Fesoterodine

Last updated
Fesoterodine
Fesoterodine.svg
Fesoterodine 3D spacefill.png
Clinical data
Trade names 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). [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]

Contents

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]

Related Research Articles

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

Bethanechol is a parasympathomimetic choline carbamate that selectively stimulates muscarinic receptors without any effect on nicotinic receptors. Unlike acetylcholine, bethanechol is not hydrolyzed by cholinesterase and will therefore have a long duration of action. Bethanechol is sold under the brand names Duvoid (Roberts), Myotonachol (Glenwood), Urecholine and Urocarb (Hamilton). The name bethanechol refers to its structure as the urethane of beta-methylcholine.

<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> Bladder medication

Oxybutynin, sold as under the brand names Ditropan among others, is a medication used to treat overactive bladder. It works similar to tolterodine, Darifenacin, and Solifenacin. While used for bed wetting in children, evidence to support this use is poor. 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 used to treat overactive bladder.

<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. Overactive bladder affects approximately 11% of the population and more than 40% of people with overactive bladder have incontinence. Conversely, about 40% to 70% of urinary incontinence is due to overactive bladder. Overactive bladder is not life-threatening, but most people with the condition have problems for years.

<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. A modified release preparation is also available, taken once daily.

<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.

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.

Treatments for overactive bladder are therapies used to treat overactive bladder or related conditions, such as urinary incontinence and frequent urination. Behavioral modification and medications are commonly used to treat this condition.

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.

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 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">Diroximel fumarate</span> Medication

Diroximel fumarate, sold under the brand name Vumerity, is a medication used for the treatment of relapsing forms of multiple sclerosis (MS). It acts as an immunosuppressant and anti-inflammatory drug. Its most common adverse effects are flushing and gastrointestinal problems.

<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. "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. 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.
  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.