Metabolite formation activities of [14C]apixaban in HLM from adult and pediatric donors and HIM at 2.5 and 25 μM drug concentrations
HLM from adult and pediatric donors and HIM at 1 mg/ml proteins were incubated with 2.5 or 25 μM apixaban in the presence of NADPH at 37°C for 60 min.
| Microsomes | Formation of Metabolites | |||||
|---|---|---|---|---|---|---|
| 2.5 μM | 25 μM | |||||
| M2 | M4 | M7 | M2 | M4 | M7 | |
| pmol/min/mg protein | ||||||
| HLM (adult) | 0.76 ± 0.11 | 0.19 ± 0.02 | 3.49 ± 0.91 | 8.39 ± 2.44 | 2.25 ± 0.99 | 33.64 ± 12.9 |
| HLM (1–6 years) | 0.68 ± 0.39 | Trace | 0.71 ± 0.17 | 3.44 ± 0.93 | 1.05 ± 0.53 | 9.84 ± 3.62 |
| HLM (<1 year) | 0.65 ± 0.09 | 0.20 ± 0.08 | 3.02 ± 0.97 | 9.96 ± 3.17 | 3.12 ± 0.99 | 37.67 ± 19.9 |
| HIM (adult) | 0.16 ± 0.02 | 0.13 ± 0.02 | 1.47 ± 0.07 | 2.08 ± 0.46 | 2.01 ± 0.47 | 10.3 ± 3.87 |