Table 1.
Dose | Individual | |||||
---|---|---|---|---|---|---|
10 mg/kg | Pharmacokinetic parameter | Cat 1 | Cat 2 | Cat 3 | Mean | |
After first dose (n = 3) | Time to maximum concentration (h) | 0.5 | 1.5 | 0.5 | 0.5 | |
Observed maximum concentration (μg/mL) | 0.35 | 0.55 | 1.3 | 0.73 | ||
Concentration at 12‐h post‐MMF administration (μg/mL) | BLLOQ | BLLOQ | BLLOQ | NA | ||
AUC0–loq (h·μg/mL) | 2.03 | 1.28 | 1.35 | 1.55 | ||
After last dose (n = 3) | Time to maximum (h) | 0.5 | 0.5 | 0.5 | 0.5 | |
Observed maximum concentration (μg/mL) | 1.23 | 3.78 | 1.88 | 2.29 | ||
Concentration at 12‐h post MMF administration (μg /mL) | BLLOQ | BLLOQ | 0.34 | NA | ||
AUC0–loq (h·μg /mL) | 1.77 | 8.54 | 4.56 | 4.95 | ||
15 mg/kg q12h | Pharmacokinetic parameter | Cat 4 | Cat 5 | Cat 6 | Mean | |
After first dose (n = 3) | Time to maximum (h) | 1 | 1 | 1 | 1 | |
Observed maximum concentration (μg/mL) | 2.24 | 4.11 | 3.24 | 3.19 | ||
Concentration at 12‐h post‐MMF administration (μg /mL) | BLLOQ | BLLOQ | 0.51 | NA | ||
AUC0–loq (h·μg/mL) | 2.15 | 5.37 | 5.47 | 4.33 | ||
After last dose (n = 2) | Time to maximum (h) | 0.25 | NA | 0.25 | 0.25 | |
Observed maximum concentration (μg/mL) | 4.84 | NA | 3.01 | 3.92 | ||
Concentration at 12‐h post MMF administration (μg /mL) | BLLOQ | NA | BLLOQ | NA | ||
AUC0–loq (h·μg /mL) | 2.52 | NA | 6.03 | 4.27 | ||
15 mg/kg q8h | Pharmacokinetic parameter | Cat 7 | Cat 8 | Cat 9 | Cat 10 | Mean |
After first dose (n = 4) | Time to maximum (h) | 0.25 | 0.5 | 1.5 | 1.5 | 0.93 |
Observed maximum concentration (μg/mL) | 3.0 | 6.63 | 0.86 | 1.40 | 2.97 | |
Concentration at 12‐h post MMF administration (μg /mL) | 0.59 | 1.36 | 0.70 | 0.60 | 0.81 | |
AUC0–loq (h·μg /mL) | 14.9 | 31.0 | 5.57 | 9.48 | 15.2 |
Abbreviations: BLLOQ, below lower limit of quantification (0.3 μg/mL); NA, not applicable.
For 10 mg/kg dosage regimen protocol, the median observed maximum plasma concentration and AUC0‐loq after the first and last dose were not different (P = .2).