TABLE 2

Transporter substrates and corresponding in vitro/in vivo inhibitors (examples with availability of IC₅₀/K_i values)

Transporter	Selected Substrates	Selected Inhibitors	IC₅₀ or K_i^{^a}	Reference
			µM
OATP1A2	Aliskiren	Naringin	75.5	Rebello et al., 2012
	Fexofenadine	Apigenin	9.3	Mandery et al., 2010
	Fexofenadine	Hesperidin	2.7	Bailey, 2010
	Fexofenadine	Naringin	3.6–24.2	Bailey, 2010; Rebello et al., 2012
OATP2B1	Fexofenadine	Apigenin	13.9	Mandery et al., 2010
	Rosuvastatin	Cyclosporine	0.07	Ho et al., 2006
	Rosuvastatin	Gemfibrozil	8	Ho et al., 2006
OATP1B1	Cerivastatin	Gemfibrozil	72	Shitara et al., 2004
OATP1B1		Gemfibrozil-1-O-β-glucuronide	24	Shitara et al., 2004
	Pitavastatin	Cyclosporine	0.24^{^a}	Hirano et al., 2006
	Pitavastatin	Clarithromycin	8.26^{^a}	Hirano et al., 2006
	Rosuvastatin	Gemfibrozil	25	Ho et al., 2006
	Rosuvastatin	Cyclosporine	0.31	Ho et al., 2006
OATP1B3	Pravastatin	Erythromycin	40% Inhibition by 10 µM	Seithel et al., 2007
	Rosuvastatin	Cyclosporine	0.06	Ho et al., 2006
NTCP	Rosuvastatin	Cyclosporine	0.37	Ho et al., 2006
	Rosuvastatin	Gemfibrozil	23	Ho et al., 2006
OAT3	Methotrexate	Indomethacin	0.61–0.98	Burckhardt and Burckhardt, 2011
	Fexofenadine	Probenecid	1.3^{^a}	Tahara et al., 2005
OCT1	Metformin	Cimetidine	104^{^a}	Ito et al., 2012b
OCT2	Metformin	Cimetidine	124^{^a}	Ito et al., 2012b
MATE1	Metformin	Cimetidine	3.8^{^a}	Ito et al., 2012b
MATE2-K	Metformin	Cimetidine	6.9^{^a}	Ito et al., 2012b
P-gp	Digoxin	Clarithromycin	4.1	Eberl et al., 2007
	Digoxin	Cyclosporine	1.3	Wandel et al., 1999
	Digoxin	Quinidine	2.2	Wandel et al., 1999
	Digoxin	Telithromycin	1.8	Eberl et al., 2007
	Digoxin	Verapamil	2.1	Wandel et al., 1999