ObjectiveHuman choriogonadotrophin (hCG) treatment of gonadotrophin‐deficient infertile men uses hCG of urinary (uhCG) or recombinant (rhCG) origin, but these treatments have not been compared nor are there studies defining rhCG dosing in men.DesignhCG products were studied in randomized cross‐over single‐dose studies of standard (Study 1, 1500 IU and 62.5 µg, respectively) or high (Study 2, 5000 IU and 250 µg) dose and a multi‐dose population pharmacology study of hCG use.ParticipantsEight (Study 1) and seven (Study 2) volunteers in cross‐over and 52 gonadotrophin‐deficient men in the multi‐dose studyMeasurementsIn cross‐over studies, serum testosterone (T), dihydrotestosterone (DHT) and estradiol by liquid chromatography‐mass spectrometry (LCMS) and serum hCG, LH, FSH, SHBG and T (observational study) by immunoassays.ResultsAfter standard and high‐dose injection, serum hCG and testosterone responses had similar timing and peak concentrations except for a mildly lower early (<48 h) serum testosterone with uhCG. In the multi‐dosing study, both hCGs had similar pharmacokinetics (pooled half‐life 5.8 days, p < .001), while serum testosterone concentrations were stable after injection and did not differ between hCG products. Bench testing verified that 20% of pens from 4/10 individuals were used inappropriately.ConclusionsAlthough hCG pharmacokinetics are not formally bioequivalent, the similar pharmacodynamic effects on serum testosterone indicate that at the doses tested both hCGs provide comparable clinical effects. The starting dose of rhCG for treating gonadotrophin‐deficient men should be 62.5 µg (6 clicks) of the rhCG pen.

中文翻译：

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男性重组和尿人绒毛膜促性腺激素的单剂量和多剂量药理学

目的人绒毛膜促性腺激素 (hCG) 治疗促性腺激素缺乏的不育男性使用尿源 hCG (uhCG) 或重组 (rhCG) 来源，但这些治疗尚未进行比较，也没有研究定义男性 rhCG 剂量。设计 hCG 产品进行了随机交叉研究‐标准剂量（研究 1，分别为 1500 IU 和 62.5 µg）或高剂量（研究 2，5000 IU 和 250 µg）的单剂量研究以及 hCG 使用的多剂量群体药理学研究。参与者八（研究 1）交叉研究中的 7 名（研究 2）志愿者和多剂量研究中的 52 名促性腺激素缺乏男性在交叉研究中，通过液相色谱-质谱法 (LCMS) 和通过免疫测定法测定血清 hCG、LH、FSH、SHBG 和 T（观察性研究）。结果在标准剂量和高剂量注射后，血清 hCG 和睾酮反应具有相似的时间和峰值浓度，但早期（<48 小时）血清睾酮水平略低。超绒毛膜促性腺激素。在多剂量研究中，两种 hCG 具有相似的药代动力学（汇总半衰期为 5.8 天，p< .001)，而注射后血清睾酮浓度稳定，并且 hCG 产品之间没有差异。实验室测试证实，4/10 个体中有 20% 的笔使用不当。 结论 尽管 hCG 药代动力学在形式上不具有生物等效性，但对血清睾酮的相似药效学作用表明，在测试剂量下，两种 hCG 提供了可比的临床效果。用于治疗促性腺激素缺乏男性的 rhCG 起始剂量应为 rhCG 笔 62.5 µg（6 次点击）。