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. Author manuscript; available in PMC: 2021 Aug 17.
Published in final edited form as: AAPS J. 2020 Aug 17;22(5):111. doi: 10.1208/s12248-020-00469-6

Table II:

Changes in Pharmacokinetic Parameters (Expressed as Ratios of Interaction / Control) in Oral Drug-Drug Interaction Studies that Affect Intestinal Xenobiotic Transporters

Victim Drug: Perpetrator Drug: Major Enzyme or Transporter Population MATDDIMATCon tmaxDDItmaxCon AUCDDIAUCCon CL/FDDICL/FCon Vss/FDDIVss/FCon MRTDDIMRTCon t1/2,zDDIt1/2,zCon Percent AUC Extrapolation (DDI/Con) Reference
Rosuvastatin (Single Dose) Rifampin (Single Dose) BCRP (Inhibition) Whites (n=7) 0.47 0.50 3.37 0.28 0.082 0.30a 0.64 1%/8% (21)
Rosuvastatin (Single Dose) Rifampin (Single Dose) BCRP (Inhibition) Asians (n=8) 0.34 0.55 3.21 0.31 0.11 0.34a 0.59 1%/7% (21)
Talinolol (Multiple Dose) Rifampin (Multiple Dose) P-gp (Induction) Healthy Men (n=8) 1.70b 1.35 0.65 1.54 1.24c 0.79c 0.85 n/a (steady-state) (22)

Pharmacokinetic values reported in the table are based on published average values, unless otherwise noted

Abbreviations: AUC, area under the curve; BCRP, breast cancer resistance protein; Con, control; CL/F, apparent clearance; DDI, drug-drug interaction; MAT, mean absorption time; MRT, mean residence time; n/a, not applicable; P-gp, P-glycoprotein; tmax, time to maximal concentration; t1/2,z, terminal half-life; Vss/F, apparent volume of distribution at steady state

a

MRT was calculated using Equation 7 and average reported values of CL/F and Vss/F

b

MAT was calculated by utilization of the steady-state relationship between reported tmax and t1/2,z (Equation 4)

c

Ratios are calculated by digitization of published average plasma concentration-time profiles and performing compartmental analysis, where steady-state MRT was calculated using Eq 6