Table 1.

EVR and SIR IC₅₀ values against OATP1B1-mediated transport of [³H]-E₂17βG, [³H]E₁S, [³H]-rosuvastatin and OATP1B3-mediated transport of [³H]-CCK-8 in HEK293-OATP1B1 and HEK293-OATP1B3 cells, respectively. IC₅₀ values are expressed as the mean ± SE from the model estimation (n=3 in triplicate). Determination of co- and pre+co- IC₅₀ values and Rvalues were calculated as described in the Materials and Methods. * indicates a statistically significant difference (p<0.05 by t-test) vs. coincubation values.

		Co-Incubation		Pre+Co-Incubation
Transporter/Substrates		IC50 (μΜ)	R	IC50 (μΜ)	R
Everolimus
OATP1B1	E217G	0.48 ± 0.07	1.09 (1.06−1.15)	0.23 ± 0.06*	1.19 (1.16–1.26)
OATP1B1	E1S	0.61 ± 0.08	1.07 (1.04−1.17)	0.16 ± 0.02*	1.27 (1.18–1.52)
OATP1B1	Rosuvastatin	1.58 ± 0.92	1.03 (1.02–1.09)	0.19 ± 0.07*	1.23 (1.10–1.42)
OATP1B3	CCK-8	0.51 ± 0.08	1.09 (1.07−1.11)	0.19 ± 0.02*	1.23 (1.21–1.25)
OATP1B1a	E1S	4.1 ± 1.1a	1.01	ND	ND
OATP1B3a	MPA	3.7 ± 1.3a	1.01	ND	ND
Sirolimus
OATP1B1	E217G	0.64 ± 0.16	1.00 (1.00–1.01)	0.22 ± 0.04	1.01 (1.01–1.02)
OATP1B1	E1S	0.83 ± 0.10	1.00 (1.00–1.01)	0.65 ± 0.12	1.00 (1.00–1.01)
OATP1B1	Rosuvastatin	0.56 ± 0.30	1.00 (1.00–1.03)	0.32 ± 0.11	1.01 (1.01–1.03)
OATP1B3	CCK-8	0.97 ± 0.20	1.00 (1.00–1.01)	0.36 ± 0.05*	1.01 (1.00–1.01)
OATP1B1a	E1S	9.8 ± 1.1a	1.00	ND	ND
OATP1B3a	MPA	1.3 ± 1.2a	1.00	ND	ND

^a, data from a previous publication²⁴; MPA, mycophenolic acid 7-o-glucuronide