Fesoterodine

Identification

Summary

Fesoterodine is an antimuscarinic agent used in the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency.

Brand Names
Toviaz
Generic Name
Fesoterodine
DrugBank Accession Number
DB06702
Background

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

Type
Small Molecule
Groups
Approved
Structure
Weight
Average: 411.5769
Monoisotopic: 411.277344055
Chemical Formula
C26H37NO3
Synonyms
  • FESO
  • Fesoterodina
  • Fesoterodine

Pharmacology

Indication

Fesoterodine is indicated for the treatment of overactive bladder in adult patients with symptoms of urge urinary incontinence, urgency, and frequency.3 It is also indicated in the treatment of neurogenic detrusor overactivity in pediatric patients ≥6 years old weighing >25 kg.3

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Treatment ofNeurogenic detrusor overactivity••••••••••••••••••••••••••• •••• •••• •• ••••••••• •••••••• •••••••
Symptomatic treatment ofOveractive bladder syndrome (oabs)•••••••••••••••••••••••• •••••••• •••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

In-vivo the fesoteridine prodrug 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
Humans
UMuscarinic acetylcholine receptor M4
antagonist
Humans
UMuscarinic acetylcholine receptor M1
antagonist
Humans
UMuscarinic acetylcholine receptor M2
antagonist
Humans
UMuscarinic acetylcholine receptor M5
antagonist
Humans
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.

Adverse Effects
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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

Pathways
Not Available
Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
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 Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbacavirAbacavir may decrease the excretion rate of Fesoterodine which could result in a higher serum level.
AbametapirThe serum concentration of Fesoterodine can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Fesoterodine can be increased when combined with Abatacept.
AbirateroneThe metabolism of Fesoterodine can be decreased when combined with Abiraterone.
AcebutololThe metabolism of Fesoterodine can be decreased when combined with Acebutolol.
Food Interactions
  • Take with or without food.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Fesoterodine fumarateEOS72165S7286930-03-8MWHXMIASLKXGBU-RNCYCKTQSA-N
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
ToviazTablet, extended release8 mgOralPfizer Europe Ma Eeig2016-09-08Not applicableEU flag
ToviazTablet, film coated, extended release4 mg/1OralPfizer Laboratories Div Pfizer Inc2008-10-31Not applicableUS flag
ToviazTablet, extended release4 mgOralPfizer Europe Ma Eeig2016-09-08Not applicableEU flag
ToviazTablet, film coated, extended release8 mg/1OralAvera McKennan Hospital2015-06-10Not applicableUS flag
ToviazTablet, extended release8 mgOralPfizer Europe Ma Eeig2016-09-08Not applicableEU flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Ach-fesoterodineTablet, extended release8 mgOralAccord Healthcare IncNot applicableNot applicableCanada flag
Ach-fesoterodineTablet, extended release4 mgOralAccord Healthcare IncNot applicableNot applicableCanada flag
Apo-fesoterodineTablet, extended release8 mgOralApotex CorporationNot applicableNot applicableCanada flag
Apo-fesoterodineTablet, extended release4 mgOralApotex CorporationNot applicableNot applicableCanada flag
Fesoterodine FumarateTablet, extended release4 mg/1OralAmneal Pharmaceuticals LLC2023-01-06Not applicableUS flag

Categories

ATC Codes
G04BD11 — Fesoterodine
Drug Categories
Chemical TaxonomyProvided by Classyfire
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
Alcohol / Amine / Amino acid or derivatives / Aralkylamine / Aromatic alcohol / Aromatic homomonocyclic compound / Benzyl alcohol / Carbonyl group / Carboxylic acid derivative / Carboxylic acid ester
show 14 more
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
Not Available
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
621G617227
CAS number
286930-02-7
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

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. [Article]
  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. [Article]
  3. FDA Approved Drug Products: TOVIAZ (fesoterodine fumarate) extended-release tablets [Link]
Human Metabolome Database
HMDB0015648
KEGG Drug
D07226
PubChem Compound
6918558
PubChem Substance
99443256
ChemSpider
5293755
RxNav
797195
ChEBI
135920
ChEMBL
CHEMBL1201764
ZINC
ZINC000001552908
PharmGKB
PA165958376
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Fesoterodine
FDA label
Download (430 KB)
MSDS
Download (102 KB)

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
PhaseStatusPurposeConditionsCount
4CompletedTreatmentAdenocarcinoma of Prostate1
4CompletedTreatmentBladder Outlet Obstruction1
4CompletedTreatmentOveractive Bladder Syndrome (OABS)9
4CompletedTreatmentOveractive Bladder Syndrome (OABS) / Urinary Urge Incontinence1
4CompletedTreatmentUrinary Incontinence (UI) / Urinary Urgency1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Tablet, extended releaseOral4 mg/1
Tablet, extended releaseOral8 mg/1
Tablet, film coated, extended releaseOral4 mg
Tablet, film coated, extended releaseOral8 mg
Tablet, extended releaseOral
Tablet, film coated, extended releaseOral4 mg/1
Tablet, film coated, extended releaseOral8 mg/1
Tablet, extended releaseOral4 mg
Tablet, film coated, extended releaseOral
Tablet, extended releaseOral8 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US6858650Yes2005-02-222023-01-03US flag
US7384980No2008-06-102019-05-11US flag
US7807715Yes2010-10-052027-12-07US flag
US7855230No2010-12-212019-05-11US flag
US7985772No2011-07-262019-05-11US flag
US8088398Yes2012-01-032027-12-07US flag
US8338478No2012-12-252019-05-11US flag
US8501723Yes2013-08-062027-12-07US flag

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-MSsplash10-03k9-8779000000-2e606385c85d52b6ad73
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-0006-9114200000-faac50e33136b7b4e9fc
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-03di-4000900000-43a471a8e77287c238f5
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-0006-9315000000-4965bc7ae400398e7a26
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-01p9-9202300000-db69989cdbade9effe1a
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-0296-6493000000-a8dbdc2c25ee7637c7da
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-0079-9025000000-f07b5c4b45c2af0ad87a
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-216.9453037
predicted
DarkChem Lite v0.1.0
[M-H]-218.1316037
predicted
DarkChem Lite v0.1.0
[M-H]-203.6327
predicted
DeepCCS 1.0 (2019)
[M+H]+217.3607037
predicted
DarkChem Lite v0.1.0
[M+H]+218.4201037
predicted
DarkChem Lite v0.1.0
[M+H]+206.02827
predicted
DeepCCS 1.0 (2019)
[M+Na]+216.4638037
predicted
DarkChem Lite v0.1.0
[M+Na]+218.1647037
predicted
DarkChem Lite v0.1.0
[M+Na]+211.94078
predicted
DeepCCS 1.0 (2019)

Targets

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Use our structured and evidence-based datasets to unlock new
insights and accelerate drug research.
Learn more
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
Learn more
Kind
Protein
Organism
Humans
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. [Article]
  2. Nilvebrant L: Tolterodine and its active 5-hydroxymethyl metabolite: pure muscarinic receptor antagonists. Pharmacol Toxicol. 2002 May;90(5):260-7. [Article]
Kind
Protein
Organism
Humans
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. [Article]
Kind
Protein
Organism
Humans
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. [Article]
Kind
Protein
Organism
Humans
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. [Article]
Kind
Protein
Organism
Humans
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. [Article]

Enzymes

Kind
Protein
Organism
Humans
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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
Kind
Protein
Organism
Humans
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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]

Transporters

Kind
Protein
Organism
Humans
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. [Article]

Drug created at May 06, 2010 16:47 / Updated at February 20, 2024 23:55