Chemical compound
- EU EMA: by INN
- US DailyMed: Fesoterodine
- US FDA: Fesoterodine
Routes of administration | By mouth |
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ATC code | |
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Legal status |
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Legal status | - CA: ℞-only
- US: ℞-only
- EU: Rx-only
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Pharmacokinetic data |
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Bioavailability | 52% (active metabolite) |
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Protein binding | 50% (active metabolite) |
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Metabolism | Liver (CYP2D6- and 3A4-mediated) |
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Elimination half-life | 7–8 hours (active metabolite) |
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Excretion | Kidney (70%) and fecal (7%) |
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Identifiers |
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CAS Number | - 286930-02-7 N
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PubChem CID | |
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IUPHAR/BPS | |
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DrugBank | - DB06702 Y
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ChemSpider | - 5293755 Y
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UNII | |
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KEGG | - D07226 Y
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ChEMBL | - ChEMBL1201764 N
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CompTox Dashboard (EPA) | - DTXSID80182853
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ECHA InfoCard | 100.184.854 |
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Chemical and physical data |
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Formula | C26H37NO3 |
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Molar mass | 411.586 g·mol−1 |
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3D model (JSmol) | |
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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 YKey:DCCSDBARQIPTGU-HSZRJFAPSA-N Y |
NY (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
- ^ "Fesoterodine (Toviaz) Use During Pregnancy". Drugs.com. 7 November 2019. Archived from the original on 29 November 2020. Retrieved 12 August 2020.
- ^ "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.
- ^ "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.
- ^ "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.
- ^ "Notice of Decision for TOVIAZ". Archived from the original on 2012-04-23. Retrieved 2012-04-20.
- ^ 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.
- ^ "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 | |
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Antagonists | - 3-Quinuclidinyl benzilate
- 4-DAMP
- Aclidinium bromide (+formoterol)
- Abediterol
- AF-DX 250
- AF-DX 384
- Ambutonium bromide
- Anisodamine
- Anisodine
- Antihistamines (first-generation) (e.g., brompheniramine, buclizine, captodiame, chlorphenamine (chlorpheniramine), cinnarizine, clemastine, cyproheptadine, dimenhydrinate, dimetindene, diphenhydramine, doxylamine, meclizine, mequitazine, perlapine, phenindamine, pheniramine, phenyltoloxamine, promethazine, propiomazine, triprolidine)
- AQ-RA 741
- Atropine
- Atropine methonitrate
- Atypical antipsychotics (e.g., clozapine, fluperlapine, olanzapine (+fluoxetine), rilapine, quetiapine, tenilapine, zotepine)
- Benactyzine
- Benzatropine (benztropine)
- Benzilone
- Benzilylcholine mustard
- Benzydamine
- BIBN 99
- Biperiden
- Bornaprine
- Camylofin
- CAR-226,086
- CAR-301,060
- CAR-302,196
- CAR-302,282
- CAR-302,368
- CAR-302,537
- CAR-302,668
- Caramiphen
- Cimetropium bromide
- Clidinium bromide
- Cloperastine
- CS-27349
- Cyclobenzaprine
- Cyclopentolate
- Darifenacin
- DAU-5884
- Desfesoterodine
- Dexetimide
- DIBD
- Dicycloverine (dicyclomine)
- Dihexyverine
- Difemerine
- Diphemanil metilsulfate
- Ditran
- Drofenine
- EA-3167
- EA-3443
- EA-3580
- EA-3834
- Emepronium bromide
- Etanautine
- Etybenzatropine (ethybenztropine)
- Fenpiverinium
- Fentonium bromide
- Fesoterodine
- Flavoxate
- Glycopyrronium bromide (+beclometasone/formoterol, +indacaterol, +neostigmine)
- Hexahydrodifenidol
- Hexahydrosiladifenidol
- Hexbutinol
- Hexocyclium
- Himbacine
- HL-031,120
- Homatropine
- Imidafenacin
- Ipratropium bromide (+salbutamol)
- Isopropamide
- J-104,129
- Hyoscyamine
- Mamba toxin 3
- Mamba toxin 7
- Mazaticol
- Mebeverine
- Meladrazine
- Mepenzolate
- Methantheline
- Methoctramine
- Methylatropine
- Methylhomatropine
- Methylscopolamine
- Metixene
- Muscarinic toxin 7
- N-Ethyl-3-piperidyl benzilate
- N-Methyl-3-piperidyl benzilate
- Nefopam
- Octatropine methylbromide (anisotropine methylbromide)
- Orphenadrine
- Otenzepad (AF-DX 116)
- Otilonium bromide
- Oxapium iodide
- Oxitropium bromide
- Oxybutynin
- Oxyphencyclimine
- Oxyphenonium bromide
- PBID
- PD-102,807
- PD-0298029
- Penthienate
- Pethidine
- pFHHSiD
- Phenglutarimide
- Phenyltoloxamine
- Pipenzolate bromide
- Piperidolate
- Pirenzepine
- Piroheptine
- Pizotifen
- Poldine
- Pridinol
- Prifinium bromide
- Procyclidine
- Profenamine (ethopropazine)
- Propantheline bromide
- Propiverine
- Quinidine
- 3-Quinuclidinyl thiochromane-4-carboxylate
- Revefenacin
- Rociverine
- RU-47,213
- SCH-57,790
- SCH-72,788
- SCH-217,443
- Scopolamine (hyoscine)
- Scopolamine butylbromide (hyoscine butylbromide)
- Silahexacyclium
- Sofpironium bromide
- Solifenacin
- SSRIsTooltip Selective serotonin reuptake inhibitors (e.g., femoxetine, paroxetine)
- Telenzepine
- Terodiline
- Tetracyclic antidepressants (e.g., amoxapine, maprotiline, mianserin, mirtazapine)
- Tiemonium iodide
- Timepidium bromide
- Tiotropium bromide
- Tiquizium bromide
- Tofenacin
- Tolterodine
- Tricyclic antidepressants (e.g., amitriptyline (+perphenazine), amitriptylinoxide, butriptyline, cidoxepin, clomipramine, desipramine, desmethyldesipramine, dibenzepin, dosulepin (dothiepin), doxepin, imipramine, lofepramine, nitroxazepine, northiaden (desmethyldosulepin), nortriptyline, protriptyline, quinupramine, trimipramine)
- Tridihexethyl
- Trihexyphenidyl
- Trimebutine
- Tripitamine (tripitramine)
- Tropacine
- Tropatepine
- Tropicamide
- Trospium chloride
- Typical antipsychotics (e.g., chlorpromazine, chlorprothixene, cyamemazine (cyamepromazine), loxapine, mesoridazine, thioridazine)
- Umeclidinium bromide (+vilanterol)
- WIN-2299
- Xanomeline
- Zamifenacin
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Precursors (and prodrugs) | |
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- See also
- Receptor/signaling modulators
- Nicotinic acetylcholine receptor modulators
- Acetylcholine metabolism/transport modulators
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