Table 2.

Drugs and xenobiotics reported to be transported by OATP1B1

Drug/xenobiotic substrates	Indication	Test system	Measurement	Km (μmol/l)	References
Pravastatin	HMG CoA reductase inhibitor	293c18 cells	Transport	30	[6]
		HEK 293	Transport		[14]
		Human hepatocytes, Xenopus oocytes	Transport	11.5	[15]
Atorvastatin	HMG CoA reductase inhibitor	HEK 293	Transport		[14]
		293c18 cells	Inhibition of pravastatin transport		[6]
	HMG CoA reductase inhibitor	HEK 293	Inhibition of Estradiol 17ß-D-Glucuronide transport		[16]
Lovastatin	HMG CoA reductase inhibitor	293c18 cells	Inhibition of pravastatin transport		[6]
Lovastatin (acid)	HMG CoA reductase inhibitor	HEK 293	Inhibition of Estradiol 17ß-D-Glucuronide transport		[16]
Cerivastatin	HMG CoA reductase inhibitor	HEK 293	Transport		[14]
Pitavastatin	HMG CoA reductase inhibitor	HEK 293	Transport	3	[17]
		Human hepatocytes	Inhibition of E217ßG and E1S		[18]
Rosuvastatin	HMG CoA reductase inhibitor	HeLa cells	Transport	4.0–7	[19]
Repaglinide	Antidiabetic agent	In-vivo	Patients with different SLCO1B1 variants have different plasma concentrations		[20]
		In-vivo	Patients with different SLCO1B1 variants have different plasma concentrations		[21]
7-ethyl-10-hydroxycamptothecin  (SN-38)	Irinotecan (anticancer agent) active metabolite	HEK 293	Transport		[22]
Benzylpenicillin	Antibiotic	HEK 293	Transport		[12]
Bosentan	Endothelin receptor antagonists	CHO cells	Transport and inhibition by cyclosporin A, rifampicin		[23]
Atrasentan	Endothelin receptor antagonists	HeLa cells	Transport		[24]
Enalaprilat	ACE inhibitor	HEK 293	Transport	262	[25]
Temocapril	ACE inhibitor	In-vivo	Patients with different SLCO1B1 variants have different plasma concentrations		[26]
Valsartan	ACE inhibitor	In-vivo	Patients with different SLCO1B1 variants have different plasma concentrations		[26]
		HEK 293 and human hepatocytes	Transport		[27]
Olmesartan	ACE inhibitor	In-vivo	Patients with different SLCO1B1variants have different plasma concentrations		[28]
		HEK 293	Transport		[29]
Caspofungin	Anti-fungal agent	HeLa cells	Transport		[30]
Troglitazone sulfate	Thiazolidinediones	oocytes	Transport		[31]
Methotrexate	Chemotherapeutic agent	HeLa cells	Transport		[11]
Arsenic	Exogenous toxin	HEK 293	Transport		[32]

Columns are, in order: drug or xenobiotic substrate; indication (how drug is used for disease treatment); test system, that is, cell system for in-vitro experiment versus in-vivo experiment; experimental measurement performed; Km, where available, and finally, reference. Several ligands were studied by different investigators and these data are listed in separate rows. Data organized by drug class.

ACE, angiotensin-converting enzyme; HMG CoA, 3-hydroxy-3-methyl-glutaryl-CoEnzyme A reductase.