Exemestane: a novel aromatase inactivator for breast cancer.
Exemestane is a unique inactivator of the aromatase enzyme and differs from the two approved aromatase inhibitors. It is well absorbed at a daily oral dose of 25 mg and produces significant suppression of aromatase and plasma estrogen levels without androgenic side effects. Toxicity is mild with menopausal symptoms predominating. Exemestane is approved for the treatment of postmenopausal women with recurrent breast cancer. In reported clinical trials, exemestane was effective in patients failing tamoxifen, megestrol acetate, or even other aromatase inhibitors in phase II trials and was superior to megestrol acetate in a phase III randomized trial in which an early survival advantage for exemestane was observed. Studies evaluating first-line exemestane for adjuvant use and as a chemopreventive agent are underway.
Jones
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Charles A. Sammons Cancer Center, Baylor University Medical Center, Dallas, Texas, USA.
Jones
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D000730:Androstadienes / Q000627:therapeutic use*; D000970:Antineoplastic Agents / Q000627:therapeutic use*; D047072:Aromatase Inhibitors; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000201:enzymology; D002986:Clinical Trials as Topic; D004791:Enzyme Inhibitors / Q000627:therapeutic use*; D005260:Female; D006801:Humans
D000730:Androstadienes; D000970:Antineoplastic Agents; D047072:Aromatase Inhibitors; D004791:Enzyme Inhibitors; C056516:exemestane