Table 5

Multisite kinetic model interaction factors to describe the various modifications of CYP3A4 activity

Effect on CYP3A4	Interaction Factor		Example
Effect on CYP3A4	α	γ^5-150	Example	δ
Activation, S showing hyperbolic kinetics	1	>1	<1	QUI effect on FEL, SV
				QUI effect on diclofenac^5-a, warfarin^b
Inhibition, S showing hyperbolic kinetics	1	<1	<1	HAL effect on FEL, QUI^c
Inhibition, S showing substrate inhibition	1	<1	<1	QUI, HAL effect on NIF
		(β < 1, could = γ)		MDZ, FEL effect on NIF^c
Partial inhibition, S showing hyperbolic kinetics	1	1	>1	NIF effect on FEL^c
				TST-MDZ^c ^e, TST-erythromycin^d, TST-Terfenadine^e
Partial inhibition, S showing sigmoidal kinetics^5-g	<1	1	>1	HAL effect on TST
Heterotropic activation, S showing sigmoidal kinetics^5-g	<1	>1	=α	TST effect on DZ^f
Heterotropic inhibition, S showing sigmoidal kinetics^5-g	<1	1	≤1	QUI effect on TST, DZ effect on TST^f

↵5-150 β (changes in K_p from SES) = 2 (equivalent binding sites).
↵5-a Ngui et al. (2000); ^bNgui et al. (2001);^cA. Galetin, unpublished data; ^dWang et al., 1997;^eWang et al., 2000; ^fKenworthy et al., 2000.
↵5-g Three-site model.