TABLE 4.
Pharmacokinetic parameters for LB80331 and LB80317 in mouse plasma and livera
| Analyte | Tmax (h) | Cmax (μM) | AUC0-36 (μM·h) | AUC0-∞ (μM·h) | t1/2 (h) |
|---|---|---|---|---|---|
| LB80331 (plasma) | 1 | 6 | 17 | 17 | 2.0 |
| LB80331 (liver) | 1 | 44 | 102 | 102 | 2.8 |
| LB80331 di- and triphosphate (liver) | 1 | 17 | 64 | 64 | 3.2 |
| LB80317 (plasma) | 4 | 0.6 | 6 | 6 | 8.6 |
| LB80317 (liver) | 1 | 243 | 3,069 | 3,353 | 9.9 |
| LB80317 di- and triphosphate (liver) | 1 | 107 | 1,883 | 2,152 | 8.3 |
a
Values round up with one or no decimal space. The units are expressed in μM (micromole per liter), as the extracted proteins were neutralized with the same volume of ammonium bicarbonate for all mice. The drug concentration was then compared on basis of the same volume. The proportion of phosphorylated LB80331 was 39% for both AUC0-36 and AUC0-∞. The proportions of phosphorylated LB80317 were 39% and 41% for AUC0-36 and AUC0-∞, respectively.