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Identification
NameMexiletine
Accession NumberDB00379  (APRD00242)
TypeSmall Molecule
GroupsApproved
Description

Antiarrhythmic agent pharmacologically similar to lidocaine. It may have some anticonvulsant properties. [PubChem]

Structure
Thumb
Synonyms
(+-)-1-(2,6-Dimethylphenoxy)propan-2-amine
(2RS)-1-(2,6-dimethylphenoxy)-2-aminopropane
1-(2,6-Dimethylphenoxy)-2-propanamine
1-(2',6'-Dimethylphenoxy)-2-aminopropane
1-Methyl-2-(2,6-xylyloxy)ethanamine
Mexiletina
Mexilétine
Mexiletinum
External Identifiers
  • Kö 1173
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Alti-mexiletinecapsule200 mgoralAltimed Pharma Inc.1997-11-072001-09-05Canada
Alti-mexiletinecapsule100 mgoralAltimed Pharma Inc.1997-11-072001-09-05Canada
Mexitil Cap 100mgcapsule100 mgoralBoehringer Ingelheim (Canada) Ltd Ltee1985-12-312002-07-25Canada
Mexitil Cap 200mgcapsule200 mgoralBoehringer Ingelheim (Canada) Ltd Ltee1985-12-312002-07-25Canada
Novo-mexiletinecapsule100 mgoralTeva Canada Limited1997-03-17Not applicableCanada
Novo-mexiletinecapsule200 mgoralTeva Canada Limited1997-02-17Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Mexiletine Hydrochloridecapsule150 mg/1oralTeva Pharmaceuticals USA Inc1995-06-05Not applicableUs
Mexiletine Hydrochloridecapsule150 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-03-16Not applicableUs
Mexiletine Hydrochloridecapsule250 mg/1oralAv Kare, Inc.2013-07-09Not applicableUs
Mexiletine Hydrochloridecapsule200 mg/1oralAv Kare, Inc.2013-07-09Not applicableUs
Mexiletine Hydrochloridecapsule150 mg/1oralAv Kare, Inc.2013-07-09Not applicableUs
Mexiletine Hydrochloridecapsule250 mg/1oralCarilion Materials Management1995-06-05Not applicableUs
Mexiletine Hydrochloridecapsule250 mg/1oralTeva Pharmaceuticals USA Inc1995-06-05Not applicableUs
Mexiletine Hydrochloridecapsule150 mg/1oralCarilion Materials Management1995-06-05Not applicableUs
Mexiletine Hydrochloridecapsule200 mg/1oralTeva Pharmaceuticals USA Inc1995-06-05Not applicableUs
Mexiletine Hydrochloridecapsule200 mg/1oralCarilion Materials Management1995-06-05Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
CirumimeruTsuruhara Seiyaku
MekiratinOhara Yakuhin
MelateMedisa Shinyaku
MeldestTaiyo Pharmaceutical
MeletinTaiwan Biotech
MequitolideTowa Yakuhin
MetorekicinChoseido Pharmaceutical
MexicordPolfa Grodzisk
MexitilBoehringer Ingelheim
MexitilenBoehringer Ingelheim
MinsetilZdravlje
MobalenTatsumi Kagaku
MugadineYung Shin
OlzoronKobayashi Kako
PoerutenYoshindo
RitalmexValeant
Teva-MexiletineTeva Neuroscience
ToiKyorin Rimedio
TumetilBoehringer Ingelheim
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Mexiletine Hydrochloride
5370-01-4
Thumb
  • InChI Key: NFEIBWMZVIVJLQ-UHFFFAOYNA-N
  • Monoisotopic Mass: 215.10769191
  • Average Mass: 215.72
DBSALT000449
Categories
UNII1U511HHV4Z
CAS number31828-71-4
WeightAverage: 179.2588
Monoisotopic: 179.131014171
Chemical FormulaC11H17NO
InChI KeyInChIKey=VLPIATFUUWWMKC-UHFFFAOYSA-N
InChI
InChI=1S/C11H17NO/c1-8-5-4-6-9(2)11(8)13-7-10(3)12/h4-6,10H,7,12H2,1-3H3
IUPAC Name
1-(2,6-dimethylphenoxy)propan-2-amine
SMILES
CC(N)COC1=C(C)C=CC=C1C
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenol ethers. These are aromatic compounds containing an ether group substituted with a benzene ring.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassPhenol ethers
Direct ParentPhenol ethers
Alternative Parents
Substituents
  • Phenol ether
  • Alkyl aryl ether
  • Ether
  • Hydrocarbon derivative
  • Primary amine
  • Organooxygen compound
  • Organonitrogen compound
  • Primary aliphatic amine
  • Amine
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of ventricular tachycardia and symptomatic premature ventricular beats, and prevention of ventricular fibrillation.
PharmacodynamicsMexiletine is a local anesthetic, antiarrhythmic agent (Class Ib), structurally similar to lidocaine, but orally active. Mexiletine has fast onset and offset kinetics, meaning that they have little or no effect at slower heart rates, and more effects at faster heart rates. It shortens the action potential duration, reduces refractoriness, and decreases Vmax in partially depolarized cells with fast response action potentials. Mexiletine either does not change the action potential duration, or decreases the action potential duration.
Mechanism of actionMexiletine, like lidocaine, inhibits the inward sodium current required for the initiation and conduction of impulses, thus reducing the rate of rise of the action potential, Phase 0. It achieves this reduced sodium current by inhibiting sodium channels. Mexiletine decreases the effective refractory period (ERP) in Purkinje fibers in the heart. The decrease in ERP is of lesser magnitude than the decrease in action potential duration (APD), which results in an increase in the ERP/APD ratio. It does not significantly affect resting membrane potential or sinus node automaticity, left ventricular function, systolic arterial blood pressure, atrioventricular (AV) conduction velocity, or QRS or QT intervals
Related Articles
AbsorptionWell absorbed (bioavailability 90%) from the gastrointenstinal tract.
Volume of distribution
  • 5 to 7 L/lg
Protein binding50-60%
Metabolism

Primarily hepatic (85%) via CYP2D6 and CYP1A2 (primarily CYP2D6).

SubstrateEnzymesProduct
Mexiletine
2-hydroxymexiletineDetails
Mexiletine
p-hydroxymexiletineDetails
Route of eliminationApproximately 10% is excreted unchanged by the kidney. The urinary excretion of N-methylmexiletine in man is less than 0.5%.
Half life10-12 hours
ClearanceNot Available
ToxicitySymptoms of overdose include nausea, hypotension, sinus bradycardia, paresthesia, seizures, bundle branch block, AV heart block, asystole, ventricular tachyarrythmia, including ventricular fibrillation, cardiovascular collapse, and coma.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Mexiletine Action PathwayDrug actionSMP00329
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9382
Caco-2 permeable+0.7357
P-glycoprotein substrateNon-substrate0.6711
P-glycoprotein inhibitor INon-inhibitor0.8781
P-glycoprotein inhibitor IINon-inhibitor0.9484
Renal organic cation transporterNon-inhibitor0.7849
CYP450 2C9 substrateNon-substrate0.8191
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateNon-substrate0.5463
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorNon-inhibitor0.941
CYP450 2D6 inhibitorInhibitor0.8932
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.9132
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6004
Ames testNon AMES toxic0.6357
CarcinogenicityNon-carcinogens0.7796
BiodegradationNot ready biodegradable0.9261
Rat acute toxicity2.6338 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8982
hERG inhibition (predictor II)Non-inhibitor0.6563
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Sandoz inc
  • Teva pharmaceuticals usa inc
  • Watson laboratories inc
  • Boehringer ingelheim
Packagers
Dosage forms
FormRouteStrength
Capsuleoral150 mg/1
Capsuleoral200 mg/1
Capsuleoral250 mg/1
Capsuleoral100 mg
Capsuleoral200 mg
Prices
Unit descriptionCostUnit
Mexitil 250 mg capsule1.85USD capsule
Mexiletine HCl 250 mg capsule1.6USD capsule
Mexiletine 250 mg capsule1.54USD capsule
Mexiletine HCl 200 mg capsule1.38USD capsule
Mexiletine 200 mg capsule1.33USD capsule
Mexitil 200 mg capsule1.23USD capsule
Novo-Mexiletine 200 mg Capsule1.19USD capsule
Mexiletine HCl 150 mg capsule1.16USD capsule
Mexiletine 150 mg capsule1.11USD capsule
Novo-Mexiletine 100 mg Capsule0.89USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point203-205 °CPhysProp
water solubility8.25 mg/mLNot Available
logP2.15MANNHOLD,R ET AL. (1990)
pKa9.2Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.538 mg/mLALOGPS
logP2.17ALOGPS
logP2.46ChemAxon
logS-2.5ALOGPS
pKa (Strongest Basic)9.52ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area35.25 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity54.97 m3·mol-1ChemAxon
Polarizability21.17 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Margarita Ortiz-Marciales, Kun Huang, Viatcheslav Stepanenko, Melvin De Jesus, Wildeliz Correa, “Method of synthesizing enantiopure mexiletine analogues and novel b-thiophenoxy and pyridyl ethers.” U.S. Patent US08012901, issued September 06, 2011.

US08012901
General ReferencesNot Available
External Links
ATC CodesC01BB02
AHFS Codes
  • 24:04.04.08
PDB EntriesNot Available
FDA labelDownload (1.21 MB)
MSDSDownload (47.1 KB)
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Mexiletine can be increased when it is combined with Abiraterone.
AcenocoumarolThe metabolism of Acenocoumarol can be decreased when combined with Mexiletine.
AcetaminophenThe metabolism of Acetaminophen can be decreased when combined with Mexiletine.
Acetylsalicylic acidThe metabolism of Acetylsalicylic acid can be decreased when combined with Mexiletine.
AlosetronThe metabolism of Alosetron can be decreased when combined with Mexiletine.
AminophyllineThe metabolism of Aminophylline can be decreased when combined with Mexiletine.
AsenapineThe metabolism of Asenapine can be decreased when combined with Mexiletine.
BendamustineThe serum concentration of Bendamustine can be increased when it is combined with Mexiletine.
BetaxololThe metabolism of Betaxolol can be decreased when combined with Mexiletine.
BortezomibThe metabolism of Mexiletine can be decreased when combined with Bortezomib.
BromazepamThe metabolism of Bromazepam can be decreased when combined with Mexiletine.
ButalbitalThe metabolism of Butalbital can be decreased when combined with Mexiletine.
CaffeineThe metabolism of Caffeine can be decreased when combined with Mexiletine.
CarbamazepineThe metabolism of Mexiletine can be increased when combined with Carbamazepine.
CitalopramThe metabolism of Mexiletine can be decreased when combined with Citalopram.
ClomipramineThe metabolism of Clomipramine can be decreased when combined with Mexiletine.
ClozapineThe serum concentration of Clozapine can be increased when it is combined with Mexiletine.
CobicistatThe serum concentration of Mexiletine can be increased when it is combined with Cobicistat.
CyclobenzaprineThe metabolism of Cyclobenzaprine can be decreased when combined with Mexiletine.
Cyproterone acetateThe serum concentration of Mexiletine can be decreased when it is combined with Cyproterone acetate.
DacarbazineThe metabolism of Dacarbazine can be decreased when combined with Mexiletine.
DarunavirThe serum concentration of Mexiletine can be increased when it is combined with Darunavir.
DeferasiroxThe serum concentration of Mexiletine can be increased when it is combined with Deferasirox.
DihydrocodeineThe metabolism of Dihydrocodeine can be decreased when combined with Mexiletine.
DuloxetineThe serum concentration of Duloxetine can be increased when it is combined with Mexiletine.
EscitalopramThe metabolism of Mexiletine can be decreased when combined with Escitalopram.
EtravirineThe serum concentration of Mexiletine can be decreased when it is combined with Etravirine.
FluoxetineThe metabolism of Mexiletine can be decreased when combined with Fluoxetine.
FlutamideThe metabolism of Flutamide can be decreased when combined with Mexiletine.
FluvoxamineThe metabolism of Mexiletine can be decreased when combined with Fluvoxamine.
FosphenytoinThe serum concentration of Mexiletine can be decreased when it is combined with Fosphenytoin.
IsomethepteneThe metabolism of Isometheptene can be decreased when combined with Mexiletine.
LidocaineThe metabolism of Lidocaine can be decreased when combined with Mexiletine.
MirtazapineThe metabolism of Mirtazapine can be decreased when combined with Mexiletine.
OlanzapineThe metabolism of Olanzapine can be decreased when combined with Mexiletine.
PanobinostatThe serum concentration of Mexiletine can be increased when it is combined with Panobinostat.
ParoxetineThe metabolism of Mexiletine can be decreased when combined with Paroxetine.
Peginterferon alfa-2bThe serum concentration of Mexiletine can be decreased when it is combined with Peginterferon alfa-2b.
PentoxifyllineThe serum concentration of Pentoxifylline can be increased when it is combined with Mexiletine.
PhenytoinThe serum concentration of Mexiletine can be decreased when it is combined with Phenytoin.
PimozideThe metabolism of Pimozide can be decreased when combined with Mexiletine.
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Mexiletine.
PropranololThe metabolism of Propranolol can be decreased when combined with Mexiletine.
RamelteonThe metabolism of Ramelteon can be decreased when combined with Mexiletine.
RasagilineThe serum concentration of Rasagiline can be increased when it is combined with Mexiletine.
RitonavirThe metabolism of Mexiletine can be decreased when combined with Ritonavir.
RopiniroleThe metabolism of Ropinirole can be decreased when combined with Mexiletine.
RopivacaineThe metabolism of Ropivacaine can be decreased when combined with Mexiletine.
StiripentolThe metabolism of Stiripentol can be decreased when combined with Mexiletine.
TasimelteonThe serum concentration of Tasimelteon can be increased when it is combined with Mexiletine.
TeriflunomideThe serum concentration of Mexiletine can be decreased when it is combined with Teriflunomide.
TheophyllineThe metabolism of Theophylline can be decreased when combined with Mexiletine.
ThiothixeneThe metabolism of Thiothixene can be decreased when combined with Mexiletine.
TiclopidineThe metabolism of Mexiletine can be decreased when combined with Ticlopidine.
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Mexiletine.
TrifluoperazineThe metabolism of Trifluoperazine can be decreased when combined with Mexiletine.
VemurafenibThe serum concentration of Mexiletine can be increased when it is combined with Vemurafenib.
VilazodoneThe metabolism of Mexiletine can be decreased when combined with Vilazodone.
VortioxetineThe metabolism of Mexiletine can be decreased when combined with Vortioxetine.
Food Interactions
  • Take with food to reduce irritation.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Voltage-gated sodium channel activity involved in sa node cell action potential
Specific Function:
This protein mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient. It is a tetrodotoxin-resistant Na(+) channel isoform. This channel is respon...
Gene Name:
SCN5A
Uniprot ID:
Q14524
Molecular Weight:
226937.475 Da
References
  1. Valdivia CR, Ackerman MJ, Tester DJ, Wada T, McCormack J, Ye B, Makielski JC: A novel SCN5A arrhythmia mutation, M1766L, with expression defect rescued by mexiletine. Cardiovasc Res. 2002 Aug 1;55(2):279-89. [PubMed:12123767 ]
  2. Chinushi M, Tagawa M, Sugiura H, Komura S, Hosaka Y, Washizuka T, Aizawa Y: Ventricular tachyarrhythmias in a canine model of LQT3: arrhythmogenic effects of sympathetic activity and therapeutic effects of mexiletine. Circ J. 2003 Mar;67(3):263-8. [PubMed:12604879 ]
  3. Fabritz L, Kirchhof P, Franz MR, Nuyens D, Rossenbacker T, Ottenhof A, Haverkamp W, Breithardt G, Carmeliet E, Carmeliet P: Effect of pacing and mexiletine on dispersion of repolarisation and arrhythmias in DeltaKPQ SCN5A (long QT3) mice. Cardiovasc Res. 2003 Mar 15;57(4):1085-93. [PubMed:12650887 ]
  4. Wang HW, Zheng YQ, Yang ZF, Li CZ, Liu YM: Effect of mexiletine on long QT syndrome model. Acta Pharmacol Sin. 2003 Apr;24(4):316-20. [PubMed:12676070 ]
  5. Napolitano C, Bloise R, Priori SG: Gene-specific therapy for inherited arrhythmogenic diseases. Pharmacol Ther. 2006 Apr;110(1):1-13. Epub 2005 Sep 15. [PubMed:16168489 ]
  6. Shimizu W, Antzelevitch C, Suyama K, Kurita T, Taguchi A, Aihara N, Takaki H, Sunagawa K, Kamakura S: Effect of sodium channel blockers on ST segment, QRS duration, and corrected QT interval in patients with Brugada syndrome. J Cardiovasc Electrophysiol. 2000 Dec;11(12):1320-9. [PubMed:11196553 ]
  7. 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
agonist
General Function:
Transcription regulatory region dna binding
Specific Function:
Ligand-activated transcriptional activator. Binds to the XRE promoter region of genes it activates. Activates the expression of multiple phase I and II xenobiotic chemical metabolizing enzyme genes (such as the CYP1A1 gene). Mediates biochemical and toxic effects of halogenated aromatic hydrocarbons. Involved in cell-cycle regulation. Likely to play an important role in the development and matu...
Gene Name:
AHR
Uniprot ID:
P35869
Molecular Weight:
96146.705 Da
References
  1. Hu W, Sorrentino C, Denison MS, Kolaja K, Fielden MR: Induction of cyp1a1 is a nonspecific biomarker of aryl hydrocarbon receptor activation: results of large scale screening of pharmaceuticals and toxicants in vivo and in vitro. Mol Pharmacol. 2007 Jun;71(6):1475-86. Epub 2007 Feb 27. [PubMed:17327465 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Nakajima M, Kobayashi K, Shimada N, Tokudome S, Yamamoto T, Kuroiwa Y: Involvement of CYP1A2 in mexiletine metabolism. Br J Clin Pharmacol. 1998 Jul;46(1):55-62. [PubMed:9690950 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Nakajima M, Kobayashi K, Shimada N, Tokudome S, Yamamoto T, Kuroiwa Y: Involvement of CYP1A2 in mexiletine metabolism. Br J Clin Pharmacol. 1998 Jul;46(1):55-62. [PubMed:9690950 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid 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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.81 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic or carcinogenic forms.
Gene Name:
CYP2E1
Uniprot ID:
P05181
Molecular Weight:
56848.42 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on September 24, 2013 00:13