Table 2.
Pharmacokinetic and pharmacodynamic parameters of enteric-coated mycophenolate sodium (EC-MPS) in 66 renal transplant patients (median and range)
| All patients | EC-MPS 1440 mg day−1 | EC-MPS 2880 mg day−1 | Significance | |
|---|---|---|---|---|
| n= 66 | n= 57 | n= 8 | P | |
| MPA AUC0–12 (µg*h ml−1) | 38 (7–130) | 38 (7–130) | 40 (20–65) | NS |
| MPA C0 (µg ml−1) | 1.8 (0.5–23) | 1.8 (0.5–23) | 1.8 (0.6–16) | NS |
| MPA C12 (µg ml−1) | 1.5 (0.3–19.4) | 1.5 (0.3–19.4) | 1.5 (0.5–9.9) | NS |
| MPA Cmin (µg ml−1) | 1.0 (0.5–3.8) | 0.9 (0.5–3.8) | 1.2 (0.5–1.5) | NS |
| MPA Cmax (µg ml−1) | 11.6 (2.2–45.7) | 12 (2.2–45.7) | 11.8 (4.7–30.8) | NS |
| MPA Tmax (h) | 3.0 (0.5–10) | 3.0 (0.5–10) | 3.0 (2.0–6.0) | NS |
| Pharmacodynamic data | ||||
| IMPDH AEC0–12 (nmol*h mg−1 protein h−1) | 74 (12–371) | 79 (12–371) | 64 (15–110) | <0.05 |
| IMPDH A0 (nmol mg−1 protein h−1) | 8.4 (1.0–28.5) | 8.5 (1.0–28.5) | 5.6 (1.1–13.3) | NS |
| IMPDH A12 (nmol mg−1 protein h−1) | 8.0 (0.5–33.5) | 8.6 (0.5–33.5) | 4.9 (0.7–15.4) | NS |
| IMPDH Amax (nmol mg−1 protein h−1) | 15 (3–48) | 15 (5–48) | 11 (3–19) | <0.05 |
| IMPDH Amin (nmol mg−1 protein h−1) | 1.7 (0–20.7) | 1.7 (0–20.7) | 1.0 (0–2.3) | <0.05 |
| IMPDH Tmin (h) | 3 (0.5–10) | 3 (0.5–10) | 3 (2–5) | NS |
| IMPDH Imax (%) | 87 (57–100) | 87 (57–100) | 93 (71–100) | NS |
Fifty-seven patients were on 1440 mg day−1 and eight patients on 2880 mg day−1. One patient was on EC-MPS 720 mg day−1 (data not shown). Significance P is given for difference between the patient groups with EC-MPS 1440 mg day−1 and with EC-MPS 2880 mg day−1 (Mann–Whitney U-test). A, enzyme activity; AEC, area under the enzyme activity curve; AUC, area under the concentration–time curve; C, concentration; EC-MPS, enteric-coated mycophenolate sodium; I, inhibition; IMPDH, inosine monophosphate dehydrogenase; MPA, mycophenolic acid; T, time.