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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.
Drug Type: Small Molecule; Approved; Investigational
Pharmacology: Anastrozole 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 Action: 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 circulatin estrogen, leading to a decreased tumor mass or delayed progression of tumor growth in some women.
Indication: For treatment of breast cancer in post-menopausal women.
Half Life: 50 hours
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CYP19A1 100 100
STAC3 96 96
PON1 96 96
CA3 90 90
GJA1 89 89
RGN 89 89
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CUB Protein Family 100 100
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    Homo sapiens Homo sapiens | Therapeutic   Therapeutic

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    Authors: David S Wishart, Craig Knox, An Chi Guo et al.

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  • Jack Cuzick
  • M Baum
  • Aman U Buzdar
  • J Cuzick
  • ATAC Trialists' Group
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  • AstraZeneca
  • Baylor Breast Care Center
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  • Vienna Medical University
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  • University of Texas M.D. Anderson Cancer Center

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