Mahler C, Denis L
Department of Endocrinology, A.Z. Middelheim, Antwerp, Belgium.
J Steroid Biochem Mol Biol. 1990 Dec 20;37(6):921-4. doi: 10.1016/0960-0760(90)90444-p.
Recently a new non-steroidal antiandrogen (Casodex) has been shown in animal experiments to possess a potent peripheral antiandrogen effect. In patients with advanced prostatic cancer however, this drug is not peripherally selectively active and blocked central brain androgen-receptors results in a rise of luteinizing hormone (LH) and testosterone (T). We treated 18 advanced prostatic cancer patients with 50 mg Casodex daily for a mean period of 42 weeks. There were no complete objective responses but partial responses were seen in a few patients. In 16 patients there was a greater than 50% reduction of pretreatment PSA levels. Endocrine evaluations showed a significant rise in LH, T and oestradiol (E), reaching peak values within the two first months with subsequent lowering of these levels afterwards but without returning to normal. The general tolerance of the drug was good, gynecomastia being the most frequent side-effect. Libido and potency, when present before start of therapy, were maintained in some patients. We conclude that this compound seems as effective as other antiandrogens, but with improved compliance, and shows less side effects in the management of advanced prostatic cancer.
最近，一种新的非甾体类抗雄激素药物（康士得）在动物实验中显示出具有强大的外周抗雄激素作用。然而，在晚期前列腺癌患者中，这种药物并非在外周具有选择性活性，阻断中枢脑雄激素受体导致促黄体生成素（LH）和睾酮（T）升高。我们对18例晚期前列腺癌患者每日给予50毫克康士得治疗，平均治疗时间为42周。未观察到完全客观缓解，但有少数患者出现部分缓解。16例患者治疗前前列腺特异性抗原（PSA）水平降低超过50%。内分泌评估显示LH、T和雌二醇（E）显著升高，在最初两个月内达到峰值，随后这些水平下降，但未恢复正常。该药物的总体耐受性良好，乳腺增生是最常见的副作用。治疗开始前存在的性欲和性功能，在一些患者中得以维持。我们得出结论，这种化合物似乎与其他抗雄激素药物一样有效，但依从性更好，在晚期前列腺癌的治疗中副作用更少。
