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Namespace Prefixes

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Statements

Subject Item
n2:DB01217
rdf:type
n3:Drug
n3:description
Anastrozole 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.
n3:dosage
n7:271B5832-363D-11E5-9242-09173F13E4C5 n7:271B5833-363D-11E5-9242-09173F13E4C5 n7:271B5834-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# 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":http://www.ncbi.nlm.nih.gov/pubmed/15639680 # 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. Epub 2009 May 26. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/19470631 # 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":http://www.ncbi.nlm.nih.gov/pubmed/16439860 # 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":http://www.ncbi.nlm.nih.gov/pubmed/19794821 # 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":http://www.ncbi.nlm.nih.gov/pubmed/19753124 # 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. Epub 2009 Apr 23. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/19389994
n3:group
investigational approved
n3:halfLife
50 hours
n3:indication
For 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.
owl:sameAs
n16:DB01217 n24:DB01217
dcterms:title
Anastrozole
adms:identifier
n20:Anastrozole n21:0310-0201-30 n22:PA448432 n23:C08159 n25:D00960 n26:2187 n27:46504987 n28:10015 n29:DB01217 n30:2704 n31:2102
n3:mechanismOfAction
Anastrozole 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.
n3:packager
n17:271B581B-363D-11E5-9242-09173F13E4C5 n17:271B581C-363D-11E5-9242-09173F13E4C5 n17:271B581A-363D-11E5-9242-09173F13E4C5 n17:271B5823-363D-11E5-9242-09173F13E4C5 n17:271B5824-363D-11E5-9242-09173F13E4C5 n17:271B5821-363D-11E5-9242-09173F13E4C5 n17:271B5822-363D-11E5-9242-09173F13E4C5 n17:271B581F-363D-11E5-9242-09173F13E4C5 n17:271B5820-363D-11E5-9242-09173F13E4C5 n17:271B581D-363D-11E5-9242-09173F13E4C5 n17:271B581E-363D-11E5-9242-09173F13E4C5 n17:271B582B-363D-11E5-9242-09173F13E4C5 n17:271B582C-363D-11E5-9242-09173F13E4C5 n17:271B5829-363D-11E5-9242-09173F13E4C5 n17:271B582A-363D-11E5-9242-09173F13E4C5 n17:271B5827-363D-11E5-9242-09173F13E4C5 n17:271B5828-363D-11E5-9242-09173F13E4C5 n17:271B5825-363D-11E5-9242-09173F13E4C5 n17:271B5826-363D-11E5-9242-09173F13E4C5 n17:271B582D-363D-11E5-9242-09173F13E4C5 n17:271B582E-363D-11E5-9242-09173F13E4C5 n17:271B5819-363D-11E5-9242-09173F13E4C5
n3:patent
n18:RE36617 n18:1337420
n3:routeOfElimination
Hepatic metabolism accounts for approximately 85% of anastrozole elimination. Renal elimination accounts for approximately 10% of total clearance.
n3:synonym
alpha,alpha,Alpha',alpha'-tetramethyl-5-(1H-1,2,4-triazol-1-ylmethyl)-m-benzenediacetonitrile Anastrozol
n3:toxicity
In rats, lethality is greater than 100 mg/kg.
n12:hasAHFSCode
n13:10-00-00
n3:foodInteraction
Food decreases the rate of absorption, but the extent of absorption is not affected.
n3:proteinBinding
40%
n3:synthesisReference
Anil Khile, Narendra Joshi, Shekhar Bhirud, "Process for the preparation of anastrozole and intermediates thereof." U.S. Patent US20060189670, issued August 24, 2006.
n9:hasConcept
n10:M0238999
foaf:page
n6:anastrozole.html n8:anastr.htm n32:ari1028.shtml
n3:IUPAC-Name
n4:271B5839-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B583F-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B583E-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B583B-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B583C-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B583D-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n4:271B584E-363D-11E5-9242-09173F13E4C5 n4:271B5837-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B5838-363D-11E5-9242-09173F13E4C5 n4:271B5850-363D-11E5-9242-09173F13E4C5 n4:271B5835-363D-11E5-9242-09173F13E4C5
n3:logS
n4:271B5836-363D-11E5-9242-09173F13E4C5
n12:hasATCCode
n33:L02BG03
n3:H-Bond-Acceptor-Count
n4:271B5845-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B5846-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B5840-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B5841-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B5843-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B5842-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B5844-363D-11E5-9242-09173F13E4C5
n3:absorption
Rapidly 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.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
120511-73-1
n3:category
n3:containedIn
n14:271B5830-363D-11E5-9242-09173F13E4C5 n14:271B5831-363D-11E5-9242-09173F13E4C5 n14:271B582F-363D-11E5-9242-09173F13E4C5
n3:Bioavailability
n4:271B584A-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B584C-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B584D-363D-11E5-9242-09173F13E4C5
n3:Melting-Point
n4:271B584F-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B5849-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B5848-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B584B-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B583A-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n4:271B5847-363D-11E5-9242-09173F13E4C5