TABLE 2

Xenobiotic substrates of OATP1B1

Substrate	K_m	Expression System	Reference
	μM
Antibacterials
Benzylpenicillin	+	HEK293	Tamai et al., 2001
Cefditoren	3.45	XO	Nakakariya et al., 2008
Cefoperazone	4.84	XO	Nakakariya et al., 2008
Cefazolin	20.8	XO	Nakakariya et al., 2008
Nafcillin	11.1	XO	Nakakariya et al., 2008
Rifampin	13	XO	Vavricka et al., 2002
	1.5	HeLa	Tirona et al., 2003
Anticancer drugs
Gimatecan	+	MDCKII	Oostendorp et al., 2009
SN-38	+	XO	Nozawa et al., 2005
Pazopanib	+		European Medicines Agency, 2010b
Lipid-lowering drugs
Atorvastatin	12.4	HEK293	Kameyama et al., 2005
Cerivastatin	+	MDCKII	Shitara et al., 2003
	+	HEK293	Kameyama et al., 2005
Ezetimibe glucuronide	+	HEK293	Oswald et al., 2008
Fluvastatin	2.4	MDCKII	Kopplow et al., 2005
	31	XO	Deng et al., 2008a
	1.4, 3.5	CHO	Noé et al., 2007
Pitavastatin	3.0	HEK293	Hirano et al., 2004
	6.7	XO	Deng et al., 2008a
Pravastatin	35	HEK293	Hsiang et al., 1999
	11.5	XO	Nakai et al., 2001
	24	MDCKII	Sasaki et al., 2002
	86	HEK293	Kameyama et al., 2005
	58	XO	Deng et al., 2008a
	109	HEK293	Furihata et al., 2009
Rosuvastatin	7.3	XO	Brown et al., 2001
	+	XO	Simonson et al., 2004
	8.5	XO	Schneck et al., 2004
	4.0	HeLa	Ho et al., 2006
	0.802	HEK293	Kitamura et al., 2008
Other cardiovascular drugs
Bosentan	44	CHO	Treiber et al., 2007
Enalapril	262	HEK293	Liu et al., 2006
Olmesartan	42.6	XO	Nakagomi-Hagihara et al., 2006
	12.8	HEK293	Yamada et al., 2007
Valsartan	+	HEK293	Maeda et al., 2006a
	1.39	HEK293	Yamashiro et al., 2006
	17.8	CHO	Poirier et al., 2009
Temocapril	+	HEK293	Maeda et al., 2006a
Torsemide	6.2	HEK293	Werner et al., 2010
HIV protease inhibitors
Darunavir	+	XO	Hartkoorn et al., 2010
Lopinavir	+	XO	Hartkoorn et al., 2010
Saquinavir	+	XO	Hartkoorn et al., 2010
Other drugs, diagnostic markers, and drugs under development
ACU154	+	MDCKII	Takada et al., 2004
Atrasentan	+	HeLa	Katz et al., 2006
Bamet-UD2	10	XO	Briz et al., 2002
Bamet-R2	10	XO	Briz et al., 2002
Bromosulfophthalein	0.1	HEK293	Cui et al., 2001
	0.3	XO	Kullak-Ublick et al., 2001
	2.4	MDCKII	Kopplow et al., 2005
	+	COS1	van der Deure et al., 2008
BQ-123	+	XO	Kullak-Ublick et al., 2001
Caspofungin	+	HeLa	Sandhu et al., 2005
DADLE	+	XO	Nozawa et al., 2003
DPDPE	+	XO	Kullak-Ublick et al., 2001
	+	XO	Abe et al., 2001
EE2S	0.087, 141	HEK293	Han et al., 2010
Fexofenadine	+	MDCKII	Matsushima et al., 2008
Flavopiridol	+	HEK293	Ni et al., 2010
Flavopiridol-glucuronide	+	HEK293	Ni et al., 2010
Gd-EOB-DTPA	700	HEK293	Leonhardt et al., 2010
Karenitecin (BNP1350)	+	MDCKII	Oostendorp et al., 2009
Methotrexate	+	XO	Abe et al., 2001
Mycophenolic acid-O-glucuronide	+	HEK293	Picard et al., 2010
Ro 48-5033	60	CHO	Treiber et al., 2007
S8921G	1.93	HEK293	Sakamoto et al., 2008
Sirolimus	+	HEK293	Oswald et al., 2010
	μM
Troglitazone sulfate	+	XO	Nozawa et al., 2004
YM785	+	HEK293	Umehara et al., 2008
Fluorescent in vitro OATP1B1 probe substrates
8-Fluorescein cAMP	2.9	CHO	Bednarczyk, 2010
CDCA-NBD	1.45	HepG2	Yamaguchi et al., 2006
CGamF	+	CHO	Annaert et al., 2010
CLF	+	CHO	de Waart et al., 2010
Fluorescein-methotrexate	3.8	CHO	Gui et al., 2010
Toxins
Arsenate	+	HEK293	Lu et al., 2006
Arsenite	+	HEK293	Lu et al., 2006
BDE47	0.31	CHO	Pacyniak et al., 2010
BDE99	0.91	CHO	Pacyniak et al., 2010
BDE153	1.91	CHO	Pacyniak et al., 2010
Demethylphalloidin	17	XO	Meier-Abt et al., 2004
Microcystin-LR	7	XO	Fischer et al., 2005
Phalloidin	39	HEK293	Fehrenbach et al., 2003
	+	XO	Herraez et al., 2009

ACU154, 0-glucuronide of PKI116 (a tyrosine kinase inhibitor); BQ-123, cyclic-pentapeptide (cyclo[d-Trp-d-Asp-l-Pro-d-Val-l-Leu]); Bamet-R2, bile acid-cisplatin derivative [cis-diammine-chloro-cholylglycinate-platinum(II)]; Bamet-UD2, bile acid-cisplatin derivative [cis-diammine-bisursodeoxycholate-platinum(II)]; BDE47, 2,2′,4,4′-tetrabromodiphenyl ether; BDE99, 2,2′,4,4′,5-pentabromodiphenyl ether; BDE153, 2,2′,4,4′,5,5′-hexabromodiphenylether; CDCA-NBD, chenodeoxychilyl-(Nepsilon-NBD)-lysine; CGamF, cholyl-glycylamido-fluorescein; CLF, cholyl-l-lysyl-fluorescein; CHO, Chinese hamster ovary; DADLE, [d-Ala²,d-Leu⁵]-enkephalin (opioid peptide analog); DPDPE, [d-penicillamine^2,5]enkephalin (opioid-receptor antagonist); EE2S, 17α-ethinylestradiol sulfate; Gd-EOB-DTPA, gadolinium-ethoxybenzyl-diethylenetriamine pentaacetic acid; HEK293, human embryonic kidney 293 cells; MDCKII, Madin-Darby canine kidney cells; Ro 48-5033, active metabolite of the endothelin antagonist bosentan; S8921G, active metabolite of the SLC10A2 inhibitor S8921; SN-38, active metabolite of the anticancer drug irinotecan; XO, Xenopus laevis oocyte; YM785, an If channel inhibitor; +, substrate of OATP1B1, but K_m not available.