catalyzed the synthesis of estrone and estradiol from the 4-en-3-one androgens androstenedione (AD) and testosterone. The aromatization process appears to proceed with three oxygenations at the C-19 position of the androgens, followed by the eventual loss of the C-19 angular methyl group and the elimination of the 1b ,2b-hydrogens, resulting in aromatization of the A-ring of the androgen molecu...

Using Western blot as the major technique, we studied the effects of the three Food and Drug Administration (FDA)-approved aromatase inhibitors (AI) on aromatase protein stability in the aromatase-overexpressing breast cancer cell line MCF-7aro. We have found that exemestane treatment significantly reduces aromatase protein level. Exemestane induces aromatase degradation in a dose-responsive ma...

Anastrozole (Arimidex), letrozole (Femara), and exemestane (Aromasin) are members of the third generation of aromatase inhibitors that has now replaced aminoglutethimide (Cytadren), the progestins, and tamoxifen (Nolvadex) as the hormonal therapy of choice in estrogen-receptor-positive, postmenopausal, metastatic breast cancer. This article will review the role of aromatase in the pathogenesis ...

Aromatase inhibitors (AIs) are most commonly used for breast cancer patients with hormone receptor positive disease. Although the side effect profile of aromatase inhibitors is well known, including common side effects like arthralgia, bone pain, arthritis, hot flashes, and more serious problems like osteoporosis, we present a case of an uncommon side effect of these medications. We report the ...

Hormone-dependent disease is an important and prevalent subtype of breast cancer. It is recognized by the presence of a functional estrogen-receptor apparatus, an indolent clinical course, a greater frequency in older women, and clinical responses to the sequential use of hormonal therapies. Antiestrogens, primarily tamoxifen (Nolvadex), have been the mainstay of hormonal therapy for metastatic...

Statins may be valuable for treating osteoporosis and have been associated with a reduced fracture risk. For example, Rejnmark et al. recently found statins to be associated with reduced fracture risk [1,2]. In another study, Scranton et al. found a significant reduction in fractures among statin users [3]. Dincer et al. have suggested that statins might reduce fractures in breast cancer patien...

Aminoglutethimide, the first aromatase inhibitor, was established in the 1970s as an active treatment for patients with advanced breast cancer, but its lack of specificity was associated with side effects. Since that time, a series of much more specific non-steroidal aromatase inhibitors has been developed which are up to 10 000 times as potent as aminoglutethimide in vivo with no evidence of i...

A number of potent and selective non-steroidal aromatase inhibitors are now available for treatment of advanced breast cancer in postmenopausal women, of which anastrozole and letrozole, in particular, represent a significant advantage over the earlier agents in terms of both efficacy and tolerability. These agents are rapidly becoming established as the second-line therapy of choice in postmen...

BACKGROUND Endocrine therapy constitutes a central modality in the treatment of oestrogen receptor (ER)-positive advanced breast cancer. PURPOSE To evaluate the evidence for endocrine treatment in postmenopausal patients with advanced breast cancer focusing on the aromatase inhibitors, letrozole, anastrozole, exemestane and fulvestrant. METHODS A review was carried out using PubMed. Randomi...

Aromatase inhibitors (AIs), such as anastrozole, are established in the treatment of hormone-dependent breast cancer. However, ∼20% of patients with hormone receptor-positive breast tumors treated with anastrozole do not respond and it remains impossible to accurately predict sensitivity. Since polymorphisms in the aromatase gene may influence the response to inhibitory drugs, we evaluated the ...