Methimazole

Identification

Name
Methimazole
Accession Number
DB00763  (APRD00002)
Type
Small Molecule
Groups
Approved
Description

A thioureylene antithyroid agent that inhibits the formation of thyroid hormones by interfering with the incorporation of iodine into tyrosyl residues of thyroglobulin. This is done by interfering with the oxidation of iodide ion and iodotyrosyl groups through inhibition of the peroxidase enzyme. [PubChem]

Structure
Thumb
Synonyms
  • 1-METHYL-1,3-dihydro-2H-imidazole-2-thione
  • 1-Methylimidazole-2(3H)-thione
  • Danantizol
  • Favistan
  • Mercazolyl
  • Methimazole
  • Strumazol
  • Thacapzol
  • Thiamazol
  • Thiamazole
  • Thiamazolum
  • Tiamazol
  • USAF el-30
External IDs
NSC 38608 / UNII-554Z48XN5E
Product Ingredients
Not Available
Product Images
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Dom-methimazoleTablet5 mgOralDominion PharmacalNot applicableNot applicableCanada
PHL-methimazoleTablet5 mgOralPharmel IncNot applicableNot applicableCanada
PMS-methimazoleTablet5 mgOralPharmascience Inc2004-11-052005-05-04Canada
TapazoleTablet10 mgOralPaladin Labs Inc2008-01-07Not applicableCanada
TapazoleTablet20 mgOralPaladin Labs IncNot applicableNot applicableCanada
Tapazole 5mg TabletTablet5 mgOralPaladin Labs Inc1951-12-31Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-methimazoleTablet5 mgOralApotex Corporation2005-03-18Not applicableCanada
MethimazoleTablet5 mg/1OralEon Labs, Inc.2001-03-27Not applicableUs
MethimazoleTablet10 mg/1OralRising Pharmaceuticals2015-09-28Not applicableUs
MethimazoleTablet10 mg/1OralRebel Distributors2010-07-07Not applicableUs49884 0641 01 nlmimage10 dd08eec7
MethimazoleTablet10 mg/1Oralbryant ranch prepack2000-04-13Not applicableUs
MethimazoleTablet5 mg/1OralRemedy Repack2013-11-12Not applicableUs
MethimazoleTablet10 mg/1OralAmerincan Health Packaging2013-06-14Not applicableUs
MethimazoleTablet10 mg/1OralEci Pharmaceuticals Llc2016-07-01Not applicableUs
MethimazoleTablet5 mg/1OralRising Pharmaceuticals2015-09-28Not applicableUs
MethimazoleTablet10 mg/1OralRemedy Repack2013-07-02Not applicableUs
MethimazoleTablet10 mg/1OralNcs Health Care Of Ky, Inc Dba Vangard Labs2001-03-27Not applicableUs
MethimazoleTablet10 mg/1OralState of Florida DOH Central Pharmacy2014-01-01Not applicableUs
MethimazoleTablet10 mg/1OralRemedy Repack2013-03-182016-10-21Us
MethimazoleTablet10 mg/1OralGolden State Medical Supply2013-01-08Not applicableUs
MethimazoleTablet5 mg/1OralPar Pharmaceutical2012-02-28Not applicableUs
MethimazoleTablet5 mg/1OralA S Medication Solutions2012-02-282017-06-20Us
MethimazoleTablet10 mg/1OralEon Labs, Inc.2001-03-27Not applicableUs
MethimazoleTablet10 mg/1OralState of Florida DOH Central Pharmacy2013-01-01Not applicableUs
MethimazoleTablet10 mg/1OralDispensing Solutions, Inc.2012-01-16Not applicableUs23155 0071 01 nlmimage10 423ca135
MethimazoleTablet10 mg/1OralExact Rx, Inc.2012-01-122017-08-29Us
MethimazoleTablet10 mg/1OralUnit Dose Services2001-03-27Not applicableUs00185 0210 01 nlmimage10 da08ed17
MethimazoleTablet5 mg/1OralBoca Pharmacal, Inc.2012-03-072017-01-31Us64376 0655 01 nlmimage10 7240b905
MethimazoleTablet5 mg/1OralPhysicians Total Care, Inc.2009-10-13Not applicableUs
MethimazoleTablet5 mg/1OralPreferreed Pharmaceuticals Inc.2015-10-06Not applicableUs
MethimazoleTablet10 mg/1Oralbryant ranch prepack2000-04-13Not applicableUs
MethimazoleTablet5 mg/1OralHeritage2012-01-16Not applicableUs
MethimazoleTablet5 mg/1OralRebel Distributors2010-07-07Not applicableUs49884 0640 01 nlmimage10 e008f017
MethimazoleTablet10 mg/1OralPar Pharmaceutical2000-04-13Not applicableUs
MethimazoleTablet5 mg/1OralEci Pharmaceuticals Llc2016-07-01Not applicableUs
MethimazoleTablet10 mg/1OralBoca Pharmacal, Inc.2012-03-072017-02-28Us
MethimazoleTablet10 mg/1OralPreferreed Pharmaceuticals Inc.2014-02-27Not applicableUs
MethimazoleTablet5 mg/1OralNcs Health Care Of Ky, Inc Dba Vangard Labs2001-03-27Not applicableUs
MethimazoleTablet10 mg/1OralState of Florida DOH Central Pharmacy2014-01-01Not applicableUs
MethimazoleTablet5 mg/1OralAmerincan Health Packaging2013-06-14Not applicableUs
MethimazoleTablet10 mg/1OralRemedy Repack2011-11-012016-11-05Us
MethimazoleTablet10 mg/1OralHeritage2012-01-16Not applicableUs
MethimazoleTablet5 mg/1OralGolden State Medical Supply2013-01-08Not applicableUs23155 0070 01 nlmimage10 6940b4b5
MethimazoleTablet5 mg/1OralExact Rx, Inc.2012-01-122018-05-31Us
TapazoleTablet10 mg/1OralRemedy Repack2013-03-132017-01-11Us
TapazoleTablet10 mg/1OralPfizer Laboratories Div Pfizer Inc.2000-03-31Not applicableUs
TapazoleTablet5 mg/1OralRemedy Repack2013-02-182016-12-23Us
TapazoleTablet5 mg/1OralPfizer Laboratories Div Pfizer Inc.2000-03-31Not applicableUs
Approved Over the Counter Products
Not Available
Unapproved/Other Products
Not Available
International/Other Brands
Danantizol (Gador S.A.) / Favistan (Temmler) / Metizol (ICN) / Strumazol (Organon) / Strumazole / Tapazole / Thacapzol (Recip) / Thycapzol (Sandoz) / Thyrozol (Merck) / Tirozol (Merck)
Brand mixtures
Not Available
Categories
UNII
554Z48XN5E
CAS number
60-56-0
Weight
Average: 114.169
Monoisotopic: 114.025168892
Chemical Formula
C4H6N2S
InChI Key
PMRYVIKBURPHAH-UHFFFAOYSA-N
InChI
InChI=1S/C4H6N2S/c1-6-3-2-5-4(6)7/h2-3H,1H3,(H,5,7)
IUPAC Name
1-methyl-2,3-dihydro-1H-imidazole-2-thione
SMILES
CN1C=CNC1=S

Pharmacology

Indication

For the treatment of hyperthyroidism, goiter, Graves disease and psoriasis.

Structured Indications
Pharmacodynamics

Used in the treatment of hyperthyroidism or an overactive thyroid gland, methimazole inhibits the synthesis of thyroid hormones and thus is effective in the treatment of hyperthyroidism. It may also be used to ameliorate hyperthyroidism in preparation for subtotal thyroidectomy or radioactive iodine therapy.

Mechanism of action

Methimazole binds to thyroid peroxidase and thereby inhibits the conversion of iodide to iodine. Thyroid peroxidase normally converts iodide to iodine (via hydrogen peroxide as a cofactor) and also catalyzes the incorporation of the resulting iodide molecule onto both the 3 and/or 5 positions of the phenol rings of tyrosines found in thyroglobulin. Thyroglobulin is degraded to produce thyroxine (T4) and tri-iodothyronine (T3), which are the main hormones produced by the thyroid gland. So methimazole effectively inhibits the production of new thyroid hormones.

TargetActionsOrganism
AThyroid peroxidase
inhibitor
Human
Absorption

Rapid with an oral bioavailability of 93%.

Volume of distribution
Not Available
Protein binding

None or minimal

Metabolism

Primarily hepatic. Metabolized rapidly, requiring frequent administration.

Route of elimination

Methimazole is excreted in the urine.

Half life

5-6 hours

Clearance
Not Available
Toxicity

Oral LD50 in rats is 2250 mg/kg. Symptoms of overdose include nausea, vomiting, epigastric distress, headache, fever, joint pain, pruritus, and edema. Aplastic anemia (pancy-topenia) or agranulocytosis may be manifested in hours to days. Less frequent events are hepatitis, nephrotic syndrome, exfoliative dermatitis, neuropathies, and CNS stimulation or depression.

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

Interactions

Drug Interactions
DrugInteractionDrug group
AcenocoumarolMethimazole may decrease the anticoagulant activities of Acenocoumarol.Approved
AcetyldigitoxinThe serum concentration of Acetyldigitoxin can be increased when it is combined with Methimazole.Approved
Ambroxol acefyllinateThe serum concentration of Ambroxol acefyllinate can be increased when it is combined with Methimazole.Experimental
AminophyllineThe serum concentration of Aminophylline can be increased when it is combined with Methimazole.Approved
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Methimazole.Approved, Investigational
ArtesunateThe serum concentration of the active metabolites of Artesunate can be reduced when Artesunate is used in combination with Methimazole resulting in a loss in efficacy.Approved
BCG vaccineThe therapeutic efficacy of Bcg can be decreased when used in combination with Methimazole.Investigational
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Methimazole.Approved
ClozapineThe risk or severity of adverse effects can be increased when Methimazole is combined with Clozapine.Approved
DeslanosideThe serum concentration of Deslanoside can be increased when it is combined with Methimazole.Approved
DicoumarolMethimazole may decrease the anticoagulant activities of Dicoumarol.Approved
DigitoxinThe serum concentration of Digitoxin can be increased when it is combined with Methimazole.Approved
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Methimazole.Approved
DyphyllineThe serum concentration of Dyphylline can be increased when it is combined with Methimazole.Approved
Ethyl biscoumacetateMethimazole may decrease the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Methimazole.Approved
FluindioneMethimazole may decrease the anticoagulant activities of Fluindione.Investigational
Iodide I-131The therapeutic efficacy of Sodium Iodide I-131 can be decreased when used in combination with Methimazole.Approved
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Methimazole.Withdrawn
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Methimazole.Approved, Investigational
OleandrinThe serum concentration of Anvirzel can be increased when it is combined with Methimazole.Experimental
OuabainThe serum concentration of Ouabain can be increased when it is combined with Methimazole.Approved
PhenindioneMethimazole may decrease the anticoagulant activities of Phenindione.Approved
PhenprocoumonMethimazole may decrease the anticoagulant activities of Phenprocoumon.Approved
PrednisoloneThe serum concentration of Prednisolone can be decreased when it is combined with Methimazole.Approved, Vet Approved
TheophyllineThe serum concentration of Theophylline can be increased when it is combined with Methimazole.Approved
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Methimazole.Withdrawn
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Methimazole.Approved
WarfarinMethimazole may decrease the anticoagulant activities of Warfarin.Approved
Food Interactions
  • Always take at the same moment in regard to meals, food may affect absorption unpredictably.

References

Synthesis Reference
Not Available
General References
Not Available
External Links
Human Metabolome Database
HMDB14901
KEGG Drug
D00401
KEGG Compound
C07190
PubChem Compound
1349907
PubChem Substance
46506536
ChemSpider
1131173
BindingDB
50241361
ChEBI
50673
ChEMBL
CHEMBL1515
Therapeutic Targets Database
DNC001429
PharmGKB
PA450422
HET
MMZ
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Methimazole
ATC Codes
H03BB02 — ThiamazoleH03BB52 — Thiamazole, combinations
AHFS Codes
  • 68:36.08
PDB Entries
Not Available
FDA label
Not Available
MSDS
Download (75.8 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1, 2CompletedTreatmentGraves´ Disease / Thyroid Associated Ophthalmopathy1
2CompletedTreatmentDermatomyositis / Polymyositis1
2SuspendedSupportive CareGlioblastoma Multiforme (GBM)1
3RecruitingTreatmentGraves Diseases / Graves Ophthalmopathy / Graves' Ophthalmopathy Worsened1
4CompletedPreventionGraves´ Disease1
4CompletedTreatmentGraves Diseases / Toxic Nodular Goitre1
4CompletedTreatmentGraves' Disease / Toxic Nodular Goitre1
4Unknown StatusDiagnosticHealthy Volunteers1
Not AvailableCompletedNot AvailableGraves Diseases1
Not AvailableCompletedTreatmentGraves Diseases1
Not AvailableCompletedTreatmentGraves' Disease1
Not AvailableTerminatedTreatmentGraves Ophthalmopathy1

Pharmacoeconomics

Manufacturers
  • Actavis totowa llc
  • Caraco pharmaceutical laboratories ltd
  • Cedar pharmaceuticals llc
  • Mylan pharmaceuticals inc
  • Sandoz inc
  • King pharmaceuticals inc
  • King pharmaceuticals research and development inc sub king pharmaceuticals inc
Packagers
Dosage forms
FormRouteStrength
TabletOral5 mg
TabletOral10 mg/1
TabletOral5 mg/1
TabletOral10 mg
TabletOral20 mg
Prices
Unit descriptionCostUnit
Methimazole powder9.49USD g
Methimazole 20 mg tablet1.9USD tablet
Tapazole 10 mg tablet1.45USD tablet
Northyx 20 mg tablet0.94USD tablet
Northyx 15 mg tablet0.82USD tablet
Methimazole 10 mg tablet0.78USD tablet
Tapazole 5 mg tablet0.66USD tablet
Northyx 10 mg tablet0.47USD tablet
Methimazole 5 mg tablet0.45USD tablet
Northyx 5 mg tablet0.29USD tablet
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)146 °CPhysProp
boiling point (°C)280 °CPhysProp
water solubility275 g/LNot Available
logP-0.34HANSCH,C ET AL. (1995)
Predicted Properties
PropertyValueSource
Water Solubility11.3 mg/mLALOGPS
logP-0.38ALOGPS
logP0.75ChemAxon
logS-1ALOGPS
pKa (Strongest Acidic)10.41ChemAxon
pKa (Strongest Basic)-3ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count0ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area15.27 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity33.23 m3·mol-1ChemAxon
Polarizability11.64 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9156
Blood Brain Barrier+0.9731
Caco-2 permeable+0.6156
P-glycoprotein substrateNon-substrate0.8213
P-glycoprotein inhibitor INon-inhibitor0.7552
P-glycoprotein inhibitor IINon-inhibitor0.944
Renal organic cation transporterNon-inhibitor0.7662
CYP450 2C9 substrateNon-substrate0.7919
CYP450 2D6 substrateNon-substrate0.8985
CYP450 3A4 substrateNon-substrate0.7849
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.9232
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.7105
Ames testNon AMES toxic0.8582
CarcinogenicityNon-carcinogens0.9348
BiodegradationNot ready biodegradable0.9815
Rat acute toxicity1.8215 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9401
hERG inhibition (predictor II)Non-inhibitor0.8416
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )

Spectra

Mass Spec (NIST)
Download (8.12 KB)
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-066r-8900000000-9230df83b87c13377bfb
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-014i-0900000000-275f9771b8d1d7486052
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-014i-0900000000-1763fdc1a812fa765250
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-014i-0900000000-78877e6d65fda61a0e67
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-014i-1900000000-c979e7cdbceb656b6a1e
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-014i-1900000000-1447e5774eda5dc3fe26
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-066r-9300000000-41d253a513ee17fed774
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-0a4i-9000000000-11684a341cebaa28c427
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-0a60-9000000000-7637560408e70990bc27
Predicted LC-MS/MS Spectrum - 10V, PositivePredicted LC-MS/MSsplash10-014i-0900000000-810e7a010dd805f3251d
Predicted LC-MS/MS Spectrum - 20V, PositivePredicted LC-MS/MSsplash10-014i-5900000000-e88140069cbfa61f9c51
Predicted LC-MS/MS Spectrum - 40V, PositivePredicted LC-MS/MSsplash10-0006-9000000000-3969b3a3102e9214d562
Predicted LC-MS/MS Spectrum - 10V, NegativePredicted LC-MS/MSsplash10-03di-0900000000-3e543dd0166f52789fcd
Predicted LC-MS/MS Spectrum - 20V, NegativePredicted LC-MS/MSsplash10-0900-9300000000-90c58541a936c6fdd275
Predicted LC-MS/MS Spectrum - 40V, NegativePredicted LC-MS/MSsplash10-0a4i-9000000000-9a1c61f319838c2ebce9

Taxonomy

Description
This compound belongs to the class of chemical entities known as imidazolethiones. These are aromatic compounds containing an imidazole ring which bears a thioketone group.
Kingdom
Chemical entities
Super Class
Organic compounds
Class
Organoheterocyclic compounds
Sub Class
Azolines
Direct Parent
Imidazolethiones
Alternative Parents
N-substituted imidazoles / Heteroaromatic compounds / Thioureas / Azacyclic compounds / Organopnictogen compounds / Organonitrogen compounds / Hydrocarbon derivatives
Substituents
N-substituted imidazole / Imidazole-2-thione / Heteroaromatic compound / Imidazole / Azole / Thiourea / Azacycle / Organic nitrogen compound / Organopnictogen compound / Hydrocarbon derivative
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
imidazoles, thioureas (CHEBI:50673 ) / a small molecule (CPD-11282 )

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Peroxidase activity
Specific Function
Iodination and coupling of the hormonogenic tyrosines in thyroglobulin to yield the thyroid hormones T(3) and T(4).
Gene Name
TPO
Uniprot ID
P07202
Uniprot Name
Thyroid peroxidase
Molecular Weight
102961.63 Da
References
  1. Sugawara M, Sugawara Y, Wen K: Methimazole and propylthiouracil increase cellular thyroid peroxidase activity and thyroid peroxidase mRNA in cultured porcine thyroid follicles. Thyroid. 1999 May;9(5):513-8. [PubMed:10365684 ]
  2. Manzon RG, Holmes JA, Youson JH: Variable effects of goitrogens in inducing precocious metamorphosis in sea lampreys (Petromyzon marinus). J Exp Zool. 2001 Apr 15;289(5):290-303. [PubMed:11241400 ]
  3. Ferreira AC, de Carvalho Cardoso L, Rosenthal D, de Carvalho DP: Thyroid Ca2+/NADPH-dependent H2O2 generation is partially inhibited by propylthiouracil and methimazole. Eur J Biochem. 2003 Jun;270(11):2363-8. [PubMed:12755690 ]
  4. Magnusson RP, Yu B, Brennan V: Effect of serum thyrotropin levels on the concentration of messenger RNA for thyroid peroxidase in the rat. Acta Endocrinol (Copenh). 1992 May;126(5):460-6. [PubMed:1320313 ]
  5. Chiovato L, Pinchera A: The microsomal/peroxidase antigen: modulation of its expression in thyroid cells. Autoimmunity. 1991;10(4):319-31. [PubMed:1663395 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
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 ]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Const...
Gene Name
CYP2A6
Uniprot ID
P11509
Uniprot Name
Cytochrome P450 2A6
Molecular Weight
56501.005 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
Inhibitor
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
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 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
Inhibitor
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
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 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
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
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
Inhibitor
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
Inhibitor
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 September 01, 2017 10:31