It has nothing to do with conversion. AI's weren't invented to stop aromatization from testosterone, but they do -- that's why bodybuilders use them. Breast cancer is exasperated by estro, which is why women use nolva.
Anastrozole
From Wikipedia, the free encyclopedia
Anastrozole (INN, trade name Arimidex, AstraZeneca) is a drug used to treat breast cancer after surgery and for metastases in post-menopausal women.
Anastrozole is an aromatase inhibitor, which means that it interrupts a critical step in the body's synthesis of estrogen. Some breast cancer cells require estrogen to grow, and eliminating estrogen suppresses their growth.
Annual sales approx $2.2bn. Patent expires 2010 in the US[1]; however, the generic form is available in some other markets.
Clinical trials
The ATAC (Arimidex, Tamoxifen, Alone or in Combination) trial was an international randomised controlled trial of 9366 women with localizedbreast cancer who received either anastrozole, tamoxifen, or both for five years, followed by five years of follow-up.[2] 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 that isestrogen receptor (ER) positive.
Another study found that the risk of recurrence was reduced 40% (with some risk of bone fracture) and that ER negative patients also benefited from switching to Arimidex.[3]
Mechanism of Action
Anastrozole inhibits the enzyme aromatase, which is responsible for convertingandrogens to estrogens. Anastrozole binds reversibly to the aromatase enzyme through competitive inhibition.
Elevated levels of estrogens may increase the severity of breast cancer, as sex hormones can cause hyperplasia and differentiation at estrogen receptor sites.
Side effects
Bone weakness : Women who switched to Arimidex (after two years on tamoxifen) reported twice as many fractures as those who continued to take tamoxifen (2.1% compared to 1%).[3]
Bisphosphonates are sometimes prescribed to prevent the osteoporosis induced by aromatase inhibitors but have another serious side effect, osteonecrosis of the jaws. Since statins have a bone strengthening effect [4], combining a statin with an aromatase inhibitor may avoid both fractures and possible cardiovascular risks [5]without jaw osteonecrosis.[6] In one study of women with breast cancer takinganastrozole, statin use was associated with a 38% reduced fracture risk, or approximately the equivalent of 10 mg Fosamax daily.
Anastrozole - Wikipedia, the free encyclopedia