Table 1.
Pharmacokinetic parameters of tenofovir and statistical comparison between tenofovir disoproxil orotate (DA-2802 319 mg) and fumarate (TDF 300 mg) after a single oral administration
| Parameters | Tenofovir disoproxil orotate (N=32) | Tenofovir disoproxil fumarate (N=32) | Geometric mean ratio (90% CI)a |
|---|---|---|---|
| Tmax (h)b | 0.87 (0.50–2.00) | 0.79 (0.50–2.00) | – |
| Cmax (ng/mL)c | 264.53±96.10 (247.87) |
284.19±73.99 (275.94) |
0.898 (0.815–0.990) |
| AUC0–t (ng × h/mL)c | 1,874.73±542.85 (1,793.10) |
2,039.10±493.74 (1,982.67) |
0.904 (0.836–0.978) |
| AUC0–inf (ng × h/mL)c | 2,111.51±559.86 (2,035.30) |
2,251.90±485.93 (2,203.27) |
0.924 (0.863–0.989) |
| t1/2 (h) | 20.45±4.56 | 19.56±3.47 | – |
| CL/F (L/h) | 165.71±66.42 | 139.18±28.91 | – |
Notes: Data expressed as arithmetic mean ± standard deviation, unless stated otherwise.
Geometric mean ratio calculations of orotate to fumarate based on log-transformed data.
Values expressed as median (minimum–maximum).
Values expressed as arithmetic mean ± standard deviation (geometric mean). “–” indicates data not shown.
Abbreviations: AUC0–t, area under the concentration-time curve to the last quantifiable concentration; AUC0–inf, area under the serum concentration–time curve from time 0 to infinity; CI, confidence interval; Cmax, maximum concentration; CL/F, apparent clearance; t1/2, elimination half-life; Tmax, time to reach Cmax.