IC50 = 0.5 Clinical study showed increased rosuvastatin µM & pravastatin exposure with the 3DAA regimen, but individual contribution unknown IC50 = 0.6 µM OCT1 IC50 = 2.5 Ritonavir (and other compounds in the 3DAA µM regimen) have low potential for clinically relevant interactions with renal transporters; OAT1 IC50 = 14 µM Clinically, tenofovir exposure was similar following co-administration with the 2DAA OAT3 IC50 = 8.1 and 3DAA regimens µM MATE1 IC50 = 3.3 µM MATE2K IC50 = 90 µM BSEP IC50 = 0.1 µM UGT1A1 IC50 = 2.1 Possible; (clinical study showed 34% µM decrease in raltegravir exposure with the 3DAA regimen, but individual contribution unknown) CYP2C9 IC50 = 9 µM Unlikely 1.08) 60 Confirmed clinically (lack of interaction with warfarin) CYP2C8 IC50 = 17 Unlikely µM CYP2C19 IC50 = 18 Unlikely; (clinical study showed 38% µM reduction in omeprazole AUC) UGT1A1 IC50 = 0.92 Possible; (clinical study showed 34% µM decrease in raltegravir exposure with the 3DAA regimen, but individual contribution unknown) IC50 = 0.9 Unlikely (R-value = 1.06) µM IC50 = 6.6 Unlikely (R-value = 1.01) µM P-gp IC50 = 16.7 Possible, but not confirmed clinically (no µM increase in digoxin exposure when administered as part of 3DAA regimen) BCRP IC50 = 15.6 µM
IC50 = 0.5 µM Clinical study showed increased rosuvastatin & pravastatin exposure with the 3DAA regimen, but individual contribution unknown IC50 = 0.6 µM OCT1 IC50 = 2.5 µM Ritonavir (and other compounds in the 3DAA regimen) have low potential for clinically relevant interactions with renal transporters; Clinically, tenofovir exposure was similar following co-administration with the 2DAA and 3DAA regimens OAT1 IC50 = 14 µM OAT3 IC50 = 8.1 µM MATE1 IC50 = 3.3 µM MATE2K IC50 = 90 µM BSEP IC50 = 0.1 µM UGT1A1 IC50 = 2.1 µM Possible; (clinical study showed 34% decrease in raltegravir exposure with the 3DAA regimen, but individual contribution unknown) CYP2C9 IC50 = 9 µM Unlikely 1.08) 60 Confirmed clinically (lack of interaction with warfarin) CYP2C8 IC50 = 17 µM Unlikely CYP2C19 IC50 = 18 µM Unlikely; (clinical study showed 38% reduction in omeprazole AUC) UGT1A1 IC50 = 0.92 µM Possible; (clinical study showed 34% decrease in raltegravir exposure with the 3DAA regimen, but individual contribution unknown) IC50 = 0.9 µM Unlikely (R-value = 1.06) IC50 = 6.6 µM Unlikely (R-value = 1.01) P-gp IC50 = 16.7 µM Possible, but not confirmed clinically (no increase in digoxin exposure when as part of 3DAA regimen) BCRP IC50 = 15.6 µM administered
auspar-paritaprevir-ritonavir-ombitasvir-dasabuvir-as-sodium-salt-and-ribavirin-170324.docx