Mirabegron
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| 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 |
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| 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 Number | 223673-61-8 |
| ATC code | G04BD12 |
| PubChem | CID 9865528 |
| ChemSpider | 8041219 |
| Synonyms | YM-178 |
| Chemical data | |
| Formula | C21H24N4O2S |
| Molar mass | 396.506 g/mol |
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Mirabegron (trade name Myrbetriq in the US and Betmiga in Europe) 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
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] Recently, mirabegron was shown to relax in vitro human and rabbit prostate smooth muscle through activation of beta3-adrenoceptor.[8] The same group also showed that mirabegron promotes smooth muscle relaxation by alpha1-adrenoceptor blockade.[9]
Adverse effects
Adverse effects by incidence:[1][5][6]
Very common (>10% incidence) adverse effects include:
- Elevated blood pressure
Common (1-10% incidence) adverse effects include:
- Xerostomia (dry mouth)
- Nasopharyngitis
- Urinary tract infection (UTI)
- Headache
- Influenza
- Constipation
- Dizziness
- Arthralgia
- Cystitis
- Back pain
- Upper respiratory tract infection (URTI)
- Sinusitis
- Diarrhea
- Tachycardia (high heart rate)
- Fatigue
- Abdominal pain
- Neoplasms (cancers)
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
- 1 2 3 4 5 6 7 "mirabegron (Rx) - Myrbetriq". Medscape Reference. WebMD. Retrieved 17 November 2013.
- ↑ 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.
- ↑ Sacco, E; Bientinesi, R; et al. (Apr 2014). "Discovery history and clinical development of mirabegron for the treatment of overactive bladder and urinary incontinence". Expert Opin Drug Discov 9 (4): 433–48. doi:10.1517/17460441.2014.892923. PMID 2455903.
- ↑ "New Drug Approvals 2012 - Pt. XIV - Mirabegron (MyrbetriqTM)". ChEMBL. 5 July 2012. Retrieved 28 September 2012.
- 1 2 "MYRBETRIQ (mirabegron) tablet, film coated, extended release [Astellas Pharma US, Inc.]". DailyMed. Astellas Pharma US, Inc. September 2012. Retrieved 17 November 2013.
- 1 2 "Betmiga 25mg & 50mg prolonged-release tablets". electronic Medicines Compendium. Astellas Pharma Ltd. 22 February 2013. Retrieved 17 November 2013.
- ↑ 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.
- ↑ Calmasini, F. B., T. Z. Candido, E. C. Alexandre, C. A. D'Ancona, D. Silva, M. A. de Oliveira, G. De Nucci, E. Antunes and F. Z. Monica (2015). "The beta-3 adrenoceptor agonist, mirabegron relaxes isolated prostate from human and rabbit: new therapeutic indication?" Prostate 75(4): 440-447.
- ↑ Alexandre, E C; Kiguti, L R; Calmasini, F B; Silva, F H; da Silva, K P; Ferreira, R; Ribeiro, C A; Mónica, F Z; Pupo, A S (2015-10-01). "Mirabegron relaxes urethral smooth muscle by a dual mechanism involving β3-adrenoceptor activation and α1-adrenoceptor blockade". British Journal of Pharmacology: n/a–n/a. doi:10.1111/bph.13367. ISSN 1476-5381.
External links
- Sacco, E.; Bientinesi, R. (2012). "Mirabegron: A review of recent data and its prospects in the management of overactive bladder". Therapeutic Advances in Urology 4 (6): 315–24. doi:10.1177/1756287212457114. PMC 3491758. PMID 23205058.
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