Table 8.
61 | 63 | |||
---|---|---|---|---|
|
||||
Parameter | IV | PO | IV | PO |
Cl (L/h/kg) | 227 | ‒ | 294 | ‒ |
T1/2 (h) | 0.85 | 1.94 | 2.98 | 3.75 |
Cmax (μM) | 1.45b | 1.20 | 0.74 b | 1.78 |
Tmax (h) | ‒ | 0.25 | ‒ | 0.25 |
AUClast (μM·h) | 0.26 | 3.2 | 0.19 | 2.5 |
Vss (L/kg) | 5.6 | ‒ | 27 | ‒ |
F(%) | ‒ | 49 | ‒ | 50 |
values calculated from drug concentration in plasma following IV (2 mg/kg) and PO (50 mg/kg) dosing. n = 3, 8-time points taken over 24 hours. Compounds 61 and 63 were formulated as solution in PBS buffered saline with 1.1 eq. NaOH (final pH 7–8).
Cmax = C0 (t = 0) for IV administration. All pharmacokinetic studies were conducted at Pharmaron Inc.