TABLE 3

Contribution of OATP2 and OATP8 to the hepatic uptake of pitavastatin and E217βG determined using transporter-selective substrates


Hepatocyte Lot

Ratio of Uptake Clearance

Estimated Clearancea
CLhep/CLtransporter
Pitavastatin
E217βG
Ract,OATP2
Ract,OATP8
OATP2
OATP8
OATP2
OATP8
μl/min/106 cells
OCF 0.833 0.291 63.8 8.92 13.2 0.218
87.7% 12.3% 98.4% 1.63%
094 1.02 0.131 77.8 4.01 16.0 0.0979
95.1% 4.91% 99.4% 0.607%
ETR 0.437 0.0757 33.5 2.32 6.91 0.0565



93.5%
6.47%
99.2%
0.812%
  • a The second line entry under “Estimated Clearance” shows the percentage of OATP2- or OATP8-mediated uptake clearance relative to the sum of the estimated clearance mediated by OATP2 and OATP8. The details of this estimation are described under Materials and Methods.