TABLE 5

Hepatic OATP inhibition interactions, in vitro to in vivo translation

Perpetrator	OATP	In Vitro Substrate	IC₅₀ (µM)	C_max/IC₅₀	AUC Ratio	C_max Ratio	In Vivo Victim	Reference
Ceftolozane	1B3	Fluo-3	25% at 1500 µM					FDA, 2014al
Ceritinib	1B1	Estradiol 17-β-glucuronide	31.8% at 5 µM					FDA, 2014ao
	1B3	Estradiol 17-β-glucuronide	24.1% at 5 µM
Dapagliflozin	1B1	Estradiol 17-β-glucuronide	69.3	0.005^b				FDA, 2014j
	1B3	Cholecystokinin octapeptide	8	0.044^b
Dasabuvir	1B1	N/S	0.9	2.32^b^,^{^c}	1.82	1.36	Pravastatin^{^d}	FDA, 2014ai
	1B3	N/S	6.6	0.32^b^,^{^c}	2.59	7.15	Rosuvatstatin^{^d}
Eliglustat	1B1	Estrone-3-sulfate	150	0.003^b				FDA, 2014e
	1B3	Fluo-3	100	0.004^b
Empagliflozin	1B1	N/S	71.8	0.009	1.00	0.95	Simvastatin	FDA, 2014n
	1B3	N/S	58.6	0.012
Idelalisib	1B1	N/S	10	0.46^b^,^{^c}	1.11	1.21	Rosuvastatin	FDA, 2014an
	1B3	N/S	7	0.66^b^,^{^c}
Ledipasvir	1B1	Fluo-3	3.5	0.29^{^c}			N/T; R^{^e} < 1.25	FDA, 2014k
	1B3	Fluo-3	6.5	0.15^{^c}			N/T; R^{^e} < 1.25
Netupitant	1B1	Estrone-3-sulfate	22% at 30 µM					FDA, 2014a
	1B3	Fluo-3	44% at 30 µM
Olaparib	1B1	N/S	20.3	0.9^{^c}			N/T; R^{^e} = 1.16	FDA, 2014s
	1B3	N/S	25% at 100 µM
Paritaprevir	1B1	N/S	0.031	61.9^b^,^{^c}	1.82	1.36	Pravastatin^{^d}	FDA, 2014ai
	1B3	N/S	0.017	112.9^b^,^{^c}	2.59	7.15	Rosuvatstatin^{^d}
Suvorexant	1B1	Pitavastatin	48% at 10 µM					FDA, 2014c
Tazobactam	1B3	Fluo-3	32.3% at 500 μg/ml					FDA, 2014al
Tedizolid (phosphate)	1B1	Estradiol 17-β-glucuronide	29% at 30 µM^{^a}					FDA, 2014ad
Vorapaxar	1B1	Pitavastatin	31% at 10 µM					FDA, 2014am
	1B3	Bromsulphthalein	45% at 10 µM

N/S, not specified; N/T, not tested.
↵^a Follow-up experiments showed no inhibition.^bRatio was calculated by the DIDB Editorial Team.
↵^c Values exceed the FDA cut-off value of 0.1.
↵^d Perpetrator was administered as the combination drug.
↵^e R = 1 + (f_u × I_i_n,max/IC₅₀).