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

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 tolerabili...

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Autores principales: Zilembo, N., Noberasco, C., Bajetta, E., Martinetti, A., Mariani, L., Orefice, S., Buzzoni, R., Di Bartolomeo, M., Di Leo, A., Laffranchi, A.
Formato: Texto
Lenguaje:English
Publicado: Nature Publishing Group 1995
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2034036/
https://www.ncbi.nlm.nih.gov/pubmed/7547212
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author Zilembo, N.
Noberasco, C.
Bajetta, E.
Martinetti, A.
Mariani, L.
Orefice, S.
Buzzoni, R.
Di Bartolomeo, M.
Di Leo, A.
Laffranchi, A.
author_facet Zilembo, N.
Noberasco, C.
Bajetta, E.
Martinetti, A.
Mariani, L.
Orefice, S.
Buzzoni, R.
Di Bartolomeo, M.
Di Leo, A.
Laffranchi, A.
author_sort Zilembo, N.
collection PubMed
description 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.
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spelling pubmed-20340362009-09-10 Endocrinological and clinical evaluation of exemestane, a new steroidal aromatase inhibitor. Zilembo, N. Noberasco, C. Bajetta, E. Martinetti, A. Mariani, L. Orefice, S. Buzzoni, R. Di Bartolomeo, M. Di Leo, A. Laffranchi, A. Br J Cancer Research Article 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. Nature Publishing Group 1995-10 /pmc/articles/PMC2034036/ /pubmed/7547212 Text en https://creativecommons.org/licenses/by/4.0/This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit https://creativecommons.org/licenses/by/4.0/.
spellingShingle Research Article
Zilembo, N.
Noberasco, C.
Bajetta, E.
Martinetti, A.
Mariani, L.
Orefice, S.
Buzzoni, R.
Di Bartolomeo, M.
Di Leo, A.
Laffranchi, A.
Endocrinological and clinical evaluation of exemestane, a new steroidal aromatase inhibitor.
title Endocrinological and clinical evaluation of exemestane, a new steroidal aromatase inhibitor.
title_full Endocrinological and clinical evaluation of exemestane, a new steroidal aromatase inhibitor.
title_fullStr Endocrinological and clinical evaluation of exemestane, a new steroidal aromatase inhibitor.
title_full_unstemmed Endocrinological and clinical evaluation of exemestane, a new steroidal aromatase inhibitor.
title_short Endocrinological and clinical evaluation of exemestane, a new steroidal aromatase inhibitor.
title_sort endocrinological and clinical evaluation of exemestane, a new steroidal aromatase inhibitor.
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2034036/
https://www.ncbi.nlm.nih.gov/pubmed/7547212
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