PMID: 3320568Jan 1, 1987Paper

Aromatase inhibitors: basic and clinical studies

Journal of Steroid Biochemistry
A M BrodieM Dowsett

Abstract

Application of aromatase inhibitors to the treatment of conditions in which estrogen plays, a role is discussed. Studies in vitro demonstrate that 4-hydroxyandrostenedione (4-OHA) is a potent inhibitor of aromatase. The compound reduces ovariant estrogen production and causes regression of carcinogen (DMBA)-induced mammary tumors in the rat. In the rhesus monkey, 4-OHA was also shown to inhibit peripheral aromatization. To date 58 postmenopausal breast cancer patients with advanced metastatic disease have received 500 mg im weekly while 31 patients received 250 mg 4-OHA orally per day. Estradiol levels were significantly reduced in all patients from a mean of 7.2 + 0.8 pg/ml to 2.8 + 0.3 pg/ml. Of patients receiving 4-OHA im 27% had partial or complete responses and in 10% of patients the disease was stabilized. Similar responses occurred in the patients receiving 4-OHA orally. These results suggest that 4-OHA is effective and that this compound and other aromatase inhibitors could be valuable new additions to the treatment of breast cancer.

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Citations

Jun 1, 1989·Journal of Steroid Biochemistry·W WoutersM Venet
Nov 20, 1990·The Journal of Steroid Biochemistry and Molecular Biology·R De CosterP A Janssen
Jan 1, 1991·The Journal of Steroid Biochemistry and Molecular Biology·E SimpsonM Waterman
Sep 1, 1992·The Journal of Steroid Biochemistry and Molecular Biology·G FalksonH C Falkson
Dec 1, 1992·The Journal of Steroid Biochemistry and Molecular Biology·H Vanden Bossche
Mar 1, 1992·The Journal of Steroid Biochemistry and Molecular Biology·E SimpsonM Waterman
Aug 1, 1995·The Journal of Steroid Biochemistry and Molecular Biology·Y J Abul-HajjM Hedge
Jul 1, 1996·The Journal of Steroid Biochemistry and Molecular Biology·M NumazawaY Tateda
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May 31, 1991·Biochemical and Biophysical Research Communications·M Numazawa, A Mutsumi
Mar 24, 2006·European Journal of Cancer : Official Journal for European Organization for Research and Treatment of Cancer (EORTC) [and] European Association for Cancer Research (EACR)·Eugene McCloskey
Jan 1, 1990·Journal of Enzyme Inhibition·R De CosterM Byloos
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Sep 1, 1993·Scandinavian Journal of Gastroenterology·R R Ettarh, K E Carr
Sep 1, 1991·Journal of Veterinary Internal Medicine·R E ElmslieG K Ogilvie
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Nov 1, 1988·Journal of Endocrinological Investigation·F Sciarra
Nov 1, 1993·Phytochemistry·S B Mahato, I Majumdar
Jul 15, 1992·Biochemical and Biophysical Research Communications·M NumazawaY Tanaka

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