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http://linked.open...gbank/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. (en)
http://linked.open...y/drugbank/dosage
http://linked.open...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 (en)
http://linked.open...gy/drugbank/group
  • approved (en)
  • investigational (en)
http://linked.open...drugbank/halfLife
  • 50 hours (en)
http://linked.open...ugbank/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. (en)
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Title
  • Anastrozole (en)
adms:identifier
http://linked.open...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. (en)
http://linked.open...drugbank/packager
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http://linked.open...outeOfElimination
  • Hepatic metabolism accounts for approximately 85% of anastrozole elimination. Renal elimination accounts for approximately 10% of total clearance. (en)
http://linked.open.../drugbank/synonym
  • Anastrozol (en)
  • alpha,alpha,Alpha',alpha'-tetramethyl-5-(1H-1,2,4-triazol-1-ylmethyl)-m-benzenediacetonitrile (en)
http://linked.open...drugbank/toxicity
  • In rats, lethality is greater than 100 mg/kg. (en)
http://linked.open.../drug/hasAHFSCode
http://linked.open...k/foodInteraction
  • Food decreases the rate of absorption, but the extent of absorption is not affected. (en)
http://linked.open...nk/proteinBinding
  • 40% (en)
http://linked.open...ynthesisReference
  • Anil Khile, Narendra Joshi, Shekhar Bhirud, "Process for the preparation of anastrozole and intermediates thereof." U.S. Patent US20060189670, issued August 24, 2006. (en)
http://linked.open...y/mesh/hasConcept
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http://linked.open...ugbank/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. (en)
http://linked.open.../affectedOrganism
  • Humans and other mammals (en)
http://linked.open...casRegistryNumber
  • 120511-73-1 (en)
http://linked.open...drugbank/category
  • (en)
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