Takezawa Y, Ito K, Suzuki K, Fukabori Y, Yamanaka H, Honma S, Mieda M, Hamataki N, Kushitani M
Department of Urology, Gunma University School of Medicine, Maebashi, Japan.
Prostate. 1995 Dec;27(6):321-8. doi: 10.1002/pros.2990270605.
The effects of the new steroidal antiandrogen, TZP-4238 on spontaneously-developed canine prostatic hyperplasia (BPH) were studied in comparison with those of chlormadinone acetate (CMA), a steroidal antiandrogen used for the treatment of BPH and prostatic cancer in Japan. Aged beagle dogs (5-9 years old) with spontaneously developed BPH (mean prostate volume, 17.7ml) were treated orally with a placebo, TZP-4238 (0.1 mg/kg/day, 0.01 mg/kg/day), or CMA (3 mg/kg/day), for 25 weeks. Prostate volume was measured by transrectal ultrasonography before treatment and every 5 weeks during treatment. TZP-4238 produced a regression in spontaneously developed canine BPH, its effects being more potent than those of CMA. TZP-4238 reduced the content of testosterone, dihydrotestosterone (DHT) and androgen receptor in the prostates of these animals, suggesting antiandrogenic mechanisms of the agent. TZP-4238 also appeared to reduce 5 alpha-reductase activity by prevention of the androgen action in prostate as described above.
将新型甾体类抗雄激素药物TZP-4238与醋酸氯地孕酮（CMA，一种在日本用于治疗良性前列腺增生症（BPH）和前列腺癌的甾体类抗雄激素药物）相比较，研究了TZP-4238对自发性犬前列腺增生症的影响。对患有自发性前列腺增生症（平均前列腺体积为17.7ml）的老年比格犬（5至9岁）口服给予安慰剂、TZP-4238（0.1mg/kg/天、0.01mg/kg/天）或CMA（3mg/kg/天），持续25周。在治疗前以及治疗期间每5周通过经直肠超声检查测量前列腺体积。TZP-4238使自发性犬前列腺增生症出现消退，其效果比CMA更强。TZP-4238降低了这些动物前列腺中睾酮、双氢睾酮（DHT）和雄激素受体的含量，提示该药物的抗雄激素作用机制。如上所述，TZP-4238似乎还通过阻止雄激素在前列腺中的作用来降低5α-还原酶活性。
