Gonzalez-Barcena D, Perez-Sanchez P, Berea-Dominguez H, Graef-Sanchez A, Becerril-Morales M, Comaru-Schally A M, Schally A V
Prostate. 1986;9(2):207-15. doi: 10.1002/pros.2990090211.
Forty patients with stage D2 prostatic carcinoma were treated for up to 30 months with D-Trp-6-LH-RH. The analog was given s.c. once daily at a dose of 1 mg/day for the first 7 days. Subsequently, the dose was reduced to 100 micrograms/day. In follow-up studies, 30 men continued this therapy for up to 24 months. Blood samples were taken before the injection of the analog and 1, 2, 4, and 6 hours later. Serum LH, FSH, and testosterone levels were measured by RIA every month for 2 years. The initial administration of 1 mg D-Trp-6-LH-RH caused a marked elevation of LH and FSH, which lasted more than 24 hours. However, 1 month later and throughout the therapy, the basal values of LH and FSH were below the normal range and no increase in serum gonadotropins levels was obtained after administration of the analog. Initial plasma testosterone was within normal limits, but during treatment with D-Trp-6-LH-RH it fell to castration levels, and no increases were seen during the 6 hours following the injection of the analog. These results show that chronic administration of D-Trp-6-LH-RH, at the doses used, blocks the pituitary-gonadal axis and that the escape phenomenon from the effects of the LH-RH agonists-induced blockade does not occur under our conditions in contrast to observations of Kerle et al with the I.C.I. Analog 118630 (8). The accumulated results reinforce the view that long-term therapy with agonists of LH-RH is the preferred alternative to surgical castration or therapy with estrogens in men with metastatic prostate cancer.
40例D2期前列腺癌患者接受了长达30个月的D-色氨酸-6-促性腺激素释放激素（D-Trp-6-LH-RH）治疗。该类似物在前7天每天皮下注射1次，剂量为1毫克/天。随后，剂量减至100微克/天。在随访研究中，30名男性继续这种治疗长达24个月。在注射该类似物前以及注射后1、2、4和6小时采集血样。在2年时间里每月通过放射免疫分析法（RIA）测定血清促黄体生成素（LH）、促卵泡生成素（FSH）和睾酮水平。最初给予1毫克D-Trp-6-LH-RH导致LH和FSH显著升高，持续超过24小时。然而，1个月后及整个治疗过程中，LH和FSH的基础值低于正常范围，注射该类似物后血清促性腺激素水平未升高。最初血浆睾酮在正常范围内，但在用D-Trp-6-LH-RH治疗期间降至去势水平，注射该类似物后6小时内未见升高。这些结果表明，以所用剂量长期给予D-Trp-6-LH-RH可阻断垂体-性腺轴，并且与Kerle等人对ICI类似物118630的观察结果（8）相反，在我们的条件下未出现LH-RH激动剂诱导的阻断作用的逃逸现象。累积结果强化了这样一种观点，即对于转移性前列腺癌男性患者，LH-RH激动剂的长期治疗是手术去势或雌激素治疗的首选替代方法。
