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Information About Anastrozole

Anastrozole is in a class of medications called nonsteroidal aromatase inhibitors. Anastrozole is a non-steroidal aromatase-inhibiting drug approved for treatment of breast cancer after surgery, as well as for metastasis in both pre and post-menopausal women. It works by decreasing the amount of estrogen the body makes. This can slow or stop the growth of many types of breast cancer cells that need estrogen to grow. 1. Medical uses The ATAC (Arimidex, Tamoxifen, Alone or in Combination) trial was an international randomised controlled trial of 9366 women with localized breast cancer who received either anastrozole, tamoxifen, or both for five years, followed by five years of follow-up.After more than 5 years the group that received anastrozole had significantly better clinical results than the tamoxifen group. The trial suggested that anastrozole is the preferred medical therapy for postmenopausal women with localized breast cancer, which is estrogen receptor (ER) positive. Another study found that the risk of recurrence was reduced 40%, but was associated with an increased risk of bone fractures. The study concluded that ER positive patients benefited from switching from tamoxifen to anastrozole in patients who have completed 2 years' adjuvant tamoxifen. A more recent trial found that anastrozole significantly reduced the incidence of breast cancer in postmenopausal women relative to placebo, and while there were side effects related to estrogen deprivation observed, the researchers concluded that this was probably not related to the treatment. Lead author Jack Cuzick was quoted by the BBC as saying, "This class of drugs is more effective than previous drugs such as tamoxifen and crucially, it has fewer side effects," adding that he thought there was now enough evidence to support offering the drug. 2. Side effects Bone weakness has been associated with anastrozole. Women who switched to anastrozole after two years on tamoxifen reported twice as many fractures as those who continued to take tamoxifen (2.1% compared to 1%).[6] Bisphosphonates are sometimes prescribed to prevent the osteoporosis induced by aromatase inhibitors. The level of circulating estradiol is likely causal here and not the anastrozole itself, and so the dose will determine likelihood of osteoporosis (estradiol inhibits osteoclasts, which resorb bone). 3. Storage and disposal Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture (not in the bathroom). Throw away any medication that is outdated or no longer needed. Talk to your pharmacist about the

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proper disposal of your medication. 4. Forget a dose Take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one. 5. Chemical properties

Name:Anastrozole Molecular Formula:C17H19N5 CAS Registry Number:120511-73-1 InChI:InChI=1/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/h 5-7,11-12H,8H2,1-4H3 Appearance:crystalline solid Molecular Weight:293.37 Density:1.08 g/cm3 Boiling Point:469.7 oC at 760 mmHg Melting Point:81-82 Flash Point:469.7 oC at 760 mmHg Storage Temperature:Store in original container in a cool dark place. Refractive index:1.791 Solubility:Insoluble

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Biological Activity:Potent and highly selective aromatase (CYP19) inhibitor (IC 50 = 15nM) that has no discernible effect on adrenocorticoid hormone synthesis. Reduces plasma estrogen levels and exhibits antitumor activity in vivo . Orally active. Usage:An aromatase inhibitor. Used as an antineoplastic.