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).^[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

Clinical data
Trade names	Fesobig , Toviaz
AHFS/Drugs.com	Monograph
MedlinePlus	a609021
License data	US DailyMed: Fesoterodine
Routes of administration	By mouth
ATC code	G04BD11 (WHO)
Legal status
Legal status	CA: ℞-only[1] US: ℞-only EU: Rx-only
Pharmacokinetic data
Bioavailability	52% (active metabolite)
Protein binding	50% (active metabolite)
Metabolism	Liver (CYP2D6- and 3A4-mediated)
Elimination half-life	7–8 hours (active metabolite)
Excretion	Kidney (70%) and fecal (7%)
Identifiers
IUPAC name [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 Y
ChemSpider	5293755 Y
UNII	621G617227
KEGG	D07226 Y
ChEMBL	ChEMBL1201764 N
CompTox Dashboard (EPA)	DTXSID80182853
ECHA InfoCard	100.184.854
Chemical and physical data
Formula	C26H37NO3
Molar mass	411.586 g·mol−1
3D model (JSmol)	Interactive image
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.^[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. "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. 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.