Table 2.
Demographics of Participants and Pharmacokinetic Parameters of Tenofovir Alafenamide Fumarate and Tenofovir in Combination With 1 of 4 Anchor Drugs
| Characteristic | Anchor Drug | Reference Adults | ||||
|---|---|---|---|---|---|---|
| TAF + DTG | TAF + ATV/r | TAF + DRV/r | TAF + LPV/r | |||
| TAF dose | <25 kg: 15 mg (n = 9) ≥25 kg: 25 mg (n = 9) |
<25 kg: 15 mg (n = 15) ≥25 kg: 25 mg (n = 17) |
<25 kg: 15 mg (n = 18) ≥25 kg: 25 mg (n = 16) |
<25 kg: 15 mg (n = 8) ≥25 kg: 25 mg (n = 12) |
25 mg TAF unboosted/10 mg TAF boosted [4, 11] | 25 mg TAF DRV/c [4] |
| Boosting | Unboosted | Boosted | Boosted | Boosted | Unboosted/boosted | Boosted |
| No. of participants | 18 | 32 | 34 | 20 | 539 | 11 |
| Demographics | ||||||
| Age, y | 10.9 (5.46–14.2) [7.64–13.1] |
9.98 (4.79–15.0) [6.83–13.2] |
10.9 (3.83–14.7) [8.92–12.7] |
11.2 (4.27–14.6) [9.38–13.4] |
… | … |
| Weight, kg | 25.9 (15.9–53.0) [19.4–35.2] |
25.8 (14.5–50.0) [20.4–33.7] |
24.0 (14.5–47.0) [21.6–32.7] |
25.5 (14.2–48.5) [22.5–41.9] |
… | … |
| BMI, kg/m2 | 16.4 (12.2–21.7) [14.4–17.4] |
15.9 (12.8–19.8) [14.4–16.9] |
14.8 (12.5–19.0) [13.9–16.5] |
15.8 (13.0–20.4) [14.0–18.2] |
… | … |
| Male sex, No. (%) | 8 (44%) | 15 (47%) | 16 (47%) | 9 (45%) | … | … |
| TAF | ||||||
| AUClast(ng*h/mL) | 285 (79) | 538 (54) | 232 (61) | 212 (98) | 206 (72) | 222 (NR) |
| Cmax (ng/mL) | 145 (91) | 309 (78) | 155 (104) | 155 (107) | 162 (51) | 181 (NR) |
| Tmax | 1.1 (0.5–4.0) | 2.0 (0.5–6.1) | 1.0 (0.5–4.1) | 1.0 (0.5–2.0) | … | … |
| % with AUC >55 ng*h/mL | 100% | 100% | 100% | 100% | … | … |
| TFV | ||||||
| AUCtau, ng*h/mL | 324 (29) | 847 (37) | 744 (26)a | 864 (46) | 293 (27) | 937 (NR) |
| Cmax, ng/mL | 19.6 (26) | 53.2 (42) | 44.5 (26) | 50.3 (43) | 15.2 (26) | 56 (NR) |
| Ctrough, ng/mL | 11.0 (35) | 28.1 (39) | 26.1 (28) | 31.2 (48) | 11 (28.5) | 33.2 (NR) |
| Tmax, h | 2.0 (1.0–4.0) | 3.0 (1.0–6.0) | 2.0 (1.0–6.1) | 2.0 (0.5–6.0) | … | … |
| % with AUC <2586 ng*h/mL | 100% | 100% | 100% | 100% | … | … |
Pharmacokinetic data (except Tmax) are presented as geometric mean with coefficient of variation (CV%); age, weight, BMI, and Tmax are presented as median (range) [interquartile range].
Abbreviations: ATV/r, atazanavir/ritonavir; AUC, area under the concentration–time curve from 0 to 24 h (AUCtau) or from 0 to the last sample with a measurable concentration (AUClast); BMI, body mass index; Cmax, highest concentration of pharmacokinetic curve; Ctrough, concentration 24 hours after dose; DRV/c, darunavir/cobicistat; DRV/r, darunavir/ritonavir; DTG, dolutegravir; LPV/r, lopinavir/ritonavir; NR, not reported; TAF, tenofovir alafenamide fumarate; TFV, tenofovir; Tmax, time maximum concentration was reached.
Based on 33 participants because the AUCtau of 1 participant could not be accurately calculated.