TABLE 6

BCRP inhibition interactions, in vitro to in vivo translation

PMR indicates the study was requested as a PMR.

Perpetrator	In Vitro Substrate	IC₅₀	[I]₁/IC₅₀	[I]₂/IC₅₀	AUC Ratio	C_max Ratio	In Vivo Victim	Reference
		µM
Alectinib	N/P	0.1	13^{^a}^,^{^b}	49729^{^a}^,^{^b}			N/T^{^c}	FDA (2015b)
Alectinib metabolite M4	N/P	2.6	0.2	N/A
Brexpiprazole	Prazosin	1.16	0.40^{^a}^,^{^b}	32^{^a}^,^{^b}	1.12		Rosuvastatin	FDA (2015v)
Brexpiprazole metabolite DM-3411	Prazosin	3.04	0.047	N/A
Cariprazine	N/P	Weak (value N/P)					N/T	FDA (2015zd)
Cobimetinib	Estrone-3-sulfate	3.3	0.16^{^a}	137^{^a}^,^{^b}			N/T	FDA (2015h)
Daclatasvir	Genistein	10.9	0.21^{^a}^,^{^b}	30^{^a}^,^{^b}	1.47	1.84	Rosuvastatin	FDA (2015j)
Isavuconazonium sulfate	N/P	92	0.19^{^a}^,^{^b}	20^{^a}^,^{^b}	No effect (value N/P)		Methotrexate	FDA (2015i)
Lesinurad	Methotrexate	62.7% at 100 µM	<0.01				N/T	FDA (2015zg)
Osimertinib	N/P	2	0.063^{^a}	320^{^b}			N/T, PMR	FDA (2015x)
Rolapitant	Cladribine	0.172	10^{^b}	8364^{^a}^,^{^b}	2.18	2.38	Sulfasalazine	FDA (2015za)
Selexipag	Methotrexate	1.9	0.017^{^a}	0.42^{^a}			N/T	FDA (2015z)
Selexipag metabolite ACT-333679	Methotrexate	5.6	N/A	N/A
Sonidegib	N/P	1.5	0.98^{^a}^,^{^b}	783^{^a}^,^{^b}			N/T	FDA (2015t)

N/P, not provided; N/T, not tested.
↵^a The ratio was calculated by the University of Washington Drug Interaction Database editorial team.
↵^b Values exceed the FDA cut-off value of 0.1 ([I]₁/ IC₅₀) or 10 ([I]₂/IC₅₀).
↵^c A clinical study was recommended in the comments by the FDA reviewers.