WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 100060
Description: Anastrazole is a nonsteroidal inhibitor of estrogen synthesis that resembles paclitaxel in chemical structure. As a third-generation aromatase inhibitor, anastrozole selectively binds to and reversibly inhibits aromatase, a cytochrome P-450 enzyme complex found in many tissues including those of the premenopausal ovary, liver, and breast; aromatase catalyzes the aromatization of androstenedione and testosterone into estrone and estradiol, the final step in estrogen biosynthesis. In estrogen-dependent breast cancers, anastrozole may inhibit tumor growth. (
MedKoo Cat#: 100060
Chemical Formula: C17H19N5
Exact Mass: 293.16405
Molecular Weight: 293.36626
Elemental Analysis: C, 69.60; H, 6.53; N, 23.87
Synonym: ZD-1033; ZD 1033; ZD1033; CCRIS 9352; HSDB 7462; ICI D1033; Anastrozole; Brand name: Arimidex. Abbreviation: ANAS.
IUPAC/Chemical Name: 2,2'-(5-((1H-1,2,4-triazol-1-yl)methyl)-1,3-phenylene)bis(2-methylpropanenitrile)
InChi Key: YBBLVLTVTVSKRW-UHFFFAOYSA-N
InChi Code: 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
SMILES Code: CC(C1=CC(CN2N=CN=C2)=CC(C(C)(C)C#N)=C1)(C)C#N
Anastrozole is an off-white powder with a molecular weight of 293.4. Anastrozole has moderate aqueous solubility (0.5 mg/mL at 25Â°C); solubility is independent of pH in the physiological range. Anastrozole is freely soluble in methanol, acetone, ethanol, and tetrahydrofuran, and very soluble in acetonitrile. Each tablet contains as inactive ingredients: lactose, magnesium stearate, hydroxypropylmethylcellulose, polyethylene glycol, povidone, sodium starch glycolate, and titanium dioxide.
The growth of many cancers of the breast is stimulated or maintained by estrogens. Treatment of breast cancer thought to be hormonally responsive (i.e., estrogen and/or progesterone receptor positive or receptor unknown) has included a variety of efforts to decrease estrogen levels (ovariectomy, adrenalectomy, hypophysectomy) or inhibit estrogen effects (antiestrogens and progestational agents). These interventions lead to decreased tumor mass or delayed progression of tumor growth in some women. In postmenopausal women, estrogens are mainly derived from the action of the aromatase enzyme, which converts adrenal androgens (primarily androstenedione and testosterone) to estrone and estradiol. The suppression of estrogen biosynthesis in peripheral tissues and in the cancer tissue itself can therefore be achieved by specifically inhibiting the aromatase enzyme. 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.
According to http://en.wikipedia.org/wiki/Anastrozole, Annual sales approx $2.2bn. Patent expires 2010 in the US; however, the generic form is available in some other markets.
1: Geisler J. Differences between the non-steroidal aromatase inhibitors anastrozole and letrozole--of clinical importance? Br J Cancer. 2011 Mar 29;104(7):1059-66. doi: 10.1038/bjc.2011.58. Epub 2011 Mar 1. Review. PubMed PMID: 21364577; PubMed Central PMCID: PMC3068499.
2: Kelly CM, Buzdar AU. Anastrozole. Expert Opin Drug Saf. 2010 Nov;9(6):995-1003. doi: 10.1517/14740338.2010.515977. Review. PubMed PMID: 20923259.
3: Nabholtz JM, Mouret-Reynier MA, Durando X, Van Praagh I, Al-Sukhun S, Ferriere JP, Chollet P. Comparative review of anastrozole, letrozole and exemestane in the management of early breast cancer. Expert Opin Pharmacother. 2009 Jun;10(9):1435-47. doi: 10.1517/14656560902953738. Review. PubMed PMID: 19445563.
4: Needleman SJ, Tobias JS. Review of the ATAC study: tamoxifen versus anastrozole in early-stage breast cancer. Expert Rev Anticancer Ther. 2008 Dec;8(12):1871-81. doi: 10.1586/14737188.8.131.521. Review. PubMed PMID: 19046107.
5: Sanford M, Plosker GL. Anastrozole: a review of its use in postmenopausal women with early-stage breast cancer. Drugs. 2008;68(9):1319-40. Review. PubMed PMID: 18547136.
6: Graham PH. Anastrozole for malignant and benign conditions: present applications and future therapeutic integrations. Expert Opin Pharmacother. 2007 Oct;8(14):2347-57. Review. PubMed PMID: 17927488.
7: Bertoli LF, Barton JC. Remission of porphyria cutanea tarda after anastrozole treatment of breast cancer. Clin Breast Cancer. 2007 Aug;7(9):716-8. Review. PubMed PMID: 17919354.
8: van Nes JG, Seynaeve C, van de Velde CJ, Nortier JW. [Optimal adjuvant hormone therapy in postmenopausal women with hormone-sensitive mammary carcinoma: tamoxifen and the aromatase inhibitors anastrozole, exemestane and letrozole]. Ned Tijdschr Geneeskd. 2006 Dec 30;150(52):2863-9. Review. Dutch. PubMed PMID: 17319217.
9: Jakesz R. The adjuvant endocrine treatment revolution: focus on anastrozole. Expert Opin Drug Metab Toxicol. 2006 Apr;2(2):301-12. Review. PubMed PMID: 16866615.
10: Buzdar AU. Anastrozole for breast cancer: recent advances and ongoing challenges. Expert Rev Anticancer Ther. 2006 Jun;6(6):839-48. Review. PubMed PMID: 16761927.