TABLE 5

Hepatic OATP inhibition interactions, in vitro to in vivo translation

Perpetrator	OATP	In Vitro Substrate	IC₅₀	C_max/IC₅₀	AUC Ratio	C_max Ratio	In Vivo Victim	Reference
			µM
Brexpiprazole	1B1	Estradiol 17-β-glucuronide	8.39	0.05			N/T	FDA (2015v)
Brexpiprazole metabolite DM-3411	1B1	Estradiol 17-β-glucuronide	9.13	0.01			N/T
Cobimetinib	1B1	Estrone-3-sulfate	118	<0.1			N/T	FDA (2015h)
	1B3	Fluo-3	85	<0.1			N/T
Daclatasvir	1B1	BMS-791553	2.3	1.02^{^a}^,^{^b}	1.47	1.84	Rosuvastatin	FDA (2015j)
	1B3	Cholecystokinin octapeptide	5.7	0.41^{^a}^,^{^b}
Deoxycholic acid	1B1	N/P	N/P	0.14^{^b}			N/T, R < 1.25	FDA (2015p)
	1B3	N/P	N/P	0.11^{^b}			N/T, R < 1.25
Edoxaban	1B1	N/P	62.7	0.01^{^a}			N/T	FDA (2015w)
	1B3	N/P	50.8	0.01^{^a}			N/T
Eluxadoline	1B1	Estradiol 17-β-glucuronide	32.6% at 400 ng/ml	N/A	1.41	1.18	Rosuvastatin	FDA (2015zc)
Isavuconazonium sulfate	1B1	N/P	11.2	1.53^{^a}^,^{^b}	1.40	1.05	Atorvastatin	FDA (2015i)
Lenvatinib	1B1	Estradiol 17-β-glucuronide	7.29	0.21^{^a}^,^{^b}			N/T	FDA (2015q)
Lesinurad	1B1	N/P	9.3	1.8^{^b}	1.01	1.17	Atorvastatin	FDA (2015zg)
	1B3	N/P	43.1	0.4^{^b}
Osimertinib	1B1	N/P	22	0.05			N/T	FDA (2015x)
	1B3	N/P	52.5	0.02			N/T
Panobinostat	1B1	N/P	N/P				N/T, R = 1	FDA (2015l)
Sacubitril	1B1	N/P	1.9	3.11^{^b}	1.30	1.75	Atorvastatin	FDA (2015k)
	1B3	N/P	3.8	1.55^{^a}^,^{^b}
Sacubitril metabolite LBQ657	1B1	N/P	126	N/A
Selexipag	1B1	Atorvastatin	2.4	0.01^{^a}			N/T	FDA (2015z)
	1B3	Taurocholic acid	1.7	0.02^{^a}			N/T
Selexipag metabolite ACT-333679	1B1	Atorvastatin	3.5	N/A			N/T
	1B3	Taurocholic acid	4.1	N/A			N/T
Tenofovir alafenamide fumarate	1B1	Fluo-3	29.8% at 100 µM	N/A				FDA (2015m)
	1B3	Fluo-3	25.5% at 100 µM	N/A

N/A, not applicable; N/P, not provided; N/T, not tested.
↵^a Ratio was calculated by the University of Washington Drug Interaction Database editorial team.
↵^b Values exceed the FDA cut-off value of 0.1.