Table 14

Substrates for and inhibitors of both CYP3A and P-gp (Wacher et al., 1995)

CYP3A substrates	P-gp	CYP3A substrates	P-gp	CYP3A substrates	P-gp
Antiarrhythmics		Chemotherapeutic agents		Hormones
Amiodarone	I	Etoposide	S	Dexamethasone	S
Lidocaine	I	Doxorubicin	S^14-a	Estradiol	S^14-b
Quinidine	I	Paclitaxel	S	Hydrocortisone	S,I
Antifungals		Vinblastine	S	Progesterone	I
Itraconazole	I	Vincristine	S	Testosterone	I
Ketoconazole	I	Vindesine	S	Others
Flavonoids		Ca-channel blockers		Digitoxin	S^14-c
Kaempferol (I)	E	Diltiazem	S,I	Erythromycin	I
Quercetin (I)	E	Felodipine	I	RU486	I
Immunosuppressants		Nicardipine	S,I	Tamoxifen	I
Cyclosporine	S,I	Nitrendipine	I	Terfenadine	I
FK506	S,I	Nifedipine	I
Rapamycin	S	Verapamil	S,I

S, Substrate; I, Inhibitor; E, Enhancer.
↵14-a Doxorubicin, a precursor of morpholino doxorubicin, is a P-gp substrate.
↵14-b 17-β estradiol glucuronide, a phase II metabolite of estradiol, is a P-gp substrate.
↵14-c Digoxin, a metabolite of digitoxin, is a P-gp substrate.