Mirabegron

Mirabegron
Clinical data

Trade names	Myrbetriq (US), Betanis (JP), Betmiga (EU, RU)
License data	EU EMA: Betmiga US FDA: Mirabegron
Pregnancy category	US: C (Risk not ruled out)
Routes of administration	Oral (tablets)
ATC code	G04BD12 (WHO)
Legal status
Legal status	UK: POM (Prescription only) US: ℞-only In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability	29–35%
Protein binding	71%
Metabolism	Hepatic via (direct) glucuronidation, amide hydrolysis, and minimal oxidative metabolism in vivo by CYP2D6 and CYP3A4. Some involvement of butylcholinesterase
Biological half-life	50 hours
Excretion	Urine (55%), faeces (34%)
Identifiers
IUPAC name 2-(2-Amino-1,3-thiazol-4-yl)-N-[4-(2-{[(2R)-2-hydroxy-2-phenylethyl]amino}ethyl)phenyl]acetamide
Synonyms	YM-178
CAS Number	223673-61-8
PubChem CID	9865528
ChemSpider	8041219
ECHA InfoCard	100.226.392
Chemical and physical data
Formula	C₂₁H₂₄N₄O₂S
Molar mass	396.506 g/mol
3D model (Jmol)	Interactive image
SMILES O=C(Nc1ccc(cc1)CCNC[C@H](O)c2ccccc2)Cc3nc(sc3)N
InChI InChI=1S/C21H24N4O2S/c22-21-25-18(14-28-21)12-20(27)24-17-8-6-15(7-9-17)10-11-23-13-19(26)16-4-2-1-3-5-16/h1-9,14,19,23,26H,10-13H2,(H2,22,25)(H,24,27)/t19-/m0/s1 Key:PBAPPPCECJKMCM-IBGZPJMESA-N

Mirabegron (trade name Myrbetriq meer-BET-trick in the US and Betmiga in Europe) is a drug for the treatment of overactive bladder. It was developed by Astellas Pharma and was approved in the United States in July 2012.

Mirabegron activates the β₃ adrenergic receptor in the detrusor muscle in the bladder, which leads to muscle relaxation and an increase in bladder capacity.

Its primary use is in the treatment of overactive bladder.

Mirabegron has also recently been shown to activate brown fat and increase metabolism. In a small study of 15 healthy, lean men, Mirabegron was shown to increase basal heart rate, metabolic rate and blood pressure which are signs of cardiovascular stimulation.

Recently, mirabegron was shown to relax in vitro human and rabbit prostatic smooth muscle through activation of β₃ adrenoceptor. The same group also showed that mirabegron promotes smooth muscle relaxation by α₁ adrenergic receptor blockade.

Adverse effects by incidence:

Very common (>10% incidence) adverse effects include:

Common (1–10% incidence) adverse effects include:

Rare (<1% incidence) adverse effects include:

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Wikipedia