Anastrozole

CAS:120511-73-1

MF:C17H19N5

MW:293.37

Synonyms:ICI-D-1033;ARIMIDEX;1-[3,5-DI-(1-METHYL-1-CYANO)-ETHYL]-BENZYL-1,2,4-TRIAZOLE;ANASTRAZOLE;ANASTROZOLE;tetramethyl-5-(1h-1,2,4-triazol-1ylmethyl) 1,3-benzenediacetionitrile;ZD-1033;1,3-benzenediacetonitrile,alpha,alpha,alpha' ,alpha' -tetramethyl-5-(1h-1,2,4-t

Properties

Melting point:81-82°C

storage temp. Store at RT

solubility DMSO: soluble40mg/mL

InChIKeyYBBLVLTVTVSKRW-UHFFFAOYSA-N

Safety Information

Symbol(GHS)

Description

Arimidex does not have the side effects of aminoglutethimide (Cytadren) and can achieve a high degree of estrogen blockade, much moreso than Cytadren. It is possible to reduce estrogen too much with Arimidex, and for this reason blood tests, or less preferably salivary tests, should be taken after the first week of use to determine if the dosing is correct.
As an aromatase inhibitor, Arimidex's mechanism of action - blocking conversion of aromatizable steroids to estrogen - is in contrast to the mechanism of action of anti-estrogens such as clomiphene (Clomid) or tamoxifen (Nolvadex), which block estrogen receptors in some tissues, and activate estrogen receptors in others. During a cycle, if using Arimidex, there is generally no need to use Clomid as well, but (as mentioned in the section on Clomid) there may still be benefits to doing so.
Arimidex at 0.5 mg/day is usually sufficient for moderate dosages of testosterone and in some cases may be too much.

Specifications

How ARIMIDEX works?
ARIMIDEX lowers the amount of oestrogen in the body. The female sex hormones oestrogen and progesterone stimulate many breast cancers to grow. Lowering the level of oestrogen can stop or slow the growth of breast cancer cells.
ARIMIDEX blocks a process called aromatisation which changes sex hormones called androgens into oestrogen. This happens mainly in the fatty tissues, muscle and the skin and needs a particular enzyme called aromatase.
Mechanism of Action:
The growth of many cancers of the breast is stimulated or maintained by estrogens.
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.
ARIMIDEX is a selective non-steroidal aromatase inhibitor. It significantly lowers serum estradiol concentrations and has no detectable effect on formation of adrenal corticosteroids or aldosterone.
Adjuvant Treatment:
ARIMIDEX is indicated for adjuvant treatment of postmenopausal women with hormone receptor-positive early breast cancer.
First-Line Treatment:
ARIMIDEX is indicated for the first-line treatment of postmenopausal women with hormone receptor-positive or hormone receptor unknown locally advanced or metastatic breast cancer.
Second-Line Treatment:
ARIMIDEX is indicated for the treatment of advanced breast cancer in postmenopausal women with disease progression following tamoxifen therapy. Patients with ER-negative disease and patients who did not respond to previous tamoxifen therapy rarely responded to ARIMIDEX.
Dosage and direction:
Follow all instructions of your doctor about treatment and dosing schedule. Do not take more of this medication than it was administered to you. Take once daily.
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