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Related Experiment Videos

Exemestane.

L J Scott1, L R Wiseman

  • 1Adis International Limited, Auckland, New Zealand. demail@adis.co.nz

Drugs
|November 7, 1999
PubMed
Summary
This summary is machine-generated.

Exemestane effectively treats advanced breast cancer by inhibiting aromatase activity. This steroidal agent offers improved outcomes and tolerability compared to megestrol in postmenopausal women.

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Area of Science:

  • Endocrinology
  • Oncology
  • Pharmacology

Background:

  • Exemestane is a steroidal aromatase inactivator used for advanced breast cancer.
  • It irreversibly binds to the aromatase enzyme's substrate binding site.
  • Postmenopausal women with advanced breast cancer are the target population.

Purpose of the Study:

  • To evaluate the efficacy and tolerability of oral exemestane (25 mg/day) as a second- or third-line treatment.
  • To compare exemestane with megestrol in postmenopausal women with advanced breast cancer.

Main Methods:

  • Phase II and III clinical trials were conducted.
  • Oral exemestane 25 mg/day was administered daily.
  • Efficacy endpoints included objective response rate, duration of overall success, time to disease progression, and survival time.

Related Experiment Videos

  • Tolerability was assessed by adverse events, including bodyweight changes.

    • Main Results:

    • Oral exemestane 25 mg/day achieved approximately 98% peripheral aromatase inactivation.
    • It reduced plasma estrone, estradiol, and estrone sulphate levels by 85-95% in postmenopausal women.
    • Phase II trials showed objective response rates of up to 28% and 26% respectively.
    • Phase III trials indicated similar objective response rates to megestrol but significantly longer duration of overall success, time to disease progression, and survival time.
    • Exemestane was well-tolerated, with fewer bodyweight changes compared to megestrol.

    Conclusions:

    • Exemestane is an effective treatment for postmenopausal women with advanced breast cancer.
    • It demonstrates superior efficacy in terms of duration of success, time to progression, and survival compared to megestrol.
    • Exemestane offers a favorable tolerability profile, particularly regarding bodyweight changes.