Use of aromatase inhibitor 4-hydroxyandrostenedione in postmenopausal breast cancer: optimization of therapeutic dose and route

4-Hydroxyandrostenedione (4-OHA) is a potent inhibitor of estrogen production by aromatase and causes suppression of plasma estradiol levels and disease regression in postmenopausal breast cancer patients. Groups of patients were given p.o. or parenteral 4-OHA, and plasma estradiol and 4-OHA levels...

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Bibliographic Details
Published in:Cancer research (Chicago, Ill.) Ill.), 1987-04, Vol.47 (7), p.1957-1961
Main Authors: DOWSETT, M, GOSS, P. E, POWLES, T. J, HUTCHINSON, G, BRODIE, A. M. H, JEFFCOATE, S. L, COOMBES, R. C
Format: Article
Language:English
Subjects:
Administration, Oral
Androstenedione - administration & dosage
Androstenedione - blood
Androstenedione - therapeutic use
Antineoplastic agents
Aromatase Inhibitors
Biological and medical sciences
Breast Neoplasms - drug therapy
Chemotherapy
Estradiol - blood
Female
Half-Life
Humans
Injections, Intramuscular
Kinetics
Medical sciences
Menopause
Pharmacology. Drug treatments
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Summary:4-Hydroxyandrostenedione (4-OHA) is a potent inhibitor of estrogen production by aromatase and causes suppression of plasma estradiol levels and disease regression in postmenopausal breast cancer patients. Groups of patients were given p.o. or parenteral 4-OHA, and plasma estradiol and 4-OHA levels were measured to enable the delineation of the minimal effective dose and optimal therapeutic regimen. A single injection of 500 mg i.m. suppressed estradiol levels to a mean 36.3 +/- 3.3% (SE) (n = 14) of base line after 4 to 7 days and maintained this suppression in six of seven patients for greater than 14 days. The half-life of 4-OHA was approximately 8 days, and when the level had fallen to less than 3 ng/ml, estradiol levels began to rise. Similar suppression was achieved by a single i.m. injection of 125 mg of 4-OHA and by 500 mg of 4-OHA p.o. daily after 1 wk, but escape from suppression was more rapid.
ISSN:0008-5472
1538-7445