LMP7 activity inhibition (IC50) measured in vitroa in U266B1 cells and PBMCs from rat, dog, and monkey and LMP7 activity inhibition (IC50) corrected for plasma protein binding obtained from PK/PD modeling of in vivo data in U266B1 cells xenografted to mouse, rat spleen tissue, and dog PBMCs, with uncertainty expressed as CV% in brackets.
| Species | In vitro IC50 (nM) | In vivo IC50 (nM) |
|---|---|---|
| Human U266B1 cells | 2 | 1.4 (25.8) |
| Rat | 9.3 | 7.1 (37.7) |
| Dog | 34.5 | 9.1 (25) |
| Monkey | 10 | ND |
ND, not determined.
aSanderson et al. (2021).