| Identification | Back Directory | [Name]
Fesoterodinefumarate | [CAS]
286930-03-8 | [Synonyms]
Toviaz
SPM 907
SMP 8272
Spm 8272
Unii-eos72165S7
Fesoterodinefumarate
Fesoterodine maleate
(R)-Fesoterodine Fumarate
Fesoterodine fuMarate salt
Fesoterodine fuMarate (Toviaz)
FESOTERODINE MALEATE INTERMEDIATES
2-((1R)-3-(Diisopropylamino)-1-phenylpropyl)-4(hydroxymethyl)phenyl isobutyrate
(R)-2-(3-(Diisopropylamino)-1-phenylpropyl)-4-methoxyphenyl isobutyrate fumarate
(R)-2-(3-(diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenyl isobutyrate fumarate
2-[(1R)-3-[Bis(1-methylethyl)amino]-1-phenylpropyl]-4-(hydroxymethyl)phenyl 2-methylpropanoate fumarate
2-Methylpropanoic Acid 2-[(1R)-3-[Bis(1-methylethyl)amino]-1-phenylpropyl]-4-(hydroxymethyl)phenyl Ester (2E)-2-Butenedioate
(R)-Fesoterodine fumarate
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) | [EINECS(EC#)]
639-689-3 | [Molecular Formula]
C30H41NO7 | [MDL Number]
MFCD28142648 | [MOL File]
286930-03-8.mol | [Molecular Weight]
527.65 |
| Questions And Answer | Back Directory | [Description]
Fesoterodine 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 activity]
Fesoterodine Fumarate (SPM 907) is a prodrug of the muscarinic receptor antagonist 5-hydroxymethyl tolterodine, used to treat overactive bladder. | [Side effects]
The 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 Properties | Back Directory | [Appearance]
White Solid | [Melting point ]
72-78°C | [storage temp. ]
Hygroscopic, Store under Inert atmosphere -20°C Freezer | [solubility ]
DMSO (Slightly), Ethanol (Slightly), Methanol (Slightly) | [form ]
Solid | [color ]
White to Off-White | [Water Solubility ]
H2O: 2mg/mL, clear | [Stability:]
Hygroscopic |
| Hazard Information | Back Directory | [Chemical Properties]
White Solid | [Uses]
(R)-Fesoterodine Fumarate is a muscarinic receptor antagonist for the treatment of Lower Urininary Tract Symptoms (LUTS). | [Uses]
Fesoterodine 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 | [Clinical Use]
Antimuscarinic:Symptomatic treatment of urinary incontinence,
frequency or urgency | [Drug interactions]
Potentially 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' | [Metabolism]
Molecular 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 / - |
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