TABLE 7.
Levels of active anabolite in unstimulated and stimulated human PBMCs incubated with TFV or CMX157 for 24 h
| Cells | Drug and concn | No. of pmol/1 × 106 cells (% relative SD)a |
||
|---|---|---|---|---|
| TFV | TFV-P | TFV-PP | ||
| Unstimulated PBMCs | TFV, 1.0 μM | ND | BLQ | 0.05 (2.4) |
| TFV, 10 μM | 0.11 (13.3) | 0.05 (5.1) | 0.15 (9.4) | |
| CMX157, 0.01 μM | ND | BLQ | 0.07 (8.9) | |
| CMX157, 0.1 μM | 0.05 (2.3) | BLQ | 0.07 (3.6) | |
| CMX157, 1.0 μM | 0.07 (7.4) | 0.05 (6.8) | 0.22 (3.2) | |
| CMX157, 10 μM | 0.19 (5.9) | 0.12 (7.7) | 1.1 (9.8) | |
| PHA/IL-2-stimulated PBMCs | TFV, 1.0 μM | BLQ | BLQ | 0.05 (4.9) |
| TFV, 10 μM | 0.09 (41.5) | BLQ | 0.22 (8.0) | |
| CMX157, 0.01 μM | BLQ | BLQ | 0.07 (12.4) | |
| CMX157, 0.1 μM | BLQ | BLQ | 0.25 (9.5) | |
| CMX157, 1.0 μM | 0.56 (14.7) | 0.30 (6.9) | 1.7 (6.3) | |
| CMX157, 10 μM | 1.9 (5.9) | 0.90 (6.2) | 5.5 (14.2) | |
a
ND, not done; BLQ, below limit of quantification.