Drug | Dose | CYP3A4 | CYP3A4 | NGMN | Reference | ||||
---|---|---|---|---|---|---|---|---|---|
KI | kinact | Ki | EC50 | Emax | AUCi | AUC | |||
mg | nM | min−1 | nM | µM | pg·h/ml | pg·h/ml | |||
LPR | 400 | 1000 | 0.11 | 7300 | 138 | 76 | Weemhoff et al. (2003); Ernest et al. (2005); Fahmi et al. (2008); Vogler et al. (2010) | ||
RTV study 1 | 100 | 170 | 0.4 | 40 | 1000 | 68.5 | 138 | 76 | Weemhoff et al. (2003); Ernest et al. (2005); Fahmi et al. (2008); Vogler et al. (2010) |
ATV | 300 | 50 | 0.049 | 2300 | 35,022 | 19,188 | Ernest et al. (2005); Fahmi et al. (2008); Hyland et al. (2008); Zhang et al. (2011) | ||
RTV study 2 | 100 | 170 | 0.4 | 40 | 1000 | 68.5 | 35,022 | 19,188 | Ernest et al. (2005); Fahmi et al. (2008); Hyland et al. (2008); Zhang et al. (2011) |
EFZ | 600 | 40,000 | 3900 | 6.5 | 6522 | 18,328 | Sevinsky 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.