Table 2.

Pharmacokinetic Data of Bumped-Kinase Inhibitors (BKIs) in Uninfected Adult Mice After Oral Dosing

BKI Compound, by Dosing Route	Dose, mg/kg	Cmax, µM	Tmax, min	AUC, µmol/L min	Half-life, min	Oral Clearance Rate, mL/min	Fecal Concentration, µM
Orala
1294	10	0.75	120	430	205	1.69	4.4
1318	10	6.5	120	2209	909	0.16	0.44
1369	10	0.26	200	47	197	0.78	5.20
1412	10	0	0	0	…b	…b	1.83
1534	10	0.23	30	58	66	10.5	10.1
1546	10	0	0	0	…b	…b	5.29
1550	10	3.9	30	309	41	2.1	0.036
1553	10	12.8	320	13725	1188	0.02	0.52
1556	25	7.0	50	2082	320	0.56	…
1557	10	0.88	30	67.4	49	10.9	1.67
1649	10	4.9	400	6416	895	0.01	5.76
Subcutaneousc
1294	60	12.7	280	12249	6066	…	0.92
1534	60	4.2	180	3223	1831	…	0.44

Abbreviations: AUC, area under the curve; C_max, maximum concentration; T_max, time at which maximum concentration was observed.

^a25 mg/kg dose.

^bNo systemic exposure detected.

^c60 mg/kg dose.