Fesoterodine

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Fesoterodine
Fesoterodine.svg
Fesoterodine 3D spacefill.png
Clinical data
Trade names Fesobig , Toviaz
AHFS/Drugs.com Monograph
MedlinePlus a609021
License data
Routes of
administration
By mouth
ATC code
Legal status
Legal status
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
  • [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 InfoCard 100.184.854 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C26H37NO3
Molar mass 411.586 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 Yes check.svgY
  • Key:DCCSDBARQIPTGU-HSZRJFAPSA-N Yes check.svgY
 X mark.svgNYes check.svgY  (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]

Related Research Articles

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<span class="mw-page-title-main">Glycopyrronium bromide</span> Chemical compound

Glycopyrronium bromide is a medication of the muscarinic anticholinergic group. It does not cross the blood–brain barrier and consequently has few to no central effects. It is given by mouth, via intravenous injection, on the skin, and via inhalation. It is a synthetic quaternary ammonium compound. The cation, which is the active moiety, is called glycopyrronium (INN) or glycopyrrolate (USAN).

<span class="mw-page-title-main">Tolterodine</span> Benzhydryl compound

Tolterodine, sold under the brand name Detrol among others, is a medication used to treat frequent urination, urinary incontinence, or urinary urgency. Effects are seen within an hour. It is taken by mouth.

<span class="mw-page-title-main">Oxybutynin</span> Medication for overactive bladder

Oxybutynin, sold under the brand name Ditropan among others, is an anticholinergic medication primarily used to treat overactive bladder. It is widely considered a first-line therapy for overactive bladder due to its well-studied side effect profile, broad applicability, and continued efficacy over long periods of time. It works similar to tolterodine, darifenacin, and solifenacin, although it is usually preferred over these medications. It is sometimes used off-label for treatment of hyperhidrosis, or excessive sweating. It has also been used off-label to treat bed wetting in children, but this use has declined, as it is most likely ineffective in this role. It is taken by mouth or applied to the skin.

<span class="mw-page-title-main">Darifenacin</span> Medication for urinary incontinence

Darifenacin is a medication used to treat urinary incontinence due to an overactive bladder. It was discovered by scientists at the Pfizer research site in Sandwich, UK under the identifier UK-88,525 and used to be marketed by Novartis. In 2010, the US rights were sold to Warner Chilcott for US$400 million.

<span class="mw-page-title-main">Solifenacin</span> Chemical compound

Solifenacin, sold as the brand name Vesicare among others, is a medicine used to treat overactive bladder and neurogenic detrusor overactivity (NDO). It may help with incontinence, urinary frequency, and urinary urgency.

<span class="mw-page-title-main">Trospium chloride</span> Chemical compound

Trospium chloride is a muscarinic antagonist used to treat overactive bladder. It has side effects typical of this class of drugs, namely dry mouth, stomach upset, and constipation; these side effects cause problems with people taking their medicine as directed. However it doesn't cause central nervous system side effects like some other muscarinic antagonists. It is in pregnancy category C and is excreted in breast milk.

<span class="mw-page-title-main">Rupatadine</span> Second generation H1-antihistamine

Rupatadine is a second generation antihistamine and platelet-activating factor antagonist used to treat allergies. It was discovered and developed by Uriach and is marketed as Rupafin and under several other trade names.

<span class="mw-page-title-main">Overactive bladder</span> Condition where a person has a frequent need to urinate

Overactive bladder (OAB) is a common condition where there is a frequent feeling of needing to urinate to a degree that it negatively affects a person's life. The frequent need to urinate may occur during the day, at night, or both. Loss of bladder control may occur with this condition. This condition is also sometimes characterized by a sudden and involuntary contraction of the bladder muscles, in response to excitement or anticipation. This in turn leads to a frequent and urgent need to urinate.

<span class="mw-page-title-main">Silodosin</span> Chemical compound

Silodosin, sold under the brand name Urief among others, is a medication for the symptomatic treatment of benign prostatic hyperplasia. It acts as an alpha-1 adrenergic receptor antagonist.

<span class="mw-page-title-main">Propiverine</span> Chemical compound

Propiverine is an anticholinergic drug used for the treatment of urinary urgency, frequency and urge incontinence, all symptoms of overactive bladder syndrome. It is a muscarinic antagonist.

<span class="mw-page-title-main">Dimethyl fumarate</span> Chemical compound

Dimethyl fumarate (DMF) is the methyl ester of fumaric acid and is named after the earth smoke plant. Dimethyl fumarate combined with three other fumaric acid esters (FAEs) is solely licensed in Germany as an oral therapy for psoriasis. Since 2013, it has been approved by the U.S. Food and Drug Administration (FDA) as a treatment option for adults with relapsing multiple sclerosis. In 2017, an oral formulation of dimethyl fumarate was approved for medical use in the European Union as a treatment for moderate-to-severe plaque psoriasis. Dimethyl fumarate is thought to have immunomodulatory properties without causing significant immunosuppression.

<span class="mw-page-title-main">Tenofovir alafenamide</span> Chemical compound

Tenofovir alafenamide, sold under the brand name Vemlidy, is an antiviral medication used against hepatitis B and HIV. It is used for the treatment of chronic hepatitis B virus (HBV) infection in adults with compensated liver disease and is given in combination with other medications for the prevention and treatment of HIV. It is taken by mouth.

Mirabegron, sold under the brand name Myrbetriq among others, is a medication used to treat overactive bladder. Its benefits are similar to antimuscarinic medication such as solifenacin or tolterodine. It is taken by mouth.

Aclidinium bromide/formoterol, sold under the brand names Duaklir and Brimica, is a fixed-dose combination medication for inhalation, used in the management of chronic obstructive pulmonary disease (COPD). It consists of aclidinium bromide, a long-acting muscarinic antagonist, and formoterol, a long-acting β2 agonist.

<span class="mw-page-title-main">Rimegepant</span> Medication for acute migraine in adults

Rimegepant, sold under the brand name Nurtec ODT among others, is a medication used for the acute treatment of migraine with or without aura in adults and the prophylactic/ preventive treatment of episodic migraine in adults. It is taken by mouth to dissolve on or under the tongue. It works by blocking CGRP receptors.

<span class="mw-page-title-main">Beclometasone/formoterol/glycopyrronium bromide</span> Combination drug

Beclometasone/formoterol/glycopyrronium, sold under the brand name Trimbow among others, is an inhalable fixed-dose combination medication for the treatment of chronic obstructive pulmonary disease (COPD) and asthma. It contains beclometasone dipropionate, formoterol fumarate dihydrate, and glycopyrronium bromide.

Glycopyrronium bromide/formoterol, sold under the brand name Bevespi Aerosphere, is a combination medication used for the maintenance treatment of chronic obstructive pulmonary disease (COPD). It is a combination of glycopyrronium bromide and formoterol. It is inhaled.

<span class="mw-page-title-main">Vibegron</span> Medication

Vibegron, sold under the brand name Gemtesa, is a medication for the treatment of overactive bladder. Vibegron is a selective beta-3 adrenergic receptor agonist.

<span class="mw-page-title-main">Relugolix/estradiol/norethisterone acetate</span> Combination medication

Relugolix/estradiol/norethisterone acetate, sold under the brand names Myfembree and Ryeqo, is a fixed-dose combination hormonal medication which is used for the treatment of heavy menstrual bleeding associated with uterine leiomyomas (fibroids) and for moderate to severe pain associated with endometriosis. It contains relugolix, an orally active gonadotropin-releasing hormone antagonist, estradiol, an estrogen, and norethisterone acetate, a progestin. The medication is taken by mouth.

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. 1 2 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.