Identification

Name
Ketotifen
Accession Number
DB00920
Description

Ketotifen is a benzocycloheptathiophene derivative3 with potent antihistaminic and mast cell stabilizing properties. It has a similar structure to some other first-generation antihistamines such as cyproheptadine and azatadine.3

Ketotifen was first developed in Switzerland in 1970 by Sandoz Pharmaceuticals and was initially marketed for the treatment of anaphylaxis.3 In the US, it is now used in an over-the-counter ophthalmic formulation for the treatment of itchy eyes associated with allergies,6 and in Canada a prescription-only oral formulation is available and indicated as an add-on therapy for children with atopic asthma.7 In addition, oral ketotifen is used in Mexico and across Europe for the treatment of various allergic symptoms and disorders,3 including urticaria, mastocytosis, and food allergy.

Type
Small Molecule
Groups
Approved
Structure
Thumb
Weight
Average: 309.425
Monoisotopic: 309.118734925
Chemical Formula
C19H19NOS
Synonyms
  • Ketotifen
  • Ketotifene
  • Ketotifeno
  • Ketotifenum

Pharmacology

Pharmacology
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Indication

Administered orally, ketotifen is indicated as an add-on medication in the chronic treatment of mild atopic asthma in children.7 It is also available as an over-the-counter ophthalmic solution which is indicated for the temporary prevention of itching of the eye due to allergic conjunctivitis.6

Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Ketotifen is a non-competitive histamine antagonist and mast cell stabilizer.6 Administered orally, it functions as a non-bronchodilator antiasthmatic drug by inhibiting the effects of endogenous substances known to be inflammatory mediators.7 While effects can take 6 to 12 weeks to become apparent,5 the use of ketotifen has been demonstrated to reduce the frequency, severity, and duration of asthma symptoms, and may allow for a reduction in the use of other asthma therapies.7

Mechanism of action

The precise mechanism(s) through which ketotifen exerts its therapeutic effects are unclear. Ketotifen is a potent and non-competitive antagonist of H1 histamine receptors, which is likely to be a significant contributor to its anti-allergic activity.7 In addition, ketotifen stabilizes mast cells and has demonstrated in vitro the ability to inhibit the release of allergic and inflammatory mediators such as histamine, leukotrienes C4 and D4 (i.e. SRS-A), and platelet-activating factor (PAF).7

Other in vivo observations thought to contribute to ketotifen's efficacy in asthma include the inhibition of various PAF-mediated processes (e.g. airway hyperreactivity, eosinophil and platelet accumulation in the airways), prevention of leukotriene-induced bronchoconstriction, and suppression of eosinophil priming.7

TargetActionsOrganism
AHistamine H1 receptor
antagonist
Humans
U6-phosphogluconate dehydrogenase, decarboxylating
inhibitor
Humans
Absorption

Following oral administration, absorption is relatively quick (with a Tmax of ~3 hours) and nearly complete as judged by plasma concentrations and urinary excretion levels - despite this, oral bioavailability is only ~50% due to a significant first-pass effect in the liver.7

Volume of distribution
Not Available
Protein binding

Ketotifen is 75% protein-bound in plasma, though the specific proteins to which it binds are unclear.7

Metabolism

Ketotifen is extensively metabolized in humans5 and three distinct metabolites have been detected in human urine. The main metabolite is the N-glucuronide, comprising roughly 50% of urinary drug product,5 with the N-demethylated nor-ketotifen and the 10-hydroxyl derivative comprising 2% and <1%, respectively.7 Nor-ketotifen appears to be equally as active as its parent drug,7 though the clinical relevance of this is unclear given the relatively small proportion in which nor-ketotifen is found in the plasma.

Formation of the N-glucuronide metabolite is carried out by several UGT enzymes, including UGT1A3, UGT1A4, and UGT2B10.2

Hover over products below to view reaction partners

Route of elimination

More than 60% of an administered dose is excreted in the urine, primarily as metabolites7 - of this material, <1% is found as unchanged drug, while the glucuronide and pharmacologically active nor-ketotifen metabolites account for 50% and 10%, respectively.5

Half-life

Ketotifen clearance is biphasic - the half-life of the distribution phase is approximately 3-5 hours and the half-life of the elimination phase is 22 hours.5

Clearance
Not Available
Adverse Effects
Medicalerrors
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Toxicity

Oral ingestion of up to 60x the recommended dose has been reported, although no fatal overdoses of ketotifen have been described.4 Symptoms of ketotifen overdosage may include significant sedation, confusion, disorientation, tachycardia, hypotension, convulsions, hyperexcitability (particularly in children), and/or reversible coma.7 If ingestion is recent, consider the use of gastric lavage or activated charcoal.7 Other treatments should be supportive and administered as necessary based on symptoms.

Physostigmine may be useful to mitigate anticholinergic effects, and short-acting barbiturates or benzodiazepines may be used if the patient presents with excitation or convulsions.7

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Ketotifen H1-Antihistamine ActionDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
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
AcarboseThe risk or severity of thrombocytopenia can be increased when Acarbose is combined with Ketotifen.
AcetohexamideThe risk or severity of thrombocytopenia can be increased when Acetohexamide is combined with Ketotifen.
AlogliptinThe risk or severity of thrombocytopenia can be increased when Alogliptin is combined with Ketotifen.
AmphetamineAmphetamine may decrease the sedative and stimulatory activities of Ketotifen.
BenzphetamineBenzphetamine may decrease the sedative and stimulatory activities of Ketotifen.
Benzylpenicilloyl polylysineKetotifen may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
BetahistineThe therapeutic efficacy of Betahistine can be decreased when used in combination with Ketotifen.
CanagliflozinThe risk or severity of thrombocytopenia can be increased when Canagliflozin is combined with Ketotifen.
ChlorpropamideThe risk or severity of thrombocytopenia can be increased when Chlorpropamide is combined with Ketotifen.
DapagliflozinThe risk or severity of thrombocytopenia can be increased when Dapagliflozin is combined with Ketotifen.
Interactions
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Food Interactions
  • Take with or without food. The co-administration of food does not significantly affect ketotifen disposition.

Products

Products
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Product Ingredients
IngredientUNIICASInChI Key
Ketotifen fumarateHBD503WORO34580-14-8YNQQEYBLVYAWNX-WLHGVMLRSA-N
International/Other Brands
Totifen (Patron) / Zasten (Novartis)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Ketotifen Ophthalmic SolutionSolutionOphthalmicSterimax Inc2013-03-07Not applicableCanada flag
ZaditenTabletOralTEVA Canada Limited1990-12-31Not applicableCanada flag
ZaditenSyrupOralTEVA Canada Limited1990-12-31Not applicableCanada flag
Zaditen - Dps 1mg/mlSolution / dropsOralNovartisNot applicableNot applicableCanada flag
ZaditorSolution0.25 mgOphthalmicLaboratoires Thea2000-08-01Not applicableCanada flag
ZaditorSolution0.345 mg/1mLOphthalmicNovartis Ophthalmics1999-07-022008-10-31US flag
ZaditorSolution0.25 mgOphthalmicNovartis2006-08-032012-01-17Canada flag
ZaditorSolution0.345 mg/1mLOphthalmicPhysicians Total Care, Inc.2002-11-042010-12-29US flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Apo-ketotifen - Syr 1mg/5mlSyrupOralApotex Corporation1996-11-072019-01-16Canada flag
Jamp-ketotifenSolutionOphthalmicJamp Pharma CorporationNot applicableNot applicableCanada flag
Novo-ketotifen - Syr 1mg/5mlSyrupOralNovopharm Limited1995-12-312015-10-26Canada flag
Novo-ketotifen Tab 1mgTabletOralNovopharm Limited1997-07-292013-02-11Canada flag
Nu-ketotifen Syrup - 1mg/5mlSyrupOralNu Pharm Inc1996-12-092012-09-04Canada flag
PMS-ketotifenSyrupOralPharmascience Inc1998-08-312013-02-07Canada flag
PMS-ketotifenTabletOralPharmascience Inc1998-08-312013-02-07Canada flag
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
AlawaySolution / drops0.25 mg/1mLOphthalmicBausch & Lomb Incorporated2006-12-01Not applicableUS flag
Alaway Preservative FreeSolution / drops0.35 mg/1mLOphthalmicBausch & Lomb Incorporated2020-09-24Not applicableUS flag
Allergy EyeSolution / drops0.25 mg/1mLOphthalmicCVS Health2011-01-072014-07-01US flag
Allergy EyeSolution / drops0.25 mg/1mLOphthalmicH.E.B.2010-09-152015-05-01US flag
Allergy Eye DropsSolution / drops0.35 mg/1mLOphthalmicH E B2014-02-25Not applicableUS flag
Allergy Eye DropsSolution / drops0.35 mg/1mLOphthalmicAdvanced Vision Research (Subsidiary of Akorn, Inc.)2013-11-14Not applicableUS flag
Allergy Eye DropsSolution / drops0.35 mg/1mLOphthalmicCardinal Health2014-01-132016-07-01US flag
Allergy Eye Original Prescription StrengthSolution / drops0.25 mg/1mLOphthalmicMeijer Distribution1995-12-122015-01-01US flag
Allergy Relief EyeSolution / drops0.25 mg/1mLOphthalmicWestern Family Foods2011-05-252015-06-01US flag
Allergy Relief Eye DropsSolution / drops0.35 mg/1mLOphthalmicKinray Inc.2014-03-182016-09-01US flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
AlawayKetotifen fumarate (0.25 mg/1mL) + Ketotifen fumarate (0.25 mg/1mL)SolutionOphthalmicBausch & Lomb Incorporated2006-12-012015-09-30US flag
AlawayKetotifen fumarate (0.25 mg/1mL) + Ketotifen fumarate (0.25 mg/1mL)SolutionOphthalmicBausch & Lomb Incorporated2006-12-012015-09-30US flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
ZaditorKetotifen fumarate (0.345 mg/1mL)SolutionOphthalmicPhysicians Total Care, Inc.2002-11-042010-12-29US flag

Categories

ATC Codes
S01GX08 — KetotifenR06AX17 — Ketotifen
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as cycloheptathiophenes. These are polycyclic compounds containing a thiophene ring fused to a 7 member carbocyclic moiety. Thiophene is 5-membered ring consisting of four carbon atoms and one sulfur atom.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Cycloheptathiophenes
Sub Class
Not Available
Direct Parent
Cycloheptathiophenes
Alternative Parents
Aryl alkyl ketones / Piperidines / Benzenoids / Thiophenes / Heteroaromatic compounds / Trialkylamines / Azacyclic compounds / Organopnictogen compounds / Organic oxides / Hydrocarbon derivatives
Substituents
Amine / Aromatic heteropolycyclic compound / Aryl alkyl ketone / Aryl ketone / Azacycle / Benzenoid / Cycloheptathiophene / Heteroaromatic compound / Hydrocarbon derivative / Ketone
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available

Chemical Identifiers

UNII
X49220T18G
CAS number
34580-13-7
InChI Key
ZCVMWBYGMWKGHF-UHFFFAOYSA-N
InChI
InChI=1S/C19H19NOS/c1-20-9-6-13(7-10-20)18-15-5-3-2-4-14(15)12-17(21)19-16(18)8-11-22-19/h2-5,8,11H,6-7,9-10,12H2,1H3
IUPAC Name
2-(1-methylpiperidin-4-ylidene)-6-thiatricyclo[8.4.0.0³,⁷]tetradeca-1(14),3(7),4,10,12-pentaen-8-one
SMILES
CN1CCC(CC1)=C1C2=C(SC=C2)C(=O)CC2=CC=CC=C12

References

Synthesis Reference

Roy W. Bryant, Ravi Parihar, Thomas Rowe, Susan Caballa, "Methods of Making and Using Stable Pharmaceutical Compositions Comprising Ketotifen and Naphazoline." U.S. Patent US20110312998, issued December 22, 2011.

US20110312998
General References
  1. Hawes EM: N+-glucuronidation, a common pathway in human metabolism of drugs with a tertiary amine group. Drug Metab Dispos. 1998 Sep;26(9):830-7. [PubMed:9733660]
  2. Kato Y, Izukawa T, Oda S, Fukami T, Finel M, Yokoi T, Nakajima M: Human UDP-glucuronosyltransferase (UGT) 2B10 in drug N-glucuronidation: substrate screening and comparison with UGT1A3 and UGT1A4. Drug Metab Dispos. 2013 Jul;41(7):1389-97. doi: 10.1124/dmd.113.051565. Epub 2013 Apr 23. [PubMed:23611809]
  3. Sokol KC, Amar NK, Starkey J, Grant JA: Ketotifen in the management of chronic urticaria: resurrection of an old drug. Ann Allergy Asthma Immunol. 2013 Dec;111(6):433-6. doi: 10.1016/j.anai.2013.10.003. Epub 2013 Oct 25. [PubMed:24267353]
  4. Jeffreys DB, Volans GN: Ketotifen overdose: surveillance of the toxicity of a new drug. Br Med J (Clin Res Ed). 1981 May 30;282(6278):1755-6. doi: 10.1136/bmj.282.6278.1755. [PubMed:6113023]
  5. Grant SM, Goa KL, Fitton A, Sorkin EM: Ketotifen. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in asthma and allergic disorders. Drugs. 1990 Sep;40(3):412-48. doi: 10.2165/00003495-199040030-00006. [PubMed:2226222]
  6. FDA Approved Drug Products: Zaditor (ketotifen fumarate) ophthalmic solution [Link]
  7. Health Canada Product Monograph: Zaditen (ketotifen fumarate) for oral administration [Link]
Human Metabolome Database
HMDB0015056
KEGG Drug
D01332
PubChem Compound
3827
PubChem Substance
46508921
ChemSpider
3695
BindingDB
94597
RxNav
6146
ChEBI
92511
ChEMBL
CHEMBL534
ZINC
ZINC000000004351
Therapeutic Targets Database
DAP000329
PharmGKB
PA450152
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Ketotifen
AHFS Codes
  • 52:02.00 — Antiallergic Agents
  • 04:00.00 — Antihistamine Drugs
  • 04:92.00 — Other Antihistamines
FDA label
Download (9.05 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentAsthma1
4CompletedTreatmentSeasonal Allergic Conjunctivitis1
4Unknown StatusTreatmentDengue Fever / Pleural Effusions1
3CompletedNot AvailableSeasonal Allergic Conjunctivitis1
3CompletedBasic ScienceFibromyalgia1
3CompletedTreatmentAtopic Dermatitis (AD)1
3CompletedTreatmentAtopy / Skin Inflammation1
3CompletedTreatmentRhinitis, Allergic, Perennial2
3CompletedTreatmentSeasonal Allergic Conjunctivitis5
3CompletedTreatmentVernal Keratoconjunctivitis1

Pharmacoeconomics

Manufacturers
  • Bausch and lomb inc
  • Akorn inc
  • Alcon inc
  • Apotex inc etobicoke site
  • Novartis pharmaceuticals corp
Packagers
  • Akorn Inc.
  • Allergan Inc.
  • Apotex Inc.
  • Bausch & Lomb Inc.
  • Ciba Vision Canada Inc.
  • Novartis AG
  • Physicians Total Care Inc.
  • Spectrum Pharmaceuticals
Dosage Forms
FormRouteStrength
SolutionOphthalmic
Solution / dropsOphthalmic0.35 mg/1mL
SolutionConjunctival; Ophthalmic
SolutionOphthalmic0.25 g/1mL
SolutionOphthalmic0.25 mg/1mL
SolutionOphthalmic
SolutionConjunctival; Ophthalmic0.5 mg
SolutionOral
CapsuleOral
GelOphthalmic
SolutionOphthalmic0.35 mg/1mL
TabletOral
SolutionOral20 mg
SyrupOral0.02 g
SyrupOral20 mg
SyrupOral
Solution / dropsOphthalmic0.345 mg/1mL
TabletOral1 MG
Solution / dropsOral
Tablet, solubleOral
SolutionOphthalmic.25 mg/1mL
Tablet, extended releaseOral
Solution / dropsOphthalmic
SolutionOphthalmic.35 mg/1mL
SolutionOphthalmic0.25 mg
SolutionOphthalmic0.345 mg/1mL
Solution / dropsOphthalmic0.25 mg/1mL
SyrupOral1 mg/5mL
Prices
Unit descriptionCostUnit
Ketotifen fumarate powder926.63USD g
Zaditor 0.025% Solution 5ml Bottle74.96USD bottle
Ketotifen fum 0.025% eye drops2.44USD ml
Refresh 0.025% eye drops2.2USD ml
Zaditor 0.025% eye drops2.15USD ml
Alaway 0.025% eye drops0.96USD ml
Zaditen 1 mg Tablet0.83USD tablet
Novo-Ketotifen 1 mg Tablet0.66USD tablet
Novo-Ketotifen 0.2 mg/ml Syrup0.14USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)190https://pdf.hres.ca/dpd_pm/00017437.PDF
water solubilityReadily solublehttps://pdf.hres.ca/dpd_pm/00017437.PDF
pKa8.43 ± 0.11https://pdf.hres.ca/dpd_pm/00017437.PDF
Predicted Properties
PropertyValueSource
Water Solubility0.00787 mg/mLALOGPS
logP3.49ALOGPS
logP3.35ChemAxon
logS-4.6ALOGPS
pKa (Strongest Acidic)12.3ChemAxon
pKa (Strongest Basic)7.15ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area20.31 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity101.73 m3·mol-1ChemAxon
Polarizability34.61 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9923
Caco-2 permeable+0.8867
P-glycoprotein substrateSubstrate0.87
P-glycoprotein inhibitor IInhibitor0.8564
P-glycoprotein inhibitor IINon-inhibitor0.7474
Renal organic cation transporterInhibitor0.8198
CYP450 2C9 substrateNon-substrate0.7542
CYP450 2D6 substrateNon-substrate0.5638
CYP450 3A4 substrateSubstrate0.6984
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorInhibitor0.8931
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.8607
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.6414
Ames testNon AMES toxic0.7576
CarcinogenicityNon-carcinogens0.9649
BiodegradationNot ready biodegradable0.9547
Rat acute toxicity2.7979 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.6336
hERG inhibition (predictor II)Non-inhibitor0.5145
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

Targets

Drugtargets
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Details
1. Histamine H1 receptor
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Histamine receptor activity
Specific Function
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamin...
Gene Name
HRH1
Uniprot ID
P35367
Uniprot Name
Histamine H1 receptor
Molecular Weight
55783.61 Da
References
  1. Mita H, Shida T: Comparison of anti-allergic activities of the histamine H1 receptor antagonists epinastine, ketotifen and oxatomide in human leukocytes. Arzneimittelforschung. 1995 Jan;45(1):36-40. [PubMed:7893266]
  2. Okabe S, Nakaji S, Tachibana M: Effect of ketotifen on acute gastric lesions and gastric secretion in rats. Jpn J Pharmacol. 1992 Jun;59(2):251-4. [PubMed:1434122]
  3. Hashimoto T, Ohata H, Honda K: Lysophosphatidic acid (LPA) induces plasma exudation and histamine release in mice via LPA receptors. J Pharmacol Sci. 2006 Jan;100(1):82-7. Epub 2006 Jan 11. [PubMed:16404130]
  4. Ito K, Sakamoto T, Hayashi Y, Morishita M, Shibata E, Sakai K, Takeuchi Y, Torii S: Role of tachykinin and bradykinin receptors and mast cells in gaseous formaldehyde-induced airway microvascular leakage in rats. Eur J Pharmacol. 1996 Jul 4;307(3):291-8. [PubMed:8836617]
  5. Yokoyama H, Iinuma K, Yanai K, Watanabe T, Sakurai E, Onodera K: Proconvulsant effect of ketotifen, a histamine H1 antagonist, confirmed by the use of d-chlorpheniramine with monitoring electroencephalography. Methods Find Exp Clin Pharmacol. 1993 Apr;15(3):183-8. [PubMed:8101246]
  6. Werner-Klein M, Goggel R, Westhof A, Erb KJ: Development and characterisation of a novel and rapid lung eosinophil influx model in the rat. Pulm Pharmacol Ther. 2008 Aug;21(4):648-56. doi: 10.1016/j.pupt.2008.03.002. Epub 2008 Apr 7. [PubMed:18490184]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Phosphogluconate dehydrogenase (decarboxylating) activity
Specific Function
Catalyzes the oxidative decarboxylation of 6-phosphogluconate to ribulose 5-phosphate and CO(2), with concomitant reduction of NADP to NADPH.
Gene Name
PGD
Uniprot ID
P52209
Uniprot Name
6-phosphogluconate dehydrogenase, decarboxylating
Molecular Weight
53139.56 Da
References
  1. Akkemik E, Budak H, Ciftci M: Effects of some drugs on human erythrocyte 6-phosphogluconate dehydrogenase: an in vitro study. J Enzyme Inhib Med Chem. 2010 Aug;25(4):476-9. doi: 10.3109/14756360903257900. [PubMed:20235752]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Retinoic acid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. Isoform 2 lacks transferase activity but acts as a negative reg...
Gene Name
UGT1A3
Uniprot ID
P35503
Uniprot Name
UDP-glucuronosyltransferase 1-3
Molecular Weight
60337.835 Da
References
  1. Kato Y, Izukawa T, Oda S, Fukami T, Finel M, Yokoi T, Nakajima M: Human UDP-glucuronosyltransferase (UGT) 2B10 in drug N-glucuronidation: substrate screening and comparison with UGT1A3 and UGT1A4. Drug Metab Dispos. 2013 Jul;41(7):1389-97. doi: 10.1124/dmd.113.051565. Epub 2013 Apr 23. [PubMed:23611809]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Protein homodimerization activity
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...
Gene Name
UGT1A4
Uniprot ID
P22310
Uniprot Name
UDP-glucuronosyltransferase 1-4
Molecular Weight
60024.535 Da
References
  1. Kato Y, Izukawa T, Oda S, Fukami T, Finel M, Yokoi T, Nakajima M: Human UDP-glucuronosyltransferase (UGT) 2B10 in drug N-glucuronidation: substrate screening and comparison with UGT1A3 and UGT1A4. Drug Metab Dispos. 2013 Jul;41(7):1389-97. doi: 10.1124/dmd.113.051565. Epub 2013 Apr 23. [PubMed:23611809]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds.
Specific Function
Glucuronosyltransferase activity
Gene Name
UGT2B10
Uniprot ID
P36537
Uniprot Name
UDP-glucuronosyltransferase 2B10
Molecular Weight
60773.485 Da
References
  1. Kato Y, Izukawa T, Oda S, Fukami T, Finel M, Yokoi T, Nakajima M: Human UDP-glucuronosyltransferase (UGT) 2B10 in drug N-glucuronidation: substrate screening and comparison with UGT1A3 and UGT1A4. Drug Metab Dispos. 2013 Jul;41(7):1389-97. doi: 10.1124/dmd.113.051565. Epub 2013 Apr 23. [PubMed:23611809]

Drug created on June 13, 2005 13:24 / Updated on April 11, 2021 00:58