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, film coated, extended release8 mg/1OralPfizer Laboratories Div Pfizer Inc.2008-10-31Not applicableUs
ToviazTablet, extended release4 mgOralPfizer Europe Ma Eeig2007-04-20Not applicableEu
ToviazTablet, extended release8 mgOralPfizer Europe Ma Eeig2007-04-20Not applicableEu
ToviazTablet, extended release4 mgOralPfizer2012-04-19Not applicableCanada
ToviazTablet, extended release8 mgOralPfizer Europe Ma Eeig2007-04-20Not applicableEu
ToviazTablet, film coated, extended release4 mg/1OralAvera McKennan Hospital2015-04-01Not applicableUs
ToviazTablet, film coated, extended release4 mg/1OralU.S. Pharmaceuticals2008-10-31Not applicableUs
ToviazTablet, extended release8 mgOralPfizer Europe Ma Eeig2007-04-20Not applicableEu
ToviazTablet, extended release8 mgOralPfizer Europe Ma Eeig2007-04-20Not applicableEu
ToviazTablet, extended release8 mgOralPfizer Europe Ma Eeig2007-04-20Not applicableEu
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Fesoterodine FumarateTablet, film coated, extended release8 mg/1OralZydus Pharmaceuticals Usa, Inc.2017-12-07Not applicableUs
Fesoterodine FumarateTablet, film coated, extended release4 mg/1OralCadila Pharnmaceuticals2017-12-07Not applicableUs
Fesoterodine FumarateTablet, film coated, extended release4 mg/1OralZydus Pharmaceuticals Usa, Inc.2017-12-07Not applicableUs
Fesoterodine FumarateTablet, film coated, extended release8 mg/1OralCadila Pharnmaceuticals2017-12-07Not applicableUs
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[C@H](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).

Associated Conditions
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
DrugInteraction
1,10-PhenanthrolineThe therapeutic efficacy of Fesoterodine can be decreased when used in combination with 1,10-Phenanthroline.
AbirateroneThe serum concentration of Fesoterodine can be increased when it is combined with Abiraterone.
AcetaminophenThe serum concentration of Fesoterodine can be increased when it is combined with Acetaminophen.
Acetyl sulfisoxazoleThe metabolism of Fesoterodine can be decreased when combined with Acetyl sulfisoxazole.
Acetylsalicylic acidAcetylsalicylic acid may decrease the excretion rate of Fesoterodine which could result in a higher serum level.
AclidiniumFesoterodine may increase the anticholinergic activities of Aclidinium.
AgmatineThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Agmatine.
AjmalineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Ajmaline.
AlbendazoleThe serum concentration of Fesoterodine can be increased when it is combined with Albendazole.
AlclometasoneThe metabolism of Alclometasone can be decreased when combined with Fesoterodine.
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
HMDB0015648
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
0WithdrawnDiagnosticBladder Dysfunction / Urinary Incontinence (UI)1
1CompletedNot AvailableHealthy Volunteers1
1CompletedNot AvailableOveractive Bladder (OAB) With Symptoms of Frequency, Urgency, and Urgency1
1CompletedNot AvailableTreatment of Overactive Bladder2
1CompletedNot AvailableUrinary Bladder, Overactive1
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 / Urinary Bladder, Overactive1
2CompletedTreatmentStress Urinary Incontinence (SUI)1
2CompletedTreatmentUrinary Bladder, Overactive1
2RecruitingOtherMild Cognitive Impairment (MCI) / Urinary Bladder, Overactive1
2RecruitingTreatmentAutonomic Dysreflexia1
2, 3TerminatedTreatmentNocturia1
3CompletedTreatmentUrge Urinary Incontinence1
3CompletedTreatmentUrinary Bladder, Overactive6
3Enrolling by InvitationTreatmentUrinary Bladder, Overactive1
3RecruitingTreatmentUrinary Bladder, Overactive1
4Active Not RecruitingTreatmentAdenocarcinoma, Prostate1
4CompletedNot AvailableUrinary Bladder, Overactive / Urinary Incontinence (UI)1
4CompletedTreatmentBladder Outlet Obstruction1
4CompletedTreatmentUrge Urinary Incontinence / Urinary Bladder, Overactive1
4CompletedTreatmentUrinary Bladder, Overactive8
4RecruitingTreatmentParkinson's Disease (PD) / Urinary Bladder, Overactive1
4RecruitingTreatmentUrinary Bladder, Overactive1
4TerminatedTreatmentUrinary Bladder, Overactive1
Not AvailableActive Not RecruitingNot AvailableUrinary Bladder, Overactive1
Not AvailableCompletedNot AvailableUrinary Bladder Diseases / Urinary Bladder, Overactive / Urologic Diseases1
Not AvailableCompletedNot AvailableUrinary Bladder, Overactive5
Not AvailableRecruitingNot AvailableUrinary Bladder, Overactive1
Not AvailableUnknown StatusNot AvailableUrinary Bladder, Overactive1
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 September 23, 2018 19:37