Pharmacokinetics of tacrolimus: clinically relevant aspects

Pharmacogenomics and personalized medicine: a review focused on their application in the Chinese population

“…Tacrolimus (also known as FK506) was first approved by the US FDA in 1994 and it has remarkably improved patient survival after organ transplant. However, tacrolimus treatment has many drawbacks, including a narrow therapeutic window, high inter-and intraindividual variability in pharmacokinetics/pharmacodynamics and severe adverse effects [4][5][6] . Therefore, a large number of studies have been devoted to exploring personalized determination for tacroli-the importance of studying ABCB1 genetics as an independent factor is minimal.…”

Clinical Pharmacokinetics of Triple Immunosuppression Scheme in Kidney Transplant (Tacrolimus, Mycophenolate Mofetil and Corticosteroids)

“…Tacrolimus is absorbed rapidily in most subjects, an oral dose of 0.15 mg/kg/12 hours at steady state, the peak concentration (Cmax) averages 45 ng/mL, with a corresponding mean time to peak concentration (Tmax) of 1.5 hours. There is a strong correlation between the area under the concentration-time curve (AUC) and the trough concentration of tacrolimus (Cmin) in whole blood, therefore doses are individualized on the basis of target whole blood trough concentrations (Staatz & Tett, 2004;Undre, 1999). In stable liver transplant recipients, the oral bioavailability of tacrolimus is decreased if it is taken after food containing moderate fat content (Bekersky et al, 2001a(Bekersky et al, , 2001b.…”

On-line solid-phase extraction high-performance liquid chromatography-tandem mass spectrometry for the quantitative analysis of tacrolimus in whole blood hemolyzate

“…Nevertheless, such sample preparation steps are labor-intensive, time-consuming, and difficult to automate, and hence, undesirable for routine procedures. Moreover, part of the tacrolimus in the whole blood is removed together with the erythrocytes [20][21][22].…”

“…For the detection of tacrolimus, we employ electrospray ionization tandem mass spectrometry (ESI-MS/MS) in a linear ion-trap mass spectrometer. Here, the use of selected reaction monitoring (SRM) shall assure high scan rates in combination with maximal selectivity and sensitivity for the analyte, allowing the quantification of tacrolimus in physiologically relevant concentrations of 5-20 ng mL −1 via external calibration [21,33].…”