Identification

Name
Entacapone
Accession Number
DB00494  (APRD00416)
Type
Small Molecule
Groups
Approved, Investigational
Description

Entacapone is a selective, reversible catechol-O-methyl transferase (COMT) inhibitor for the treatment of Parkinson's disease. It is a member of the class of nitrocatechols. When administered concomittantly with levodopa and a decarboxylase inhibitor (e.g., carbidopa), increased and more sustained plasma levodopa concentrations are reached as compared to the administration of levodopa and a decarboxylase inhibitor.

Structure
Thumb
Synonyms
  • (E)-alpha-Cyano-N,N-diethyl-3,4-dihydroxy-5-nitrocinnamamide
  • Entacapona
  • Entacapone
  • Entacaponum
  • N,N-diethyl-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl) acrylamide
External IDs
OR 611 / OR-611
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
ComtanTablet, film coated200 mg/1OralNovartis1999-10-19Not applicableUs
ComtanTablet, film coated200 mgOralNovartis Europharm Limited1998-09-22Not applicableEu
ComtanTablet, film coated200 mg/1OralCardinal Health2000-01-012018-05-25Us
ComtanTablet200 mgOralNovartis2001-06-21Not applicableCanada
ComtanTablet, film coated200 mgOralNovartis Europharm Limited1998-09-22Not applicableEu
ComtanTablet, film coated200 mgOralNovartis Europharm Limited1998-09-22Not applicableEu
ComtessTablet, film coated200 mgOralOrion Corporation1998-09-16Not applicableEu
ComtessTablet, film coated200 mgOralOrion Corporation1998-09-16Not applicableEu
ComtessTablet, film coated200 mgOralOrion Corporation1998-09-16Not applicableEu
ComtessTablet, film coated200 mgOralOrion Corporation1998-09-16Not applicableEu
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-entacaponeTablet200 mgOralApotex CorporationNot applicableNot applicableCanada
Auro-entacaponeTablet200 mgOralAuro Pharma IncNot applicableNot applicableCanada
EntacaponeTablet200 mg/1OralMacleods Pharmaceuticals Limited2017-06-06Not applicableUs
EntacaponeTablet, film coated200 mg/1OralSun Pharmaceutical Industries, Inc.2013-04-01Not applicableUs
EntacaponeTablet, film coated200 mg/1OralAvera McKennan Hospital2015-09-232018-05-22Us
EntacaponeTablet, film coated200 mg/1OralWockhardt2012-09-30Not applicableUs
EntacaponeTablet, film coated200 mg/1OralSunshine Lake Pharma Co., Ltd.2018-10-10Not applicableUs
EntacaponeTablet, film coated200 mg/1OralAv Pak2016-12-05Not applicableUs
EntacaponeTablet, film coated200 mg/1OralWockhardt2012-09-30Not applicableUs
EntacaponeTablet200 mg/1OralAjanta Pharma Limited2017-08-31Not applicableUs
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Carbidopa, levodopa and entacaponeEntacapone (200 mg/1) + Carbidopa hydrate (18.75 mg/1) + Levodopa (75 mg/1)Tablet, film coatedOralSun Pharma Global FZE2012-10-02Not applicableUs
Carbidopa, Levodopa and EntacaponeEntacapone (200 mg/1) + Carbidopa hydrate (37.5 mg/1) + Levodopa (150 mg/1)Tablet, film coatedOralWockhardt2012-02-29Not applicableUs
Carbidopa, Levodopa and EntacaponeEntacapone (200 mg/1) + Carbidopa hydrate (31.25 mg/1) + Levodopa (125 mg/1)Tablet, film coatedOralMylan Pharmaceuticals2013-10-28Not applicableUs
Carbidopa, Levodopa and EntacaponeEntacapone (200 mg/1) + Carbidopa hydrate (18.75 mg/1) + Levodopa (75 mg/1)Tablet, film coatedOralMylan Pharmaceuticals2013-10-28Not applicableUs
Carbidopa, Levodopa and EntacaponeEntacapone (200 mg/1) + Carbidopa hydrate (25 mg/1) + Levodopa (100 mg/1)Tablet, film coatedOralWockhardt2012-02-29Not applicableUs
Carbidopa, Levodopa and EntacaponeEntacapone (200 mg/1) + Carbidopa hydrate (37.5 mg/1) + Levodopa (150 mg/1)Tablet, film coatedOralWockhardt2012-02-29Not applicableUs
Carbidopa, levodopa and entacaponeEntacapone (200 mg/1) + Carbidopa hydrate (25 mg/1) + Levodopa (100 mg/1)Tablet, film coatedOralSun Pharma Global FZE2012-05-222018-03-31Us
Carbidopa, Levodopa and EntacaponeEntacapone (200 mg/1) + Carbidopa hydrate (18.75 mg/1) + Levodopa (75 mg/1)Tablet, film coatedOralWockhardt2012-02-29Not applicableUs
Carbidopa, levodopa and entacaponeEntacapone (200 mg/1) + Carbidopa hydrate (31.25 mg/1) + Levodopa (125 mg/1)Tablet, film coatedOralSun Pharma Global FZE2012-10-02Not applicableUs
Carbidopa, Levodopa and EntacaponeEntacapone (200 mg/1) + Carbidopa hydrate (50 mg/1) + Levodopa (200 mg/1)Tablet, film coatedOralMylan Pharmaceuticals2013-10-28Not applicableUs00378 8305 01 nlmimage10 f148f8d7
International/Other Brands
Anxopone (Root) / Comtade (Novartis) / Comtan / Comtess (Orion)
Categories
UNII
4975G9NM6T
CAS number
130929-57-6
Weight
Average: 305.286
Monoisotopic: 305.101170605
Chemical Formula
C14H15N3O5
InChI Key
JRURYQJSLYLRLN-BJMVGYQFSA-N
InChI
InChI=1S/C14H15N3O5/c1-3-16(4-2)14(20)10(8-15)5-9-6-11(17(21)22)13(19)12(18)7-9/h5-7,18-19H,3-4H2,1-2H3/b10-5+
IUPAC Name
(2E)-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethylprop-2-enamide
SMILES
CCN(CC)C(=O)C(=C\C1=CC(=C(O)C(O)=C1)[N+]([O-])=O)\C#N

Pharmacology

Indication

Used as an adjunct to levodopa / carbidopa in the symptomatic treatment of patients with idiopathic Parkinson's Disease who experience the signs and symptoms of end-of-dose "wearing-off".

Associated Conditions
Pharmacodynamics

Entacapone is structurally and pharmacologically related to tolcapone, but unlike tolcapone, is not associated with hepatotoxicity. Entacapone is used in the treatment of Parkinson’s disease as an adjunct to levodopa/carbidopa therapy. Entacapone is a selective and reversible inhibitor of catechol-O-methyltransferase (COMT). In mammals, COMT is distributed throughout various organs with the highest activities in the liver and kidney. COMT also occurs in the heart, lung, smooth and skeletal muscles, intestinal tract, reproductive organs, various glands, adipose tissue, skin, blood cells and neuronal tissues, especially in glial cells. COMT catalyzes the transfer of the methyl group of S-adenosyl-L-methionine to the phenolic group of substrates that contain a catechol structure. Physiological substrates of COMT include dopa, catecholamines (dopamine, norepinephrine, and epinephrine) and their hydroxylated metabolites. The function of COMT is the elimination of biologically active catechols and some other hydroxylated metabolites. COMT is responsible for the elimination of biologically active catechols and some other hydroxylated metabolites. In the presence of a decarboxylase inhibitor, COMT becomes the major metabolizing enzyme for levodopa, catalyzing the it to 3-methoxy-4-hydroxy-L-phenylalanine (3-OMD) in the brain and periphery.

Mechanism of action

The mechanism of action of entacapone is believed to be through its ability to inhibit COMT in peripheral tissues, altering the plasma pharmacokinetics of levodopa. When entacapone is given in conjunction with levodopa and an aromatic amino acid decarboxylase inhibitor, such as carbidopa, plasma levels of levodopa are greater and more sustained than after administration of levodopa and an aromatic amino acid decarboxylase inhibitor alone. It is believed that at a given frequency of levodopa administration, these more sustained plasma levels of levodopa result in more constant dopaminergic stimulation in the brain, leading to a greater reduction in the manifestations of parkinsonian syndrome.

TargetActionsOrganism
ACatechol O-methyltransferase
inhibitor
Human
Absorption

Entacapone is rapidly absorbed (approximately 1 hour). The absolute bioavailability following oral administration is 35%.

Volume of distribution
  • 20 L
Protein binding

98% (bind to serum albumin)

Metabolism

Metabolized via isomerization to the cis-isomer, followed by direct glucuronidation of the parent and cis-isomer.

Route of elimination

Entacapone is almost completely metabolized prior to excretion, with only a very small amount (0.2% of dose) found unchanged in urine. As only about 10% of the entacapone dose is excreted in urine as parent compound and conjugated glucuronide, biliary excretion appears to be the major route of excretion of this drug.

Half life

0.4-0.7 hour

Clearance
  • 850 mL/min
Toxicity

Side effect include increase the occurrence of orthostatic hypotension, severe rhabdomyolysis, dyskinesia, hallucinations, hyperkinesia, hypokinesia, dizziness, fatigu,e gastrointestinal effects including abdominal pain constipation diarrhea nausea

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
2-HydroxyestradiolThe metabolism of 2-Hydroxyestradiol can be decreased when combined with Entacapone.
2,5-Dimethoxy-4-ethylthioamphetamineThe risk or severity of adverse effects can be increased when Entacapone is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3,4-MethylenedioxyamphetamineThe risk or severity of adverse effects can be increased when Entacapone is combined with 3,4-Methylenedioxyamphetamine.
4-Bromo-2,5-dimethoxyamphetamineThe risk or severity of adverse effects can be increased when Entacapone is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-MethoxyamphetamineThe risk or severity of adverse effects can be increased when Entacapone is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamineThe risk or severity of adverse effects can be increased when Entacapone is combined with 5-methoxy-N,N-dimethyltryptamine.
7-NitroindazoleThe risk or severity of adverse effects can be increased when Entacapone is combined with 7-Nitroindazole.
AcepromazineThe risk or severity of adverse effects can be increased when Entacapone is combined with Acepromazine.
AceprometazineThe risk or severity of adverse effects can be increased when Entacapone is combined with Aceprometazine.
AcetazolamideThe risk or severity of adverse effects can be increased when Entacapone is combined with Acetazolamide.
Food Interactions
  • Take without regard to meals.

References

Synthesis Reference

Pandurang Deshpande, Parven Luthra, Anand Pandey, Dharmesh Dhameliya, "Process for the preparation of (E)-2-cyano-3-(3, 4-dihydroxy-5-nitrophenyl)-N, N-diethyl-2-propenamide (entacapone)." U.S. Patent US20060258877, issued November 16, 2006.

US20060258877
General References
  1. Najib J: Entacapone: a catechol-O-methyltransferase inhibitor for the adjunctive treatment of Parkinson's disease. Clin Ther. 2001 Jun;23(6):802-32; discussion 771. [PubMed:11440283]
  2. Chong BS, Mersfelder TL: Entacapone. Ann Pharmacother. 2000 Sep;34(9):1056-65. [PubMed:10981253]
  3. Poewe WH, Deuschl G, Gordin A, Kultalahti ER, Leinonen M: Efficacy and safety of entacapone in Parkinson's disease patients with suboptimal levodopa response: a 6-month randomized placebo-controlled double-blind study in Germany and Austria (Celomen study). Acta Neurol Scand. 2002 Apr;105(4):245-55. [PubMed:11939936]
  4. Brooks DJ, Sagar H: Entacapone is beneficial in both fluctuating and non-fluctuating patients with Parkinson's disease: a randomised, placebo controlled, double blind, six month study. J Neurol Neurosurg Psychiatry. 2003 Aug;74(8):1071-9. [PubMed:12876237]
  5. Forsberg M, Lehtonen M, Heikkinen M, Savolainen J, Jarvinen T, Mannisto PT: Pharmacokinetics and pharmacodynamics of entacapone and tolcapone after acute and repeated administration: a comparative study in the rat. J Pharmacol Exp Ther. 2003 Feb;304(2):498-506. [PubMed:12538800]
  6. Kaakkola S: Clinical pharmacology, therapeutic use and potential of COMT inhibitors in Parkinson's disease. Drugs. 2000 Jun;59(6):1233-50. [PubMed:10882160]
External Links
Human Metabolome Database
HMDB0012226
KEGG Drug
D00781
KEGG Compound
C07943
PubChem Compound
5281081
PubChem Substance
46508734
ChemSpider
4444537
BindingDB
50108879
ChEBI
4798
ChEMBL
CHEMBL953
Therapeutic Targets Database
DAP000608
PharmGKB
PA164748726
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Entacapone
ATC Codes
N04BX02 — Entacapone
AHFS Codes
  • 28:36.12 — Catechol-o-methyltransferase (Comt) Inhibitors
FDA label
Download (52.6 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0CompletedHealth Services ResearchMethamphetamine Dependence1
1CompletedNot AvailableHealthy Volunteers2
1CompletedBasic ScienceCocaine Abuse1
1CompletedTreatmentHealthy Volunteers4
1CompletedTreatmentParkinson's Disease (PD)7
1CompletedTreatmentPharmacokinetics1
1, 2Active Not RecruitingTreatmentChronic Orthostatic Intolerance / Tachycardia1
1, 2CompletedTreatmentParkinson's Disease (PD)1
1, 2TerminatedTreatmentAutonomic Nervous System Diseases / Multiple System Atrophy (MSA) / Parkinson's Disease (PD)1
1, 2Unknown StatusTreatmentBMI >30 kg/m21
2CompletedPreventionParkinson's Disease (PD)1
2CompletedTreatmentParkinson's Disease (PD)3
2RecruitingTreatmentParkinson's Disease (PD)1
2TerminatedTreatmentParkinson´s Disease1
2, 3CompletedTreatmentDependence, Cocaine1
3CompletedPreventionParkinson's Disease (PD)1
3CompletedTreatmentParkinson's Disease (PD)3
4CompletedTreatmentIdiopathic Parkinson's Disease1
4CompletedTreatmentParkinson's Disease (PD)6
4CompletedTreatmentParkinson's Disease With End of Dose "Wearing Off" / Parkinson's Disease With End of Dose Wearing Off1
4TerminatedTreatmentParkinson's Disease (PD)1
4WithdrawnTreatmentParkinson's Disease (PD)1
Not AvailableActive Not RecruitingBasic ScienceImpulsive Behaviors1
Not AvailableCompletedTreatmentSchizophrenic Disorders1
Not AvailableRecruitingNot AvailableAtypical Parkinson Disease / Corticobasal Degeneration / Gait, Frontal / Multiple System Atrophy (MSA) / Parkinson's Disease (PD) / Parkinsonian Disorders / Progressive Supranuclear Palsy (PSP)1
Not AvailableRecruitingTreatmentParkinson's Disease (PD) / Sleep disorders and disturbances1

Pharmacoeconomics

Manufacturers
  • Orion corp
Packagers
  • Cardinal Health
  • Dipharma
  • Kaiser Foundation Hospital
  • Neuland Laboratories Ltd.
  • Novartis AG
  • Orion Corporation
  • Resource Optimization and Innovation LLC
  • Vangard Labs Inc.
Dosage forms
FormRouteStrength
TabletOral200 mg
Tablet, film coatedOral200 mg
TabletOral200 mg/1
Tablet, film coatedOral200 mg/1
TabletOral
Tablet, film coatedOral
Prices
Unit descriptionCostUnit
Comtan 200 mg tablet2.96USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5135950No1992-08-042010-10-31Us
CA2342634No2008-01-292019-09-13Canada
CA1334967No1995-03-282012-03-28Canada
US6599530No2003-07-292018-09-14Us
US6500867No2002-12-312020-06-29Us
US6797732No2004-09-282020-06-29Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
logP2.8Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0797 mg/mLALOGPS
logP2.5ALOGPS
logP1.63ChemAxon
logS-3.6ALOGPS
pKa (Strongest Acidic)5.68ChemAxon
pKa (Strongest Basic)-0.036ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area130.38 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity80.51 m3·mol-1ChemAxon
Polarizability29.48 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9185
Blood Brain Barrier-0.9104
Caco-2 permeable-0.5817
P-glycoprotein substrateSubstrate0.64
P-glycoprotein inhibitor INon-inhibitor0.7342
P-glycoprotein inhibitor IINon-inhibitor0.8442
Renal organic cation transporterNon-inhibitor0.9311
CYP450 2C9 substrateNon-substrate0.8406
CYP450 2D6 substrateNon-substrate0.8932
CYP450 3A4 substrateNon-substrate0.5057
CYP450 1A2 substrateNon-inhibitor0.7003
CYP450 2C9 inhibitorNon-inhibitor0.581
CYP450 2D6 inhibitorNon-inhibitor0.8548
CYP450 2C19 inhibitorNon-inhibitor0.6098
CYP450 3A4 inhibitorNon-inhibitor0.5133
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7901
Ames testAMES toxic0.5803
CarcinogenicityNon-carcinogens0.561
BiodegradationNot ready biodegradable0.9457
Rat acute toxicity2.6750 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8608
hERG inhibition (predictor II)Non-inhibitor0.8332
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
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0a4i-0329000000-8d20a5650e9c1b1c8275

Taxonomy

Description
This compound belongs to the class of organic compounds known as hydroxycinnamic acids and derivatives. These are compounds containing an cinnamic acid (or a derivative thereof) where the benzene ring is hydroxylated.
Kingdom
Organic compounds
Super Class
Phenylpropanoids and polyketides
Class
Cinnamic acids and derivatives
Sub Class
Hydroxycinnamic acids and derivatives
Direct Parent
Hydroxycinnamic acids and derivatives
Alternative Parents
Nitrophenols / Nitrobenzenes / Nitroaromatic compounds / Catechols / 1-hydroxy-4-unsubstituted benzenoids / 1-hydroxy-2-unsubstituted benzenoids / Tertiary carboxylic acid amides / Propargyl-type 1,3-dipolar organic compounds / Organic oxoazanium compounds / Nitriles
show 5 more
Substituents
Hydroxycinnamic acid or derivatives / Nitrophenol / Nitrobenzene / Nitroaromatic compound / Catechol / 1-hydroxy-4-unsubstituted benzenoid / 1-hydroxy-2-unsubstituted benzenoid / Phenol / Monocyclic benzene moiety / Benzenoid
show 21 more
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
monocarboxylic acid amide, catechols, nitrile (CHEBI:4798)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
O-methyltransferase activity
Specific Function
Catalyzes the O-methylation, and thereby the inactivation, of catecholamine neurotransmitters and catechol hormones. Also shortens the biological half-lives of certain neuroactive drugs, like L-DOP...
Gene Name
COMT
Uniprot ID
P21964
Uniprot Name
Catechol O-methyltransferase
Molecular Weight
30036.77 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. Najib J: Entacapone: a catechol-O-methyltransferase inhibitor for the adjunctive treatment of Parkinson's disease. Clin Ther. 2001 Jun;23(6):802-32; discussion 771. [PubMed:11440283]
  3. Chong BS, Mersfelder TL: Entacapone. Ann Pharmacother. 2000 Sep;34(9):1056-65. [PubMed:10981253]
  4. Holm KJ, Spencer CM: Entacapone. A review of its use in Parkinson's disease. Drugs. 1999 Jul;58(1):159-77. [PubMed:10439935]
  5. Poewe WH, Deuschl G, Gordin A, Kultalahti ER, Leinonen M: Efficacy and safety of entacapone in Parkinson's disease patients with suboptimal levodopa response: a 6-month randomized placebo-controlled double-blind study in Germany and Austria (Celomen study). Acta Neurol Scand. 2002 Apr;105(4):245-55. [PubMed:11939936]
  6. Brooks DJ, Sagar H: Entacapone is beneficial in both fluctuating and non-fluctuating patients with Parkinson's disease: a randomised, placebo controlled, double blind, six month study. J Neurol Neurosurg Psychiatry. 2003 Aug;74(8):1071-9. [PubMed:12876237]
  7. Forsberg M, Lehtonen M, Heikkinen M, Savolainen J, Jarvinen T, Mannisto PT: Pharmacokinetics and pharmacodynamics of entacapone and tolcapone after acute and repeated administration: a comparative study in the rat. J Pharmacol Exp Ther. 2003 Feb;304(2):498-506. [PubMed:12538800]
  8. Tai CH, Wu RM: Catechol-O-methyltransferase and Parkinson's disease. Acta Med Okayama. 2002 Feb;56(1):1-6. [PubMed:11873938]
  9. Kaakkola S: Clinical pharmacology, therapeutic use and potential of COMT inhibitors in Parkinson's disease. Drugs. 2000 Jun;59(6):1233-50. [PubMed:10882160]
  10. Ruottinen HM, Rinne UK: COMT inhibition in the treatment of Parkinson's disease. J Neurol. 1998 Nov;245(11 Suppl 3):P25-34. [PubMed:9808337]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
O-methyltransferase activity
Specific Function
Catalyzes the O-methylation, and thereby the inactivation, of catecholamine neurotransmitters and catechol hormones. Also shortens the biological half-lives of certain neuroactive drugs, like L-DOP...
Gene Name
COMT
Uniprot ID
P21964
Uniprot Name
Catechol O-methyltransferase
Molecular Weight
30036.77 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]
Kind
Protein
Organism
Human
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. This isoform has specificity for phenols. Isoform 2 lacks trans...
Gene Name
UGT1A9
Uniprot ID
O60656
Uniprot Name
UDP-glucuronosyltransferase 1-9
Molecular Weight
59940.495 Da
References
  1. Lautala P, Ethell BT, Taskinen J, Burchell B: The specificity of glucuronidation of entacapone and tolcapone by recombinant human UDP-glucuronosyltransferases. Drug Metab Dispos. 2000 Nov;28(11):1385-9. [PubMed:11038168]
  2. Kurkela M, Garcia-Horsman JA, Luukkanen L, Morsky S, Taskinen J, Baumann M, Kostiainen R, Hirvonen J, Finel M: Expression and characterization of recombinant human UDP-glucuronosyltransferases (UGTs). UGT1A9 is more resistant to detergent inhibition than other UGTs and was purified as an active dimeric enzyme. J Biol Chem. 2003 Feb 7;278(6):3536-44. Epub 2002 Nov 14. [PubMed:12435745]
  3. Luukkanen L, Taskinen J, Kurkela M, Kostiainen R, Hirvonen J, Finel M: Kinetic characterization of the 1A subfamily of recombinant human UDP-glucuronosyltransferases. Drug Metab Dispos. 2005 Jul;33(7):1017-26. Epub 2005 Mar 31. [PubMed:15802387]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
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

Drug created on June 13, 2005 07:24 / Updated on November 17, 2018 07:09