Kpuu of ethyl ester prodrug (PF-06757303) and its corresponding active diacid (PF-06649298) in human hepatocytes
| Incubation Time (min) | Kpuu of Active Diacid (PF-06649298) When Incubated Diacid | Kpuu of Prodrug (PF-06757303) When Incubated Prodrug | Kpuu of Active Diacid (PF-06649298) When Incubated Prodrug |
|---|---|---|---|
| 15 | 1.1 ± 0.2 | 0.07 ± 0.01 | 71 ± 21 |
| 40 | 1.5 ± 0.1 | 0.07 ± 0.01 | 71 ± 6 |
| 120 | 3.0 ± 0.2 | 0.07 ± 0.001 | 59 ± 2 |
Kpuu was measured at hepatocyte cell density of 0.5 million cells/ml and 1 μM test compound concentration.