Purpose: Endocrine therapy is a well-recognized approach to the treatment o
f postmenopausal patients with advanced breast cancer, particularly those w
ith estrogen receptor-positive tumors. The availability of anti-aromatase a
gents, both reversible (nonsteroidal) and irreversible (steroidal), provide
s clinicians with additional hormonal treatment options. Methods: A MEDLINE
search was conducted to identify studies that evaluated anti-aromatase the
rapy in the treatment of postmenopausal women with advanced breast cancer.
In selecting studies, priority was given to randomized, controlled trials.
Results: Tamoxifen is the standard first-line therapy for advanced breast c
ancer. However, recent results have demonstrated the efficacy of newer anti
-aromatase agents in this setting. Among patients who have progressed after
tamoxifen therapy, anti-aromatase agents have emerged as first choice ther
apy based on their better tolerability and improved efficacy compared with
megestrol acetate. Exemestane and anastrozole (irreversible and reversible
anti-aromatase agents, respectively) have demonstrated survival benefits ov
er megestrol acetate in second-line therapy. Antiaromatase agents have also
demonstrated efficacy in patients who have failed multiple hormonal therap
ies. Based on these data, an algorithm for the treatment of postmenopausal
women with advanced breast cancer is proposed. Conclusions: The enhanced to
lerability and superior efficacy of anti-aromatase inhibitors compared with
megestrol acetate has resulted in these agents becoming the endocrine trea
tment of choice for women with advanced breast cancer who have progressed a
fter tamoxifen treatment. The increased use of tamoxifen in the adjuvant se
tting and the demonstrated activity of aromatase inhibitors in first-line t
herapy will further increase the role of these agents.