Anastrole
Brand names,
Anastrole
Analogs
Anastrole
Brand Names Mixture
Anastrole
Chemical_Formula
C17H19N5
Anastrole
RX_link
http://www.rxlist.com/cgi/generic2/anastr.htm
Anastrole
fda sheet
Anastrole
msds (material safety sheet)
Anastrole
Synthesis Reference
P.N. Edwards, M.S. Large, U.S. pat. 4,935,437(1989).
Anastrole
Molecular Weight
293.366 g/mol
Anastrole
Melting Point
130.14 oC
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H2O Solubility
0.5 mg/mL
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State
Solid
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LogP
4.501
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Dosage Forms
Tablet (1 mg)
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Indication
For treatment of breast cancer in post-menopausal women.
Anastrole
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.
Anastrole
Absorption
Well absorbed into the systemic cirulation following oral administration. Food does not affect the extent of absorption.
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side effects and Toxicity
In rats, lethality is greater than 100 mg/kg.
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Patient Information
ARIMIDEX is a prescription medicine that is approved by the Food and Drug
Administration (FDA) for adjuvant treatment (treatment following surgery
with or without radiation) in postmenopausal women with hormone receptor-positive
early breast cancer. Approval was based on study results from patients taking
ARIMIDEX as adjuvant treatment for a median of 21/2 years. In this ongoing study,
further follow-up of patients will be required to determine the long-term results,
including side effects and survival. ARIMIDEX significantly reduced the risk of
breast cancer returning compared with tamoxifen in this study, the largest-ever
breast cancer treatment trial. These results represent a preliminary comparison
with tamoxifen from this ongoing clinical trial.
Anastrole
Organisms Affected
Humans and other mammals