Table 4.
In vivo plasma and brain pharmacokinetic parameters of AST-004 in mice following intraperitoneal or intravenous administration of either MRS2365 or AST-004
Compound administered | Compound monitored | Route of administration | Dose (mg/kg; μmol/kg) | Tissue | Pharmacokinetic parameters | ||||
---|---|---|---|---|---|---|---|---|---|
C0 or Cmax (ng/mL or ng/g) | CLp (mL/min/kg) | Vdss (L/kg) | AUC (ng-h/mL) |
T1/2 (h) | |||||
MRS2365 | AST-004 | I.P. | 0.27; 0.5 | Plasma | 64.5 | - | - | 29.3b | 0.3 |
Brain | 6.2 | - | - | 1.7c | - | ||||
AST-004 | AST-004 | I.P. | 0.15; 0.5 | Plasma | 49.5 | - | - | 30.1b | 0.3 |
Brain | 3.2 | - | - | 1.2c | - | ||||
AST-004 | AST-004 | I.V.a | 0.25; 0.8 | Plasma | 115 | 132 | 2.2 | 31.6b | 0.5 |
Results are the means of 3 mice per timepoint
aLLOQ for AST-004 plasma was 0.1 ng/mL
bAUC (0-Inf)
cAUC (0–0.5 h)
-Not determined