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Exemestane

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Abstract

  • ▴ Exemestane is a steroidal agent which causes inactivation of the aromatase enzyme by binding irreversibly to the substrate binding site.

  • ▴ Oral exemestane 25 mg/day inactivates peripheral aromatase activity (R-98% inactivation) and reduces basal plasma estrone, estradiol and estrone sulphate levels by 85 to 95% in postmenopausal women with advanced breast cancer.

  • ▴ Phase II trials indicate that oral exemestane 25 mg/day is an effective second- or third-line agent in the treatment of postmenopausal women with advanced breast cancer (achieving an objective response in up to 28 and 26% of patients, respectively).

  • ▴ Results from a phase III trial indicate that exemestane achieves a similar objective response rate to megestrol as a second-line therapy; however, exemestane achieved a significantly longer duration of overall success, time to disease progression and survival time.

  • ▴ Exemestane is at least as well tolerated as megestrol, but is associated with significantly fewer bodyweight changes, mainly bodyweight gain (≥10%). Other common adverse events are hot flushes, nausea and fatigue.

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Authors and Affiliations

  1. Adis International Limited, 41 Centorian Drive, Private Bag 65901, Mairangi Bay, Auckland, 10, New Zealand

    Lesley J. Scott & Lynda R. Wiseman

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  1. Lesley J. Scott
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  2. Lynda R. Wiseman
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Correspondence to Lesley J. Scott.

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Scott, L.J., Wiseman, L.R. Exemestane. Drugs 58, 675–680 (1999). https://doi.org/10.2165/00003495-199958040-00007

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  • DOI: https://doi.org/10.2165/00003495-199958040-00007

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