Table 5. PK–PD Study of BMS-986242 (25) vs Linrodostat vs Epacadostat in Human SKOV3 Xenograft Tumor Mouse Model.
| compound | dose (mg/kg) | PKa | PDb |
|---|---|---|---|
| BMS-986242 (25) | 3c | 9.6 | 45% |
| BMS-986242 (25) | 10c | 21.1 | 58% |
| BMS-986242 (25) | 30c | 61.0 | 59% |
| linrodostat (1) | 60c | 34.9 | 61% |
| epacadostat (2) | 100d | 48.0 | 54% |
a
PK is AUC (0–24 h) in μM*h measured in the tumor.
b
PD is percent kynurenine AUEC (0–24 h) reduction measured in the tumor. %Kyn reduction was measured at steady state after the 5th dose, calculated as the area under Kyn concentration–time curve from 0 to 24 h and compared with that of vehicle control.
c
QD PO dosing.
d
BID PO dosing.