Fesoterodine Fumarate

Catalog No.S2240

Fesoterodine Fumarate is a prodrug of 5-hydroxymethyl tolterodine that is a muscarinic AChR receptor antagonist, used to treat overactive bladder syndrome.

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Fesoterodine Fumarate  Chemical Structure

Fesoterodine Fumarate Chemical Structure
Molecular Weight: 527.65

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Fesoterodine Fumarate is available in the following compound libraries:

Product Information

Product Description

Biological Activity

Description Fesoterodine Fumarate is a prodrug of 5-hydroxymethyl tolterodine that is a muscarinic AChR receptor antagonist, used to treat overactive bladder syndrome.
Targets AChR [1]
In vitro Fesoterodine is rapidly and extensively converted to 5-HMT, such that the pharmacologic activity appears to be primarily attributable to 5-HMT. [1] Fesoterodine is a competitive antagonist of cholinergic agonist-stimulated responses in human M1-M5 cell lines and has a similar potency and selectivity profile to the radioligand-binding studies. Fesoterodine causes a rightward shift of the concentration-response curve for carbachol with no depression of the maximum in rat bladder strips, and concentration-dependently reduces contractions induced by electrical field stimulation (EFS). [2] Fesoterodine is hydrolyzed by nonspecific esterases to 5-hydroxmethyl tolterodine (5-HMT), which is the active metabolite and is responsible for all its antimuscarinic activity. [3]
In vivo
Features

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Malhotra B, et al. Curr Med Chem, 2009, 16(33), 4481-4489.

[2] Ney P, et al. BJU Int, 2008, 101(8), 1036-1042.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-06-25)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02240459 Not yet recruiting Overactive Bladder|Mild Cognitive Impairment University of Alberta|Pfizer May 2016 Phase 2
NCT02676154 Recruiting Autonomic Dysreflexia University of British Columbia|Pfizer|International Colla  ...more University of British Columbia|Pfizer|International Collaboration On Repair Discoveries (ICORD)|Vancouver Coastal Health February 2016 Phase 2
NCT02614482 Recruiting Overactive Bladder Stéphane Bolduc|Pfizer|Centre Hospitalier Universitaire d  ...more Stéphane Bolduc|Pfizer|Centre Hospitalier Universitaire de Québec, CHU de Québec October 2015 Phase 3
NCT02501928 Recruiting Urinary Bladder, Neurogenic Pfizer June 2015 Phase 3
NCT02385500 Not yet recruiting Urinary Bladder, Overactive|Parkinson Disease Sir Mortimer B. Davis - Jewish General Hospital March 2015 Phase 4

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Chemical Information

Download Fesoterodine Fumarate SDF
Molecular Weight (MW) 527.65
Formula

C26H37NO3.C4H4O4

CAS No. 286930-03-8
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms SPM 907
Solubility (25°C) * In vitro DMSO 100 mg/mL (189.51 mM)
Water 100 mg/mL (189.51 mM)
Ethanol 100 mg/mL (189.51 mM)
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name (R)-2-(3-(diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenyl isobutyrate fumarate

Tech Support

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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