Fesoterodine

Chemical compound
  • EU EMA: by INN
  • US DailyMed: Fesoterodine
  • US FDA: Fesoterodine
Routes of
administrationBy mouthATC code
  • G04BD11 (WHO)
Legal statusLegal status
  • CA: ℞-only
  • US: ℞-only
  • EU: Rx-only
Pharmacokinetic dataBioavailability52% (active metabolite)Protein binding50% (active metabolite)MetabolismLiver (CYP2D6- and 3A4-mediated)Elimination half-life7–8 hours (active metabolite)ExcretionKidney (70%) and fecal (7%)Identifiers
  • [2-[(1R)-3-(Di(propan-2-yl)amino)-1-phenylpropyl]-4-(hydroxymethyl)phenyl] 2-methylpropanoate
CAS Number
  • 286930-02-7 ☒N
PubChem CID
  • 6918558
IUPHAR/BPS
  • 7473
DrugBank
  • DB06702 checkY
ChemSpider
  • 5293755 checkY
UNII
  • 621G617227
KEGG
  • D07226 checkY
ChEMBL
  • ChEMBL1201764 ☒N
CompTox Dashboard (EPA)
  • DTXSID80182853 Edit this at Wikidata
ECHA InfoCard100.184.854 Edit this at WikidataChemical and physical dataFormulaC26H37NO3Molar mass411.586 g·mol−13D model (JSmol)
  • Interactive image
  • O=C(Oc1ccc(cc1[C@@H](c2ccccc2)CCN(C(C)C)C(C)C)CO)C(C)C
  • InChI=1S/C26H37NO3/c1-18(2)26(29)30-25-13-12-21(17-28)16-24(25)23(22-10-8-7-9-11-22)14-15-27(19(3)4)20(5)6/h7-13,16,18-20,23,28H,14-15,17H2,1-6H3/t23-/m1/s1 checkY
  • Key:DCCSDBARQIPTGU-HSZRJFAPSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Fesoterodine (INN, used as the fumarate under the brand name Toviaz) is an antimuscarinic drug developed by Schwarz Pharma AG to treat overactive bladder syndrome (OAB).[2] It was approved by the European Medicines Agency in April 2007,[3] the US Food and Drug Administration on October 31, 2008 [4] and Health Canada on February 9, 2012.[5]

Fesoterodine is a prodrug. It is broken down into its active metabolite, desfesoterodine, by plasma esterases.

Efficacy

Fesoterodine has the advantage of allowing more flexible dosage than other muscarinic antagonists.[6] Its tolerability and side effects are similar to other muscarinic antagonists and as a new drug seems unlikely to make great changes in practices of treatment for overactive bladder.[6]

A Japanese study from 2017, showed that urgency and urge incontinence are improved after 3 days administration of the drug, with full efficacy able to be judged after 7 days administration. Overactive bladder was found to be resolved in 88% of patients after seven days usage. [7]

References

  1. ^ "Fesoterodine (Toviaz) Use During Pregnancy". Drugs.com. 7 November 2019. Archived from the original on 29 November 2020. Retrieved 12 August 2020.
  2. ^ "Fesoterodine, New Drug Candidate For Treatment For Overactive Bladder – Pfizer To Acquire Exclusive Worldwide Rights". Medical News Today. 17 April 2006. Archived from the original on 16 May 2011. Retrieved 2 November 2007.
  3. ^ "Toviaz: European Public Assessment Report, Revision 3 - Published 02/06/08". European Medicines Agency. 2 June 2008. Archived from the original on 2008-04-01.
  4. ^ "Pfizer's Toviaz (fesoterodine fumarate) Receives FDA Approval for the Treatment of Overactive Bladder" (Press release). Pfizer Inc. 2008-10-31. Archived from the original on 2018-09-20. Retrieved 2008-11-06.
  5. ^ "Notice of Decision for TOVIAZ". Archived from the original on 2012-04-23. Retrieved 2012-04-20.
  6. ^ a b Vella M, Cardozo L (September 2011). "Review of fesoterodine". Expert Opinion on Drug Safety. 10 (5): 805–8. doi:10.1517/14740338.2011.591377. PMID 21639817. S2CID 9653506.
  7. ^ "Sato N, Fuji K, Ogawa Y (2017). "Transactions of The Showa University Society: The 335th Meeting". The Showa University Journal of Medical Sciences. 29 (2): 201–217. doi:10.15369/sujms.29.201. ISSN 2185-0968.

External links

  • "Fesoterodine". Drug Information Portal. U.S. National Library of Medicine.
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mAChRsTooltip Muscarinic acetylcholine receptors
Agonists
Antagonists
Precursors
(and prodrugs)
See also
Receptor/signaling modulators
Nicotinic acetylcholine receptor modulators
Acetylcholine metabolism/transport modulators
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