. 2016 Mar 10;18(3):589–604. doi: 10.1208/s12248-016-9889-y

Table II.

Data Generated on AZ12470164 During the Early Clinical Development Phase

Parameters considered in retrospective analysis	AZ12470164
Human hepatocyte CL_int (μL/min/10⁶ cells)	100
Predicted clearance from human hepatocytes (mL/min/kg)	14.3^a
Intestinal microsomal CL_int (μL/min/mg); rat/dog/human	17/54/334
F _G (%); mouse/rat/dog/human	ND/74/51/15^b
Calculated F _H (%); mouse/rat/dog/human	69/84/25^c
Calculated in vivo F _a × F _G (%); mouse/rat/dog/human	>100/20/50 to 120/ND^d
Predicted F _a × F _G from in vitro data (%); mouse/rat/dog/human	ND/26/51/10

^aThe predicted clearance from hepatocytes was scaled using the well-stirred model and a lab-specific empirical correction factor according to (51)

^b F _G was scaled from activated intestinal microsomes using the Q _gut model (29)

^cThe pre-clinical F _H was calculated from IV PK studies whereas the human value was predicted from scaled cryopreserved human hepatocytes

^dThe in vivo F _a × F _G was calculated from IV and oral PK data using the indirect method given by F _oral/F _H = F _a × F _G