Iveson T J, Smith I E, Ahern J, Smithers D A, Trunet P F, Dowsett M
Breast Unit, Royal Marsden Hospital, London, United Kingdom.
J Clin Endocrinol Metab. 1993 Aug;77(2):324-31. doi: 10.1210/jcem.77.2.8345035.
We have performed a phase I study of the effect of a single dose of CGS 20267, an oral nonsteroidal aromatase inhibitor, in 12 healthy volunteer postmenopausal women. Each subject received 2 single doses of CGS 20267 (0.1, 0.5, or 2.5 mg) or placebo separated by a washout period of at least 6 weeks. There was statistically significant suppression of serum estrone and estradiol at all three doses of CGS 20267 tested. Serum estrone and estradiol concentrations were maximally suppressed by 76% and 79% from baseline levels, respectively. Urinary excretion of estrone and estradiol was also suppressed, although this did not reach statistical significance. Serum concentrations of aldosterone, cortisol, 17 alpha-hydroxyprogesterone, androstenedione, testosterone, FSH, LH, and TSH were unaffected by CGS 20267. The drug was well tolerated, with no significant side-effects. This study has shown CGS 20267 to be a potent and specific aromatase inhibitor, and further studies are now needed to assess its clinical efficacy.
我们对12名绝经后健康志愿者女性进行了一项关于单剂量口服非甾体芳香化酶抑制剂CGS 20267效果的I期研究。每位受试者接受2次单剂量的CGS 20267（0.1、0.5或2.5毫克）或安慰剂，中间间隔至少6周的洗脱期。在所测试的CGS 20267的所有三个剂量下，血清雌酮和雌二醇均受到具有统计学意义的抑制。血清雌酮和雌二醇浓度分别从基线水平最大抑制了76%和79%。雌酮和雌二醇的尿排泄也受到抑制，尽管这未达到统计学意义。醛固酮、皮质醇、17α-羟孕酮、雄烯二酮、睾酮、促卵泡激素、促黄体生成素和促甲状腺激素的血清浓度不受CGS 20267影响。该药物耐受性良好，无明显副作用。这项研究表明CGS 20267是一种强效且特异性的芳香化酶抑制剂，现在需要进一步研究来评估其临床疗效。
