TABLE 1

General properties on statins and rifampicin as perpetrator drug

Oral doses (in milligrams) applied in vivo, fraction absorbed, and bolus applied to the portal vein of ex vivo perfused livers (in milligrams).

Substrate (Victim Drug)Transporters InvolvedMetabolismFraction AbsorbedOral DosesBolus Applied to Ex Vivo Liver
%mg
AtorvastatinNTCP, OATP1B1, OATP1B3, and OATP2B1a,bCYP3A4a,b12c10g0.104
PitavastatinBCRP, NTCP, OATP1B1, and OATP1B3a,bCYP2C9c
CYP2C8
60c2c0.141
RosuvastatinOATP1B1, OATP1B3, NTCP, MRP2, and BCRPa,bCYP2C9d50e10h1.400
Perpetrator drug
Rifampicin95f600a,b67.7
  • aTakehara et al. (2018).

  • bMori et al. (2019).

  • cMukhtar et al. (2005).

  • dSchneck et al. (2004).

  • eSjöberg et al. (2013).

  • fZwolska et al. (1998).

  • gLennernäs (2003).

  • hBergman et al. (2006).