Prediction of transporter-mediated drug-drug interactions and phenotyping of hepatobiliary transporters involved in the clearance of E7766, a novel macrocycle-bridged dinucleotide

Data Supplement

• Supplemental Figure 1 -

  Supplemental Figure 1 - Uptake activity of positive controls in the presence and absence of inhibitors in uptake transporter-expressing cells (A) or efflux transporter-expressing vesicles (B).
  

• Supplemental Figure 2 -

  Supplemental Figure 2 - Time-dependent uptake of E7766 with HEK293-control (empty circle, A, B), HEK293-OATP1B1 (solid circle, A) and HEK293-OAPT1B3 (solid circle, B) cells. All experiments were run in triplicates.

• Supplemental Figure 3 -

  Supplemental Figure 3 - Systemic unbound concentration versus time profile of Rifampicin in mice after i.v. bolus coadministration of E7766 and Rifampicin. Data are presented as mean ± SD (N=3).
  

• Supplemental Table 1 -

  Supplemental Table 1 - Permeability assessment of E7766 in LLC-PK1 cells.
  

• Supplemental Table 2 -

  Supplemental Table 2 - OATP1B1 and OATP1B3 protein expression levels in human hepatocytes and HEK293FT overexpressing cell lines.

• Supplemental Table 3 -

  Supplemental Table 3 - Demographic information of hepatocyte donor used in SCHH study. 

• Supplemental Table 4 -

  Supplemental Table 4 - Summary of input parameters of Rifampicin used to conduct drug-drug  interaction simulation of E7766.