Wenderoth U K, Happ J, Krause U, Adenauer H, Jacobi G H
Eur Urol. 1982;8(6):343-7. doi: 10.1159/000473554.
This investigation on 12 well-defined patients with untreated, advanced prostatic adenocarcinoma establishes the gonadotropin-releasing hormone analogue D-Ser(But)6-nonapeptide-ethylamide (Hoe 766) as an effective, safe and non-toxic form of medical castration. Hoe 766 was given either as subcutaneous injections of 2 x 200 micrograms/day over 14 days and pernasal application (3 x 400 micrograms/day) thereafter, or as subcutaneous injections of 3 x 1,000 micrograms/day over 6 days and pernasal application thereafter in the dosage mentioned above. Both dose regimens were equally effective: pituitary overstimulation between days 3 and 6 with a rise of serum HL and testosterone; pituitary and testicular desensitization with LH and testosterone decline between days 6 and 14; medical castration with average serum testosterone levels maintained around 0.5 ng/ml for up to 12 weeks. Except for transient hot flashes in 4 patients, no clinical or laboratory side effects were observed. It is concluded from this study that the gonadotropin-releasing hormone analogue. Hoe 766, is a valuable alternative to conventional contrasexual measures for prostate cancer palliation. To improve the patient's compliance, however, the smallest single pernasal dosage effective for maintenance of down-regulation and steroidogenic arrest has still to be determined.
这项针对12例未经治疗的晚期前列腺腺癌明确患者的研究表明，促性腺激素释放激素类似物D-Ser(But)6-九肽乙酰胺（Hoe 766）是一种有效、安全且无毒的药物去势形式。Hoe 766的给药方式为：先皮下注射2×200微克/天，持续14天，之后经鼻给药（3×400微克/天）；或者先皮下注射3×1000微克/天，持续6天，之后按上述剂量经鼻给药。两种给药方案效果相同：第3至6天垂体过度刺激，血清促黄体生成素（HL）和睾酮升高；第6至14天垂体和睾丸脱敏，促黄体生成素（LH）和睾酮下降；药物去势后血清睾酮平均水平维持在0.5纳克/毫升左右长达12周。除4例患者出现短暂潮热外，未观察到临床或实验室副作用。本研究得出结论，促性腺激素释放激素类似物Hoe 766是前列腺癌姑息治疗中传统抗雄激素措施的一种有价值替代方法。然而，为提高患者依从性，仍需确定维持下调和类固醇生成抑制有效的最小单次经鼻剂量。
