Zumoff B, Levin J, Bradlow H L, Hellman L
J Clin Endocrinol Metab. 1977 Jun;44(6):1203-5. doi: 10.1210/jcem-44-6-1203.
Calusterone (7beta, 17alpha-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 andorsterone/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.
卡鲁睾酮（7β, 17α-二甲基睾酮）是一种17-烷基化的、口服有效的雄激素类固醇，用于治疗乳腺癌。在4例乳腺癌患者中研究了这种类固醇对14C-睾酮代谢及内源性尿雄激素代谢产物排泄的影响。示踪剂的总葡萄糖醛酸代谢产物显著减少，雄酮/表雄酮比值升高2至4倍，且未鉴定的极性代谢产物生成增加。内源性雄激素代谢产物排泄总量及雄酮/表雄酮比值均无显著变化。这些变化与我们在肝硬化中所见相似。结论是，卡鲁睾酮对睾酮代谢的影响，如同其对皮质醇或雌二醇代谢的影响一样，代表了口服17-烷基化类固醇对肝脏结构和功能的非特异性影响，可能与其在乳腺癌中的治疗作用无关。
