Figure 1.
Graphical representation of the clinical study design. Twelve (12) healthy volunteers received a single dose of 1000 mg MMF (CellCept®, pro-drug of MPA) and four (4) healthy volunteers received a single dose of placebo. PK and PD samples were taken pre-dose (0 h) and at 0.5 h, 1 h, 2 h, 3 h, 4 h, 24 h, and 7 days post-dose. PD samples were directly used for the measurement of IMPDH activity or first stimulated with PHA to measure cytokine production and T cell proliferation. The pre-dose PD samples were used to study the in vitro dose–effect relationship for MPA by adding a range of concentrations of 50, 10, 2, 0.4, and 0.08 μg/L MPA to the whole-blood stimulation. Post-dose PD samples were used to study ex vivo effects of MPA after a single dose of MMF.
