Yamanaka H, Kosaku N, Makino T, Shida K
Hinyokika Kiyo. 1983 Sep;29(9):1133-45.
The anti-androgen activity of allylestrenol was studied in the rat, and it was found to have an activity which was equivalent to that of chlormadinone acetate. The direct anti-prostatic activity is the result of the following mechanism: inhibition of serum testosterone uptake into the prostate, inhibition of testosterone-5 alpha-reductase activity and inhibition of 5 alpha-DHT . receptor complex formation. Large doses of allylestrenol administered to normal mature rats, inhibit the hypothalamus-pituitary-gonadal axis, and atrophy of the prostate will be more marked due to an indirect effect as a result of the reduction in the serum testosterone level. Based on this finding, we performed a clinical trial with allylestrenol in patients with hypertrophy of the prostate and cancer of the prostate. We administered 45 mg a day allylestrenol to 19 patients with prostatic hypertrophy and obtained satisfactory clinical results in so far as improvement of micturition and reduction in prostate mass was concerned. We also administered 90 mg a day of allylestrenol to 4 patients with cancer of the prostate and obtained a cytostatic effect.
研究了烯丙雌醇在大鼠体内的抗雄激素活性，发现其活性与醋酸氯地孕酮相当。其直接的抗前列腺活性是由以下机制导致的：抑制血清睾酮摄入前列腺、抑制睾酮-5α-还原酶活性以及抑制5α-双氢睾酮受体复合物的形成。给正常成熟大鼠大剂量服用烯丙雌醇，会抑制下丘脑-垂体-性腺轴，由于血清睾酮水平降低产生的间接作用，前列腺萎缩会更加明显。基于这一发现，我们对前列腺增生和前列腺癌患者进行了烯丙雌醇的临床试验。我们给19例前列腺增生患者每天服用45毫克烯丙雌醇，就排尿改善和前列腺体积缩小而言，取得了满意的临床效果。我们还给4例前列腺癌患者每天服用90毫克烯丙雌醇，获得了细胞生长抑制效果。
