Vol 8, No 6 (2012)
Review paper
Published online: 2013-01-24
The place of exemestane in the treatment of advanced breast cancer in postmenopausal patients
Onkol. Prak. Klin 2012;8(6):246-251.
Abstract
„Third generation” aromatase inhibitors (AIs) are compounds with proven efficacy in the treatment of
early and advanced hormone sensitive breast cancer in postmenopausal women. Due to the distinct
mechanism of interaction with aromatase, AIs are divided into steroidal (exemestane) and nonsteroidal
(anastrozole, letrozole) inhibitors. AIs inhibit activity of aromatase — an enzyme involved in the conversion
of androgens (testosterone, androstenedione) into estrogens (estrone, 17-beta estradiol). In several phase
III studies all „third generation” AIs shown to be superior to tamoxifen and progestins in advanced breast
cancer. Due to partial non-cross resistance, sequential use of steroidal and nonsteroidal AIs may provide
considerable clinical benefit. Since non-steroidal AIs are typically used in first-line treatment, exemestane
constitutes a valuable second or third line treatment option. Recently, a combination of exemestane with
everolimus, an m-TOR (mammalian target of rapamycine) inhibitor, has been shown to provide clinical
benefit in patients progressing on nonsteroidal AIs.
early and advanced hormone sensitive breast cancer in postmenopausal women. Due to the distinct
mechanism of interaction with aromatase, AIs are divided into steroidal (exemestane) and nonsteroidal
(anastrozole, letrozole) inhibitors. AIs inhibit activity of aromatase — an enzyme involved in the conversion
of androgens (testosterone, androstenedione) into estrogens (estrone, 17-beta estradiol). In several phase
III studies all „third generation” AIs shown to be superior to tamoxifen and progestins in advanced breast
cancer. Due to partial non-cross resistance, sequential use of steroidal and nonsteroidal AIs may provide
considerable clinical benefit. Since non-steroidal AIs are typically used in first-line treatment, exemestane
constitutes a valuable second or third line treatment option. Recently, a combination of exemestane with
everolimus, an m-TOR (mammalian target of rapamycine) inhibitor, has been shown to provide clinical
benefit in patients progressing on nonsteroidal AIs.
Keywords: advanced breast cancerendocrine therapyaromatase inhibitorsexemestane