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The influence of aminoglutethimide and its analogue rogletimide on peripheral aromatisation in breast cancer.

The influence of the prototype aromatase inhibitor Aminoglutethimide (AG) and its analogue Rogletimide (RG) on peripheral aromatisation were investigated in 13 postmenopausal women with advanced breast cancer. Seven patients received AG 1,000 mg daily plus Hydrocortisone (HC) cover and six received...

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Autores principales: MacNeill, F. A., Jones, A. L., Jacobs, S., Lønning, P. E., Powles, T. J., Dowsett, M.
Formato: Texto
Lenguaje:English
Publicado: Nature Publishing Group 1992
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1977412/
https://www.ncbi.nlm.nih.gov/pubmed/1419608
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author MacNeill, F. A.
Jones, A. L.
Jacobs, S.
Lønning, P. E.
Powles, T. J.
Dowsett, M.
author_facet MacNeill, F. A.
Jones, A. L.
Jacobs, S.
Lønning, P. E.
Powles, T. J.
Dowsett, M.
author_sort MacNeill, F. A.
collection PubMed
description The influence of the prototype aromatase inhibitor Aminoglutethimide (AG) and its analogue Rogletimide (RG) on peripheral aromatisation were investigated in 13 postmenopausal women with advanced breast cancer. Seven patients received AG 1,000 mg daily plus Hydrocortisone (HC) cover and six received RG as dose escalation of 200 mg bd, 400 mg bd and 800 mg bd. In vivo aromatase inhibition was investigated using the double bolus injection technique with [4-14C] oestrone ([4-14C]E1) and [6,7-3H] androstenedione ([6,7-3H]4A) followed by a 96 h urine collection. The labelled urinary oestrogens were separated and purified by chromatography and HPLC. Plasma oestradiol (E2) was also measured. AG mean aromatase inhibition was 90.6% +/- 1.8 s.e.m. and E2 suppression 75.7% +/- 7.3 s.e.m. RG mean aromatase inhibition was 50.6% +/- 9.8 s.e.m. at 200 mg bd, 63.5% +/- 5.7 s.e.m. at 400 mg bd and 73.8% +/- 5.8 s.e.m. at 800 mg bd. E2 suppression was 30.7% +/- 9.5 s.e.m., 40.2% +/- 10.3 s.e.m. and 57.6% +/- 9.2 s.e.m. respectively. These results confirm the efficacy of AG as an aromatase inhibitor. RG produced dose dependent E2 suppression and aromatase inhibition, but even at the maximum tolerated dose of 800 mg bd had sub-optimal aromatase inhibition and oestradiol suppression compared with AG.
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spelling pubmed-19774122009-09-10 The influence of aminoglutethimide and its analogue rogletimide on peripheral aromatisation in breast cancer. MacNeill, F. A. Jones, A. L. Jacobs, S. Lønning, P. E. Powles, T. J. Dowsett, M. Br J Cancer Research Article The influence of the prototype aromatase inhibitor Aminoglutethimide (AG) and its analogue Rogletimide (RG) on peripheral aromatisation were investigated in 13 postmenopausal women with advanced breast cancer. Seven patients received AG 1,000 mg daily plus Hydrocortisone (HC) cover and six received RG as dose escalation of 200 mg bd, 400 mg bd and 800 mg bd. In vivo aromatase inhibition was investigated using the double bolus injection technique with [4-14C] oestrone ([4-14C]E1) and [6,7-3H] androstenedione ([6,7-3H]4A) followed by a 96 h urine collection. The labelled urinary oestrogens were separated and purified by chromatography and HPLC. Plasma oestradiol (E2) was also measured. AG mean aromatase inhibition was 90.6% +/- 1.8 s.e.m. and E2 suppression 75.7% +/- 7.3 s.e.m. RG mean aromatase inhibition was 50.6% +/- 9.8 s.e.m. at 200 mg bd, 63.5% +/- 5.7 s.e.m. at 400 mg bd and 73.8% +/- 5.8 s.e.m. at 800 mg bd. E2 suppression was 30.7% +/- 9.5 s.e.m., 40.2% +/- 10.3 s.e.m. and 57.6% +/- 9.2 s.e.m. respectively. These results confirm the efficacy of AG as an aromatase inhibitor. RG produced dose dependent E2 suppression and aromatase inhibition, but even at the maximum tolerated dose of 800 mg bd had sub-optimal aromatase inhibition and oestradiol suppression compared with AG. Nature Publishing Group 1992-10 /pmc/articles/PMC1977412/ /pubmed/1419608 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
MacNeill, F. A.
Jones, A. L.
Jacobs, S.
Lønning, P. E.
Powles, T. J.
Dowsett, M.
The influence of aminoglutethimide and its analogue rogletimide on peripheral aromatisation in breast cancer.
title The influence of aminoglutethimide and its analogue rogletimide on peripheral aromatisation in breast cancer.
title_full The influence of aminoglutethimide and its analogue rogletimide on peripheral aromatisation in breast cancer.
title_fullStr The influence of aminoglutethimide and its analogue rogletimide on peripheral aromatisation in breast cancer.
title_full_unstemmed The influence of aminoglutethimide and its analogue rogletimide on peripheral aromatisation in breast cancer.
title_short The influence of aminoglutethimide and its analogue rogletimide on peripheral aromatisation in breast cancer.
title_sort influence of aminoglutethimide and its analogue rogletimide on peripheral aromatisation in breast cancer.
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1977412/
https://www.ncbi.nlm.nih.gov/pubmed/1419608
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