Parameter | UK-294,315 | UK-338,003 | ||||
---|---|---|---|---|---|---|
Rat (n = 2) | Human (n = 10) | Rat (n = 2) | Human (n = 5) | |||
Intravenous dose (mg/kg) | 0.5 | N.A.a | 0.5 | N.A. | ||
Elimination half-life (h) | 1.0 | N.A. | 1.0 | N.A. | ||
Plasma clearance (ml/min/kg) | 91 | N.A. | 22 | N.A. | ||
Unbound intrinsic plasma clearance (ml/min/kg) | 61250 | N.A. | 40 | N.A. | ||
Volume of distribution (l/kg) | 5.6 | N.A. | 1.7 | N.A. | ||
Unbound volume of distribution (l/kg) | 70 | N.A. | 24 | N.A. | ||
Oral dose (mg/kg) | 4 | 0.86b | 1.0 | 0.02c | ||
Cmax (ng/ml) | 14 | 63 (41) | 105 | 7.5 (1.56) | ||
Tmax (h) | 4 | 0.7 (0.42) | 0.5 | 1.3 (0.27) | ||
Elimination half-life (h) | 2.8 | 12 (2.4) | 2.9 | 11.4 (2.14) | ||
Oral bioavailability (%) | 11 | n/a | 42 | n/a |