Table 4. Pharmacokinetic Parameters Following 20 mg/kg oral and 5 mg/kg Intravenous Dosing in Micea.
oral PKb parameters |
intravenous PK parameters |
|||||||
---|---|---|---|---|---|---|---|---|
cmpd | Cmax (μM) | Tmax (h) | AUC (μM·h) | T1/2 (h) | F (%) | Vss (L/kg) | CL (mL/min/kg) | T1/2 (h) |
17 | 0.02 | 1.7 | 0.12 | 3.39 | 0.24 | 0.99 | 16.2 | 2.12 |
18 | 8.3 | 0.5 | 11.14 | 1.35 | 51.6 | 0.90 | 39.7 | 0.62 |
19 | 5.2 | 0.5 | 12.4 | 1.63 | 51.9 | 1.02 | 34.0 | 0.42 |
20 | 20.5 | 0.5 | 31.2 | 3.63 | 60 | 0.96 | 19.3 | 0.83 |
Cmax, maximum concentration of drug in plasma; Tmax, time to maximum concentration of drug in plasma; AUC, area under the curve extrapolated to infinity; Vss, volume of distribution at steady state; CL, clearance; T1/2, half-life; F, oral bioavailability;
Formulation used for oral and intravenous dosing is PEG300/D5W (3:1, V/V).