TABLE 2

Summary of mechanistic static model based predictions of OAT-mediated DDIs with probenecid

CompoundsProbenecid DosePredicted Change in CLSecPredicted Change in Renal ClearanceObserved Change in Renal ClearancePredicted/Observed RatioReferences for Observed Change in Renal Clearance
%
Acyclovir1g32320.05(Laskin et al., 1982)
Adefovir0.5g2920151.32(Maeda et al., 2014)
Adefovir0.75g5034560.61(Maeda et al., 2014)
Adefovir1.5g7653481.09(Maeda et al., 2014)
Benzylpenicillin0.5g4337500.74(Maeda et al., 2014)
Benzylpenicillin0.75g6556541.04(Maeda et al., 2014)
Benzylpenicillin1.5g8675780.96(Maeda et al., 2014)
Bumetanide1g8468850.80(Odlind et al., 1983)
Cefazolin1g8342381.10(Brown et al., 1993)
Cimetidine0.5g4235251.42(Gisclon et al., 1989)
Famotidine1.5g8662640.97(Inotsume et al., 1990)
Fexofenadine1g8049680.72(Yasui-Furukori et al., 2005; Liu et al., 2008)
Furosemide1g8382721.14(Chennavasin et al., 1979)
Ganciclovir1g21190.08(Cimoch et al., 1998)
Methotrexate1g8262551.13(Aherne et al., 1978)
Olmesartan0.5g5550331.51(Li et al., 2014)
Oseltamivir acid0.5g5232520.62(Hill et al., 2002)
Zalcitabine0.5g4234420.81(Massarella et al., 1996)
  • Predictions were based on mean transport rates from Table 1.

  • Change in renal clearance was assumed to be same as change in total IV clearance.