Table 3.
Comparison of dolutegravir pharmacokinetic (PK) parameters by body weight at each intensive PK sampling visit
| Pharmacokinetic visit at a median of 4.5 weeks on dolutegravir |
Pharmacokinetic visit at a median of 32 weeks on dolutegravir |
|||||
|---|---|---|---|---|---|---|
| Parameter | 20 to <40 kg (N = 18) | ≥40 kg (N = 7) | P value | 20 to <40 kg (N = 17) | ≥40 Kg (N = 8) | P value |
| T1/2 | 9.1 (8.1 – 10.7) | 11.4 (8.3 – 15.1) | 0.215 | 8..5 (7.6 – 10.3) | 12.0 (6.3 – 17.4) | 0.503 |
| Tmax (h) | 4.1 (2.7 – 4.2) | 3.9 (1.2 – 4.2) | 0.431 | 4.0 (1.1 – 4.1) | 4.0 (1.0 – 4.3) | 1.000 |
| Cmax (mg/L) | 8.9 (7.1 – 11.7) | 5.6 (4.1 – 6.4) | 0.002 | 7.7 (6.7 – 12.0) | 4.6 (4.2 – 6.2) | 0.006 |
| C24h (mg/L) | 1.8 (1.3 – 2.6) | 1.5 (0.8 – 2.2) | 0.289 | 1.4 (1.2 – 2.3) | 1.3 (0.7 – 1.9) | 0.503 |
| AUC0-24h (mg *h/mL) | 125.1 (88.9 – 148.6) | 86.8 (46.8 – 101.8) | 0.032 | 114.9 (74.7 – 140.9) | 66.3 (53.2 – 98.8) | 0.016 |
| Vd/F (L) | 6.5 (3.9 – 7.6) | 12.7 (9.0 – 17.2) | 0.008 | 5.8 (4.0 – 7.4) | 13.0 (9.5 – 18.1) | 0.007 |
| CL/F (L/h) | 0.41 (0.34 – 0.56) | 0.58 (0.49 – 1.1) | 0.032 | 0.44 (0.36 – 0.67) | 0.76 (0.52 – 0.95) | 0.013 |
T1/2, half-life, Tmax, time to peak concentration; Cmax, peak concentration; C24h, concentration at 24 hours post-dose, AUC0-24h, total area under the curve from time 0 hours to 24hours; Vd/F, apparent volume of distribution, CL/F, apparent oral clearance.