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Fesoterodine

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Fesoterodine
Space-filling model of the fesoterodine molecule
Clinical data
Trade namesFesobig , Toviaz
AHFS/Drugs.comMonograph
MedlinePlusa609021
License data
Routes of
administration
By mouth
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability52% (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
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.184.854 Edit this at Wikidata
Chemical and physical data
FormulaC26H37NO3
Molar mass411.586 g·mol−1
3D model (JSmol)
  • 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

[edit]

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

[edit]
  1. ^ "Product monograph brand safety updates". Health Canada. 6 June 2024. Retrieved 8 June 2024.
  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.