TABLE 5

Inhibition of OATP1B1 by drugs and related compounds in vitro

InhibitorIC50 or KiReference
μM
Amprenavir12.8Annaert et al., 2010
Atazanavir1.5Annaert et al., 2010
Atorvastatin0.87Hsiang et al., 1999; Chen et al., 2005
Atorvastatin lactone2.6Chen et al., 2005
Beclomethasone6.7Gui et al., 2010
Bezafibrate45.2Gui et al., 2009
Bromocriptine0.7Gui et al., 2010
Bromosulfophthalein0.044–0.6König et al., 2000b; Nakai et al., 2001; Fehrenbach et al., 2003; Fischer et al., 2005; Annaert et al., 2010; Han et al., 2010
Carbamazepine188Gui et al., 2008, 2009
Caspofungin+Sandhu et al., 2005
Chenodeoxycholic acid3.4Gui et al., 2009
Ciglitazone+Gui et al., 2009
Clarithromycin8.26–96Hirano et al., 2006; Seithel et al., 2007
Clotrimazole7.6–9.0Gui et al., 2008, 2009
Cyclosporine0.021–2.2Fehrenbach et al., 2003; Shitara et al., 2003; Tirona et al., 2003; Campbell et al., 2004; Simonson et al., 2004; Hirano et al., 2006; Ho et al., 2006; Treiber et al., 2007; Amundsen et al., 2010; Bednarczyk, 2010
Darunavir3.1Annaert et al., 2010
Digoxin31.7Hirano et al., 2006
Elacridar+Oostendorp et al., 2009
Eltrombopag2.71European Medicines Agency, 2010a
Erythromycin11.4–217Hirano et al., 2006; Seithel et al., 2007
Estradiol3.3Gui et al., 2009
Estropipate0.06Gui et al., 2010
Fenofibrate105.2Gui et al., 2009
Gd-EOB-DTPA600Leonhardt et al., 2010
Gemfibrozil4.0–72Schneck et al., 2004; Shitara et al., 2004; Hirano et al., 2006; Ho et al., 2006; Noé et al., 2007
Gemfibrozil-1-O-glucuronide22.6–24Shitara et al., 2004; Hirano et al., 2006
Glyburide0.746–1.14Hirano et al., 2006; Bednarczyk, 2010
Hyperforin0.82Tirona et al., 2003
Indinavir5.84–18.4Tirona et al., 2003; Campbell et al., 2004; Hirano et al., 2006; Annaert et al., 2010
Indocyanine green0.112Cui et al., 2001
Irinotecan+Nozawa et al., 2005
Ketoconazole19.2Hirano et al., 2006; Gui et al., 2009
Lovastatin6.1Hsiang et al., 1999; Sandhu et al., 2005; Gui et al., 2008
Lovastatin acid4.0Chen et al., 2005
Lovastatin lactone12.7–28Chen et al., 2005; Gui et al., 2009
Lopinavir0.5Annaert et al., 2010
Metyrapone+Gui et al., 2008, 2009
Miconazole+Gui et al., 2009
Mifepristone2.2–3.3Gui et al., 2008, 2009
Moricizine8.1Gui et al., 2010
Nelfinavir0.93Tirona et al., 2003
Niflumic acid3.7Gui et al., 2010
Paclitaxel0.03Gui et al., 2008, 2009
Pantoprazole+Oostendorp et al., 2009
Pazopanib0.79U.S. Food and Drug Administration, 2009
Phenytoin+Gui et al., 2009
Pioglitazone+Nozawa et al., 2004
Pravastatin21.8Gui et al., 2009; Hsiang et al., 1999
Ramipril4.0Gui et al., 2010
Repaglinide1.1–2.2Bachmakov et al., 2008; Gui et al., 2010
Resveratrol11.2Gui et al., 2010
Rifampin0.477–17Vavricka et al., 2002; Tirona et al., 2003; Hirano et al., 2006; Lau et al., 2007; Treiber et al., 2007; Gui et al., 2008; Annaert et al., 2010; Bednarczyk, 2010; Gui et al., 2010; Leonhardt et al., 2010
Rifamycin SV0.171–2Vavricka et al., 2002; Campbell et al., 2004; Chen et al., 2005; Hirano et al., 2006; Seithel et al., 2007; Sharma et al., 2009
Ritonavir0.71–1.4Tirona et al., 2003; Hirano et al., 2006; Annaert et al., 2010
Rosiglitazone6.0Nozawa et al., 2004; Bachmakov et al., 2008
Roxithromycin153Seithel et al., 2007
Saquinavir1.2–1.8Tirona et al., 2003; Campbell et al., 2004; Hirano et al., 2006; Annaert et al., 2010
Sildenafil1.5Treiber et al., 2007
Simvastatin+Hsiang et al., 1999
Simvastatin acid3.6Nakai et al., 2001; Chen et al., 2005
Simvastatin lactone9.7Chen et al., 2005
Sirolimus6.49Oswald et al., 2010
SN-38+Nozawa et al., 2005
Tacrolimus0.611–3.7Fehrenbach et al., 2003; Hirano et al., 2006; Amundsen et al., 2010
Telithromycin121Seithel et al., 2007
Telmisartan0.436Hirano et al., 2006
μM
Thyroxine3.5–3.85Gui et al., 2009; Bednarczyk, 2010
Troglitazone1.0–1.2Gui et al., 2008, 2009
Troglitazone sulfate+Nozawa et al., 2004
Valsartan8.96Hirano et al., 2006
Valspodar+Oostendorp et al., 2009
Verapamil+Oostendorp et al., 2009
Zosuquidar+Oostendorp et al., 2009; Leonhardt et al., 2010
  • Gd-EOB-DTPA, gadolinium-ethoxybenzyl-diethylenetriamine pentaacetic acid; IC50, inhibitor concentration producing 50% inhibition of transporter activity; SN-38, an active metabolite of irinotecan; +, inhibits OATP1B1, but IC50/Ki not available.