TABLE 2

In vitro IC₅₀ values for inhibition of SLC transporter-mediated substrate uptake by MKIs and in vivo unbound plasma concentrations (C_max,u)

MKI	IC₅₀	C_max,u^{^a}	C_max,u/IC₅₀	References
	µM
OATP1A2
Afatinib	1.17	0.009	0.01	http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/201292s002lbl.pdf; Wind et al., 2013
Cediranib	0.03	0.006	0.20	Yamamoto et al., 2009; McTigue et al., 2012
Erlotinib	1.10	0.322	0.29	Yamamoto et al., 2008; van Erp et al., 2009
Foretanib^{^b}	3.55	0.016^{^c}	0.004^{^c}	Naing et al., 2012
Gefitinib	0.88	0.090	0.10	Nakagawa et al., 2003; van Erp et al., 2009
Neratinib^{^b}	0.39	0.013^{^c}	0.03^{^c}	Wong et al., 2009
Nilotinib	1.46	0.085	0.06	Hazarika et al., 2008; Tanaka et al., 2010; Larson et al., 2012
Pelitinib^{^b}	3.77	0.008^{^c}	0.02^{^c}	Erlichman et al., 2006
Sunitinib	2.03	0.007	0.003	van Erp et al., 2009; Shirao et al., 2010
Vandetanib	2.45	0.037	0.02	Mross et al., 2009
OATP1B3
Erlotinib	1.19	0.322	0.27	Yamamoto et al., 2008; van Erp et al., 2009
Neratinib^{^b}	0.65	0.013^{^c}	0.02^{^c}	Wong et al., 2009
OATP2B1
Afatinib	2.08	0.009	0.004	http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/201292s002lbl.pdf; Wind et al., 2013
Erlotinib	0.03	0.322	10.7	Yamamoto et al., 2008; van Erp et al., 2009
Gefitinib	0.65	0.090	0.14	Nakagawa et al., 2003; van Erp et al., 2009
Neratinib^{^b}	2.68	0.013^{^c}	0.01^{^c}	Wong et al., 2009
Nilotinib	2.67	0.085	0.03	Hazarika et al., 2008; Tanaka et al., 2010
Pelitinib^{^b}	2.01	0.008^{^c}	0.004^{^c}	Erlichman et al., 2006
OAT3
Nilotinib	0.41	0.051	0.13	Hazarika et al., 2008; Tanaka et al., 2010
OCT1
Bosutinib	2.06	0.016	0.01	http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/203341s001lbl.pdf; Hsyu et al., 2013
OCTN2
Cediranib	2.49	0.006	0.002	Yamamoto et al., 2009; McTigue et al., 2012

↵^a Calculated as C_max × f_u.
↵^b Information on C_max,u unavailable.
↵^c A conservative estimate of f_u = 0.1, consistent with a number of other MKIs was used in these calculations.