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Identification
NameFesoterodine
Accession NumberDB06702
TypeSmall Molecule
GroupsApproved
Description

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

Structure
Thumb
Synonyms
FESO
Fesoterodine
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Toviaztablet, film coated, extended release4 mg/1oralPfizer Laboratories Div Pfizer Inc2008-10-31Not applicableUs
Toviaztablet, film coated, extended release8 mg/1oralU.S. Pharmaceuticals2008-10-31Not applicableUs
Toviaztablet, film coated, extended release8 mg/1oralCardinal Health2008-10-31Not applicableUs
Toviaztablet, film coated, extended release4 mg/1oralCardinal Health2008-10-31Not applicableUs
Toviaztablet (extended-release)8 mgoralPfizer Canada Inc2012-04-19Not applicableCanada
Toviaztablet, film coated, extended release8 mg/1oralPhysicians Total Care, Inc.2010-09-15Not applicableUs
Toviaztablet (extended-release)4 mgoralPfizer Canada Inc2012-04-19Not applicableCanada
Toviaztablet, film coated, extended release4 mg/1oralPhysicians Total Care, Inc.2010-08-23Not applicableUs
Toviaztablet, film coated, extended release4 mg/1oralAvera Mc Kennan Hospital2015-04-01Not applicableUs
Toviaztablet, film coated, extended release8 mg/1oralPfizer Laboratories Div Pfizer Inc2008-10-31Not applicableUs
Toviaztablet, film coated, extended release4 mg/1oralU.S. Pharmaceuticals2008-10-31Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Fesoterodine fumarate
286930-03-8
Thumb
  • InChI Key: MWHXMIASLKXGBU-RNCYCKTQSA-N
  • Monoisotopic Mass: 527.288302671
  • Average Mass: 527.649
DBSALT000085
Categories
UNII621G617227
CAS number286930-02-7
WeightAverage: 411.5769
Monoisotopic: 411.277344055
Chemical FormulaC26H37NO3
InChI KeyInChIKey=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
Taxonomy
DescriptionThis 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.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassDiphenylmethanes
Direct ParentDiphenylmethanes
Alternative Parents
Substituents
  • Diphenylmethane
  • Phenylpropylamine
  • Phenol ester
  • Benzyl alcohol
  • Aralkylamine
  • Tertiary aliphatic amine
  • Tertiary amine
  • Carboxylic acid ester
  • Monocarboxylic acid or derivatives
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Aromatic alcohol
  • Primary alcohol
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Alcohol
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of overactive bladder (with symptoms of urinary frequency, urgency, or urge incontinence).
PharmacodynamicsFesoterodine 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 actionFesoterodine, 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.
Related Articles
AbsorptionTmax (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 binding5-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 eliminationRenal: 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 life7-8 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.

ToxicityRat, 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
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
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 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Tablet (extended-release)oral4 mg
Tablet (extended-release)oral8 mg
Tablet, film coated, extended releaseoral4 mg/1
Tablet, film coated, extended releaseoral8 mg/1
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6858650 No2002-07-032022-07-03Us
US7384980 No1999-05-112019-05-11Us
US7807715 No2007-06-072027-06-07Us
US7855230 No1999-05-112019-05-11Us
US7985772 No1999-05-112019-05-11Us
US8088398 No2007-06-072027-06-07Us
US8338478 No1999-05-112019-05-11Us
US8501723 No2007-06-072027-06-07Us
Properties
StateSolid
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 FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
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
ATC CodesG04BD11
AHFS Codes
  • 12:08.08
PDB EntriesNot Available
FDA labelDownload (430 KB)
MSDSDownload (102 KB)
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Abiraterone.
AclidiniumAclidinium may increase the anticholinergic activities of Fesoterodine.
AmiodaroneThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Amiodarone.
AprepitantThe serum concentration of Fesoterodine can be increased when it is combined with Aprepitant.
AtazanavirThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Atazanavir.
BexaroteneThe serum concentration of Fesoterodine can be decreased when it is combined with Bexarotene.
BoceprevirThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Boceprevir.
BosentanThe serum concentration of Fesoterodine can be decreased when it is combined with Bosentan.
Botulinum Toxin Type AFesoterodine may increase the anticholinergic activities of Botulinum Toxin Type A.
Botulinum Toxin Type BFesoterodine may increase the anticholinergic activities of Botulinum Toxin Type B.
BupropionThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Bupropion.
CelecoxibThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Celecoxib.
CeritinibThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Ceritinib.
ChloroquineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Chloroquine.
ChlorpromazineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Chlorpromazine.
CimetidineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Cimetidine.
Cimetropium BromideFesoterodine may increase the anticholinergic activities of Cimetropium Bromide.
CinacalcetThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Cinacalcet.
ClarithromycinThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Clarithromycin.
ClobazamThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Clobazam.
ClomipramineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Clomipramine.
ClozapineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Clozapine.
CobicistatThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Cobicistat.
CocaineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Cocaine.
ConivaptanThe serum concentration of Fesoterodine can be increased when it is combined with Conivaptan.
DabrafenibThe serum concentration of Fesoterodine can be decreased when it is combined with Dabrafenib.
DarifenacinThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Darifenacin.
DarunavirThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Darunavir.
DasatinibThe serum concentration of Fesoterodine can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Fesoterodine can be decreased when it is combined with Deferasirox.
DelavirdineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Delavirdine.
DesipramineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Desipramine.
DiphenhydramineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Diphenhydramine.
DronabinolFesoterodine may increase the tachycardic activities of Dronabinol.
DronedaroneThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Dronedarone.
DuloxetineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Duloxetine.
EliglustatThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Eliglustat.
EluxadolineFesoterodine may increase the activities of Eluxadoline.
EthanolEthanol may increase the central nervous system depressant (CNS depressant) activities of Fesoterodine.
FluconazoleThe metabolism of Fesoterodine can be decreased when combined with Fluconazole.
FluoxetineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Fluoxetine.
FluvoxamineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Fluvoxamine.
FosaprepitantThe serum concentration of Fesoterodine can be increased when it is combined with Fosaprepitant.
Fusidic AcidThe serum concentration of Fesoterodine can be increased when it is combined with Fusidic Acid.
Glucagon recombinantThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Glucagon recombinant.
HaloperidolThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Haloperidol.
IdelalisibThe serum concentration of Fesoterodine can be increased when it is combined with Idelalisib.
ImipramineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Imipramine.
IndinavirThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Indinavir.
Ipratropium bromideIpratropium bromide may increase the anticholinergic activities of Fesoterodine.
IsoniazidThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Isoniazid.
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Fesoterodine.
ItraconazoleThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Itraconazole.
IvacaftorThe serum concentration of Fesoterodine can be increased when it is combined with Ivacaftor.
KetoconazoleThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Ketoconazole.
LorcaserinThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Lorcaserin.
LuliconazoleThe serum concentration of Fesoterodine can be increased when it is combined with Luliconazole.
MethadoneThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Methadone.
MethotrimeprazineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Methotrimeprazine.
MianserinMianserin may increase the anticholinergic activities of Fesoterodine.
MifepristoneThe serum concentration of Fesoterodine can be increased when it is combined with Mifepristone.
MirabegronThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Mirabegron.
MitotaneThe serum concentration of Fesoterodine can be decreased when it is combined with Mitotane.
MorphineThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Morphine.
NefazodoneThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Nefazodone.
NelfinavirThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Nelfinavir.
NetupitantThe serum concentration of Fesoterodine can be increased when it is combined with Netupitant.
NicardipineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Nicardipine.
NilotinibThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Nilotinib.
PalbociclibThe serum concentration of Fesoterodine can be increased when it is combined with Palbociclib.
PanobinostatThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Panobinostat.
ParoxetineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Paroxetine.
PhenytoinThe metabolism of Fesoterodine can be increased when combined with Phenytoin.
PosaconazoleThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Posaconazole.
Potassium ChlorideFesoterodine may increase the ulcerogenic activities of Potassium Chloride.
PramlintidePramlintide may increase the anticholinergic activities of Fesoterodine.
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Fesoterodine.
PromazineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Promazine.
QuinidineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Quinidine.
QuinineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Quinine.
RamosetronFesoterodine may increase the activities of Ramosetron.
RitonavirThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Ritonavir.
RolapitantThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Rolapitant.
SaquinavirThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Saquinavir.
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Fesoterodine.
SertralineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Sertraline.
SiltuximabThe serum concentration of Fesoterodine can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Fesoterodine can be increased when it is combined with Simeprevir.
St. John's WortThe serum concentration of Fesoterodine can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Fesoterodine can be increased when it is combined with Stiripentol.
SulpirideThe therapeutic efficacy of Sulpiride can be decreased when used in combination with Fesoterodine.
TacrineThe therapeutic efficacy of Fesoterodine can be decreased when used in combination with Tacrine.
TelaprevirThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Telaprevir.
TelithromycinThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Telithromycin.
TerbinafineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Terbinafine.
ThioridazineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Thioridazine.
TiclopidineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Ticlopidine.
TiotropiumFesoterodine may increase the anticholinergic activities of Tiotropium.
TipranavirThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Tipranavir.
TocilizumabThe serum concentration of Fesoterodine can be decreased when it is combined with Tocilizumab.
TopiramateThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Topiramate.
TranylcypromineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Tranylcypromine.
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Fesoterodine.
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Fesoterodine.
VoriconazoleThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Voriconazole.
Food Interactions
  • Take with or without food.

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 action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM3
Uniprot ID:
P20309
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 action of G proteins. Primary transducing effect is inhibition of adenylate cyclase.
Gene Name:
CHRM4
Uniprot ID:
P08173
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 action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM1
Uniprot ID:
P11229
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 action of G proteins. Primary transducing effect is adenylate cyclase inhibition. Signaling promotes phospholipase C activity, leading to the release of inositol trisphosphate (IP3); this then trigge...
Gene Name:
CHRM2
Uniprot ID:
P08172
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 action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM5
Uniprot ID:
P08912
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
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 antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
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
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 ]
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Drug created on May 06, 2010 10:47 / Updated on July 25, 2016 01:54