TABLE 7

BCRP inhibition interactions, in vitro to in vivo translation

Perpetrator	In Vitro Substrate	IC₅₀ (µM)	[I]₁/IC₅₀	[I]₂/IC₅₀	AUC Ratio	C_max Ratio	In Vivo Victim	Reference
Dasabuvir	N/S	15.6	0.13^{^a}	130^{^a}	2.59	7.15	Rosuvastatin^{^b}	FDA, 2014ai
Empagliflozin	N/S	114	0.006	1.90				FDA, 2014n
Ledipasvir	Hoechst 33342	38.1% at 1 µM						FDA, 2014k
Netupitant	Estrone-3-sulfate	6	0.25^{^a}	346^{^a}^,^{^c}			^{^e}	FDA, 2014a
Olodaterol	Estrone-3-sulfate	10–100	1.04 × 10⁻⁶^{^c}					FDA, 2014ae
Paritaprevir	N/S	0.59	3.25^{^a}	1328^{^a}	2.59	7.15	Rosuvastatin^{^b}	FDA, 2014ai
Suvorexant	Methotrexate	10–15 (62% at 15 µM)	0.117^{^a}^,^{^c}	28^{^a}^,^{^d}				FDA, 2014c
Tedizolid (phosphate)	Genistein	51.1	0.16^{^a}	31.7^{^a}^,^{^c}			PMR	FDA, 2014ad
Vorapaxar	Methotrexate	2.5	0.064	6.8				FDA, 2014am