TABLE 2

Donor information and nonlinear regression analysis of CYP3A4 induction in human and cynomolgus monkey hepatocytes

Species	Donor Information				Endpoint	Rifampicin		Hyperforin^a
Species	Vendor/Lot	Sex	Age	Ethnicity	Endpoint	EC₅₀	E_max^b	EC₅₀	E_max^b
						μM	%RIF	μM	%RIF
Human	CellzDirect HU0693	M	41	White	RNA	14.23	177.5	0.37	63.5
	CellzDirect HU0693	M	41	White	Activity	1.94	109.5	0.32	71.5
	CellzDirect HU0694	F	54	White	RNA	6.48	169.5	0.51	104.6
	CellzDirect HU0694	F	54	White	Activity	0.76	116.8	0.23	69.7
	CellzDirect HU0965	F	27	White	RNA	3.06	131.0	1.27	66.5
	CellzDirect HU0965	F	27	White	Activity	0.93	107.5	0.32	57.9
Cynomolgus monkey	CellzDirect	M			RNA	12.18	151.1	3.28	118.2
	CellzDirect	M			Activity	0.67	104.5	1.54	66.0
	CellzDirect	M			RNA	3.38	100.0	3.01	46.9
	CellzDirect	M			Activity	1.68	101.2	0.98	68.5
	Celsis	M			RNA	6.16	131.0	2.64	28.1
	Celsis	M			Activity	2.34	101.5	1.50	74.1

↵a Nonlinear regression analysis for CYP3A induction in human hepatocytes was performed with the partial data set (0–1.56 μM) because of the observed cytotoxicity at higher concentrations of hyperforin.
↵b Percentage of induction response compared with that of rifampicin at 12.5 μM.