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Identification
NameAnastrozole
Accession NumberDB01217  (APRD00016)
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionAnastrozole is a drug indicated in the treatment of breast cancer in post-menopausal women. It is used both in adjuvant therapy (i.e. following surgery) and in metastatic breast cancer. It decreases the amount of estrogens that the body makes. Anastrozole belongs in the class of drugs known as aromatase inhibitors. It inhibits the enzyme aromatase, which is responsible for converting androgens (produced by women in the adrenal glands) to estrogens.
Structure
Thumb
Synonyms
alpha,alpha,Alpha',alpha'-tetramethyl-5-(1H-1,2,4-triazol-1-ylmethyl)-m-benzenediacetonitrile
Anastrozol
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Accel-anastrozole Tabletstablet1 mgoralAccel Pharma IncNot applicableNot applicableCanada
Ach-anastrozoletablet1 mgoralAccord Healthcare Inc2012-10-25Not applicableCanada
Act Anastrozoletablet1 mgoralActavis Pharma Company2012-10-25Not applicableCanada
Anastrozoletablet1 mgoralSanis Health Inc2015-07-22Not applicableCanada
Anastrozoletablet1 mgoralPro Doc Limitee2012-11-22Not applicableCanada
Arimidextablet1 mg/1oralAstra Zeneca Pharmaceuticals Lp1996-01-16Not applicableUs
Arimidextablet1 mg/1oralPhysicians Total Care, Inc.2004-02-19Not applicableUs
Arimidex Tab 1mgtablet1 mgoralAstrazeneca Canada Inc1996-08-30Not applicableCanada
Auro-anastrozoletablet1 mgoralAuro Pharma Inc2013-06-12Not applicableCanada
Bio-anastrozoletablet1 mgoralBiomed Pharma2013-01-15Not applicableCanada
Ipg-anastrozoletablet1 mgoralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Jamp-anastrozoletablet1 mgoralJamp Pharma Corporation2012-10-25Not applicableCanada
Mar-anastrozoletablet1 mgoralMarcan Pharmaceuticals Inc2012-10-25Not applicableCanada
Med-anastrozoletablet1 mgoralGeneric Medical Partners Inc2012-10-25Not applicableCanada
Mint-anastrozoletablet1 mgoralMint Pharmaceuticals Inc2012-10-25Not applicableCanada
Mylan-anastrozoletablet1 mgoralMylan Pharmaceuticals Ulc2012-10-25Not applicableCanada
Nat-anastrozoletablet1 mgoralNatco Pharma (Canada) Inc2015-02-03Not applicableCanada
PMS-anastrozoletablet1 mgoralPharmascience Inc2012-10-25Not applicableCanada
Ran-anastrozoletablet1 mgoralRanbaxy Pharmaceuticals Canada Inc.2012-10-25Not applicableCanada
Riva-anastrozoletablet1 mgoralLaboratoire Riva Inc2012-10-26Not applicableCanada
Sandoz Anastrozoletablet1 mgoralSandoz Canada Incorporated2012-07-26Not applicableCanada
Taro-anastrozoletablet1 mgoralTaro Pharmaceuticals Inc2012-10-25Not applicableCanada
Teva-anastrozoletablet1 mgoralTeva Canada Limited2012-10-25Not applicableCanada
Van-anastrozoletablet1 mgoralVanc Pharmaceuticals Inc2015-06-08Not applicableCanada
Zinda-anastrozoletablet1 mgoralStason Pharmaceuticals Inc2013-06-18Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Anastrozoletablet1 mg/1oralProficient Rx LP2010-06-28Not applicableUs
Anastrozoletablet1 mg/1oralRising Pharmaceuticals, Inc.2010-06-01Not applicableUs
Anastrozoletablet1 mg/1oralRoxane Laboratories, Inc.2010-06-28Not applicableUs
Anastrozoletablet1 mg/1oralPhysicians Total Care, Inc.2010-07-01Not applicableUs
Anastrozoletablet, coated1 mg/1oralBlue Point Laboratories2014-01-01Not applicableUs
Anastrozoletablet1 mg/1oralPd Rx Pharmaceuticals, Inc.2010-06-28Not applicableUs
Anastrozoletablet, coated1 mg/1oralCadila Healthcare Limited2010-06-27Not applicableUs
Anastrozoletablet, film coated1 mg/1oralSandoz Inc2010-06-28Not applicableUs
Anastrozoletablet, coated1 mg/1oralAmerican Health Packaging2015-11-01Not applicableUs
Anastrozoletablet1 mg/1oralAccord Healthcare Inc.2010-06-22Not applicableUs
Anastrozoletablet1 mg/1oralAPP Pharmaceuticals, LLC2010-06-28Not applicableUs
Anastrozoletablet, film coated1 mg/1oralTeva Pharmaceuticals USA Inc2010-06-28Not applicableUs
Anastrozoletablet, film coated1 mg/1oralDr. Reddy's Laboratories Limited2010-06-28Not applicableUs
Anastrozoletablet, coated1 mg/1oralAmerican Health Packaging2010-06-27Not applicableUs
Anastrozoletablet, film coated1 mg/1oralUDL Laboratories, Inc.2010-07-23Not applicableUs
Anastrozoletablet1 mg/1oralDispensing Solutions, Inc.2010-06-28Not applicableUs
Anastrozoletablet1 mg/1oralMajor Pharmaceuticals2010-06-15Not applicableUs
Anastrozoletablet, film coated1 mg/1oralKremers Urban Pharmaceuticals Inc.2011-01-05Not applicableUs
Anastrozoletablet1 mg/1oralStason Pharmaceuticals, Inc2010-06-28Not applicableUs
Anastrozoletablet1 mg/1oralRebel Distributors Corp2010-07-01Not applicableUs
Anastrozoletablet1 mg/1oralbryant ranch prepack2010-06-28Not applicableUs
Anastrozoletablet1 mg/1oralKAISER FOUNDATION HOSPITALS2010-07-13Not applicableUs
Anastrozoletablet, film coated1 mg/1oralGolden State Medical Supply, Inc.2012-05-31Not applicableUs
Anastrozoletablet, coated1 mg/1oralZydus Pharmaceuticals (USA) Inc.2010-06-27Not applicableUs
Anastrozoletablet1 mg/1oralNorthwind Pharmaceuticals, LLC2014-11-07Not applicableUs
Anastrozoletablet, film coated1 mg/1oralKadmon Pharmaceuticals, LLC2010-06-28Not applicableUs
Anastrozoletablet1 mg/1oralMajor Pharmaceuticals2010-12-26Not applicableUs
Anastrozoletablet, film coated1 mg/1oralSun Pharmaceutical Industries Limited2010-07-16Not applicableUs
Anastrozoletablet1 mg/1oralRebel Distributors Corp2010-06-28Not applicableUs
Anastrozoletablet, film coated1 mg/1oralSynthon Pharmaceuticals, Inc.2010-06-28Not applicableUs
Anastrozoletablet, film coated1 mg/1oralMylan Pharmaceuticals Inc.2010-06-28Not applicableUs
Anastrozoletablet, film coated1 mg/1oralApotex Corp.2012-05-31Not applicableUs
Anastrozoletablet1 mg/1oralAvera Mc Kennan Hospital2015-03-01Not applicableUs
Anastrozoletablet1 mg/1oralBreckenridge Pharmaceutical, Inc.2010-06-28Not applicableUs
Anastrozoletablet1 mg/1oralAscend Laboratories, LLC2010-06-28Not applicableUs
Apo-anastrozoletablet1 mgoralApotex Inc2012-10-25Not applicableCanada
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AnastroleNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII2Z07MYW1AZ
CAS number120511-73-1
WeightAverage: 293.3663
Monoisotopic: 293.164045633
Chemical FormulaC17H19N5
InChI KeyInChIKey=YBBLVLTVTVSKRW-UHFFFAOYSA-N
InChI
InChI=1S/C17H19N5/c1-16(2,9-18)14-5-13(8-22-12-20-11-21-22)6-15(7-14)17(3,4)10-19/h5-7,11-12H,8H2,1-4H3
IUPAC Name
2-[3-(1-cyano-1-methylethyl)-5-(1H-1,2,4-triazol-1-ylmethyl)phenyl]-2-methylpropanenitrile
SMILES
CC(C)(C#N)C1=CC(=CC(CN2C=NC=N2)=C1)C(C)(C)C#N
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as benzyl cyanides. These are organic compounds containing an acetonitrile with one hydrogen replaced by a phenyl group.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassBenzyl cyanides
Direct ParentBenzyl cyanides
Alternative Parents
Substituents
  • Phenylpropane
  • Benzyl-cyanide
  • Phenylmethylamine
  • Heteroaromatic compound
  • 1,2,4-triazole
  • Azole
  • Azacycle
  • Organoheterocyclic compound
  • Nitrile
  • Carbonitrile
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors
Pharmacology
IndicationFor adjuvant treatment of hormone receptor positive breast cancer , as well as hormonal treatment of advanced breast cancer in post-menopausal women. Has also been used to treat pubertal gynecomastia and McCune-Albright syndrome; however, manufacturer states that efficacy for these indications have not been established.
PharmacodynamicsAnastrozole is a potent and selective non-steroidal aromatase inhibitor indicated for the treatment of advanced breast cancer in post-menopausal women with disease progression following tamoxifen therapy. Many breast cancers have estrogen receptors and growth of these tumors can be stimulated by estrogens. In post-menopausal women, the principal source of circulating estrogen (primarily estradiol) is conversion of adrenally-generated androstenedione to estrone by aromatase in peripheral tissues, such as adipose tissue, with further conversion of estrone to estradiol. Many breast cancers also contain aromatase; the importance of tumor-generated estrogens is uncertain. Treatment of breast cancer has included efforts to decrease estrogen levels by ovariectomy premenopausally and by use of anti-estrogens and progestational agents both pre- and post-menopausally, and these interventions lead to decreased tumor mass or delayed progression of tumor growth in some women. Anastrozole is a potent and selective non-steroidal aromatase inhibitor. It significantly lowers serum estradiol concentrations and has no detectable effect on formation of adrenal corticosteroids or aldosterone.
Mechanism of actionAnastrozole selectively inhibits aromatase. The principal source of circulating estrogen (primarily estradiol) is conversion of adrenally-generated androstenedione to estrone by aromatase in peripheral tissues. Therefore, aromatase inhibition leads to a decrease in serum and tumor concentration of estrogen, leading to a decreased tumor mass or delayed progression of tumor growth in some women. Anastrozole has no detectable effect on synthesis of adrenal corticosteroids, aldosterone, and thyroid hormone.
Related Articles
AbsorptionRapidly absorbed into the systemic cirulation following oral administration. Peak plasma concentrations are usually attained within 2 hours under fasting conditions, with steady-state plasma concentrations attained in approximately 7 days.
Volume of distributionNot Available
Protein binding40%
Metabolism

Hepatic. Metabolized mainly by N-dealkylation, hydroxylation, and glucuronidation to inactive metabolites. Primary metabolite is an inactive triazole.

Route of eliminationHepatic metabolism accounts for approximately 85% of anastrozole elimination. Renal elimination accounts for approximately 10% of total clearance.
Half life50 hours
ClearanceNot Available
ToxicityIn rats, lethality is greater than 100 mg/kg.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9965
Blood Brain Barrier+0.9382
Caco-2 permeable+0.5516
P-glycoprotein substrateNon-substrate0.6405
P-glycoprotein inhibitor INon-inhibitor0.764
P-glycoprotein inhibitor IINon-inhibitor0.7662
Renal organic cation transporterNon-inhibitor0.512
CYP450 2C9 substrateNon-substrate0.803
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.5761
CYP450 1A2 substrateNon-inhibitor0.6218
CYP450 2C9 inhibitorNon-inhibitor0.7616
CYP450 2D6 inhibitorNon-inhibitor0.9183
CYP450 2C19 inhibitorNon-inhibitor0.6404
CYP450 3A4 inhibitorNon-inhibitor0.6501
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7038
Ames testNon AMES toxic0.6394
CarcinogenicityNon-carcinogens0.8068
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.5564 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9464
hERG inhibition (predictor II)Non-inhibitor0.8878
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Tabletoral1 mg/1
Tablet, coatedoral1 mg/1
Tablet, film coatedoral1 mg/1
Tabletoral1 mg
Prices
Unit descriptionCostUnit
Anastrozole 100% powder1326.52USD g
Arimidex 1 mg tablet15.3USD tablet
Aromasin 25 mg tablet14.04USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA1337420 No1995-10-242012-10-24Canada
USRE36617 No1993-06-272010-06-27Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point130.14 °CNot Available
water solubility0.5 mg/mLNot Available
logP2.4Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0661 mg/mLALOGPS
logP2.31ALOGPS
logP3.03ChemAxon
logS-3.6ALOGPS
pKa (Strongest Basic)2.25ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area78.29 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity97.47 m3·mol-1ChemAxon
Polarizability31.97 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
GC-MSGC-MS Spectrum - GC-MSNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
References
Synthesis Reference

Anil Khile, Narendra Joshi, Shekhar Bhirud, “Process for the preparation of anastrozole and intermediates thereof.” U.S. Patent US20060189670, issued August 24, 2006.

US20060189670
General References
  1. Howell A, Cuzick J, Baum M, Buzdar A, Dowsett M, Forbes JF, Hoctin-Boes G, Houghton J, Locker GY, Tobias JS: Results of the ATAC (Arimidex, Tamoxifen, Alone or in Combination) trial after completion of 5 years' adjuvant treatment for breast cancer. Lancet. 2005 Jan 1-7;365(9453):60-2. [PubMed:15639680 ]
  2. Mauras N, Bishop K, Merinbaum D, Emeribe U, Agbo F, Lowe E: Pharmacokinetics and pharmacodynamics of anastrozole in pubertal boys with recent-onset gynecomastia. J Clin Endocrinol Metab. 2009 Aug;94(8):2975-8. doi: 10.1210/jc.2008-2527. Epub 2009 May 26. [PubMed:19470631 ]
  3. Nabholtz JM: Role of anastrozole across the breast cancer continuum: from advanced to early disease and prevention. Oncology. 2006;70(1):1-12. Epub 2006 Jan 26. [PubMed:16439860 ]
  4. Milani M, Jha G, Potter DA: Anastrozole Use in Early Stage Breast Cancer of Post-Menopausal Women. Clin Med Ther. 2009 Mar 31;1:141-156. [PubMed:19794821 ]
  5. Gangadhara S, Bertelli G: Long-term efficacy and safety of anastrozole for adjuvant treatment of early breast cancer in postmenopausal women. Ther Clin Risk Manag. 2009 Aug;5(4):291-300. Epub 2009 May 4. [PubMed:19753124 ]
  6. Santen RJ, Brodie H, Simpson ER, Siiteri PK, Brodie A: History of aromatase: saga of an important biological mediator and therapeutic target. Endocr Rev. 2009 Jun;30(4):343-75. doi: 10.1210/er.2008-0016. Epub 2009 Apr 23. [PubMed:19389994 ]
External Links
ATC CodesL02BG03
AHFS Codes
  • 10:00.00
PDB EntriesNot Available
FDA labelDownload (258 KB)
MSDSDownload (57.3 KB)
Interactions
Drug Interactions
Drug
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Anastrozole.
BazedoxifeneThe therapeutic efficacy of Anastrozole can be decreased when used in combination with Bazedoxifene.
BevacizumabBevacizumab may increase the cardiotoxic activities of Anastrozole.
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Anastrozole.
ChlorotrianiseneThe therapeutic efficacy of Anastrozole can be decreased when used in combination with Chlorotrianisene.
Conjugated Equine EstrogensThe therapeutic efficacy of Anastrozole can be decreased when used in combination with Conjugated Equine Estrogens.
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Anastrozole.
DeslanosideDeslanoside may decrease the cardiotoxic activities of Anastrozole.
DienestrolThe therapeutic efficacy of Anastrozole can be decreased when used in combination with Dienestrol.
DiethylstilbestrolThe therapeutic efficacy of Anastrozole can be decreased when used in combination with Diethylstilbestrol.
DigitoxinDigitoxin may decrease the cardiotoxic activities of Anastrozole.
DigoxinDigoxin may decrease the cardiotoxic activities of Anastrozole.
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Anastrozole.
EstradiolThe therapeutic efficacy of Anastrozole can be decreased when used in combination with Estradiol.
EstriolThe therapeutic efficacy of Anastrozole can be decreased when used in combination with Estriol.
EstroneThe therapeutic efficacy of Anastrozole can be decreased when used in combination with Estrone.
Ethinyl EstradiolThe therapeutic efficacy of Anastrozole can be decreased when used in combination with Ethinyl Estradiol.
GenisteinThe therapeutic efficacy of Anastrozole can be decreased when used in combination with Genistein.
HexestrolThe therapeutic efficacy of Anastrozole can be decreased when used in combination with Hexestrol.
MestranolThe therapeutic efficacy of Anastrozole can be decreased when used in combination with Mestranol.
MethadoneThe serum concentration of Methadone can be increased when it is combined with Anastrozole.
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Anastrozole.
OuabainOuabain may decrease the cardiotoxic activities of Anastrozole.
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Anastrozole.
Polyestradiol phosphateThe therapeutic efficacy of Anastrozole can be decreased when used in combination with Polyestradiol phosphate.
QuinestrolThe therapeutic efficacy of Anastrozole can be decreased when used in combination with Quinestrol.
Synthetic Conjugated Estrogens, AThe therapeutic efficacy of Anastrozole can be decreased when used in combination with Synthetic Conjugated Estrogens, A.
Synthetic Conjugated Estrogens, BThe therapeutic efficacy of Anastrozole can be decreased when used in combination with Synthetic Conjugated Estrogens, B.
TamoxifenThe serum concentration of Anastrozole can be decreased when it is combined with Tamoxifen.
TiboloneThe therapeutic efficacy of Anastrozole can be decreased when used in combination with Tibolone.
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Anastrozole.
ZeranolThe therapeutic efficacy of Anastrozole can be decreased when used in combination with Zeranol.
Food Interactions
  • Food decreases the rate of absorption, but the extent of absorption is not affected.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Oxygen binding
Specific Function:
Catalyzes the formation of aromatic C18 estrogens from C19 androgens.
Gene Name:
CYP19A1
Uniprot ID:
P11511
Molecular Weight:
57882.48 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. Mauras N, Bishop K, Merinbaum D, Emeribe U, Agbo F, Lowe E: Pharmacokinetics and pharmacodynamics of anastrozole in pubertal boys with recent-onset gynecomastia. J Clin Endocrinol Metab. 2009 Aug;94(8):2975-8. doi: 10.1210/jc.2008-2527. Epub 2009 May 26. [PubMed:19470631 ]
  3. Nabholtz JM: Role of anastrozole across the breast cancer continuum: from advanced to early disease and prevention. Oncology. 2006;70(1):1-12. Epub 2006 Jan 26. [PubMed:16439860 ]
  4. Jakesz R, Greil R, Gnant M, Schmid M, Kwasny W, Kubista E, Mlineritsch B, Tausch C, Stierer M, Hofbauer F, Renner K, Dadak C, Rucklinger E, Samonigg H: Extended adjuvant therapy with anastrozole among postmenopausal breast cancer patients: results from the randomized Austrian Breast and Colorectal Cancer Study Group Trial 6a. J Natl Cancer Inst. 2007 Dec 19;99(24):1845-53. Epub 2007 Dec 11. [PubMed:18073378 ]
  5. Cuzick J: Anastrozole. Drugs Today (Barc). 2005 Apr;41(4):227-39. [PubMed:16034487 ]
  6. Rugo HS: The breast cancer continuum in hormone-receptor-positive breast cancer in postmenopausal women: evolving management options focusing on aromatase inhibitors. Ann Oncol. 2008 Jan;19(1):16-27. Epub 2007 Aug 9. [PubMed:17693420 ]
  7. Milani M, Jha G, Potter DA: Anastrozole Use in Early Stage Breast Cancer of Post-Menopausal Women. Clin Med Ther. 2009 Mar 31;1:141-156. [PubMed:19794821 ]
  8. Gangadhara S, Bertelli G: Long-term efficacy and safety of anastrozole for adjuvant treatment of early breast cancer in postmenopausal women. Ther Clin Risk Manag. 2009 Aug;5(4):291-300. Epub 2009 May 4. [PubMed:19753124 ]
  9. Santen RJ, Brodie H, Simpson ER, Siiteri PK, Brodie A: History of aromatase: saga of an important biological mediator and therapeutic target. Endocr Rev. 2009 Jun;30(4):343-75. doi: 10.1210/er.2008-0016. Epub 2009 Apr 23. [PubMed:19389994 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Oxygen binding
Specific Function:
Catalyzes the formation of aromatic C18 estrogens from C19 androgens.
Gene Name:
CYP19A1
Uniprot ID:
P11511
Molecular Weight:
57882.48 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:
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 ]
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
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:
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 August 17, 2016 12:23