Table 1. Comparison of ezetimibe binding affinity and cross-species efficacy.
| Species | KD, nM | ED50, mg/Kg |
|---|---|---|
| Mouse | 12,000 | 0.5000 |
| Rat | 542 | 0.0300 |
| Monkey | 41 | 0.0005 |
The KD values refer to [3H]EZE-gluc binding to enterocyte BBM preparations, as determined in the absence of detergents. The in vivo ED50 values are from cholesterol absorption and cholesterol feeding studies with ezetimibe in rat (2), monkey (2), and mouse (22). The correlation suggests the binding data are measuring the target of ezetimibe in vivo.