Effects of Race on the Pharmacokinetics of Tacrolimus in Transplantation Patients

OBJECTIVE: To investigate the population pharmacokinetics of the oral tacrolimus among transplant recipients of different ethnic background, to establish pharmacokinetics model of tacrolimus and provide scientific reference for individual therapy scheme of tacrolimus in different transplant recipients. METHODS: The literatures about the pharmacokinetics of tacrolimus were retrieved from PubMed and Wangfang database, and related pharmacokinetics data of transplant recipients were collected from published clinical trials literatures. Nonlinear mixed effects model(NONMEM) was used to analyze the collected data statistically to establish population pharmacokinetics model. Pattern evaluation and Bootstrap validation of model were conducted. RESULTS: The population pharmacokinetics of tacrolimus was in line with one-compartment model. The apparent clearance (CL/F) of tacrolimus was lower in the Caucasian subjects (11.1 L/h) than in the Asian subjects (15.7 L/h). The population pharmacokinetics of apparent clearance of tacrolimus: CL=[15.7×Race+11.1×(1-Race)]×(Dose/10)0.116. CONCLUSIONS: Population pharmacokinetics of tacrolimus can be affected by race.