Celgene Corporation, 86 Morris Avenue, Summit, NJ 07091, USA.
J Clin Pharmacol. 2010 Jul;50(7):767-74. doi: 10.1177/0091270009355157. Epub 2010 Feb 16.
Lenalidomide is a thalidomide analog and an immunomodulatory drug with demonstrated efficacy in various hematological malignancies. The distribution of lenalidomide into semen was evaluated in healthy subjects. Twenty-four male subjects were randomized into 4 equal groups for semen collection. All subjects received lenalidomide 25 mg once daily for 4 days. After the last dose, a single semen sample was collected from subjects, at approximately 2, 24, 72, and 168 hours for groups 1, 2, 3, and 4, respectively, and serial blood sampling was performed for 24 hours in all groups. The mean lenalidomide concentration in semen was 478 ng/mL at 2 hours and 10.0 ng/mL at 24 hours, which was higher than was the corresponding drug concentration in plasma (219 ng/mL at 2 hours and undetectable at 24 hours) but roughly paralleled the time course in plasma for drug elimination. The mean amount of lenalidomide was 1379 ng/ejaculate at 2 hours and 35 ng/ejaculate at 24 hours. The maximal drug content in a single ejaculate was <2000 ng (<0.01% of the daily 25-mg dose). Lenalidomide was undetectable in semen at 72 and 168 hours. Therefore, lenalidomide is essentially eliminated from seminal reservoirs by 72 hours postdose.
来那度胺是一种沙利度胺类似物，也是一种免疫调节剂，在多种血液系统恶性肿瘤中均显示出疗效。本研究评价了来那度胺在健康受试者精液中的分布情况。24 名男性受试者被随机分为 4 组，采集精液。所有受试者均接受来那度胺 25 mg，每日 1 次，连用 4 天。末次给药后，第 1、2、3 和 4 组受试者分别在约 2、24、72 和 168 小时采集单次精液样本，所有组均在 24 小时内进行连续采血。2 小时时，精液中平均来那度胺浓度为 478ng/ml，24 小时时为 10.0ng/ml，高于同期血浆中药物浓度（2 小时时为 219ng/ml，24 小时时无法检出），但与血浆中药物消除的时间过程大致平行。2 小时时，平均来那度胺排泄量为 1379ng/次射精，24 小时时为 35ng/次射精。单次射精中药物含量最高值<2000ng（<每日 25mg 剂量的 0.01%）。72 和 168 小时时，精液中无法检出来那度胺。因此，来那度胺在给药后 72 小时基本从精液贮库中消除。
