TABLE 4.
E2072 and E2072-homodisulfide plasma pharmacokinetic parameters in monkeys after intravenous and oral administration of 5 mg/kg E2072a
Cmax | Tmax | AUCinf | Clb | Vdb | t½,β | %F | |
---|---|---|---|---|---|---|---|
ng/ml | h | ng · h/ml | l/h/kg | l/kg | h | ||
E2072 | |||||||
i.v. | 68,013.3 ± 2698.4 | 0.08 ± 0.00 | 63,622.1 ± 7821.8 | 0.022 ± 0.003 | 0.72 ± 0.06 | 23.0 ± 1.2 | |
p.o. | 10,454.3 ± 1032.2 | 0.42 ± 0.14 | 24,935.6 ± 740.7 | 0.057 ± 0.003 | 0.79 ± 0.31 | 9.57 ± 3.43 | 39.1% |
E2072-homodisulfide | |||||||
i.v. | 3272.8 ± 964.8 | 3.33 ± 1.15 | 105,771.6 ± 39,413.9 | – | – | 21.0 ± 0.95 | |
p.o. | 133.6 ± 14.6 | 5.33 ± 2.31 | 25,270.8 ± 6198.1 | – | – | 20.0 ± 1.85 |
Data are presented as mean ± S.D.; n = 3 monkeys per dose group.
For intravenous data, Cl and Vd are presented. For oral data, apparent clearance (Cl/F) and apparent volume (Vd/F) are presented.