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Exemestane is an irreversible, steroidal aromatase inactivator of type I, structurally related to the natural substrate 4-androstenedione. It acts as a false substrate for the aromatase enzyme, and is processed to an intermediate that binds irreversibly to the active site of the enzyme causing its inactivation, an effect also known as " suicide ...
Exemestane went through clinical trials in the 1990s and received FDA approval in 1999, marketed as Aromasin. Indication for exemestane is advanced breast cancer in postmenopausal women, where the cancer has progressed following tamoxifen therapy. Exemestane is the first oral aromatase inactivator. [5]
It can be used at a dosage of up to 500 mg four times per day (2,000 mg/day). [ 1 ] [ 8 ] It is used as an aromatase inhibitor to inhibit peripheral estrogen production by mouth at a dosage of 125 mg twice per day (250 mg/day total), without significant suppression of adrenal steroidogenesis at this dosage. [ 17 ]
The price of generic tadalafil can vary based on the dosage, but most versions of generic tadalafil cost $10 to $13 per tablet. When used daily, generic tadalafil can be less than $3 per pill ($79 ...
Ovarian stimulation with the aromatase inhibitor letrozole has been proposed for ovulation induction in order to treat unexplained female infertility. In a multi-center study funded by the National Institute of Child Health and Development, ovarian stimulation with letrozole resulted in a significantly lower frequency of multiple gestation (i.e., twins or triplets) but also a lower frequency ...
The price paid by pharmacists and doctors is determined mainly by the number of license holders, the sales value of the original brand, and the ease of manufacture. A typical price decay graph will show a "scalloped" curve, [25] which usually starts at the brand-name price on the day of generic launch and then falls as competition intensifies ...
Anastrozole works by reversibly binding to the aromatase enzyme, and through competitive inhibition blocks the conversion of androgens to estrogens in peripheral (extragonadal) tissues. [25] The medication has been found to achieve 96.7% to 97.3% inhibition of aromatase at a dosage of 1 mg/day and 98.1% inhibition of aromatase at a dosage of 10 ...
[19] [20] [61] It has been used orally at very high doses (30 mg/day) in the treatment of therapy-naive breast cancer and orally at low doses (2 to 6 mg/day) in the treatment of breast cancer in women who were previously treated with and benefited from but acquired resistance to aromatase inhibitors.