TABLE 1

IC50 values of GEM and GEM-1-O-glu on the OATP2-mediated uptake and metabolism of [14C]CERa




GEM

GEM-1-O-glu
μM
OATP2-mediated uptake 72.4 ± 28.4 24.3 ± 19.8
CYP2C8-mediated metabolism 28.0 ± 4.3 4.07 ± 1.23
CYP3A4-mediated metabolism
372 ± 100
243 ± 59
  • a All data are represented as the mean ± computer-calculated S.D.