Repaglinide drug-drug interactions in vivo with details on main P450 enzymes involved, administered repaglinide dose, number of subjects, change in repaglinide AUC, and change in metabolite AUC ratios

InhibitorMain P450 InvolvedRepaglinide DoseNo. SubjectsFold Change in Repaglinide AUCFold Change in M2/M1 AUC RatioFold Change in M2/M4 AUC RatioReference
GemfibrozilaCYP2C80.25128.1Not reportedNot reportedNiemi et al., 2003
ItraconazoleCYP3A40.25121.4Not reportedNot reportedNiemi et al., 2003
Gemfibrozila + ItraconazoleCYP2C8 + CYP3A40.251219Not reportedNot reportedNiemi et al., 2003
GemfibrozilaCYP2C80.25105.0–7.0b0.39–0.57b2.3–9.7bTornio et al., 2008
AtorvastatinaCYP3A40.2524N.S.–1.2c1.05–1.3c0.87–1.1cKalliokoski et al., 2008a
GemfibrozilaCYP2C80.25247.3–8.2c0.38–0.52c6.4–10.4cKalliokoski et al., 2008a
GemfibrozilaCYP2C80.2591.0–7.6b0.42–1.2b0.94–18bBackman et al., 2009
TelithromycinCYP3A40.25121.83.90.80Kajosaari et al., 2006b
MontelukastCYP2C80.2512N.S.1.10.98Kajosaari et al., 2006b
Telithromycin + montelukastCYP3A4 + CYP2C80.25121.9d4.30.82Kajosaari et al., 2006b
PioglitazoneCYP2C8 + CYP3A40.2512N.S.Not reportedNot reportedKajosaari et al., 2006a
ClarithromycinCYP3A40.2591.4Not reportedNot reportedNiemi et al., 2001
TrimethoprimCYP2C80.2591.6Not reportedNot reportedNiemi et al., 2004
CyclosporineaCYP3A40.25122.4Not reportedNot reportedKajosaari et al., 2005
KetoconazoleCYP3A428N.S.Not reportedNot reportedHatorp et al., 2003
BezafibrateCYP2C80.2512N.S.Not reportedNot reportedKajosaari et al., 2004
FenofibrateCYP2C80.2512N.S.Not reportedNot reportedKajosaari et al., 2004
  • N.S., not significant.

  • a OATP1B1 also involved.

  • b Depending on time interval between repaglinide and gemfibrozil doses.

  • c Depending on SLCO1B1 genotype.

  • d Not significantly different from telithromycin phase.