Inhibitor | IC50 or Ki | Reference |
---|---|---|
μM | ||
Amprenavir | 12.8 | Annaert et al., 2010 |
Atazanavir | 1.5 | Annaert et al., 2010 |
Atorvastatin | 0.87 | Hsiang et al., 1999; Chen et al., 2005 |
Atorvastatin lactone | 2.6 | Chen et al., 2005 |
Beclomethasone | 6.7 | Gui et al., 2010 |
Bezafibrate | 45.2 | Gui et al., 2009 |
Bromocriptine | 0.7 | Gui et al., 2010 |
Bromosulfophthalein | 0.044–0.6 | König et al., 2000b; Nakai et al., 2001; Fehrenbach et al., 2003; Fischer et al., 2005; Annaert et al., 2010; Han et al., 2010 |
Carbamazepine | 188 | Gui et al., 2008, 2009 |
Caspofungin | + | Sandhu et al., 2005 |
Chenodeoxycholic acid | 3.4 | Gui et al., 2009 |
Ciglitazone | + | Gui et al., 2009 |
Clarithromycin | 8.26–96 | Hirano et al., 2006; Seithel et al., 2007 |
Clotrimazole | 7.6–9.0 | Gui et al., 2008, 2009 |
Cyclosporine | 0.021–2.2 | Fehrenbach 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 |
Darunavir | 3.1 | Annaert et al., 2010 |
Digoxin | 31.7 | Hirano et al., 2006 |
Elacridar | + | Oostendorp et al., 2009 |
Eltrombopag | 2.71 | European Medicines Agency, 2010a |
Erythromycin | 11.4–217 | Hirano et al., 2006; Seithel et al., 2007 |
Estradiol | 3.3 | Gui et al., 2009 |
Estropipate | 0.06 | Gui et al., 2010 |
Fenofibrate | 105.2 | Gui et al., 2009 |
Gd-EOB-DTPA | 600 | Leonhardt et al., 2010 |
Gemfibrozil | 4.0–72 | Schneck et al., 2004; Shitara et al., 2004; Hirano et al., 2006; Ho et al., 2006; Noé et al., 2007 |
Gemfibrozil-1-O-glucuronide | 22.6–24 | Shitara et al., 2004; Hirano et al., 2006 |
Glyburide | 0.746–1.14 | Hirano et al., 2006; Bednarczyk, 2010 |
Hyperforin | 0.82 | Tirona et al., 2003 |
Indinavir | 5.84–18.4 | Tirona et al., 2003; Campbell et al., 2004; Hirano et al., 2006; Annaert et al., 2010 |
Indocyanine green | 0.112 | Cui et al., 2001 |
Irinotecan | + | Nozawa et al., 2005 |
Ketoconazole | 19.2 | Hirano et al., 2006; Gui et al., 2009 |
Lovastatin | 6.1 | Hsiang et al., 1999; Sandhu et al., 2005; Gui et al., 2008 |
Lovastatin acid | 4.0 | Chen et al., 2005 |
Lovastatin lactone | 12.7–28 | Chen et al., 2005; Gui et al., 2009 |
Lopinavir | 0.5 | Annaert et al., 2010 |
Metyrapone | + | Gui et al., 2008, 2009 |
Miconazole | + | Gui et al., 2009 |
Mifepristone | 2.2–3.3 | Gui et al., 2008, 2009 |
Moricizine | 8.1 | Gui et al., 2010 |
Nelfinavir | 0.93 | Tirona et al., 2003 |
Niflumic acid | 3.7 | Gui et al., 2010 |
Paclitaxel | 0.03 | Gui et al., 2008, 2009 |
Pantoprazole | + | Oostendorp et al., 2009 |
Pazopanib | 0.79 | U.S. Food and Drug Administration, 2009 |
Phenytoin | + | Gui et al., 2009 |
Pioglitazone | + | Nozawa et al., 2004 |
Pravastatin | 21.8 | Gui et al., 2009; Hsiang et al., 1999 |
Ramipril | 4.0 | Gui et al., 2010 |
Repaglinide | 1.1–2.2 | Bachmakov et al., 2008; Gui et al., 2010 |
Resveratrol | 11.2 | Gui et al., 2010 |
Rifampin | 0.477–17 | Vavricka 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 SV | 0.171–2 | Vavricka et al., 2002; Campbell et al., 2004; Chen et al., 2005; Hirano et al., 2006; Seithel et al., 2007; Sharma et al., 2009 |
Ritonavir | 0.71–1.4 | Tirona et al., 2003; Hirano et al., 2006; Annaert et al., 2010 |
Rosiglitazone | 6.0 | Nozawa et al., 2004; Bachmakov et al., 2008 |
Roxithromycin | 153 | Seithel et al., 2007 |
Saquinavir | 1.2–1.8 | Tirona et al., 2003; Campbell et al., 2004; Hirano et al., 2006; Annaert et al., 2010 |
Sildenafil | 1.5 | Treiber et al., 2007 |
Simvastatin | + | Hsiang et al., 1999 |
Simvastatin acid | 3.6 | Nakai et al., 2001; Chen et al., 2005 |
Simvastatin lactone | 9.7 | Chen et al., 2005 |
Sirolimus | 6.49 | Oswald et al., 2010 |
SN-38 | + | Nozawa et al., 2005 |
Tacrolimus | 0.611–3.7 | Fehrenbach et al., 2003; Hirano et al., 2006; Amundsen et al., 2010 |
Telithromycin | 121 | Seithel et al., 2007 |
Telmisartan | 0.436 | Hirano et al., 2006 |
μM | ||
Thyroxine | 3.5–3.85 | Gui et al., 2009; Bednarczyk, 2010 |
Troglitazone | 1.0–1.2 | Gui et al., 2008, 2009 |
Troglitazone sulfate | + | Nozawa et al., 2004 |
Valsartan | 8.96 | Hirano 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.