Fesoterodinefumarate

Fesoterodinefumarate
  • CAS No.:286930-03-8
Other grades of this product :
Fesoterodinefumarate Basic information
Description Biological activity Side effects
Product Name:Fesoterodinefumarate
Synonyms:Fesoterodine maleate;2-[(1R)-3-[Bis(1-methylethyl)amino]-1-phenylpropyl]-4-(hydroxymethyl)phenyl 2-methylpropanoate fumarate;Propanoic acid, 2-methyl-, 2-((1R)-3-(bis(1-methylethyl)amino)-1-phenylpropyl)-4-(hydroxymethyl)phenyl ester, (2E)-2-butenedioate (1:1) (salt);Spm 8272;Toviaz;Unii-eos72165S7;Fesoterodinefumarate;(R)-Fesoterodine Fumarate
CAS:286930-03-8
MF:C30H41NO7
MW:527.65
EINECS:639-689-3
Product Categories:Toviaz;Amines;Aromatics Compounds;Aromatics;Intermediates & Fine Chemicals;Pharmaceuticals
Mol File:286930-03-8.mol
Fesoterodinefumarate Chemical Properties
Melting point 72-78°C
storage temp. Inert atmosphere,2-8°C
solubility DMSO (Slightly), Ethanol (Slightly), Methanol (Slightly)
form Solid
color White to Off-White
Stability:Hygroscopic
Safety Information
MSDS Information
Fesoterodinefumarate Usage And Synthesis
DescriptionFesoterodine fumarate is a new drug for the treatment of overactive bladder syndrome developed by Pfizer, which was approved by the US FDA in October 2008. Fesoterodine fumarate is a prodrug, which is rapidly hydrolyzed in blood after oral administration to 5-hydroxymethyl tolterodine (5-HMT), which is also the active metabolite of tolterodine.
Biological activityFesoterodine Fumarate (SPM 907) is a prodrug of the muscarinic receptor antagonist 5-hydroxymethyl tolterodine, used to treat overactive bladder.
Side effectsThe most common side effects was dry mouth, which was observed in the placebo group, the product 4 in the Phase II and Phase III clinical trials (a total of 2 859 patients, 2 288 taking this product for 8 to 12 weeks). The incidences of dry mouth at mg/d and 8 mg/d were 7%, 19%, and 35%, respectively, and the incidences of drug discontinuation due to dry mouth were 0.4%, 0.4%, and 0.8%, respectively. The second most common adverse reaction was constipation. The incidence of constipation in the placebo group and the 4 mg/d and 8 mg/d groups of this product was 2%, 4% and 6%, respectively. Other reported adverse events included loss of appetite, nausea, epigastric pain, urinary tract infection, upper respiratory tract infection, dry eyes, dysuria, urinary retention, cough, peripheral edema, back pain, insomnia, abnormal liver function, and rash.
Chemical PropertiesWhite Solid
UsesFesoterodine fumarate (Toviaz) is an antimuscarinic agent and is rapidly de-esterified to its active metabolite 5-hydroxymethyl tolterodine that is a muscarinic receptor antagonist. Fesoterodine fumarate (Toviaz) is used to treat the symptoms of overactiv
Uses(R)-Fesoterodine Fumarate is a muscarinic receptor antagonist for the treatment of Lower Urininary Tract Symptoms (LUTS). It is very similar to Tolterodine (T535800).
Clinical UseAntimuscarinic:Symptomatic treatment of urinary incontinence, frequency or urgency
Drug interactionsPotentially hazardous interactions with other drugs Anti-arrhythmics: increased risk of antimuscarinic side effects with disopyramide. Antifungals: dose reduction advised with itraconazole and ketoconazole. Antivirals: dose reduction advised with atazanavir, indinavir, ritonavir and saquinavir. Induction of CYP3A4 may lead to subtherapeutic plasma levels. Concomitant use with CYP3A4 inducers (e.g. carbamazepine, rifampicin, phenobarbital, phenytoin, St John's Wort) is not recommended. Co-administration of a potent CYP2D6 inhibitor may result in increased exposure and adverse events. A dose reduction to 4 mg may be needed' See 'Other information'
MetabolismMolecular weight (daltons) 527.7 % Protein binding 50 (metabolite) % Excreted unchanged in urine 70 (as metabolites) Volume of distribution (L/kg) 169 Litres Half-life - normal/ESRF (hrs) 7 / -
Fesoterodinefumarate Preparation Products And Raw materials

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