Table 9 Dog pharmacokinetic parameters of S733 and SJ311 after oral administration
From: Selecting an anti-malarial clinical candidate from two potent dihydroisoquinolones
Dose (mg/kg) | (+)-SJ733 | (+)-SJ311 | ||
|---|---|---|---|---|
3 | 30 | 3 | 30 | |
Cmax (µM) | 3.0 ± 0.7 | 25.6 ± 2.1 | 4.0 ± 0.8 | 35.0 ± 5.1 |
Tmax (h) | 0.83 | 1.67 | 3.3 ± 1.2 | 3.0 ± 1.7 |
Half life (h) | 11.4 ± 5.0 | 5.3 ± 0.7 | 6.1 ± 0.6 | 6.7 ± 1.4 |
AUCinf (h.µM) | 40.6 ± 12.9 | 243 ± 52.9 | 56.2 ± 12.1 | 601 ± 137 |
CL (L/h/kg) | 0.169 ± 0.055 | 0.274 ± 0.067 | 0.121 ± 0.030 | 0.113 ± 0.025 |
V (L/kg) | 2.6 ± 0.8 | 2.1 ± 0.8 | 1.1 ± 0.4 | 1.1 ± 0.4 |
F% | 115 ± 29 | 73.7 ± 16.1 | 73.0 ± 15.8 | 77.9 ± 17.7 |
Dose in urine (%) | 2.8 ± 0.2 | 3.1 ± 1.9 | 34.7 ± 15.9 | 33.4 |