TABLE 5

Comparison of enzyme inactivation kinetic constants using testosterone–6β-hydroxylation activity of CYP3A4 and CYP3A5 as indication of residual activity

Drug and Metabolite	K_I		k_Inact		k_Inact/K_I		t_1/2		Partition Ratio
Drug and Metabolite	CYP3A4	CYP3A5	CYP3A4	CYP3A5	CYP3A4	CYP3A5	CYP3A4	CYP3A5	CYP3A4	CYP3A5
	μM	μM	minute⁻¹	minute⁻¹	minute⁻¹⋅mM⁻¹	minute⁻¹⋅mM⁻¹	minutes	minutes
Dronedarone	0.87	2.19	0.039	0.0056	44.83	2.56	17.8	123.1	51.1	32.2
NDBD	6.24	5.45	0.099	0.056	15.87	10.28	7.0	12.3	35.3	36.6
Clarithromycin	2.25	N.A.	0.04	N.A.	17.78	N.A.	N.A.	N.A.	N.A.	N.A.
Erythromycin	0.92	N.A.	0.058	N.A.	63.04	N.A.	N.A.	N.A.	N.A.	N.A.
Amprenavir	0.26	0.20	0.73	0.35	2808	1750	N.A.	N.A.	N.A.	N.A.

N.A., not determined.