Identification

Name
Anastrozole
Accession Number
DB01217
Description

Anastrozole is a non-steroidal aromatase inhibitor (AI), similar to letrozole, used to decrease circulating estrogen levels in the treatment of postmenopausal women with estrogen-responsive breast cancer.10 Anastrozole is also related to exemestane, a steroidal AI, but its non-steroidal nature provides stark advantages including a lack of steroid-associated adverse effects such as weight gain and acne.4 Aromatase inhibitors, including anastrozole, have become endocrine drugs of choice in the treatment of postmenopausal breast cancer due to a more favourable efficacy and adverse effect profile as compared to earlier estrogen receptor modulators such as tamoxifen.5,8

Anastrozole was first approved for use in the United States in 1995.10

Type
Small Molecule
Groups
Approved, Investigational
Structure
Thumb
Weight
Average: 293.3663
Monoisotopic: 293.164045633
Chemical Formula
C17H19N5
Synonyms
  • Anastrozol
  • Anastrozole
  • α,α,α',α'-Tetramethyl-5-(1H-1,2,4-triazol-1-ylmethyl)-m-benzenediacetonitrile
External IDs
  • ICI D1033
  • ICI-D1033
  • ZD-1033
  • ZD1033

Pharmacology

Indication

Anastrozole is indicated as adjunct therapy in the treatment of hormone receptor-positive early breast cancer in postmenopausal women, and as a first-line treatment for hormone receptor-positive (or hormone receptor-unknown) locally advanced or metastatic breast cancer in postmenopausal women.10 It may also be used in the treatment of advanced breast cancer in postmenopausal women who experience disease progression despite treatment with tamoxifen.11,10

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
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Pharmacodynamics

Anastrozole prevents the conversion of adrenal androgens (e.g. testosterone) to estrogen in peripheral and tumour tissues. As the growth of many breast cancers is stimulated and/or maintained by the presence of estrogen, anastrozole helps to treat these cancers by decreasing the levels of circulating estrogens.12,9 Anastrozole has a relatively long duration of action allowing for once daily dosing - serum estradiol is reduced by approximately 70% within 24 hours of beginning therapy with 1mg once daily, and levels remain suppressed for up to 6 days following cessation of therapy.10

The incidence of ischemic cardiovascular events was increased during anastrozole therapy and patients with pre-existing ischemic heart disease should consider the risks and benefits of anastrozole before beginning therapy. Anastrozole has also been reported to decrease spine and hip bone mineral density (BMD), so consideration should be given to monitoring of BMD in patients receiving long-term therapy.10,8

Mechanism of action

Anastrazole exerts its anti-estrogenic effects via selective and competitive inhibition of the aromatase enzyme found predominantly in the adrenal glands, liver, and fatty tissues.5 Many breast cancers are hormone receptor-positive, meaning their growth is stimulated and/or maintained by the presence of hormones such as estrogen or progesterone.10 In postmenopausal women, estrogen is primarily derived from the conversion of adrenally-produced androgens into estrogens by the aromatase enzyme - by competitively inhibiting the biosynthesis of estrogen at these enzymes, anastrozole effectively suppresses circulating estrogen levels and, subsequently, the growth of hormone receptor-positive tumours.5,9

TargetActionsOrganism
ACytochrome P450 19A1
inhibitor
Humans
Absorption

Anastrozole is rapidly absorbed and Tmax is typically reached within 2 hours of dosing under fasted conditions.5,12 Coadministration with food reduces the rate but not the overall extent of absorption - mean Cmax decreased by 16% and the median Tmax was extended to 5 hours when anastrozole was administered 30 minutes after ingestion of food,10 though this relatively minor alteration in absorption kinetics is not expected to result in clinically significant effects.11

Volume of distribution

The volume of distribution of anastrozole into brain tissue in mice is 3.19 mL/g. Distribution into the CNS is limited due to the activity of P-gp efflux pumps at the blood brain barrier, of which anastrozole is a substrate.2

Protein binding

Anastrozole is 40% protein bound in plasma10 and appears to be independent of plasma concentration.12

Metabolism

Anastrozole is primarily metabolized in the liver via oxidation and glucuronidation to a number of inactive metabolites, including hydroxyanastrozole (both free and glucuronidated) and anastrozole glucuronide.1,10,12 Oxidation to hydroxyanastrozole is catalyzed predominantly by CYP3A4 (as well as CYP3A5 and CYP2C8, to a lesser extent) and the direct glucuronidation of anastrozole appears to be catalyzed mainly by UGT1A4.1

Anastrozole may also undergo N-dealkylation to form triazole and 3,5-Bis-(2-methylpropiononitrile)-benzoic acid.1 Labels for anastrozole state the main metabolite found in plasma following administration is triazole,10,12 but a recent pharmacokinetic study was unable to detect any products of N-dealkylation in vitro.1

Hover over products below to view reaction partners

Route of elimination

Hepatic metabolism accounts for approximately 85% of anastrozole elimination.10 Approximately 10% of the administered dosage is eliminated unchanged in the urine.12,13

Half-life

The elimination half-life of anastrozole is approximately 50 hours.10,12,5

Clearance

Anastrozole's clearance is mainly via hepatic metabolism and can therefore be altered in patients with hepatic impairment - patients with stable hepatic cirrhosis exhibit an apparent oral clearance approximately 30% lower compared with patients with normal liver function.10,12 Conversely, renal impairment has a negligible effect on total drug clearance as the renal route is a relatively minor clearance pathway for anastrozole. In volunteers with severe renal impairment, renal clearance was reduced by 50% while total clearance was only reduced by approximately 10%.10,12

Adverse Effects
Learn about our commercial Adverse Effects data.
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Toxicity

The reported oral TDLo in a human woman is 1.68 mg/kg given intermittently over the course of 12 weeks.14 Knowledge of the signs and symptoms of anastrozole overdose is incomplete as there are no documented descriptions of a patient receiving more than 60mg,13 a dose which was administered to a healthy male volunteer and was well-tolerated.10,12 There is no antidote for anastrozole and treatment should be supportive and symptomatic, including close monitoring of patient vital signs. As anastrozole exhibits relatively low protein binding, dialysis may be helpful and should be considered in select cases.10,12

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

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbataceptThe metabolism of Anastrozole can be increased when combined with Abatacept.
AbirateroneThe metabolism of Anastrozole can be decreased when combined with Abiraterone.
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Anastrozole.
AdalimumabThe metabolism of Anastrozole can be increased when combined with Adalimumab.
AlmotriptanThe metabolism of Anastrozole can be decreased when combined with Almotriptan.
AlpelisibThe metabolism of Anastrozole can be decreased when combined with Alpelisib.
AminophenazoneThe metabolism of Aminophenazone can be decreased when combined with Anastrozole.
AmiodaroneThe metabolism of Amiodarone can be decreased when combined with Anastrozole.
AmitriptylineThe metabolism of Anastrozole can be decreased when combined with Amitriptyline.
AmodiaquineThe metabolism of Anastrozole can be decreased when combined with Amodiaquine.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
  • Take with or without food. Co-administration with food reduces the rate, but not the overall extent, of absorption.

Products

Product Images
International/Other Brands
Asiolex
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
AnastrozoleTablet1 mgOralSanis Health Inc2015-07-22Not applicableCanada flag
AnastrozoleTablet, film coated1 mg/1OralGlobal Pharmaceuticals2013-06-052013-08-26US flag
AnastrozoleTablet1 mgOralPro Doc Limitee2012-11-22Not applicableCanada flag
AnastrozoleTablet, coated1 mg/1OralBoscogen, Inc.2011-03-31Not applicableUS flag
ArimidexTablet1 mg/1OralPhysicians Total Care, Inc.2004-02-19Not applicableUS flag
ArimidexTablet1 mg/1OralAstraZeneca Pharmaceuticals LP1996-01-162019-06-30US flag
ArimidexTablet1 mg/1OralANI Pharmaceuticals, Inc.2018-06-26Not applicableUS flag
Arimidex Tab 1mgTabletOralAstra Zeneca1996-08-30Not applicableCanada flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Accel-anastrozole TabletsTabletOralAccel Pharma IncNot applicableNot applicableCanada flag
Ach-anastrozoleTabletOralAccord Healthcare Inc2012-10-25Not applicableCanada flag
AnastrozoleTablet1 mg/1OralNucare Pharmaceuticals,inc.2010-06-22Not applicableUS flag
AnastrozoleTablet1 mg/1OralPreferred Pharmaceuticals, Inc.2016-10-24Not applicableUS flag68788 677420180913 8702 1iaodhg
AnastrozoleTablet, coated1 mg/1OralAmerican Health Packaging2016-01-15Not applicableUS flag
AnastrozoleTablet1 mg/1OralPhysicians Total Care, Inc.2010-07-01Not applicableUS flag
AnastrozoleTablet1 mg/1OralFresenius Kabi USA, LLC2010-06-282012-10-18US flag
AnastrozoleTablet1 mg/1OralDispensing Solutions, Inc.2010-06-28Not applicableUS flag
AnastrozoleTablet1 mg/1OralAccord Healthcare Inc.2010-06-22Not applicableUS flag
AnastrozoleTablet, film coated1 mg/1OralMylan Institutional2010-06-112013-09-30US flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Testosterone / AnastrozoleAnastrozole (20 mg/1) + Testosterone (200 mg/1)PelletOralQualgen Llc2017-11-14Not applicableUS flag

Categories

ATC Codes
L02BG03 — Anastrozole
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as phenylpropanes. These are organic compounds containing a phenylpropane moiety.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Phenylpropanes
Direct Parent
Phenylpropanes
Alternative Parents
Triazoles / Heteroaromatic compounds / Nitriles / Azacyclic compounds / Organopnictogen compounds / Hydrocarbon derivatives
Substituents
1,2,4-triazole / Aromatic heteromonocyclic compound / Azacycle / Azole / Carbonitrile / Heteroaromatic compound / Hydrocarbon derivative / Nitrile / Organic nitrogen compound / Organoheterocyclic compound
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
nitrile, triazoles (CHEBI:2704)

Chemical Identifiers

UNII
2Z07MYW1AZ
CAS number
120511-73-1
InChI Key
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-yl)methyl]phenyl]-2-methylpropanenitrile
SMILES
CC(C)(C#N)C1=CC(=CC(CN2C=NC=N2)=C1)C(C)(C)C#N

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. Kamdem LK, Liu Y, Stearns V, Kadlubar SA, Ramirez J, Jeter S, Shahverdi K, Ward BA, Ogburn E, Ratain MJ, Flockhart DA, Desta Z: In vitro and in vivo oxidative metabolism and glucuronidation of anastrozole. Br J Clin Pharmacol. 2010 Dec;70(6):854-69. doi: 10.1111/j.1365-2125.2010.03791.x. [PubMed:21175441]
  2. Miyajima M, Kusuhara H, Takahashi K, Takashima T, Hosoya T, Watanabe Y, Sugiyama Y: Investigation of the effect of active efflux at the blood-brain barrier on the distribution of nonsteroidal aromatase inhibitors in the central nervous system. J Pharm Sci. 2013 Sep;102(9):3309-19. doi: 10.1002/jps.23600. Epub 2013 May 27. [PubMed:23712697]
  3. Gervasini G, Jara C, Olier C, Romero N, Martinez R, Carrillo JA: Polymorphisms in ABCB1 and CYP19A1 genes affect anastrozole plasma concentrations and clinical outcomes in postmenopausal breast cancer patients. Br J Clin Pharmacol. 2017 Mar;83(3):562-571. doi: 10.1111/bcp.13130. Epub 2016 Oct 18. [PubMed:27747906]
  4. Buzdar AU, Robertson JF, Eiermann W, Nabholtz JM: An overview of the pharmacology and pharmacokinetics of the newer generation aromatase inhibitors anastrozole, letrozole, and exemestane. Cancer. 2002 Nov 1;95(9):2006-16. doi: 10.1002/cncr.10908. [PubMed:12404296]
  5. Barros-Oliveira MDC, Costa-Silva DR, Andrade DB, Borges US, Tavares CB, Borges RS, Silva JM, Silva BBD: Use of anastrozole in the chemoprevention and treatment of breast cancer: A literature review. Rev Assoc Med Bras (1992). 2017 Apr;63(4):371-378. doi: 10.1590/1806-9282.63.04.371. [PubMed:28614542]
  6. Grimm SW, Dyroff MC: Inhibition of human drug metabolizing cytochromes P450 by anastrozole, a potent and selective inhibitor of aromatase. Drug Metab Dispos. 1997 May;25(5):598-602. [PubMed:9152599]
  7. Kelly CM, Buzdar AU: Anastrozole. Expert Opin Drug Saf. 2010 Nov;9(6):995-1003. doi: 10.1517/14740338.2010.515977. [PubMed:20923259]
  8. Cuzick J, Sestak I, Baum M, Buzdar A, Howell A, Dowsett M, Forbes JF: Effect of anastrozole and tamoxifen as adjuvant treatment for early-stage breast cancer: 10-year analysis of the ATAC trial. Lancet Oncol. 2010 Dec;11(12):1135-41. doi: 10.1016/S1470-2045(10)70257-6. Epub 2010 Nov 17. [PubMed:21087898]
  9. Gobbi S, Rampa A, Belluti F, Bisi A: Nonsteroidal aromatase inhibitors for the treatment of breast cancer: an update. Anticancer Agents Med Chem. 2014 Jan;14(1):54-65. [PubMed:23869785]
  10. FDA Approved Drug Products: Arimidex (anastrozole) oral tablets [Link]
  11. EMA Approved Drugs: Anastrozole [Link]
  12. DPD Approved Drugs: Anastrozole [Link]
  13. Medsafe NZ: Anastrozole [Link]
  14. CaymenChem: Anastrozole MSDS [Link]
Human Metabolome Database
HMDB0015348
KEGG Drug
D00960
KEGG Compound
C08159
PubChem Compound
2187
PubChem Substance
46504987
ChemSpider
2102
BindingDB
10015
RxNav
84857
ChEBI
2704
ChEMBL
CHEMBL1399
ZINC
ZINC000000000941
Therapeutic Targets Database
DAP000627
PharmGKB
PA448432
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Anastrozole
AHFS Codes
  • 10:00.00 — Antineoplastic Agents

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedHealth Services ResearchBreast Cancer1
4CompletedTreatmentBreast Cancer4
4CompletedTreatmentEarly Breast Cancer1
4CompletedTreatmentEndometriosis1
4CompletedTreatmentHormono-depending Adjuvant Breast Cancer1
4CompletedTreatmentHypogonadism / Obesity, Severe1
4RecruitingTreatmentBMI >30 kg/m2 / Hypogonadism, Hypogonadotropic1
4RecruitingTreatmentEarly Breast Cancer1
4RecruitingTreatmentNeoplasms, Breast1
4Unknown StatusTreatmentBreast Cancer1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Accord Healthcare
  • Ascend Laboratories LLC
  • AstraZeneca Inc.
  • Breckenridge Pharmaceuticals
  • Cadila Healthcare Ltd.
  • Cypress Pharmaceutical Inc.
  • Doctor Reddys Laboratories Ltd.
  • Kaiser Foundation Hospital
  • Karalex Pharmaceuticals
  • Lake Erie Medical and Surgical Supply
  • Medisca Inc.
  • Murfreesboro Pharmaceutical Nursing Supply
  • Mylan
  • Physicians Total Care Inc.
  • Resource Optimization and Innovation LLC
  • Roxane Labs
  • Sandoz
  • Teva Pharmaceutical Industries Ltd.
  • Three Rivers Pharmaceuticals LLC
  • UDL Laboratories
  • Zeneca Pharma Inc.
  • Zydus Pharmaceuticals
Dosage Forms
FormRouteStrength
Tablet, film coatedOral1 MG
Tablet, film coated1 mg
TabletOral1 mg/1
TabletOral1 mg
Tablet, coatedOral1 mg/1
Tablet, film coatedOral1 mg/1
Tablet
Tablet, film coatedOral
TabletOral
Tablet, coated1 mg
Tablet, coatedOral1 mg
Tablet1 mg
PelletOral
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)Region
USRE36617No2000-03-142010-06-27US flag
CA1337420No1995-10-242012-10-24Canada flag
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

    Learn more

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubility0.53 mg/mLCanadian label (DPD)
logP1.58Canadian label (DPD)
pKa1.4Canadian label (DPD)
Predicted Properties
PropertyValueSource
Water Solubility0.0661 mg/mLALOGPS
logP2.31ALOGPS
logP3.03ChemAxon
logS-3.6ALOGPS
pKa (Strongest Basic)2ChemAxon
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 RuleNoChemAxon
MDDR-like RuleNoChemAxon
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)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, 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, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-004l-1390000000-8636c0aef7d79b805328
MS/MS Spectrum - , positiveLC-MS/MSsplash10-004l-0190000000-739ac0c546bb150b1c60
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-004i-0090000000-8ccdc5fa9f18334eae92

Targets

Details
1. Cytochrome P450 19A1
Kind
Protein
Organism
Humans
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
Uniprot Name
Aromatase
Molecular Weight
57882.48 Da
References
  1. Buzdar AU, Robertson JF, Eiermann W, Nabholtz JM: An overview of the pharmacology and pharmacokinetics of the newer generation aromatase inhibitors anastrozole, letrozole, and exemestane. Cancer. 2002 Nov 1;95(9):2006-16. doi: 10.1002/cncr.10908. [PubMed:12404296]
  2. Miller WR: Aromatase inhibitors: mechanism of action and role in the treatment of breast cancer. Semin Oncol. 2003 Aug;30(4 Suppl 14):3-11. [PubMed:14513432]
  3. Kelly CM, Buzdar AU: Anastrozole. Expert Opin Drug Saf. 2010 Nov;9(6):995-1003. doi: 10.1517/14740338.2010.515977. [PubMed:20923259]
  4. FDA Approved Drug Products: Arimidex (anastrozole) oral tablets [Link]
  5. DPD Approved Drugs: Anastrozole [Link]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
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. Kamdem LK, Liu Y, Stearns V, Kadlubar SA, Ramirez J, Jeter S, Shahverdi K, Ward BA, Ogburn E, Ratain MJ, Flockhart DA, Desta Z: In vitro and in vivo oxidative metabolism and glucuronidation of anastrozole. Br J Clin Pharmacol. 2010 Dec;70(6):854-69. doi: 10.1111/j.1365-2125.2010.03791.x. [PubMed:21175441]
  2. Grimm SW, Dyroff MC: Inhibition of human drug metabolizing cytochromes P450 by anastrozole, a potent and selective inhibitor of aromatase. Drug Metab Dispos. 1997 May;25(5):598-602. [PubMed:9152599]
  3. FDA Approved Drug Products: Arimidex (anastrozole) oral tablets [Link]
  4. DPD Approved Drugs: Anastrozole [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
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
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. Kamdem LK, Liu Y, Stearns V, Kadlubar SA, Ramirez J, Jeter S, Shahverdi K, Ward BA, Ogburn E, Ratain MJ, Flockhart DA, Desta Z: In vitro and in vivo oxidative metabolism and glucuronidation of anastrozole. Br J Clin Pharmacol. 2010 Dec;70(6):854-69. doi: 10.1111/j.1365-2125.2010.03791.x. [PubMed:21175441]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
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
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. Kamdem LK, Liu Y, Stearns V, Kadlubar SA, Ramirez J, Jeter S, Shahverdi K, Ward BA, Ogburn E, Ratain MJ, Flockhart DA, Desta Z: In vitro and in vivo oxidative metabolism and glucuronidation of anastrozole. Br J Clin Pharmacol. 2010 Dec;70(6):854-69. doi: 10.1111/j.1365-2125.2010.03791.x. [PubMed:21175441]
  2. FDA Approved Drug Products: Arimidex (anastrozole) oral tablets [Link]
  3. DPD Approved Drugs: Anastrozole [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Protein homodimerization activity
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...
Gene Name
UGT1A4
Uniprot ID
P22310
Uniprot Name
UDP-glucuronosyltransferase 1-4
Molecular Weight
60024.535 Da
References
  1. Kamdem LK, Liu Y, Stearns V, Kadlubar SA, Ramirez J, Jeter S, Shahverdi K, Ward BA, Ogburn E, Ratain MJ, Flockhart DA, Desta Z: In vitro and in vivo oxidative metabolism and glucuronidation of anastrozole. Br J Clin Pharmacol. 2010 Dec;70(6):854-69. doi: 10.1111/j.1365-2125.2010.03791.x. [PubMed:21175441]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Retinoic acid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. Isoform 2 lacks transferase activity but acts as a negative reg...
Gene Name
UGT1A3
Uniprot ID
P35503
Uniprot Name
UDP-glucuronosyltransferase 1-3
Molecular Weight
60337.835 Da
References
  1. Kamdem LK, Liu Y, Stearns V, Kadlubar SA, Ramirez J, Jeter S, Shahverdi K, Ward BA, Ogburn E, Ratain MJ, Flockhart DA, Desta Z: In vitro and in vivo oxidative metabolism and glucuronidation of anastrozole. Br J Clin Pharmacol. 2010 Dec;70(6):854-69. doi: 10.1111/j.1365-2125.2010.03791.x. [PubMed:21175441]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Glucuronosyltransferase activity
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds.Its unique specificity for 3,4-catechol estrogens and estriol su...
Gene Name
UGT2B7
Uniprot ID
P16662
Uniprot Name
UDP-glucuronosyltransferase 2B7
Molecular Weight
60694.12 Da
References
  1. Kamdem LK, Liu Y, Stearns V, Kadlubar SA, Ramirez J, Jeter S, Shahverdi K, Ward BA, Ogburn E, Ratain MJ, Flockhart DA, Desta Z: In vitro and in vivo oxidative metabolism and glucuronidation of anastrozole. Br J Clin Pharmacol. 2010 Dec;70(6):854-69. doi: 10.1111/j.1365-2125.2010.03791.x. [PubMed:21175441]
Kind
Protein
Organism
Humans
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. Grimm SW, Dyroff MC: Inhibition of human drug metabolizing cytochromes P450 by anastrozole, a potent and selective inhibitor of aromatase. Drug Metab Dispos. 1997 May;25(5):598-602. [PubMed:9152599]
  2. FDA Approved Drug Products: Arimidex (anastrozole) oral tablets [Link]
  3. DPD Approved Drugs: Anastrozole [Link]
Kind
Protein
Organism
Humans
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. Grimm SW, Dyroff MC: Inhibition of human drug metabolizing cytochromes P450 by anastrozole, a potent and selective inhibitor of aromatase. Drug Metab Dispos. 1997 May;25(5):598-602. [PubMed:9152599]
  2. FDA Approved Drug Products: Arimidex (anastrozole) oral tablets [Link]
  3. DPD Approved Drugs: Anastrozole [Link]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Miyajima M, Kusuhara H, Takahashi K, Takashima T, Hosoya T, Watanabe Y, Sugiyama Y: Investigation of the effect of active efflux at the blood-brain barrier on the distribution of nonsteroidal aromatase inhibitors in the central nervous system. J Pharm Sci. 2013 Sep;102(9):3309-19. doi: 10.1002/jps.23600. Epub 2013 May 27. [PubMed:23712697]
  2. Gervasini G, Jara C, Olier C, Romero N, Martinez R, Carrillo JA: Polymorphisms in ABCB1 and CYP19A1 genes affect anastrozole plasma concentrations and clinical outcomes in postmenopausal breast cancer patients. Br J Clin Pharmacol. 2017 Mar;83(3):562-571. doi: 10.1111/bcp.13130. Epub 2016 Oct 18. [PubMed:27747906]

Drug created on June 13, 2005 07:24 / Updated on October 21, 2020 01:55

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