Endocrinological and clinical evaluation of exemestane, a new steroidal aromatase inhibitor

N. Zilembo, C. Noberasco, E. Bajetta, A. Martinetti, L. Mariani, S. Orefice, R. Buzzoni, M. Di Bartolomeo, A. Di Leo, A. Laffranchi, E. Di Salle

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The androstenedione derivative, exemestane (FCE 24304), is a new orally active irreversible aromatase inhibitor. Fifty-six post-menopausal advanced breast cancer patients entered this study to evaluate the activity of four low exemestane doses in reducing oestrogen levels. The drug's tolerability and clinical efficacy were also assessed. Exemestane was orally administered to four consecutive groups at daily doses of 25, 12.5, 5 and 2.5 mg, and the changes in oestrogen, gonadotrophins, sex-hormone binding globulin and dehydroepiandrosterone sulphate levels were evaluated. Drug selectivity was studied by measuring 17-hydroxycorticosteroid urinary levels. After 7 days of treatment, mean oestrone and oestradiol levels had decreased by respectively 64% and 65% (a decrease which was maintained over time); in the 2.5 mg group, oestrone sulphate levels also decreased by 74%. Gonadotrophin levels were significantly higher, whereas no changes in the other serum hormone levels or any interference with adrenal synthesis were detected. Treatment tolerability was satisfactory: nausea and dyspepsia were reported in 16% of patients. The overall objective response rate was 18%. In conclusion, exemestane is effective in reducing oestrogen levels at all of the tested doses and shows interesting clinical activity.

Original languageEnglish
Pages (from-to)1007-1012
Number of pages6
JournalBritish Journal of Cancer
Issue number4
Publication statusPublished - 1995


  • Advanced disease
  • Aromatase inhibitor
  • Breast cancer
  • Exemestane
  • Post-menopausal patients

ASJC Scopus subject areas

  • Cancer Research
  • Oncology


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