Identification

Name
Fesoterodine
Accession Number
DB06702
Type
Small Molecule
Groups
Approved
Description

Fesoterodine is an antimuscarinic prodrug for the treatment of overactive bladder syndrome.

Structure
Thumb
Synonyms
  • FESO
  • Fesoterodine
Product Ingredients
IngredientUNIICASInChI Key
Fesoterodine fumarateEOS72165S7286930-03-8MWHXMIASLKXGBU-RNCYCKTQSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
ToviazTablet, extended release8 mgOralPfizer2012-04-19Not applicableCanada
ToviazTablet, extended release8 mgOralPfizer2007-04-20Not applicableEu
ToviazTablet, extended release8 mgOralPfizer2007-04-20Not applicableEu
ToviazTablet, film coated, extended release4 mg/1OralPhysicians Total Care, Inc.2010-08-23Not applicableUs
ToviazTablet, extended release4 mgOralPfizer2007-04-20Not applicableEu
ToviazTablet, film coated, extended release8 mg/1OralCardinal Health2008-10-31Not applicableUs
ToviazTablet, extended release8 mgOralPfizer2007-04-20Not applicableEu
ToviazTablet, extended release4 mgOralPfizer2007-04-20Not applicableEu
ToviazTablet, extended release8 mgOralPfizer2007-04-20Not applicableEu
ToviazTablet, extended release4 mgOralPfizer2007-04-20Not applicableEu
Categories
UNII
621G617227
CAS number
286930-02-7
Weight
Average: 411.5769
Monoisotopic: 411.277344055
Chemical Formula
C26H37NO3
InChI Key
DCCSDBARQIPTGU-HSZRJFAPSA-N
InChI
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
IUPAC Name
2-[(1R)-3-[bis(propan-2-yl)amino]-1-phenylpropyl]-4-(hydroxymethyl)phenyl 2-methylpropanoate
SMILES
CC(C)N(CC[[email protected]](C1=CC=CC=C1)C1=C(OC(=O)C(C)C)C=CC(CO)=C1)C(C)C

Pharmacology

Indication

For the treatment of overactive bladder (with symptoms of urinary frequency, urgency, or urge incontinence).

Structured Indications
Pharmacodynamics

Fesoterodine is a prodrug. In-vivo it is broken down into its active metabolite, 5-hydroxymethyl tolterodine (5-HMT), by plasma esterases. The 5-hydroxymethyl metabolite, which exhibits an antimuscarinic activity. Both urinary bladder contraction and salivation are mediated via cholinergic muscarinic receptors. Therefore, acting as a competitive muscarinic receptor antagonist, fesoterodine ultimately acts to decrease the detrusor pressure by its muscarinic antagonism, thereby decreasing bladder contraction and consequently, the urge to urinate.

Mechanism of action

Fesoterodine, once converted to its active metabolite, 5-hydroxymethyltolterodine, acts as a competitive antagonists at muscarinic receptors. This results in the inhibition of bladder contraction, decrease in detrusor pressure, and an incomplete emptying of the bladder.

TargetActionsOrganism
AMuscarinic acetylcholine receptor M3
antagonist
Human
UMuscarinic acetylcholine receptor M4
antagonist
Human
UMuscarinic acetylcholine receptor M1
antagonist
Human
UMuscarinic acetylcholine receptor M2
antagonist
Human
UMuscarinic acetylcholine receptor M5
antagonist
Human
Absorption

Tmax (5-HMT): 5 hours post-adminitration of fesoterodine. AUC (0,∞)= 49.5 ng·h/ ml
Bioavailability, 5-HMT = 52%

Volume of distribution

IV, 5-HMT: 169 L

Protein binding

5-HMT: 50% to albumin and alpha1-acid glycoprotein

Metabolism

Metabolized by ubiquitous, nonspecific esterases to transform fesoterodine into 5-HMT Extensive metabolism via CYP2D6 and CYP3A4 into inactive metabolites

Route of elimination

Renal: 70% of fesoterodine was recovered in urine as 5-HMT; 35% carboxy metabolite; 18% carboxy-N-desisopropylmetabolite, and 1% N-desisopropyl metabolite Fecal: 7% Hepatic: fesoterodine elimination via CYP2D6 and CYP3A4

Half life

7-8 hours for the active metabolite 5-hydroxymethyl tolterodine

Clearance

5-HMT, healthy subjects: 14.4 L/h 5-HMT is also secreted into the nephron.

Toxicity

Rat, Oral, LD50: ~ 681 mg/kg Mouse, Oral, LD50: ~ 316 mg/kg Rat, Intravenous, NOAEL: 10 mg/kg Mouse, Intravenous, NOAEL: 10 mg/kg

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Interacting Gene/EnzymeAllele nameGenotype(s)Defining Change(s)Type(s)DescriptionDetails
Cytochrome P450 2D6CYP2D6*3Not AvailableC alleleEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*4Not AvailableC alleleEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*5Not AvailableWhole-gene deletionEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*6Not Available1707delTEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*7Not Available2935A>CEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*8Not Available1758G>TEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*11Not Available883G>CEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*12Not Available124G>AEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*13Not AvailableCYP2D7/2D6 hybrid gene structureEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*14ANot Available1758G>AEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*15Not Available137insT, 137_138insTEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*19Not Available2539_2542delAACTEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*20Not Available1973_1974insGEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*21Not Available2573insCEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*31Not Available-1770G>A / -1584C>G  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*36Not Available100C>T / -1426C>T  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*38Not Available2587_2590delGACTEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*40Not Available1863_1864ins(TTT CGC CCC)2Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*42Not Available3259_3260insGTEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*44Not Available2950G>CEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*47Not Available100C>T / -1426C>T  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*51Not Available-1584C>G / -1235A>G  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*56Not Available3201C>TEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*57Not Available100C>T / 310G>T  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*62Not Available4044C>TEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*68ANot Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*68BNot AvailableSimilar but not identical switch region compared to CYP2D6*68A. Found in tandem arrangement with CYP2D6*4.Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*69Not Available2988G>A / -1426C>T  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*92Not Available1995delCEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*100Not Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*101Not Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer.Details

Interactions

Drug Interactions
DrugInteractionDrug group
1,10-PhenanthrolineThe therapeutic efficacy of Fesoterodine can be decreased when used in combination with 1,10-Phenanthroline.Experimental
AbirateroneThe serum concentration of Fesoterodine can be increased when it is combined with Abiraterone.Approved
AcebutololThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Acebutolol.Approved
AclidiniumAclidinium may increase the anticholinergic activities of Fesoterodine.Approved
AjmalineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Ajmaline.Approved, Investigational
AlcuroniumThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Alcuronium.Experimental
AlfentanilThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Alfentanil.Approved, Illicit
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Alphacetylmethadol.Experimental, Illicit
AlphaprodineThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Alphaprodine.Illicit
AmbenoniumThe therapeutic efficacy of Fesoterodine can be decreased when used in combination with Ambenonium.Approved
AmiodaroneThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Amitriptyline.Approved
AmlodipineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Amlodipine.Approved
AmodiaquineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Amodiaquine.Approved, Investigational
AmphetamineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Amphetamine.Approved, Illicit
Anisotropine MethylbromideThe risk or severity of adverse effects can be increased when Anisotropine Methylbromide is combined with Fesoterodine.Approved
AntipyrineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Antipyrine.Approved
AprepitantThe serum concentration of Fesoterodine can be increased when it is combined with Aprepitant.Approved, Investigational
AripiprazoleThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Aripiprazole.Approved, Investigational
ArtemetherThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Artemether.Approved
AsenapineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Asenapine.Approved
AtazanavirThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Atazanavir.Approved, Investigational
AtomoxetineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Atomoxetine.Approved
AtorvastatinThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Atorvastatin.Approved
AtracuriumThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Atracurium.Experimental, Investigational
Atracurium besylateThe risk or severity of adverse effects can be increased when Atracurium besylate is combined with Fesoterodine.Approved
AtropineThe risk or severity of adverse effects can be increased when Atropine is combined with Fesoterodine.Approved, Vet Approved
AzelastineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Azelastine.Approved
BenactyzineThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Benactyzine.Withdrawn
BendroflumethiazideThe serum concentration of Bendroflumethiazide can be increased when it is combined with Fesoterodine.Approved
BenzatropineThe risk or severity of adverse effects can be increased when Benzatropine is combined with Fesoterodine.Approved
BetaxololThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Betaxolol.Approved
BezitramideThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Bezitramide.Experimental, Illicit, Withdrawn
BicalutamideThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Bicalutamide.Approved
BiperidenThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Biperiden.Approved, Investigational
BoceprevirThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Boceprevir.Approved, Withdrawn
BornaprineThe risk or severity of adverse effects can be increased when Bornaprine is combined with Fesoterodine.Experimental
BortezomibThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Fesoterodine can be decreased when it is combined with Bosentan.Approved, Investigational
Botulinum Toxin Type AFesoterodine may increase the anticholinergic activities of Botulinum Toxin Type A.Approved, Investigational
Botulinum Toxin Type BFesoterodine may increase the anticholinergic activities of Botulinum Toxin Type B.Approved
BrompheniramineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Brompheniramine.Approved
BuprenorphineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BupropionThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Bupropion.Approved
ButorphanolThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Butorphanol.Approved, Illicit, Vet Approved
CarbamazepineThe metabolism of Fesoterodine can be increased when combined with Carbamazepine.Approved, Investigational
CarbinoxamineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Carbinoxamine.Approved
CarfentanilThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Carfentanil.Illicit, Investigational, Vet Approved
CarteololThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Carteolol.Approved
CelecoxibThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Ceritinib.Approved
CerivastatinThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Cerivastatin.Withdrawn
ChloroquineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Chloroquine.Approved, Vet Approved
ChlorothiazideThe serum concentration of Chlorothiazide can be increased when it is combined with Fesoterodine.Approved, Vet Approved
ChlorphenamineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Chlorphenamine.Approved
ChlorphenoxamineThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Chlorphenoxamine.Withdrawn
ChlorpromazineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Chlorpromazine.Approved, Vet Approved
ChlorthalidoneThe serum concentration of Chlorthalidone can be increased when it is combined with Fesoterodine.Approved
CholecalciferolThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Cholecalciferol.Approved, Nutraceutical
CimetidineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Cimetidine.Approved
CimetropiumFesoterodine may increase the anticholinergic activities of Cimetropium.Experimental, Investigational
CinacalcetThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Cinacalcet.Approved
CisaprideThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Cisapride.Approved, Investigational, Withdrawn
CitalopramThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Citalopram.Approved
ClarithromycinThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Clarithromycin.Approved
ClemastineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Clemastine.Approved
ClobazamThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Clobazam.Approved, Illicit
ClomipramineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Clomipramine.Approved, Vet Approved
ClotrimazoleThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Clotrimazole.Approved, Vet Approved
ClozapineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Clozapine.Approved
CobicistatThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Cobicistat.Approved
CocaineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Cocaine.Approved, Illicit
CodeineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Codeine.Approved, Illicit
ConivaptanThe serum concentration of Fesoterodine can be increased when it is combined with Conivaptan.Approved, Investigational
CoumaphosThe therapeutic efficacy of Fesoterodine can be decreased when used in combination with Coumaphos.Vet Approved
CrizotinibThe metabolism of Fesoterodine can be decreased when combined with Crizotinib.Approved
CyclopenthiazideThe serum concentration of Cyclopenthiazide can be increased when it is combined with Fesoterodine.Experimental
CyclopentolateThe risk or severity of adverse effects can be increased when Cyclopentolate is combined with Fesoterodine.Approved
CyclosporineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Cyclosporine.Approved, Investigational, Vet Approved
Cyproterone acetateThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Cyproterone acetate.Approved, Investigational
DabrafenibThe serum concentration of Fesoterodine can be decreased when it is combined with Dabrafenib.Approved
DarifenacinThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Darifenacin.Approved, Investigational
DarunavirThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Darunavir.Approved
DasatinibThe serum concentration of Fesoterodine can be increased when it is combined with Dasatinib.Approved, Investigational
DecamethoniumThe therapeutic efficacy of Fesoterodine can be decreased when used in combination with Decamethonium.Approved
DeferasiroxThe serum concentration of Fesoterodine can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Delavirdine.Approved
DemecariumThe therapeutic efficacy of Fesoterodine can be decreased when used in combination with Demecarium.Approved
DeramciclaneThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Deramciclane.Investigational
DesipramineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Desipramine.Approved
DesloratadineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Desloratadine.Approved, Investigational
DexetimideThe risk or severity of adverse effects can be increased when Dexetimide is combined with Fesoterodine.Withdrawn
DexfenfluramineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Dexfenfluramine.Approved, Illicit, Investigational, Withdrawn
DexmedetomidineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Dexmedetomidine.Approved, Vet Approved
DexmethylphenidateThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Dexmethylphenidate.Approved
DextroamphetamineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Dextroamphetamine.Approved, Illicit
DextromethorphanThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Dextromethorphan.Approved
DextromoramideThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Dextromoramide.Experimental, Illicit
DextropropoxypheneThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Dextropropoxyphene.Approved, Illicit, Investigational, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Dezocine.Approved, Investigational
DiacereinThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Diacerein.Approved, Investigational
DichlorvosThe therapeutic efficacy of Fesoterodine can be decreased when used in combination with Dichlorvos.Vet Approved
DicyclomineThe risk or severity of adverse effects can be increased when Dicyclomine is combined with Fesoterodine.Approved
DihydrocodeineThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Dihydrocodeine.Approved, Illicit
DihydroergotamineThe metabolism of Fesoterodine can be decreased when combined with Dihydroergotamine.Approved
DihydroetorphineThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Dihydroetorphine.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Dihydromorphine.Experimental, Illicit
DiltiazemThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Diltiazem.Approved
Dimethyl sulfoxideThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Dimethyl sulfoxide.Approved, Vet Approved
DiphenhydramineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Diphenhydramine.Approved
DiphenoxylateThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Diphenoxylate.Approved, Illicit
DistigmineThe therapeutic efficacy of Fesoterodine can be decreased when used in combination with Distigmine.Experimental
DisulfiramThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Disulfiram.Approved
DolasetronThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Dolasetron.Approved
DonepezilThe therapeutic efficacy of Fesoterodine can be decreased when used in combination with Donepezil.Approved
DosulepinThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Dosulepin.Approved
DoxepinThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Doxepin.Approved
DoxorubicinThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Doxorubicin.Approved, Investigational
DoxycyclineThe metabolism of Fesoterodine can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DPDPEThe risk or severity of adverse effects can be increased when Fesoterodine is combined with DPDPE.Investigational
DronabinolFesoterodine may increase the tachycardic activities of Dronabinol.Approved, Illicit
DronedaroneThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Dronedarone.Approved
DuloxetineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Duloxetine.Approved
EchothiophateThe therapeutic efficacy of Fesoterodine can be decreased when used in combination with Echothiophate.Approved
EdrophoniumThe therapeutic efficacy of Fesoterodine can be decreased when used in combination with Edrophonium.Approved
EfavirenzThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Efavirenz.Approved, Investigational
EliglustatThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Eliglustat.Approved
EluxadolineFesoterodine may increase the constipating activities of Eluxadoline.Approved
EmeproniumThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Emepronium.Experimental
EnasidenibThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Enasidenib.Approved
EntacaponeThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Entacapone.Approved, Investigational
EnzalutamideThe serum concentration of Fesoterodine can be decreased when it is combined with Enzalutamide.Approved
EpinastineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Epinastine.Approved, Investigational
ErythromycinThe metabolism of Fesoterodine can be decreased when combined with Erythromycin.Approved, Vet Approved
EscitalopramThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Escitalopram.Approved, Investigational
EtanautineThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Etanautine.Experimental
EthanolEthanol may increase the central nervous system depressant (CNS depressant) activities of Fesoterodine.Approved
EthopropazineThe risk or severity of adverse effects can be increased when Ethopropazine is combined with Fesoterodine.Approved
EthylmorphineThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Ethylmorphine.Approved, Illicit
EtoricoxibThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Etoricoxib.Approved, Investigational
EtorphineThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Etorphine.Illicit, Vet Approved
EtybenzatropineThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Etybenzatropine.Experimental
FelodipineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Felodipine.Approved, Investigational
FenfluramineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Fenfluramine.Illicit, Investigational, Withdrawn
FentanylThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FenthionThe therapeutic efficacy of Fesoterodine can be decreased when used in combination with Fenthion.Vet Approved
FexofenadineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Fexofenadine.Approved
FlecainideThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Flecainide.Approved, Withdrawn
FluconazoleThe metabolism of Fesoterodine can be decreased when combined with Fluconazole.Approved
FluoxetineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Fluoxetine.Approved, Vet Approved
FluphenazineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Fluphenazine.Approved
FluvastatinThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Fluvastatin.Approved
FluvoxamineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Fesoterodine can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Fesoterodine can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Fesoterodine can be increased when combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Fesoterodine can be increased when it is combined with Fusidic Acid.Approved
GalantamineThe therapeutic efficacy of Fesoterodine can be decreased when used in combination with Galantamine.Approved
GallamineThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Gallamine.Experimental
Gallamine TriethiodideThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Fesoterodine.Approved
GefitinibThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Gefitinib.Approved, Investigational
Glucagon recombinantThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Glucagon recombinant.Approved
Glycerol PhenylbutyrateThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Glycerol Phenylbutyrate.Approved
GlycopyrroniumFesoterodine may increase the anticholinergic activities of Glycopyrronium.Approved, Investigational, Vet Approved
GranisetronThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Granisetron.Approved, Investigational
HalofantrineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Halofantrine.Approved
HaloperidolThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Haloperidol.Approved
HeroinThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Heroin.Approved, Illicit, Investigational
HexamethoniumThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Hexamethonium.Experimental
HistamineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Histamine.Approved, Investigational
HomatropineThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Homatropine.Approved
Huperzine AThe therapeutic efficacy of Fesoterodine can be decreased when used in combination with Huperzine A.Investigational
HydrochlorothiazideThe serum concentration of Hydrochlorothiazide can be increased when it is combined with Fesoterodine.Approved, Vet Approved
HydrocodoneThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Hydrocodone.Approved, Illicit
HydroflumethiazideThe serum concentration of Hydroflumethiazide can be increased when it is combined with Fesoterodine.Approved, Investigational
HydromorphoneThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Hydromorphone.Approved, Illicit
HydroxychloroquineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Hydroxychloroquine.Approved
HydroxyureaThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Hydroxyurea.Approved
HydroxyzineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Hydroxyzine.Approved
HyoscyamineThe risk or severity of adverse effects can be increased when Hyoscyamine is combined with Fesoterodine.Approved
IdarubicinThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Idarubicin.Approved
IdelalisibThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Idelalisib.Approved
ImatinibThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Imatinib.Approved
ImipramineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Imipramine.Approved
IndapamideThe serum concentration of Indapamide can be increased when it is combined with Fesoterodine.Approved
IndinavirThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Indinavir.Approved
indisulamThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with indisulam.Investigational
IpidacrineThe therapeutic efficacy of Fesoterodine can be decreased when used in combination with Ipidacrine.Experimental
Ipratropium bromideThe risk or severity of adverse effects can be increased when Ipratropium bromide is combined with Fesoterodine.Approved
IrbesartanThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Irbesartan.Approved, Investigational
IsavuconazoniumThe metabolism of Fesoterodine can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoflurophateThe therapeutic efficacy of Fesoterodine can be decreased when used in combination with Isoflurophate.Approved, Investigational, Withdrawn
IsoniazidThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Isoniazid.Approved
IsradipineThe metabolism of Fesoterodine can be decreased when combined with Isradipine.Approved
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Fesoterodine.Investigational
ItraconazoleThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Fesoterodine can be increased when it is combined with Ivacaftor.Approved
KetobemidoneThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Ketobemidone.Approved, Investigational
KetoconazoleThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Ketoconazole.Approved, Investigational
LabetalolThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Labetalol.Approved
LansoprazoleThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Lansoprazole.Approved, Investigational
LercanidipineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Lercanidipine.Approved, Investigational
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Levomethadyl Acetate.Approved, Investigational
LevorphanolThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Levorphanol.Approved
LevosalbutamolThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Levosalbutamol.Approved
LidocaineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Lidocaine.Approved, Vet Approved
LofentanilThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Lofentanil.Illicit
LomustineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Lomustine.Approved
LopinavirThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Lopinavir.Approved
LoratadineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Loratadine.Approved
LorcaserinThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Lorcaserin.Approved
LovastatinThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Fesoterodine can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Fesoterodine can be decreased when it is combined with Lumacaftor.Approved
LumefantrineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Lumefantrine.Approved
MalathionThe therapeutic efficacy of Fesoterodine can be decreased when used in combination with Malathion.Approved, Investigational
ManidipineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Manidipine.Approved, Investigational
MazaticolThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Mazaticol.Experimental
MecamylamineThe risk or severity of adverse effects can be increased when Mecamylamine is combined with Fesoterodine.Approved
MefloquineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Mefloquine.Approved
MemantineThe therapeutic efficacy of Fesoterodine can be decreased when used in combination with Memantine.Approved, Investigational
MeptazinolThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Meptazinol.Experimental
MepyramineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Mepyramine.Approved, Vet Approved
MethadoneThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Methadone.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Methadyl Acetate.Approved, Illicit
MethamphetamineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Methamphetamine.Approved, Illicit
Methanesulfonyl FluorideThe therapeutic efficacy of Fesoterodine can be decreased when used in combination with Methanesulfonyl Fluoride.Investigational
MethanthelineThe risk or severity of adverse effects can be increased when Methantheline is combined with Fesoterodine.Approved, Investigational
MethazolamideThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Methazolamide.Approved
MethimazoleThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Methimazole.Approved
MethotrimeprazineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Methotrimeprazine.Approved
MethoxsalenThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Methoxsalen.Approved
MethyclothiazideThe serum concentration of Methyclothiazide can be increased when it is combined with Fesoterodine.Approved
MethylnaltrexoneThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Methylnaltrexone.Approved
MethylphenidateThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Methylphenidate.Approved, Investigational
Methylscopolamine bromideThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Methylscopolamine bromide.Approved
MetixeneThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Metixene.Approved
MetoclopramideThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Metoclopramide.Approved, Investigational
MetolazoneThe serum concentration of Metolazone can be increased when it is combined with Fesoterodine.Approved
MetoprololThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Metoprolol.Approved, Investigational
MianserinThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Mianserin.Approved, Investigational
MibefradilThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Mibefradil.Investigational, Withdrawn
MiconazoleThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Miconazole.Approved, Investigational, Vet Approved
MidodrineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Midodrine.Approved
MidostaurinThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Midostaurin.Approved
MifepristoneThe serum concentration of Fesoterodine can be increased when it is combined with Mifepristone.Approved, Investigational
MinaprineThe therapeutic efficacy of Fesoterodine can be decreased when used in combination with Minaprine.Approved
MirabegronThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Mirabegron.Approved
MirtazapineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Mirtazapine.Approved
MitotaneThe serum concentration of Fesoterodine can be decreased when it is combined with Mitotane.Approved
MoclobemideThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Moclobemide.Approved
MorphineThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Morphine.Approved, Investigational
NabiloneFesoterodine may increase the tachycardic activities of Nabilone.Approved, Investigational
NalbuphineThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Nalbuphine.Approved
NaloxegolThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Naloxegol.Approved
NefazodoneThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Nelfinavir.Approved
NeostigmineThe therapeutic efficacy of Fesoterodine can be decreased when used in combination with Neostigmine.Approved, Vet Approved
NetupitantThe serum concentration of Fesoterodine can be increased when it is combined with Netupitant.Approved
NevirapineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Nevirapine.Approved
NiacinThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Niacin.Approved, Investigational, Nutraceutical
NicardipineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Nicardipine.Approved
NicomorphineThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Nicomorphine.Experimental
NicotinamideThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Nicotinamide.Approved
NifedipineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Nifedipine.Approved
NilotinibThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Nilotinib.Approved, Investigational
NormethadoneThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Normethadone.Approved, Illicit
NortriptylineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Nortriptyline.Approved
OlanzapineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Olanzapine.Approved, Investigational
OlaparibThe metabolism of Fesoterodine can be decreased when combined with Olaparib.Approved
OmeprazoleThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Omeprazole.Approved, Investigational, Vet Approved
OndansetronThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Ondansetron.Approved
OpiumThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Opium.Approved, Illicit
OrphenadrineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Fesoterodine.Approved
OsimertinibThe serum concentration of Fesoterodine can be increased when it is combined with Osimertinib.Approved
OspemifeneThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Ospemifene.Approved
OtiloniumThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Otilonium.Experimental, Investigational
OxamniquineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Oxamniquine.Approved
OxitropiumThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Oxitropium.Investigational
OxprenololThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Oxprenolol.Approved
OxybutyninThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Oxybutynin.Approved, Investigational
OxycodoneThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Oxycodone.Approved, Illicit, Investigational
OxymetholoneThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Oxymetholone.Approved, Illicit
OxymorphoneThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Oxymorphone.Approved, Investigational, Vet Approved
OxyphenoniumThe risk or severity of adverse effects can be increased when Oxyphenonium is combined with Fesoterodine.Approved
PalbociclibThe serum concentration of Fesoterodine can be increased when it is combined with Palbociclib.Approved
PancuroniumThe risk or severity of adverse effects can be increased when Pancuronium is combined with Fesoterodine.Approved
PanobinostatThe serum concentration of Fesoterodine can be increased when it is combined with Panobinostat.Approved, Investigational
ParaoxonThe therapeutic efficacy of Fesoterodine can be decreased when used in combination with Paraoxon.Experimental
ParoxetineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Paroxetine.Approved, Investigational
PazopanibThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Pazopanib.Approved
Peginterferon alfa-2bThe serum concentration of Fesoterodine can be decreased when it is combined with Peginterferon alfa-2b.Approved
PentamidineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Pentamidine.Approved
PentazocineThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Pentazocine.Approved, Vet Approved
PentobarbitalThe metabolism of Fesoterodine can be increased when combined with Pentobarbital.Approved, Vet Approved
PentoliniumThe risk or severity of adverse effects can be increased when Pentolinium is combined with Fesoterodine.Approved
PergolideThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Pergolide.Approved, Investigational, Vet Approved, Withdrawn
PerhexilineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Perhexiline.Approved, Investigational
PerphenazineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Perphenazine.Approved
PethidineThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Pethidine.Approved
PhenazocineThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Phenazocine.Experimental
PhenglutarimideThe risk or severity of adverse effects can be increased when Phenglutarimide is combined with Fesoterodine.Experimental
PhenobarbitalThe metabolism of Fesoterodine can be increased when combined with Phenobarbital.Approved
PhenoperidineThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Phenoperidine.Experimental
PhentermineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Phentermine.Approved, Illicit
Phenylbutyric acidThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Phenylbutyric acid.Approved, Investigational
PhenytoinThe metabolism of Fesoterodine can be increased when combined with Phenytoin.Approved, Vet Approved
PhysostigmineThe therapeutic efficacy of Fesoterodine can be decreased when used in combination with Physostigmine.Approved
PimozideThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Pimozide.Approved
PindololThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Pindolol.Approved
PioglitazoneThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Pioglitazone.Approved, Investigational
PipecuroniumThe risk or severity of adverse effects can be increased when Pipecuronium is combined with Fesoterodine.Approved
PipotiazineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Pipotiazine.Approved, Investigational
PirenzepineThe risk or severity of adverse effects can be increased when Pirenzepine is combined with Fesoterodine.Approved
PiritramideThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Piritramide.Investigational
PolythiazideThe serum concentration of Polythiazide can be increased when it is combined with Fesoterodine.Approved
PosaconazoleThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Posaconazole.Approved, Investigational, Vet Approved
Potassium ChlorideFesoterodine may increase the ulcerogenic activities of Potassium Chloride.Approved, Withdrawn
PramlintidePramlintide may increase the anticholinergic activities of Fesoterodine.Approved, Investigational
PravastatinThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Pravastatin.Approved
PraziquantelThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Praziquantel.Approved, Vet Approved
PrimaquineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Primaquine.Approved
PrimidoneThe metabolism of Fesoterodine can be increased when combined with Primidone.Approved, Vet Approved
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Fesoterodine.Approved
ProguanilThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Proguanil.Approved
PromazineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Promazine.Approved, Vet Approved
PromethazineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Promethazine.Approved
PropafenoneThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Propafenone.Approved
PropanthelineThe risk or severity of adverse effects can be increased when Propantheline is combined with Fesoterodine.Approved
PropiverineThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Propiverine.Approved, Investigational
PropofolThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Propofol.Approved, Investigational, Vet Approved
Propoxyphene napsylateThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Propoxyphene napsylate.Approved
PropranololThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Propranolol.Approved, Investigational
PyridostigmineThe therapeutic efficacy of Fesoterodine can be decreased when used in combination with Pyridostigmine.Approved
PyrimethamineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Pyrimethamine.Approved, Vet Approved
QuetiapineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Quetiapine.Approved
QuinethazoneThe serum concentration of Quinethazone can be increased when it is combined with Fesoterodine.Approved
QuinidineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Quinidine.Approved
QuinineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Quinine.Approved
RabeprazoleThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Rabeprazole.Approved, Investigational
RamosetronFesoterodine may increase the constipating activities of Ramosetron.Approved, Investigational
RanitidineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Ranitidine.Approved
RanolazineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Ranolazine.Approved, Investigational
ReboxetineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Reboxetine.Approved, Investigational
RemifentanilThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Remifentanil.Approved
RheinThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Rhein.Experimental
RifabutinThe metabolism of Fesoterodine can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Fesoterodine can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Fesoterodine can be increased when combined with Rifapentine.Approved
RisperidoneThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Risperidone.Approved, Investigational
RitonavirThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Ritonavir.Approved, Investigational
RivastigmineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Rivastigmine.Approved, Investigational
RolapitantThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Rolapitant.Approved
RopiniroleThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Ropinirole.Approved, Investigational
RosiglitazoneThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Rosiglitazone.Approved, Investigational
RotigotineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Rotigotine.Approved
RutinThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Rutin.Experimental, Investigational
SaquinavirThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Saquinavir.Approved, Investigational
ScopolamineThe risk or severity of adverse effects can be increased when Scopolamine is combined with Fesoterodine.Approved
Scopolamine butylbromideThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Scopolamine butylbromide.Approved, Vet Approved
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Fesoterodine.Approved, Investigational
SelegilineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Selegiline.Approved, Investigational, Vet Approved
SertralineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Sertraline.Approved
SildenafilThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Fesoterodine can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Fesoterodine can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Simvastatin.Approved
SolifenacinThe risk or severity of adverse effects can be increased when Solifenacin is combined with Fesoterodine.Approved
SorafenibThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Sorafenib.Approved, Investigational
SparteineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Sparteine.Experimental
St. John's WortThe serum concentration of Fesoterodine can be decreased when it is combined with St. John's Wort.Investigational, Nutraceutical
StiripentolThe serum concentration of Fesoterodine can be increased when it is combined with Stiripentol.Approved
SufentanilThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Sufentanil.Approved, Investigational
SulconazoleThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Sulconazole.Approved
SulfanilamideThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Sulfanilamide.Approved
SulfaphenazoleThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Sulfaphenazole.Approved
SulfisoxazoleThe metabolism of Fesoterodine can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulpirideThe therapeutic efficacy of Sulpiride can be decreased when used in combination with Fesoterodine.Approved, Investigational
TacrineThe therapeutic efficacy of Fesoterodine can be decreased when used in combination with Tacrine.Investigational, Withdrawn
TamoxifenThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Tamoxifen.Approved
TapentadolThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Tapentadol.Approved
TegaserodThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Tegaserod.Investigational, Withdrawn
TelaprevirThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Telaprevir.Approved, Withdrawn
TelithromycinThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Telithromycin.Approved
TemsirolimusThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Temsirolimus.Approved
TerbinafineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Terbinafine.Approved, Investigational, Vet Approved
TerfenadineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Terfenadine.Withdrawn
ThioridazineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Thioridazine.Approved, Withdrawn
ThiothixeneThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Thiothixene.Approved
TicagrelorThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Ticagrelor.Approved
TiclopidineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Ticlopidine.Approved
TilidineThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Tilidine.Experimental
TimololThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Timolol.Approved
TioconazoleThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Tioconazole.Approved
TiotropiumFesoterodine may increase the anticholinergic activities of Tiotropium.Approved
TipranavirThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Tipranavir.Approved, Investigational
TocilizumabThe serum concentration of Fesoterodine can be decreased when it is combined with Tocilizumab.Approved
TolterodineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Fesoterodine.Approved, Investigational
TopiramateThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Topiramate.Approved
TramadolThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Tramadol.Approved, Investigational
TranylcypromineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Tranylcypromine.Approved
TrichlorfonThe therapeutic efficacy of Fesoterodine can be decreased when used in combination with Trichlorfon.Vet Approved
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Fesoterodine.Approved, Vet Approved
TrihexyphenidylThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Fesoterodine.Approved
TrimethaphanThe risk or severity of adverse effects can be increased when Trimethaphan is combined with Fesoterodine.Approved, Investigational
TripelennamineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Tripelennamine.Approved, Vet Approved
TriprolidineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Triprolidine.Approved
TropatepineThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Tropatepine.Experimental
TropicamideThe risk or severity of adverse effects can be increased when Tropicamide is combined with Fesoterodine.Approved
TrospiumThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Trospium.Approved
TubocurarineThe risk or severity of adverse effects can be increased when Tubocurarine is combined with Fesoterodine.Approved
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Fesoterodine.Approved
VecuroniumThe risk or severity of adverse effects can be increased when Vecuronium is combined with Fesoterodine.Approved
VemurafenibThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Vemurafenib.Approved
VenlafaxineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Venlafaxine.Approved
VerapamilThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Verapamil.Approved
VernakalantThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Vernakalant.Approved, Investigational
VilazodoneThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Vilazodone.Approved
VinblastineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Vinblastine.Approved
VinorelbineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Vinorelbine.Approved, Investigational
VoriconazoleThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Voriconazole.Approved, Investigational
YohimbineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Yohimbine.Approved, Vet Approved
ZafirlukastThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Zafirlukast.Approved, Investigational
ZiprasidoneThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Ziprasidone.Approved
ZucapsaicinThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Zucapsaicin.Approved
Food Interactions
  • Take with or without food.

References

Synthesis Reference

Claus Meese, "CHIRAL INTERMEDIATE, PROCESS FOR PRODUCING THE SAME AND ITS USE IN THE MANUFACTURE OF TOLTERODINE, FESOTERODINE, OR THE ACTIVE METABOLITE THEREOF." U.S. Patent US20090192224, issued July 30, 2009.

US20090192224
General References
  1. Malhotra B, Dickins M, Alvey C, Jumadilova Z, Li X, Duczynski G, Gandelman K: Effects of the moderate CYP3A4 inhibitor, fluconazole, on the pharmacokinetics of fesoterodine in healthy subjects. Br J Clin Pharmacol. 2011 Aug;72(2):263-9. doi: 10.1111/j.1365-2125.2011.04007.x. [PubMed:21545485]
  2. Malhotra B, Gandelman K, Sachse R, Wood N, Michel MC: The design and development of fesoterodine as a prodrug of 5-hydroxymethyl tolterodine (5-HMT), the active metabolite of tolterodine. Curr Med Chem. 2009;16(33):4481-9. [PubMed:19835561]
External Links
Human Metabolome Database
HMDB15648
KEGG Drug
D07226
PubChem Compound
6918558
PubChem Substance
99443256
ChemSpider
5293755
ChEBI
135920
ChEMBL
CHEMBL1201764
PharmGKB
PA165958376
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Fesoterodine
ATC Codes
G04BD11 — Fesoterodine
AHFS Codes
  • 86:12.04 — Antimuscarinics
FDA label
Download (430 KB)
MSDS
Download (102 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableHealthy Volunteers1
1CompletedNot AvailableOveractive Bladder1
1CompletedNot AvailableOveractive Bladder (OAB) With Symptoms of Frequency, Urgency, and Urgency1
1CompletedNot AvailableTreatment of Overactive Bladder2
1CompletedBasic ScienceHealthy Volunteers1
1CompletedBasic ScienceUrinary Bladder, Overactive1
1CompletedTreatmentFood / Therapeutic Equivalency1
1CompletedTreatmentHealthy Volunteers1
1CompletedTreatmentOveractive Bladder With Symptoms of Frequency, Urgency, and Urge Urinary Incontinence1
1TerminatedTreatmentHealthy Volunteers1
2CompletedTreatmentNeurogenic Detrusor Overactivity / Overactive Bladder1
2CompletedTreatmentOveractive Bladder1
2CompletedTreatmentStress Urinary Incontinence (SUI)1
2RecruitingOtherMild Cognitive Impairment (MCI) / Overactive Bladder1
2RecruitingTreatmentAutonomic Dysreflexia1
2, 3TerminatedTreatmentNocturia1
3Active Not RecruitingTreatmentUrge Urinary Incontinence1
3CompletedTreatmentOveractive Bladder5
3CompletedTreatmentOveractive Bladder Syndrome1
3Enrolling by InvitationTreatmentOveractive Bladder1
3RecruitingTreatmentOveractive Bladder1
4Active Not RecruitingTreatmentAdenocarcinoma, Prostate1
4CompletedNot AvailableOveractive Bladder / Urinary Incontinence (UI)1
4CompletedTreatmentOveractive Bladder4
4CompletedTreatmentOveractive Bladder / Urge Urinary Incontinence1
4CompletedTreatmentUrinary Bladder, Overactive4
4RecruitingTreatmentOveractive Bladder1
4RecruitingTreatmentParkinson's Disease (PD) / Urinary Bladder, Overactive1
4TerminatedTreatmentOveractive Bladder1
4Unknown StatusTreatmentBladder Outlet Obstruction1
Not AvailableCompletedNot AvailableOveractive Bladder4
Not AvailableCompletedNot AvailableOveractive Bladder (OAB)1
Not AvailableCompletedNot AvailableOveractive Bladder / Urinary Bladder Diseases / Urinary Bladder Overactive / Urologic Diseases1
Not AvailableUnknown StatusNot AvailableOveractive Bladder1
Not AvailableUnknown StatusTreatmentUrinary Bladder, Overactive1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Tablet, extended releaseOral4 mg
Tablet, extended releaseOral8 mg
Tablet, film coated, extended releaseOral4 mg/1
Tablet, film coated, extended releaseOral8 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6858650No2002-07-032022-07-03Us
US7384980No1999-05-112019-05-11Us
US7807715No2007-06-072027-06-07Us
US7855230No1999-05-112019-05-11Us
US7985772No1999-05-112019-05-11Us
US8088398No2007-06-072027-06-07Us
US8338478No1999-05-112019-05-11Us
US8501723No2007-06-072027-06-07Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilityHighly soluble MSDS
Predicted Properties
PropertyValueSource
Water Solubility0.00205 mg/mLALOGPS
logP5.45ALOGPS
logP5.7ChemAxon
logS-5.3ALOGPS
pKa (Strongest Acidic)14.98ChemAxon
pKa (Strongest Basic)10.64ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area49.77 Å2ChemAxon
Rotatable Bond Count11ChemAxon
Refractivity124.08 m3·mol-1ChemAxon
Polarizability48.29 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9535
Blood Brain Barrier+0.5648
Caco-2 permeable+0.7699
P-glycoprotein substrateSubstrate0.5268
P-glycoprotein inhibitor INon-inhibitor0.5556
P-glycoprotein inhibitor IINon-inhibitor0.625
Renal organic cation transporterInhibitor0.6025
CYP450 2C9 substrateNon-substrate0.6853
CYP450 2D6 substrateNon-substrate0.5151
CYP450 3A4 substrateSubstrate0.5939
CYP450 1A2 substrateInhibitor0.6306
CYP450 2C9 inhibitorNon-inhibitor0.7227
CYP450 2D6 inhibitorInhibitor0.6255
CYP450 2C19 inhibitorNon-inhibitor0.7334
CYP450 3A4 inhibitorNon-inhibitor0.5718
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6144
Ames testNon AMES toxic0.646
CarcinogenicityNon-carcinogens0.7213
BiodegradationNot ready biodegradable0.9385
Rat acute toxicity2.4003 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9196
hERG inhibition (predictor II)Inhibitor0.5602
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as diphenylmethanes. These are compounds containing a diphenylmethane moiety, which consists of a methane wherein two hydrogen atoms are replaced by two phenyl groups.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Diphenylmethanes
Direct Parent
Diphenylmethanes
Alternative Parents
Phenol esters / Phenoxy compounds / Benzyl alcohols / Aralkylamines / Trialkylamines / Carboxylic acid esters / Amino acids and derivatives / Monocarboxylic acids and derivatives / Primary alcohols / Organopnictogen compounds
show 4 more
Substituents
Diphenylmethane / Phenol ester / Phenoxy compound / Benzyl alcohol / Aralkylamine / Amino acid or derivatives / Carboxylic acid ester / Tertiary amine / Tertiary aliphatic amine / Carboxylic acid derivative
show 14 more
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
Not Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Receptor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM3
Uniprot ID
P20309
Uniprot Name
Muscarinic acetylcholine receptor M3
Molecular Weight
66127.445 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  2. Nilvebrant L: Tolterodine and its active 5-hydroxymethyl metabolite: pure muscarinic receptor antagonists. Pharmacol Toxicol. 2002 May;90(5):260-7. [PubMed:12076307]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Guanyl-nucleotide exchange factor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM4
Uniprot ID
P08173
Uniprot Name
Muscarinic acetylcholine receptor M4
Molecular Weight
53048.65 Da
References
  1. Mansfield KJ, Chandran JJ, Vaux KJ, Millard RJ, Christopoulos A, Mitchelson FJ, Burcher E: Comparison of receptor binding characteristics of commonly used muscarinic antagonists in human bladder detrusor and mucosa. J Pharmacol Exp Ther. 2009 Mar;328(3):893-9. doi: 10.1124/jpet.108.145508. Epub 2008 Nov 24. [PubMed:19029429]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Phosphatidylinositol phospholipase c activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM1
Uniprot ID
P11229
Uniprot Name
Muscarinic acetylcholine receptor M1
Molecular Weight
51420.375 Da
References
  1. Nilvebrant L: Tolterodine and its active 5-hydroxymethyl metabolite: pure muscarinic receptor antagonists. Pharmacol Toxicol. 2002 May;90(5):260-7. [PubMed:12076307]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
G-protein coupled acetylcholine receptor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM2
Uniprot ID
P08172
Uniprot Name
Muscarinic acetylcholine receptor M2
Molecular Weight
51714.605 Da
References
  1. Mansfield KJ, Chandran JJ, Vaux KJ, Millard RJ, Christopoulos A, Mitchelson FJ, Burcher E: Comparison of receptor binding characteristics of commonly used muscarinic antagonists in human bladder detrusor and mucosa. J Pharmacol Exp Ther. 2009 Mar;328(3):893-9. doi: 10.1124/jpet.108.145508. Epub 2008 Nov 24. [PubMed:19029429]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Phosphatidylinositol phospholipase c activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM5
Uniprot ID
P08912
Uniprot Name
Muscarinic acetylcholine receptor M5
Molecular Weight
60073.205 Da
References
  1. Mansfield KJ, Chandran JJ, Vaux KJ, Millard RJ, Christopoulos A, Mitchelson FJ, Burcher E: Comparison of receptor binding characteristics of commonly used muscarinic antagonists in human bladder detrusor and mucosa. J Pharmacol Exp Ther. 2009 Mar;328(3):893-9. doi: 10.1124/jpet.108.145508. Epub 2008 Nov 24. [PubMed:19029429]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Malhotra B, Guan Z, Wood N, Gandelman K: Pharmacokinetic profile of fesoterodine. Int J Clin Pharmacol Ther. 2008 Nov;46(11):556-63. [PubMed:19000553]
  2. Malhotra B, Dickins M, Alvey C, Jumadilova Z, Li X, Duczynski G, Gandelman K: Effects of the moderate CYP3A4 inhibitor, fluconazole, on the pharmacokinetics of fesoterodine in healthy subjects. Br J Clin Pharmacol. 2011 Aug;72(2):263-9. doi: 10.1111/j.1365-2125.2011.04007.x. [PubMed:21545485]
  3. Malhotra B, Sachse R, Wood N: Evaluation of drug-drug interactions with fesoterodine. Eur J Clin Pharmacol. 2009 Jun;65(6):551-60. doi: 10.1007/s00228-009-0648-1. Epub 2009 Apr 4. [PubMed:19347334]
  4. Malhotra BK, Wood N, Sachse R: Influence of age, gender, and race on pharmacokinetics, pharmacodynamics, and safety of fesoterodine. Int J Clin Pharmacol Ther. 2009 Sep;47(9):570-8. [PubMed:19761716]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Malhotra B, Guan Z, Wood N, Gandelman K: Pharmacokinetic profile of fesoterodine. Int J Clin Pharmacol Ther. 2008 Nov;46(11):556-63. [PubMed:19000553]
  2. Malhotra B, Dickins M, Alvey C, Jumadilova Z, Li X, Duczynski G, Gandelman K: Effects of the moderate CYP3A4 inhibitor, fluconazole, on the pharmacokinetics of fesoterodine in healthy subjects. Br J Clin Pharmacol. 2011 Aug;72(2):263-9. doi: 10.1111/j.1365-2125.2011.04007.x. [PubMed:21545485]
  3. Malhotra B, Sachse R, Wood N: Evaluation of drug-drug interactions with fesoterodine. Eur J Clin Pharmacol. 2009 Jun;65(6):551-60. doi: 10.1007/s00228-009-0648-1. Epub 2009 Apr 4. [PubMed:19347334]
  4. Malhotra BK, Wood N, Sachse R: Influence of age, gender, and race on pharmacokinetics, pharmacodynamics, and safety of fesoterodine. Int J Clin Pharmacol Ther. 2009 Sep;47(9):570-8. [PubMed:19761716]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Chancellor MB, Staskin DR, Kay GG, Sandage BW, Oefelein MG, Tsao JW: Blood-brain barrier permeation and efflux exclusion of anticholinergics used in the treatment of overactive bladder. Drugs Aging. 2012 Apr 1;29(4):259-73. doi: 10.2165/11597530-000000000-00000. [PubMed:22390261]

Drug created on May 06, 2010 10:47 / Updated on November 19, 2017 20:34