TABLE 6

Examples of drug-drug interactions caused by inhibition of OATP1B1

InhibitorSubstrateAUC IncreaseReference
fold
Atazanavir/ritonavirRosuvastatin2.1Busti et al., 2008
AtorvastatinRepaglinide1.2Kalliokoski et al., 2008a
ClarithromycinPravastatin2.1Jacobson, 2004
CyclosporineBosentan2Binet et al., 2000
Caspofungin1.4Merck and Co., 2010
Atorvastatin7.4aÅsberg et al., 2001
8.7aHermann et al., 2004
15.3aLemahieu et al., 2005
Cerivastatin3.8aMück et al., 1999
Fluvastatin3.1–3.6Park et al., 2001
Irinotecan1.2–7.3 (SN-38)Innocenti et al., 2004
Lovastatin20aOlbricht et al., 1997
Methotrexate1.2Fox et al., 2003
Pitavastatin5Hasunuma et al., 2003
Pravastatin10Regazzi et al., 1993
5–7Olbricht et al., 1997
9.9Hedman et al., 2004
Repaglinide2.4aKajosaari et al., 2005b
Rosuvastatin7.1Simonson et al., 2004
Simvastatin2.6aArnadottir et al., 1993
8aIchimaru et al., 2001
EltrombopagRosuvastatin1.6European Medicines Agency, 2010a
GemfibrozilAtorvastatin1.2Backman et al., 2005
Cerivastatin5.6bBackman et al., 2002
FluvastatinNo changeSpence et al., 1995
Lovastatin2.8Kyrklund et al., 2001
Pitavastatin1.5Mathew et al., 2004
Pravastatin2Kyrklund et al., 2003
Repaglinide8.1bNiemi et al., 2003c
Rosuvastatin1.9Schneck et al., 2004
Simvastatin2.9Backman et al., 2000
Lopinavir/ritonavirRosuvastatin2.1Kiser et al., 2008
RifampincAtorvastatin7.3Lau et al., 2007
Atorvastatin4.3–9.3He et al., 2009
Glyburide2.3Zheng et al., 2009
  • a Inhibition of CYP3A4 also involved.

  • b Inhibition of CYP2C8 is probably the main mechanism of the interaction.

  • c Single-dose administration.