Identification

Name
Mexiletine
Accession Number
DB00379  (APRD00242)
Type
Small Molecule
Groups
Approved, Investigational
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 IDs
Kö 1173
Product Ingredients
IngredientUNIICASInChI Key
Mexiletine Hydrochloride606D60IS385370-01-4NFEIBWMZVIVJLQ-UHFFFAOYSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Mexiletine HClCapsule150 mg/1OralWatson Pharmaceuticals2008-04-29Not applicableUs
Mexiletine HClCapsule250 mg/1OralWatson Pharmaceuticals2008-04-29Not applicableUs
Mexiletine HClCapsule200 mg/1OralWatson Pharmaceuticals2008-04-29Not applicableUs
MexitilCapsule200 mg/1OralBoehringer Ingelheim1985-12-302005-01-04Us
MexitilCapsule150 mg/1OralPhysicians Total Care, Inc.1985-12-302000-06-30Us
MexitilCapsule250 mg/1OralBoehringer Ingelheim1985-12-302005-01-04Us
MexitilCapsule200 mg/1OralPhysicians Total Care, Inc.1985-12-302013-06-30Us
MexitilCapsule150 mg/1OralBoehringer Ingelheim1985-12-302005-01-04Us
Mexitil Cap 100mgCapsule100 mgOralBoehringer Ingelheim (Canada) Ltd Ltee1985-12-312002-07-25Canada
Mexitil Cap 200mgCapsule200 mgOralBoehringer Ingelheim (Canada) Ltd Ltee1985-12-312002-07-25Canada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Alti-mexiletineCapsule100 mgOralAltimed Pharma Inc.1997-11-072001-09-05Canada
Alti-mexiletineCapsule200 mgOralAltimed Pharma Inc.1997-11-072001-09-05Canada
Mexiletine HydrochlorideCapsule250 mg/1OralAvKARE, Inc.2013-07-09Not applicableUs
Mexiletine HydrochlorideCapsule250 mg/1OralCarilion Materials Management1995-06-05Not applicableUs00093 8741 01 nlmimage10 9a364d42
Mexiletine HydrochlorideCapsule200 mg/1OralTeva Pharmaceuticals USA, Inc.1995-06-05Not applicableUs0093 874020180907 15195 1stmpeo
Mexiletine HydrochlorideCapsule200 mg/1OralAvera McKennan Hospital2015-10-262018-06-26Us
Mexiletine HydrochlorideCapsule150 mg/1OralAvKARE, Inc.2013-07-09Not applicableUs
Mexiletine HydrochlorideCapsule150 mg/1OralPhysicians Total Care, Inc.1995-06-052003-06-30Us
Mexiletine HydrochlorideCapsule150 mg/1OralTeva Pharmaceuticals USA, Inc.1995-06-05Not applicableUs00093 8739 01 nlmimage10 9f364fb2
Mexiletine HydrochlorideCapsule150 mg/1OralCarilion Materials Management1995-06-05Not applicableUs68151 298520180907 15195 hzzzo
International/Other Brands
Cirumimeru (Tsuruhara Seiyaku) / Mekiratin (Ohara Yakuhin) / Melate (Medisa Shinyaku) / Meldest (Taiyo Pharmaceutical) / Meletin (Taiwan Biotech) / Mequitolide (Towa Yakuhin) / Metorekicin (Choseido Pharmaceutical) / Mexicord (Polfa Grodzisk) / Mexitil (Boehringer Ingelheim) / Mexitilen (Boehringer Ingelheim) / Minsetil (Zdravlje) / Mobalen (Tatsumi Kagaku) / Mugadine (Yung Shin) / Olzoron (Kobayashi Kako) / Poeruten (Yoshindo) / Ritalmex (Valeant) / Teva-Mexiletine (Teva Neuroscience) / Toi (Kyorin Rimedio) / Tumetil (Boehringer Ingelheim)
Categories
UNII
1U511HHV4Z
CAS number
31828-71-4
Weight
Average: 179.2588
Monoisotopic: 179.131014171
Chemical Formula
C11H17NO
InChI Key
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

Pharmacology

Indication

For the treatment of ventricular tachycardia and symptomatic premature ventricular beats, and prevention of ventricular fibrillation.

Associated Conditions
Pharmacodynamics

Mexiletine 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 action

Mexiletine, 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

TargetActionsOrganism
ASodium channel protein type 5 subunit alpha
inhibitor
Human
UAryl hydrocarbon receptor
agonist
Human
Absorption

Well absorbed (bioavailability 90%) from the gastrointenstinal tract.

Volume of distribution
  • 5 to 7 L/lg
Protein binding

50-60%

Metabolism

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

Route of elimination

Approximately 10% is excreted unchanged by the kidney. The urinary excretion of N-methylmexiletine in man is less than 0.5%.

Half life

10-12 hours

Clearance
Not Available
Toxicity

Symptoms 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
PathwayCategory
Mexiletine Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Mexiletine.
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Mexiletine.
3-isobutyl-1-methyl-7H-xanthineThe metabolism of 3-isobutyl-1-methyl-7H-xanthine can be decreased when combined with Mexiletine.
3,5-diiodothyropropionic acidThe metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Mexiletine.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Mexiletine.
4-MethoxyamphetamineThe metabolism of 4-Methoxyamphetamine can be decreased when combined with Mexiletine.
5-androstenedioneThe metabolism of 5-androstenedione can be decreased when combined with Mexiletine.
6-Deoxyerythronolide BThe metabolism of Mexiletine can be decreased when combined with 6-Deoxyerythronolide B.
6-O-benzylguanineThe metabolism of 6-O-benzylguanine can be decreased when combined with Mexiletine.
7-DeazaguanineThe metabolism of 7-Deazaguanine can be decreased when combined with Mexiletine.
Food Interactions
  • Take with food to reduce irritation.

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 References
Not Available
External Links
Human Metabolome Database
HMDB0014523
KEGG Compound
C07220
PubChem Compound
4178
PubChem Substance
46505491
ChemSpider
4034
BindingDB
50117271
ChEBI
6916
ChEMBL
CHEMBL558
Therapeutic Targets Database
DAP000505
PharmGKB
PA450488
IUPHAR
2629
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Mexiletine
ATC Codes
C01BB02 — Mexiletine
AHFS Codes
  • 24:04.04.08 — Class Ib Antiarrythmics
FDA label
Download (1.21 MB)
MSDS
Download (47.1 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedBasic ScienceDrug-induced QT Interval Prolongation / Pharmacodynamics / Pharmacokinetics1
1CompletedTreatmentIrritable Bowel Syndrome (IBS)1
2Active Not RecruitingTreatmentSporadic Amyotrophic Lateral Sclerosis1
2CompletedTreatmentAmputations / Pain, Chronic1
2CompletedTreatmentBlepharospasm / Dystonias / Spasms1
2CompletedTreatmentCharcot Marie Tooth Disease1
2CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections / Peripheral Nervous System Diseases1
2CompletedTreatmentMyotonia / Non-dystrophic Myotonias1
2CompletedTreatmentNon Dystrophic Myotonia1
2CompletedTreatmentSporadic Amyotrophic Lateral Sclerosis1
2CompletedTreatmentSteinert's Disease1
3CompletedPreventionArrythmias / Cardiovascular Disease (CVD) / Heart Arrest / Heart Diseases / Myocardial Infarction / Ventricular Fibrillation1
3CompletedTreatmentArrhythmia of ventricular origin / Arrythmias / Cardiovascular Disease (CVD) / Death, Sudden,Cardiac / Heart Diseases / Ventricular Fibrillation / Ventricular Tachycardia (VT)1
3CompletedTreatmentDiabetic Neuropathies / Pain NOS / Paresthesia1
3CompletedTreatmentMyotonia Congenita / Non-dystrophic Myotonias / Paramyotonia Congenita1
4CompletedTreatmentCryptogenic Sensory Polyneuropathy1
4CompletedTreatmentMuscle Cramps in Amyotrophic Lateral Sclerosis1

Pharmacoeconomics

Manufacturers
  • Sandoz inc
  • Teva pharmaceuticals usa inc
  • Watson laboratories inc
  • Boehringer ingelheim
Packagers
  • Atlantic Biologicals Corporation
  • Kaiser Foundation Hospital
  • Murfreesboro Pharmaceutical Nursing Supply
  • Novopharm Ltd.
  • Nucare Pharmaceuticals Inc.
  • Physicians Total Care Inc.
  • Prescript Pharmaceuticals
  • Roxane Labs
  • Southwood Pharmaceuticals
  • Teva Pharmaceutical Industries Ltd.
  • Warrick Pharmaceuticals Corp.
Dosage forms
FormRouteStrength
CapsuleOral100 mg
CapsuleOral200 mg
CapsuleOral150 mg/1
CapsuleOral200 mg/1
CapsuleOral250 mg/1
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.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)203-205 °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 RuleNoChemAxon
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)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
GC-MS Spectrum - EI-BGC-MSsplash10-0a4i-9100000000-6d40293ed4e486f9cf9e
GC-MS Spectrum - CI-BGC-MSsplash10-0a4i-9300000000-147905f020f0139cfe20
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
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-9400000000-d9f9d0eeea2a47e42771
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-9300000000-76838bfcf2fd2b0e2b17
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-9400000000-c5920fd67439f418b86f
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-9500000000-b5f13a7a078d1c192691
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-9500000000-24a61cef86793ffcf760
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-9400000000-d740cc5fc7a9b2b380a6
MS/MS Spectrum - , positiveLC-MS/MSsplash10-01q9-0900000000-083bab651324c62f4cd5
MS/MS Spectrum - , positiveLC-MS/MSsplash10-01q9-0900000000-feace6e16ed93a4bd13e
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-9400000000-94985b5db6692d615971
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-9300000000-c1e103780c7df279dc6c
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-9400000000-d077857c1d4a1d567c03
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-9500000000-9ef54de393ed768d242f
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-9500000000-9a364fda721f96e6e368

Taxonomy

Description
This 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.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Phenol ethers
Sub Class
Not Available
Direct Parent
Phenol ethers
Alternative Parents
m-Xylenes / Phenoxy compounds / Alkyl aryl ethers / Organopnictogen compounds / Monoalkylamines / Hydrocarbon derivatives
Substituents
Phenol ether / Xylene / M-xylene / Phenoxy compound / Alkyl aryl ether / Monocyclic benzene moiety / Ether / Amine / Hydrocarbon derivative / Primary amine
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
aromatic ether, primary amino compound (CHEBI:6916)

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 pr...
Gene Name
SCN5A
Uniprot ID
Q14524
Uniprot Name
Sodium channel protein type 5 subunit alpha
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...
Gene Name
AHR
Uniprot ID
P35869
Uniprot Name
Aryl hydrocarbon receptor
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
Substrate
Inhibitor
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 un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
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. Wei X, Dai R, Zhai S, Thummel KE, Friedman FK, Vestal RE: Inhibition of human liver cytochrome P-450 1A2 by the class IB antiarrhythmics mexiletine, lidocaine, and tocainide. J Pharmacol Exp Ther. 1999 May;289(2):853-8. [PubMed:10215663]
  4. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
  5. Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers [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...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
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 un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
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 ...
Gene Name
CYP2E1
Uniprot ID
P05181
Uniprot Name
Cytochrome P450 2E1
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
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]

Drug created on June 13, 2005 07:24 / Updated on December 10, 2018 06:10