Body
PK Parameter | Initial Dose: RAL 1.5 mg/kg Once Daily RAL-Naive (n = 25)d |
Initial Dose: RAL1.5 mg/kg Once Daily RAL-Exposed (n = 10) |
Days 15–18: RAL 3.0 mg/kg Twice Daily RAL-Naive (n = 24)e |
Days 15–18: RAL 3.0 mg/kg Twice Daily RAL-Exposed (n = 9)f |
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GM (CV%) | Target | GM (CV%) | Target | GM (CV%) | Target | GM (CV%) | Target | |
AUC0-24h (mg·h/L)a |
38.2 (42.0%) | Met: 13 Above: 11 Below: 0 |
42.9 (25.3%) | Met: 4 Above: 6 Below: 0 |
------- | --------- | -------- | ------- |
AUC0-12h (mg·h/L) |
-------- | -------- | --------- | -------- | 14.3 (49.5%) | Met: 14 Above: 8 Below: 1 |
18.3 (62.8%) |
Met: 3 Above: 5 Below: 1 |
Ctrough (ng/mL)b |
948 (84.0%) | Above: 25 Below: 0 |
946 (74.0%) | Met: 10 Above: 0 |
176 (162.1%) | Above: 22 Below: 2 |
274 (176.4%) | Above: 8 Below: 2 |
Cmax (ng/mL)c |
2,350 (36.5%) | Below: 25 Above: 0 |
2,565.3 (23.1%) | Met: 10 Above: 0 |
2,849 (47.5%) | Below: 24 Above: 0 |
3,667 (46.3%) | Met: 9 Above: 0 |
Tmax (hours) |
5.4 (71.5%) | N/A | 3.8 (88.8%) | N/A | 2.3 (77.1%) | N/A | 1.9 (52.3%) | N/A |
T½ (hours) |
15.8 (101.4%) | N/A | 14.4 (69.5%) | N/A | 2.5 (34.1%) | N/A | 2.9 (20.1%) | N/A |
a AUC targets: AUC0-24h 12–40 mg·h/L and AUC0-12h 6–20 mg·h/L. b Ctrough concentration >33 ng/mL. For initial dose, Clast collected at 24 hours was used. For Days 15 to 18, C12h was estimated when the 12 hours post-dose sample was collected earlier than 12 hours after dosing (the protocol specified a sample collection time of 8 to 12 hours post dose). c Cmax <8,724 ng/mL. d AUC0-24h could not be estimated for one infant. eAUC0-12h could not be estimated for one infant with delayed absorption. f AUC0-12h and Cmax could not be estimated for one infant with incomplete sample collection. Key: AUC = area under the curve; Clast = last measurable plasma concentration; Cmax = maximum concentration; Ctrough = trough concentration; CV = coefficient of variation; GM = geometric mean; PK = pharmacokinetic; RAL = raltegravir; T1/2 = half-life; Tmax = time to reach maximum concentration |