Table 1.
Plasma tenofovir, plasma tenofovir alafenamide, plasma emtricitabine and intracellular tenofovir diphosphate and emtricitabine triphosphate PK parameters following 28 days of administration of 25/200 mg of tenofovir alafenamide/emtricitabine once daily, co-administration of 25/200 mg of tenofovir alafenamide/emtricitabine once daily and rifampicin for 28 days and following 28 days of 300 mg of tenofovir disoproxil fumarate in healthy volunteers
| PK parameter | TFV |
TAF |
FTC |
||||
|---|---|---|---|---|---|---|---|
| TAF/FTC | TAF/FTC+RIF | TDF | TAF/FTC | TAF/FTC+RIF | TAF/FTC | TAF/FTC+RIF | |
| C max (ng/mL) | 18 (16–22) | 6 (6–7) | 249 (214–289) | 64 (51–80) | 32 (27–39) | 1559 (1369–1774 ) | 1578 (1347–1849) |
| GCV (%) | 34 | 38 | 44 | 53 | |||
| C 24 (ng/mL) | 7 (6–9) | 3 (3–4) | 52 (45–60) | – | – | 89 (76–104) | 62 (53–72) |
| GCV (%) | 26 | 43 | |||||
| AUC0–24 (ng·h/mL) | 208 (172–251) | 95 (84–106) | 2307 (2040–2609) | 88 (69–112) | 39 (31–49) | 9299 (8262–10465) | 9160 (8418–9966) |
| GCV (%) | 30 | 36 | 53 | 59 | |||
| T max (h) | 1.3 (1.1–1.6) | 2 (1.5–2.7) | 1.7 (1.4–2.1) | 1.3 (1–1.7) | 1.4 (1.1–1.7) | 2.1 (1.7–2.4) | 1.9 (1.5–2.4) |
|
|
|||||||
|
TFV-DP |
FTC-TP |
||||||
| TAF/FTC | TAF/FTC+RIF | TDF | TAF/FTC | TAF/FTC+RIF | |||
|
|
|||||||
| C max (fmol/106 cells) | 808.2 (618.4–1056.4) | 499.4 (375.8–663.5) | 113.5 (81.9–157.2) | 14620.0 (11641.4–18360.6) | 14425.5 (11482.8–18122.4) | ||
| GCV (%) | 69 | 64 | |||||
| C 24 (fmol/106 cells) | 613.8 (481.1–783.1) | 352.9 (250.7–496.7) | 85.1 (63.7–113.7) | 9463.1 (7727.5–11588.6) | 8259.5 (6410.0–10642.7) | ||
| GCV (%) | 82 | 102 | |||||
| AUC0–24 (fmol·h/106 cells) | 13052.6 (8864.8–19218.8) | 8325.8 (6015.0–11524.3) | 1976.4 (1484.4–2631.6) | 230200.3 (161076.5–328990.8) | 237695.3 (185749.6–304167.8) | ||
| GCV (%) | 87 | 58 | |||||
| T max (h) | 4 (2.2–7.3) | 9.0 (3.8–11.8) | 3.2 (1.6–5.4) | 3.5 (2.3–5.3) | 7.0 (4.3–9.2) | ||
Data are GM (95% CI) except for T max, which is reported as median (IQR).
TFV, tenofovir; TAF, tenofovir alafenamide; FTC, emtricitabine; TFV-DP, tenofovir diphosphate; FTC-TP, emtricitabine triphosphate; RIF, rifampicin; TDF, tenofovir disoproxil fumarate.