TABLE 1

In vitro values of perpetrators and NGMN AUC values from clinical studies

DrugDoseCYP3A4CYP3A4NGMNReference
KIkinactKiEC50EmaxAUCiAUC
mgnMmin−1nMµMpg·h/mlpg·h/ml
LPR40010000.11730013876Weemhoff et al. (2003); Ernest et al. (2005); Fahmi et al. (2008); Vogler et al. (2010)
RTV study 11001700.440100068.513876Weemhoff et al. (2003); Ernest et al. (2005); Fahmi et al. (2008); Vogler et al. (2010)
ATV300500.049230035,02219,188Ernest et al. (2005); Fahmi et al. (2008); Hyland et al. (2008); Zhang et al. (2011)
RTV study 21001700.440100068.535,02219,188Ernest et al. (2005); Fahmi et al. (2008); Hyland et al. (2008); Zhang et al. (2011)
EFZ60040,00039006.5652218,328Sevinsky et al. (2011); Siccardi et al. (2013); Xu and Desta (2013)
  • KI, perpetrator irreversible inhibition constant; kinact, perpetrator maximum irreversible inactivation rate constant; Ki, perpetrator reversible inhibitor constant; EC50, perpetrator concentration of inducer causing half-maximal induction; Emax, perpetrator fold induction in enzyme activities, AUCi is the NGMN (victim) plasma concentration versus time AUC in the presence of an inhibitor and AUC is the NGMN plasma concentration versus time AUC in the absence of an inhibitor.