Mirabegron

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Mirabegron
Mirabegron2DACS2.svg
Systematic (IUPAC) name
2-(2-Amino-1,3-thiazol-4-yl)-N-[4-(2-{[(2R)-2-hydroxy-2-phenylethyl]amino}ethyl)phenyl]acetamide
Clinical data
Trade names Myrbetriq (US), Betanis (Japan), Betmiga (EU)
Licence data EMA:Link, US FDA:link
Pregnancy
category
  • US: C (Risk not ruled out)
Legal status
Routes of
administration
Oral
Pharmacokinetic data
Bioavailability 29-35%[1]
Protein binding 71%[1]
Metabolism Hepatic via (direct) glucuronidation, amide hydrolysis, and minimal oxidative metabolism in vivo by CYP2D6 and CYP3A4. Some involvement of butylcholinesterase[1]
Biological half-life 50 hours[1]
Excretion Urine (55%), faeces (34%)[1]
Identifiers
CAS Registry Number 223673-61-8
ATC code G04BD12
PubChem CID: 9865528
ChemSpider 8041219
Synonyms YM-178
Chemical data
Formula C21H24N4O2S
Molecular mass 396.506 g/mol

Mirabegron (formerly YM-178, trade name Myrbetriq, Betmiga in Spain) is a drug for the treatment of overactive bladder.[2] It was developed by Astellas Pharma and was approved in the United States in July 2012.[3]

Mirabegron activates the β3 adrenergic receptor in the detrusor muscle in the bladder, which leads to muscle relaxation and an increase in bladder capacity.[4]

Medical uses[edit]

Its primary use is in the treatment of overactive bladder.[1][5][6] 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. [7]

Adverse effects[edit]

Adverse effects by incidence:[1][5][6]

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

  • Elevated blood pressure

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

Rare (<1% incidence) adverse effects include:

  • Palpitations
  • Blurred vision
  • Glaucoma
  • Dyspepsia (indigestion)
  • Gastritis
  • Abdominal distension
  • Rhinitis
  • Elevations in liver enzymes (GGT, AST, ALT & LDH)
  • Renal and urinary disorders (e.g., nephrolithiasis, bladder pain)
  • Reproductive system disorders (e.g., vulvovaginal pruritis, vaginal infection)
  • Skin and subcutaneous tissue disorders (e.g., urticaria, leukocytoclastic vasculitis, rash, pruritus, purpura, lip edema)
  • Stevens-Johnson syndrome associated with increased serum ALT, AST and bilirubin
  • Urinary retention

References[edit]

  1. ^ a b c d e f g "mirabegron (Rx) - Myrbetriq". Medscape Reference. WebMD. Retrieved 17 November 2013. 
  2. ^ Gras, J (2012). "Mirabegron for the treatment of overactive bladder". Drugs of today (Barcelona, Spain : 1998) 48 (1): 25–32. doi:10.1358/dot.2012.48.1.1738056. PMID 22384458. 
  3. ^ Sacco E, Bientinesi R, et al. Discovery history and clinical development of mirabegron for the treatment of overactive bladder and urinary incontinence. Expert Opin Drug Discov. 2014 Apr;9(4):433-48. doi: 10.1517/17460441.2014.892923. Epub 2014 Feb 22.PMID 2455903
  4. ^ "New Drug Approvals 2012 - Pt. XIV - Mirabegron (MyrbetriqTM)". ChEMBL. 5 July 2012. Retrieved 28 September 2012. 
  5. ^ a b "MYRBETRIQ (mirabegron) tablet, film coated, extended release [Astellas Pharma US, Inc.]". DailyMed. Astellas Pharma US, Inc. September 2012. Retrieved 17 November 2013. 
  6. ^ a b "Betmiga 25mg & 50mg prolonged-release tablets". electronic Medicines Compendium. Astellas Pharma Ltd. 22 February 2013. Retrieved 17 November 2013. 
  7. ^ Cypess, Aaron; Weiner, Lauren; Roberts-Toler, Carla; Elía, Elisa; Kessler, Skyler; Kahn, Peter; English, Jeffrey; Chatman, Kelly; Trauger, Sunia; Doria, Alessandro; Kolodny, Gerald (6 January 2015). "Activation of Human Brown Adipose Tissue by a β3-Adrenergic Receptor Agonist". Cell Metabolism 21 (1): 33–38. doi:10.1016/j.cmet.2014.12.009. PMID 25565203. Retrieved 26 January 2015. 

External links[edit]