caa a22 4500 386389586 CHVBK 20180307112109.0 cr unu---uuuuu 161130s1989 xx s 000 0 eng 10.1017/S0269727000010757 doi S0269727000010757 pii (NATIONALLICENCE)cambridge-10.1017/S0269727000010757 Aromatase inhibitors in human breast cancer [Elektronische Daten] The results of a phase I/II study in advanced breast cancer in postmenopausal women of the aromatase inhibitors 4-hydroxyandrostenedione (40HA), miconazole and CGS16949A are described. 40HA, a steroidal compound which is an irreversible inhibitor of aromatase, has been administered to 131 patients by weekly (500 mg) or fortnightly (250 mg) i.m. injections, and daily (500 mg) by mouth. The overall response rate (complete regression (CR) and partial regression (PR)) was 33%; all three dose schedules had similar clinical efficacy. Oestradiol levels were suppressed to a mean of 37-45% of pretreatment values with oral and with weekly i.m. 40HA; suppression was marginally suboptimal with 250 mg i.m. fortnightly. 40HA was well tolerated, especially when administered by fortnightly injections; this dose schedule is to be preferred to weekly injections. Significant oestradiol suppression and clinical responses did not occur with the imidazole antifungal, miconazole, which was administered to twenty-two patients at doses of 500-1000 mg daily. The non-steroidal aromatase inhibitor, CGS16949A, induced comparable oestradiol suppression to 40HA at doses of 0.6-4 mg daily; 0.6 mg daily appears to be suboptimal. Five of thirty-one patients treated had objective responses, and disease stabilised for at least six months in nine patients. Some suppression of aldosterone occurred with doses of 2 and 4 mg daily, but clinical toxicity of the compound was minor. Copyright © Royal Society of Edinburgh 1989 Oestrogen Deprivation - Novel Methods nationallicence Coombes R. C. Clinical Oncology Unit, St George's Hospital Medical School, Cranmer Terrace, London SW17 ORE, U.K. Stein R. C. Clinical Oncology Unit, St George's Hospital Medical School, Cranmer Terrace, London SW17 ORE, U.K. Dowsett M. Department of Endocrinology, Royal Marsden Hospital, Fulham Road, London SW3 6JJ, U.K. Proceedings of the Royal Society of Edinburgh. Section B. Biological Sciences Royal Society of Edinburgh Scotland Foundation 95(1989), 283-291 0269-7270 95<283 1989 95 PRB https://doi.org/10.1017/S0269727000010757 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1017/S0269727000010757 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Coombes R. C. Clinical Oncology Unit, St George's Hospital Medical School, Cranmer Terrace, London SW17 ORE, U.K NATIONALLICENCE 700 1- Stein R. C. Clinical Oncology Unit, St George's Hospital Medical School, Cranmer Terrace, London SW17 ORE, U.K NATIONALLICENCE 700 1- Dowsett M. Department of Endocrinology, Royal Marsden Hospital, Fulham Road, London SW3 6JJ, U.K NATIONALLICENCE 773 0- Proceedings of the Royal Society of Edinburgh. Section B. Biological Sciences Royal Society of Edinburgh Scotland Foundation 95(1989), 283-291 0269-7270 95<283 1989 95 PRB CC0 http://creativecommons.org/publicdomain/zero/1.0 nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-cambridge