TABLE 1.
Simulated median pharmacokinetic parameters of tenofovir following inhibition of factors involved in drug absorption of TDFa
| Inhibited factor(s) | Cmax (ng ml−1) | Tmax (h) | AUC0–24 (ng · h ml−1) | C24 (ng ml−1) |
|---|---|---|---|---|
| None (control) | 238 | 3 | 3,036 | 43 |
| ABCB1 | 377 | 2 | 4,480 | 51 |
| ABCB1 + CES | 538 | 2 | 6,018 | 68 |
| Lipase | 1,013 | 3 | 12,873 | 199 |
| ABCB1 + lipase | 1,409 | 3 | 17,322 | 235 |
| ABCB1 + CES + lipase | 1,642 | 3 | 19,250 | 228 |
a
Parameters were determined following 6 days of once-daily oral dosing of 300 mg of TDF in 100 healthy male subjects.