Table 2.
The preclinical data of NVP-CGM09719.
| NVP-CGM097 |
MDM2/MDM4 IC50 (nmol/L) |
GI50 (μmol/L) |
CYP3A4 IC50 (μmol/L) |
LogP |
LogPe |
Clint in human LM (μL/min/mg) |
|||
| 1.7/2000 |
0.35 |
17.0 |
5.8 |
−4.6 |
52.3 |
||||
| Dose (mg/kg) |
CL (mL/min/kg) |
VSS (L/kg) |
t1/2term (h) |
AUC p.o. (nmol/L·h/L) |
Cmaxp.o. (nmol/L/L) |
Tmaxp.o. (h) |
BAV (F%) |
PPB (%) |
|
| Mouse | 1/3 | 5 | 2.6 | 6.4 | 3337 | 207 | 4.0 | 71 | >99 |
| Rat | 1/3 | 7 | 6.4 | 12.1 | 2779 | 134 | 4.5 | 85 | >99 |
| Dog | 0.1/0.3 | 3 | 4.2 | 19.8 | 5993 | 251 | 2.7 | 74 | >99 |
| Monkey | 0.1/0.3 | 4 | 2.0 | 8.3 | 3730 | 363 | 1.3 | 57 | >99 |