Experience with exemestane in the treatment of early and advanced breast cancer.
BACKGROUND
Exemestane represents the only steroidal third-generation aromatase inactivator implemented for breast cancer therapy.


OBJECTIVE
Present clinical and translational data defining the role of exemestane as an aromatase inhibitor.


METHODS
Literature search including PubMed and ISI Web of Science.


CONCLUSIONS
Exemestane potently inhibits in vivo aromatization resembling anastrozole and letrozole. Randomized trials have revealed superiority for exemestane compared to conventional therapy in metastatic breast cancer. In addition sequential treatment with tamoxifen (for 2 - 3 years) followed by exemestane (for 3 - 2 years) has revealed superiority with respect not only to relapse-free but also borderline improvement in overall survival in adjuvant therapy. Several studies now confirm lack of cross-resistance between non-steroidal aromatase inhibitors and exemestane, which could be due to exemestane's low androgen-agonistic activity through its 17-hydro metabolite.
Lønning
Per Eystein
PE
Institute of Medicine and Department of Oncology, Haukeland University Hospital, Bergen, Norway. per.lønning@helse-bergen.no
Geisler
Jürgen
J
D000730:Androstadienes / Q000009:adverse effects / Q000191:economics / Q000493:pharmacokinetics / Q000627:therapeutic use*; D000818:Animals; D000970:Antineoplastic Agents / Q000009:adverse effects / Q000191:economics / Q000493:pharmacokinetics / Q000627:therapeutic use*; D047072:Aromatase Inhibitors / Q000009:adverse effects / Q000191:economics / Q000493:pharmacokinetics / Q000627:therapeutic use*; D001943:Breast Neoplasms / Q000188:drug therapy*; D005260:Female; D006801:Humans; D009362:Neoplasm Metastasis / Q000188:drug therapy / Q000473:pathology
D000730:Androstadienes; D000970:Antineoplastic Agents; D047072:Aromatase Inhibitors; C056516:exemestane