Table 6.
In Vivo PK Data for Analogue 14 Following IV and PO Administration in CD-1 Micea
| route | dose (mg/kg) | C0b (ng/mL) | CLc (L/(h kg)) | t1/2d (h) | Vsse (L/kg) | AUClastf (h ng/mL) | AUCINFg (h ng/mL) | %Fj |
|---|---|---|---|---|---|---|---|---|
| IV | 2 | 1622 (267) | 0.354 (0.139) | 5.08 (0.814) | 2.18 (0.585) | 6214 (2321) | 6242 (2303) | NA |
| route | dose (mg/kg) | Cmaxh (ng/mL) | Tmaxi (h) | t1/2d (h) | Vsse (mL/kg) | AUClastf (h ng/mL) | AUCINFg (h ng/mL) | %F j |
| PO | 5 | 1563 (115) | 0.42 (0.14) | 5.38 (0.624) | NA | 16 040 (2778) | 16 073 (2783) | 103 (17.8) |
Data are represented as the mean with standard deviation in parentheses (mean (SD)). Dosing groups consisted of three drug naïve adult male CD-1 mice. IV administration: test article was administered at the 2 mg/kg dose; test article vehicle = 3% dimethylacetamide (DMA)/45% poly(ethylene glycol) 300 (PEG300)/12% ethanol/40% sterile water; PO administration: test article was administered at the 5 mg/kg dose, vehicle = 2% Tween 80 in 0.9% saline.
Observed initial concentration of compound in blood at time zero.
Total body clearance.
Apparent half-life of the terminal phase of elimination of compound from blood.
Volume of distribution at steady state.
Area under the blood concentration versus time curve from 0 to the last time point that the compound was quantifiable in blood.
Area under the blood concentration versus time curve from 0 to infinity.
Maximum observed concentration of compound in blood.
Time of maximum observed concentration of compound in blood.
Bioavailability; F = (AUCINFpo × doseiv)/AUCINFiv × dosepo.