Abstract
Anastrozole (Arimidex™) is a third-generation aromatase inhibitor which has been shown to possess superior efficacy and tolerability over established endocrine agents in advanced breast cancer. Inhibition of aromatase prevents the conversion of androgen substrates to oestrogen, its sole source in postmenopausal women, thereby leading to regression of hormone-sensitive breast carcinomas. Clinical pharmacology data indicate that anastrozole is a potent aromatase inhibitor, providing near-maximal suppression of serum and intratumoural oestrogens to below detectable levels. Anastrozole may offer greater selectivity compared with other aromatase inhibitors, being without any intrinsic endocrine effects and with no apparent effect on the synthesis of adrenal steroids. It is well tolerated and has a convenient once-daily dosing regimen, ensuring maximum patient compliance. A major clinical programme has demonstrated that anastrozole is superior to the standard endocrine therapy, tamoxifen, for the first-line treatment of postmenopausal women with hormone-sensitive advanced breast cancer. Its superior efficacy in advanced disease, together with its improved tolerability and convenient dosage, make it a suitable agent to be assessed for the treatment of early breast cancer in postmenopausal women. This was investigated in the largest single adjuvant breast cancer study ever to be carried out, the ATAC (Arimidex, tamoxifen, alone or in combination) trial, which has now completed recruitment, with the first efficacy and safety data awaited. © 2001 Cancer Research Campaign
Keywords: anastrozole, aromatase inhibitor, tamoxifen, advanced breast cancer, adjuvant therapy, postmenopausal
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