Mannaerts B, Shoham Z, Schoot D, Bouchard P, Harlin J, Fauser B, Jacobs H, Rombout F, Coelingh Bennink H
Medical R & D Unit, Organon International, Oss, The Netherlands.
Fertil Steril. 1993 Jan;59(1):108-14.
To assess safety, pharmacokinetic, and pharmacodynamic properties of recombinant human follicle-stimulating hormone (FSH; Org 32489, Organon International, Oss, The Netherlands) after a single intramuscular injection in the buttock.
In a prospective study, safety variables, serum FSH, luteinizing hormone, inhibin, estradiol (females only), and testosterone (males only) were evaluated up to a maximum of 11 days after injection of 300 IU recombinant FSH.
Four specialist Reproductive Endocrinology and Infertility units.
Fifteen men and women exhibiting all pituitary gonadotropin deficiency.
A single bolus of 300 IU recombinant FSH was well tolerated, and no drug-related adverse effects were noted. Comparison of before and after treatment safety variables, including serum antirecombinant FSH antibodies, showed no changes of clinical relevance. Analysis of serum FSH levels revealed comparable elimination half-lives of 44 +/- 14 (mean +/- SD) and 32 +/- 12 hours in women and men volunteers, respectively. In contrast, peak FSH concentrations were significantly lower in women than in men volunteers (4.3 +/- 1.7 versus 7.4 +/- 2.8 IU/L), and the time required to reach peak levels of FSH was significantly longer in women than in men (27 +/- 5 versus 14 +/- 8 hours). The area under the serum level versus time curve tended to be smaller in women than in men volunteers (339 +/- 105 versus 452 +/- 183 IU/L x hours), but the difference did not reach statistical significance. Together these data suggest that recombinant FSH is absorbed from its intramuscular depot to a lower rate and extent in women than in men. In both sexes a relationship between serum FSH levels and body weight was apparent. During the experimental period, other hormones remained low at baseline levels or were only slightly increased.
Our findings indicate that recombinant FSH is well tolerated and that it is absorbed from its intramuscular depot to a higher rate and extent in men than in women. After intramuscular administration, its half-life is in good agreement with that previously reported for natural FSH.
评估重组人促卵泡激素（FSH；Org 32489，欧加农国际公司，荷兰奥斯）单次臀部肌肉注射后的安全性、药代动力学和药效学特性。
在一项前瞻性研究中，在注射300 IU重组FSH后长达11天的时间里，对安全性变量、血清FSH、促黄体生成素、抑制素、雌二醇（仅女性）和睾酮（仅男性）进行评估。
四个专业生殖内分泌与不孕不育科室。
15名表现出所有垂体促性腺激素缺乏的男性和女性。
单次推注300 IU重组FSH耐受性良好，未观察到与药物相关的不良反应。治疗前后安全性变量的比较，包括血清抗重组FSH抗体，未显示出具有临床相关性的变化。血清FSH水平分析显示，女性和男性志愿者的消除半衰期分别为44±14（平均值±标准差）和32±12小时。相比之下，女性志愿者的FSH峰值浓度显著低于男性（4.3±1.7对7.4±2.8 IU/L），女性达到FSH峰值水平所需的时间显著长于男性（27±5对14±8小时）。女性志愿者血清水平-时间曲线下面积倾向于小于男性（339±105对452±183 IU/L·小时），但差异未达到统计学意义。这些数据共同表明，重组FSH从肌肉注射部位的吸收速率和程度在女性中低于男性。在两性中，血清FSH水平与体重之间的关系明显。在实验期间，其他激素在基线水平保持较低或仅略有升高。
我们的研究结果表明，重组FSH耐受性良好，且从肌肉注射部位的吸收速率和程度在男性中高于女性。肌肉注射后，其半衰期与先前报道的天然FSH半衰期一致。
