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The Effect of 7β, 17-Dimethyltestosterone (Calusterone®) on Testosterone Metabolism in Women with Advanced Breast Cancer

Department of Oncology and the Institute for Steroid Research, Montefiore Hospital and Medical Center Bronx, New York

Calusterone® (7β, 17-dimethyltestosterone) is a 17-alkylated, orally active androgenic steroid used in the treatment of breast cancer. The effect of this steroid on the metabolism of ¹⁴C-testosterone and the excretion of endogenous urinary androgen metabolites has been studied in four patients with breast cancer. Total glucuronide metabolites of the tracer decreased significantly, the androsterone/etiocholanolone ratio rose by a factor of 2–4, and there was increased formation of uncharacterized polar metabolites. There was no significant change in either the sum of the excretion of endogenous androgen metabolites or the androsterone/etiocholanolone ratio. The changes resemble those we have seen in cirrhosis of the liver. It is concluded that the effects of Calusterone on testosterone metabolism, like its effects on cortisol or estradiol metabolism, represent nonspecific effects of an orally administered 17-alkylated steroid on hepatic structure and function, and probably bear no relationship to its therapeutic effect in breast cancer.

Supported in part by grants CA-07304 from the National Cancer Institute and RR-53 from the General Clinical Research Centers Branch, National Institutes of Health, Bethesda, Md.

Received November 29, 1976.