Yatscoff R W, LeGatt D F, Kneteman N M
Department of Laboratory Medicine and Pathology, University of Alberta, Edmonton, Canada.
Ther Drug Monit. 1993 Dec;15(6):478-82. doi: 10.1097/00007691-199312000-00004.
Rapamycin (RAPA) is a new immunosuppressive drug with a potency similar to that of FK506 and up to a 100-fold greater than that of cyclosporine (CsA). RAPA has shown to be efficacious in the prolongation of allograft survival in a number of animal models. In early studies, RAPA was administered on a dose/weight basis, with little attention given to its effective blood concentration. Details describing the approaches used to establish a therapeutic range for the drug in animal transplant models are described. Guidelines for therapeutic monitoring of the drug are proposed. It is hoped that such preclinical work in animals will facilitate establishment of monitoring protocols for the drug in clinical trials.
雷帕霉素（RAPA）是一种新型免疫抑制药物，其效力与FK506相似，比环孢素（CsA）高100倍。在许多动物模型中，RAPA已被证明在延长同种异体移植物存活方面有效。在早期研究中，RAPA是按剂量/体重给药的，很少关注其有效血药浓度。本文描述了在动物移植模型中确定该药物治疗范围所采用方法的详细信息。提出了该药物治疗监测的指导原则。希望这种动物临床前工作将有助于在临床试验中建立该药物的监测方案。
