Methylandrostenediol

Abstract

Methylandrostenediol‡ was chosen for clinical trial in patients with metastatic cancer of the breast because it was the first of a series of compounds tested which on bioassay showed renotropic effects on experimental hydronephrosis in female adult mice resembling those of testosterone propionate. The method and results of these bioassays will be published elsewhere(l). The marked degree of protection afforded the tubular epithelial cells by testosterone propionate and methylandrostenediol in experimental hydronephrosis is illustrated in Fig. 1. This renotropic property of methylandrostenediol is at present under investigation in human renal disorders. Testosterone, vinyl testosterone, cis testosterone, testosterone tocap-tate and testosterone carbonate failed to give such renal protection.

Methylandrostenediol was given to 7 women with metastasizing cancer of the breast for periods of 1 to 7 months, and in doses varying from 25 mg in oil given intramuscularly to 100 mg per day intramuscularly in aqueous suspension. The latter dose was found to be clinically the most effective. Pellets of 60 mg implanted every 20 to 30 days were also used. The maximal total dose was 10 g given intramuscularly in aqueous suspension.§

The patients were women ranging in age from 34 to 64 years, in whom cancer of the breast had been diagnosed as being of from 1 to 8 years duration prior to the initiation of methylandrostenediol therapy. Subjective improvement with varying degrees of euphoria and a sense of well-being occurred in all cases and lasted for from 1 to 7 months under therapy. Objective clear-cut calcification of bone lesions studied by X-ray was found in 2 patients and one is shown in Fig. 2 and 3. Soft tissue lesions regressed in 2 other instances under methylandrostenediol therapy. Studies of blood chemistry (phosphorus, calcium, alkaline phosphatase, NPN and total protein) showed trends comparable to those seen in the course of chemotherapy of breast cancer with testosterone and are illustrated in Fig. 4.