TABLE 2.
Summary of Pharmacokinetic Parameters for Abacavir, Lamivudine, and Lopinavir
| Drug | Cohort | PK Parameter | Median (Min to Max) | Geometric Mean | 90% CI |
| ABC* | 1A + 1B | AUC0–12 (µg.h/mL) | 31.12 (13.85–63.35) | 29.87 | 26.29 to 33.93 |
| AUC0–inf (µg.h/mL) | 36.12 (16.37–89.91) | 34.81 | 29.90 to 40.53 | ||
| AUC0–12/AUC0–inf ratio | 0.87 (0.70–0.98) | 0.86 | 0.83 to 0.89 | ||
| Cmax (µg/mL) | 4.93 (2.55–7.24) | 4.79 | 4.38 to 5.23 | ||
| Tmax (h) | 2.0 (0.9–4.0) | — | — | ||
| C12 (µg/mL) | 0.93 (0.12–2.95) | 0.757 | 0.57 to 1.01 | ||
| CL/F (L/h/kg) | 0.23 (0.13–0.51) | 0.25 | 0.22 to 0.29 | ||
| Dose (mg/kg) | 8.61 (6.63–11.36) | — | — | ||
| 3TC* | 1A + 1B | AUC0–12 (µg.h/mL) | 13.38 (2.80–22.14) | 12.61 | 10.72 to 14.83 |
| AUC0–inf (µg.h/mL) | 16.00 (3.26–26.47) | 14.28 | 12.06 to 16.92 | ||
| AUC0–12/AUC0–inf ratio | 0.90 (0.75–0.95) | 0.88 | 0.86 to 0.90 | ||
| Cmax (µg/mL) | 2.09 (0.57–3.18) | 2.00 | 1.75 to 2.29 | ||
| Tmax (h) | 3.1 (2.0–4.1) | — | — | ||
| C12 (µg/mL) | 0.39 (0.09–0.75) | 0.33 | 0.26 to 0.41 | ||
| CL/F (L/h/kg) | 0.27 (0.16–1.23) | 0.31 | 0.26 to 0.35 | ||
| Dose (mg/kg) | 4.30 (3.31–5.68) | — | — | ||
| LPV* | 1A + 1B | AUC0–12 (µg.h/mL) | 4.89 (0–26.33) | 3.49 | 2.13 to 5.72 |
| AUC0–inf (µg.h/mL) | NC | NC | NC | ||
| AUC0–12/AUC0–inf ratio | NC | NC | NC | ||
| Cmax (µg/mL) | 0.75 (<0.05 to 4.06) | 0.58 | 0.38 to 0.90 | ||
| Tmax (h) | 4.1 (1.1–8.1) | — | — | ||
| C12 (µg/mL) | 0.11 (<0.05 to 2.31) | 0.21 | 0.12 to 0.37 | ||
| CL/F (L/h/kg) | NC | NC | NC | ||
| Dose (mg/kg) | 11.48 (8.84–15.15) | — | — | ||
| Dose (mg/m2) | 181 (154–215) | — | — |
3TC, lamivudine; ABC, abacavir; C12, 12-hours post-dose; CL/F, apparent clearance; inf, infinity; LPV, lopinavir; NC, cannot calculate; PK, pharmacokinetic.
*
Reference data for comparison with PETITE study AUC0–inf: PENTA-15 children, ABC and 3TC steady state, AUC0–12SS were 5.43 µg.h/mL (95% CI: 4.45 to 6.62) at 8.0 mg/kg twice daily and 4.74 µg.h/mL (95% CI: 3.95 to 5.70) at 4.0 mg/kg twice daily, respectively.[19] In the study conducted by Foissac et al, infants aged 6 weeks, with median (range) LPV steady-state AUC0–12SS 54.5 µg.h/mL (33.9–85.8), received LPV/r 40/10 mg twice daily.[27]