Table 2. Comparison of BMS-986158 and 15 Preclinical PK Parameters17.
mouse |
rat |
dog |
monkey |
|||||
---|---|---|---|---|---|---|---|---|
BMS-986158 | 15 | BMS-986158 | 15 | BMS-986158 | 15 | BMS-986158 | 15 | |
dose (iv/po, mg/kg) | 1.75/5.0 | 1.0/3.0 | 1.0/5.0 | 1.0/5.0 | 0.1/0.3 | 0.1/0.3 | 0.1/0.3 | 0.1/0.3 |
CLp ((mL/min)/kg) | 12 | 4.2 | 41 | 18 | 15 | 13 | 32 | 4.3 |
Vd (L/kg) | 1.9 | 1.4 | 4.3 | 2.9 | 5.3 | 5.8 | 4.2 | 1.3 |
half-life (iv, h) | 1.9 | 3.4 | 4.2 | 4.1 | 5.6 | 7.6 | 2.0 | 4.0 |
F (%) | 100 | 100 | 47 | 74 | 59 | 73 | 16 | 85 |
AUC (po, nM·h) | 18000 | 25000 | 2000 | 6600 | 410 | 550 | 85 | 1900 |