Anastrozole can be used in pre-menopausal women as well
-anastrozole is an 'aromatase inhibitor', used in treatment of breast cancer.
-the enzyme aromatase is found in a number of human tissues and cells, including ovarian granulosa cells, the placental syncytio-trophoblast, adipose and skin fibroblasts, bone, and the brain, and it locally catalyzes the conversion of C(19) steroids to estrogens.
-aromatase expression in adipose tissue and possibly the skin primarily accounts for the extraglandular (peripheral) formation of estrogen
-fibroblasts at the tumor site in breast cancer tend to synthesize higher levels of aromatase.
-androstenedione is aromatised to estradione which subsequently is converted into estradiol in extra-glandular (peripheral) sites such as adipose tissue and skin fibroblasts. Estradiol produced in this manner is the cause of tumor growth, more so in post menopausal women than premenopausal women. Thus, anastrozole is more useful in former cases, but can also be used in latter cases.
-it is highly effective on estrogen receptor positive tumors.
- used in pre-menopausal (as well as post-menopausal women) after mastectomy, to treat metastases.
-also used alone or in combination with tamoxifen, in the pre-menopausal patients who do not respond to tamoxifen alone.
-can also be used safely in treatment of benign prostatic hyperplasia and gynaecomastia in elderly men.
-most significant adverse effects include osteoporosis and hyperlipidemia, both of which can be prevented using bisphosphonates and statins.