Table 8. In Vitro Safety Profiling of Proteasome Inhibitors31 a.
| cmp | 4 | 5 | 6 | 7 |
| MNT −S9 | positive | negative | negative | negative |
| MNT +S9 | negative | positive | negative | negative |
| hERG binding [μM] | 10.9 | 4.1 | 13.8 | >30 |
| q-patch [μM] | 7.8 | 0.9 | 1.9 | 12.7 |
| efficacious dose [mg/kg] | 150 qd | 100 qd | 100 qd | 15 bid |
| fCmax[μM] | 0.22 | 0.12 | 0.20 | 0.07 |
| TI (hERG) | 50 | 33 | 70 | 403 |
| TI (q-patch) | 36 | 7 | 10 | 170 |
a
cmp: compound; MNT: micronucleus test; +S9: in the presence of the rat liver S9 fraction; −S9: in the absence of rat liver S9 fraction, hERG: human ether-a-go-go-related gene; q-patch: automated patch clamp; TI: therapeutic index.