Hedayat S, Kershner R P, Su G
Department of Mathematics, Statistics, and Computer Science (M/C 249), University of Illinois at Chicago 60607-7045, USA.
J Biopharm Stat. 1996 Nov;6(4):411-24. doi: 10.1080/10543409608835153.
FK506 (tacrolimus) has been shown to be a safe and effective immunosuppressant for the prevention of organ rejection after liver and kidney transplantation. Like cyclosporine, the use of FK506 has been associated with some adverse effects such as toxicity and organ rejection. Therapeutic monitoring of the whole-blood FK506 drug concentrations has been used in an effort to determine how the concentration of FK506 in the blood is related to the development of toxicity or the risk for organ rejection. Cox regression analysis of two recent clinical trials of FK506 in patients receiving kidney and liver transplants shows a significant correlation between the whole-blood FK506 concentrations and the incidence of both toxicity and organ rejection. Because of these relationships and the pharmacokinetics of FK506, therapeutic monitoring of the whole-blood FK506 levels is expected to be helpful for minimizing the risks of both toxicity and rejection in liver and kidney transplants.
FK506（他克莫司）已被证明是一种安全有效的免疫抑制剂，可预防肝移植和肾移植后的器官排斥反应。与环孢素一样，使用FK506也会产生一些不良反应，如毒性和器官排斥。对全血FK506药物浓度进行治疗药物监测，旨在确定血液中FK506的浓度与毒性发展或器官排斥风险之间的关系。对最近两项FK506用于肾移植和肝移植患者的临床试验进行的Cox回归分析表明，全血FK506浓度与毒性和器官排斥的发生率之间存在显著相关性。鉴于这些关系以及FK506的药代动力学，对全血FK506水平进行治疗药物监测有望有助于降低肝移植和肾移植中毒性和排斥反应的风险。
