ABSTRACT

I. ABSTRACT Since the introduction of aminoglutethimide, the first aromatase inhibitor, for breast cancer treatment 30 years ago, these drugs have achieved increasing importance in the therapy of advanced breast cancer and are currently being evaluated in the adjuvant setting. The third-generation aromatase inhibitors and inactivators-principally anastrozole, letrozole, and exemestane-all exhibit potent biochemical efficacy, with 97-99% aromatase inhibition. In addition, these drugs are well tolerated, and clinical studies have revealed their superiority over conventional drugs (aminoglutethimide and megestrol acetate) in second-line therapy.