TABLE 1

IC₅₀ values and binding constants for CYP3A4 and CYP3A7

Values presented ± S.E.

	IC₅₀ ± S.E.		K_d ± S.E.
	µM
Imidazoles	CYP3A4	CYP3A7	CYP3A4	CYP3A7
Clotrimazole	0.18 ± 0.01	0.27 ± 0.03^*	Type II; 0.016 ± 0.004	Type II; 0.010 ± 0.003
Liarozole	0.32 ± 0.03	1.9 ± 0.4^**	Type II; 0.52 ± 0.03	Type II; 4.1 ± 0.3^**
Ketoconazole	1.2 ± 0.07	9.2 ± 2^**	Type II; 0.69 ± 0.05	Type II; 11 ± 0.4^**
Oxiconazole	0.80 ± 0.01	2.9 ± 0.4^**	Type II; 0.032 ± 0.005	Type II; 0.84 ± 0.1^**
Tioconazole	1.0 ± 0.06	4.9 ± 0.7^**	Type II; 0.030 ± 0.002	Type II; 1.2 ± 0.1^**
Miconazole	1.7 ± 0.1	3.2 ± 0.3^**	Type II; 0.071 ± 0.007	Type II; 0.85 ± 0.08^**
Econazole	0.55 ± 0.01	6.9 ± 0.6^**	Type II; 0.11 ± 0.01	Type II; 1.8 ± 0.1^**
Imidazole	3100 ± 400	11,000 ± 2000^*	Type II; 1000 ± 60	Type II; 1700 ± 80^**
Triazoles
Fluconazole	>200 µM	>200 µM	rII→II; Type II K_d 22 ± 1.6	Little/no absorbance change
Fosfluconazole	>200 µM	>200 µM	Little/no absorbance change	Little/no absorbance change
Letrozole	>500 µM	>1 mM	rII→II; Type II K_d 400 ± 50	Little/no absorbance change
Terconazole	>10 µM	>35 µM	Type II; 3.1 ± 0.2	Little/no absorbance change
Posaconazole	2.4 ± 0.4	8.1 ± 1.9^*	Type II 0.65 ± 0.02	Little/no absorbance change

↵* P < 0.05%;
↵** P < 0.01% compared with CYP3A4.