4-Hydroxyandrostenedione treatment for postmenopausal patients with advanced breast cancer

Aromatase inhibitors as adjuvant treatment of breast cancer

“…However, its clinical efficacy [6] was soon revealed to be due to inhibition of peripheral aromatisation [7], the final step in estrogen synthesis in postmenopausal women [8]. This discovery, together with the subsequent observation by Coombes et al [9] that 4-hydroxyandrostenedione, a steroidal aromatase inactivator with no adrenotoxic effects, may cause tumor regression, established aromatase inhibition as a novel therapeutic strategy for endocrine treatment of advanced breast cancer in postmenopausal women.…”

David Kupfer and the Metabolism Connection: On Aromatase Inhibitors and Tamoxifen

“…Once 4-hydroxyandrostenedione (4-OHA), the first selective aromatase inhibitor to reach clinical trials, was found to be effective in patients with breast cancer (Coombs et al, 1984;Goss et al, 1986), the question of the place for aromatase inhibitors in treatment was then of considerable interest. Oncologists' confidence in tamoxifen was strong and grew out of years of experience with the drug.…”

Aromatase inhibitors for breast cancer

“…The first AI introduced into clinical use was aminoglutethimide [7] and multiple generations of AI have followed [8][9][10][11][12], because the first generation AI had an unselective mechanism of action, inhibiting a number of enzymes involved in steroid synthesis and resulting in undesirable side effects including the need for glucocorticoid replacement [13]. Three such third generation AI are now clinically available-anastrozole, letrozole, and exemestane.…”