TABLE 4

Pharmacokinetic and toxicokinetic summary of AZ’0908

Dose	No. of Animals	Anticipated AUC_ther	Day 1						Day 14
Dose	No. of Animals	Anticipated AUC_ther	C_max Parent	AUC_0–24 Parent	C_max M1	AUC_0–24 M1	AUC_0–24 M1/AUC_0–24 Parent (ratio)	AUC_0–24 Parent/Dose	C_max Parent	AUC_0–24 Parent	AUC_0–24 Parent/AUC_ther (ratio)	AUC_0–24 Parent/Dose
		μMh^a	μM	μMh	μM	μMh			μM	μMh
10 μmol/kg	3	118	11	58	0.6	11	0.2	5.8	NA	NA	NA	NA
435 μmol/kg	5	118	375	2220	NA	NA	NA	5.1	415	2520	21	5.8
900 μmol/kg	5	118	540	5030	NA	NA	NA	5.6	480	5000	42	5.6

AUC_0–24, area under the curve for 24 hours; AUC_ther, area under plasma concentration time curve needed for therapeutic effect; NA, not available.
↵^a AUC_ther was based on the assumption that a steady-state concentration (C_ss) average corresponding to 10 times the AZ’0908 whole blood assay IC₅₀ values was needed.