron does not cause the cardiovascular adverse effects of other adrenergic agonists that are active at thebeta-1 andbeta-2 adrenergic receptors. Beta-3 adrenergic agonists activatebrown adipose tissue (BAT) and increaseenergy expenditure, leading to research interest in their development asweight loss drugs.[14] A combination of mirabegron andmetformin was studied in mice and caused greater weight loss than either drug alone.[15] A human study in obese individuals found an increase ininsulin sensitivity but no significant weight change, which was hypothesized to be due to low levels of BAT in obese humans and/or the low dose of mirabegron used in the study.[16]
^abc"Betmiga EPAR".European Medicines Agency. 17 September 2018. Retrieved28 April 2020. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
^Sacco E, Bientinesi R, Tienforti D, Racioppi M, Gulino G, D'Agostino D, et al. (April 2014). "Discovery history and clinical development of mirabegron for the treatment of overactive bladder and urinary incontinence".Expert Opinion on Drug Discovery.9 (4):433–448.doi:10.1517/17460441.2014.892923.PMID24559030.S2CID26424400.
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