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
Pregnancy
category
  • US: C (Risk not ruled out)
    Routes of
    administration
    Oral
    ATC code
    Legal status
    Legal status
    • In general: ℞ (Prescription only)
    Pharmacokinetic data
    Bioavailability52% (active metabolite)
    Protein binding50% (active metabolite)
    MetabolismHepatic (CYP2D6- and 3A4-mediated)
    Elimination half-life7–8 hours (active metabolite)
    ExcretionRenal (70%) and fecal (7%)
    Identifiers
    CAS Number
    PubChem CID
    IUPHAR/BPS
    DrugBank
    ChemSpider
    UNII
    KEGG
    ChEMBL
    CompTox Dashboard (EPA)
    ECHA InfoCard100.184.854
    Chemical and physical data
    FormulaC26H37NO3
    Molar mass411.278 g/mol g·mol−1
    3D model (JSmol)
     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 7 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. (2011). "Review of fesoterodine". Expert Opinion on Drug Safety. 10 (5): 805–808. doi:10.1517/14740338.2011.591377. PMID 21639817.
    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.
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