A new irreversible aromatase inhibitor, 6-methylenandrosta-1,4-diene-3,17-dione (FCE 24304): antitumor activity and endocrine effects in rats with DMBA-induced mammary tumors

Cancer Chemotherapy and Pharmacology
T ZaccheoE di Salle

Abstract

The antitumor activity of the new irreversible aromatase inhibitor 6-methylenandrosta-1,4-diene-3,17-dione (FCE 24304) was studied in rats with 7,12-dimethylbenzanthracene (DMBA)-induced tumors; several endocrine parameters were evaluated in these animals. The compound was given s.c. and p.o. twice daily, 6 days/week, for 4 weeks. The control group showed 13% tumor regression (0% complete remission, CR; 13% partial remission, PR). FCE 24304 given s.c. induced 44% (22 + 22) regressions at the dose of 3 mg/kg per day, 70% (40 + 30) at 10 mg/kg per day, 73% (27 + 46) at 30 mg/kg per day, and 70% (50 + 20) at 100 mg/kg per day. FCE 24304 given orally induced 25% (17 + 8) tumor regressions at 30 mg/kg per day and 50% (17 + 33) at 100 mg/kg per day. Rats were killed 4 h after the last dose and the aromatase activity of ovarian microsomes (OAA) was evaluated. OAA was reduced by 56% after s.c. treatment with 3 mg/kg per day FCE 24304; complete OAA suppression (greater than or equal to 96%) was obtained starting at 10 mg/kg per day s.c. Oral treatment slightly reduced OAA only at a dose of 100 mg/kg per day (36%). Body weight increased in all the groups s.c. treated with FCE 24304 but not in those treated orally. The weights of the pitu...Continue Reading

Citations

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