Therapeutic indices of SCH 351591 and cilomilast
| Parameter | SCH 351591 | Cilomilast |
|---|---|---|
| Guinea pig HIB | ||
| MED (mg/kg p.o.) | 0.3 | 3 |
| C max (μg/ml) @MED | 0.24 | 0.5 |
| AUC (μg · h/ml) @ MED | 1.7 | 4.9 |
| Ferret emesis | ||
| MND (mg/kg p.o.) | 5 | 1 |
| C max (μg/ml) @ MND | 3.5 | 2.4 |
| AUC (μg · h/ml) @ MND | 26.7 | 18.3 |
| Therapeutic ratio | ||
| C max @ MND/C max @MED | 15 | 5 |
| AUC @ MND/AUC @ MED | 16 | 4 |
MED against hyperventilation-induced bronchospasm in guinea pigs (Fig.5A) and maximum nonemetic dose (MND) against emesis in ferrets (Table8) were determined under comparable experimental conditions for both compounds after a single dose.