Fesoterodine

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).[1] It was approved by the European Medicines Agency in April 2007,[2] the US Food and Drug Administration on October 31, 2008 [3] and Health Canada on February 9, 2012.[4]

Fesoterodine
Clinical data
Trade namesToviaz
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
IUPAC name
  • [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
Chemical and physical data
FormulaC26H37NO3
Molar mass411.586 g·mol−1
3D model (JSmol)
SMILES
  • O=C(Oc1ccc(cc1[C@@H](c2ccccc2)CCN(C(C)C)C(C)C)CO)C(C)C
InChI
  • 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 Y
  • Key:DCCSDBARQIPTGU-HSZRJFAPSA-N Y
 NY (what is this?)  (verify)

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.[5] 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.[5]

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. [6]

References
  1. "Fesoterodine, New Drug Candidate For Treatment For Overactive Bladder – Pfizer To Acquire Exclusive Worldwide Rights". Medical News Today. 17 April 2006.
  2. "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.
  3. "Pfizer's Toviaz (fesoterodine fumarate) Receives FDA Approval for the Treatment of Overactive Bladder" (Press release). Pfizer Inc. 2008-10-31. Retrieved 2008-11-06.
  4. "Notice of Decision for TOVIAZ". Archived from the original on 2012-04-23. Retrieved 2012-04-20.
  5. 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.
  6. "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.
  • "Fesoterodine". Drug Information Portal. U.S. National Library of Medicine.
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