TABLE 4

Summary of literature reports describing OATP expression profiling after addition of inducer to cultured human primary hepatocytes and human liver tissue slices in vitro

InduceraReported Mean Fold-Change (vs. Control)bReference
OATP1B1OATP1B3OATP2B1CYP3A4PgpMRP2BCRP
RIF1.0NRNR232.6NRNRChen et al., 2011
Phenobarbital1.3NRNR212.3NRNR
RIFc1.30.90.88.91.50.70.7Schaefer et al., 2012
Phenobarbitalc1.41.51.3154.32.42.0
RIF0.8NRNR401.91.40.8Badolo et al., 2015
Phenobarbital1.2NRNR452.22.12.0
RIF≤1.0≤1.0≤1.0≥20NRNRNRHan et al., 2017
RIF2.3NRNR171.78.2NRSahi et al., 2006
RIFd3.10.52.9752.5NR1.5Moscovitz et al., 2018
RIFeNR0.6NR13.74.82.5NROlinga et al., 2008
PhenobarbitaleNR5.6NR8.62.612.4NR
RIF0.90.61.5592.01.41.3Niu et al., 2019
RIF2.4≤1.0≤1.0372.92.52.7Jigorel et al., 2006
PhenobarbitalfNR≤1.0≤1.0NR4.43.83.7
RIF2.51.0NR5.52.51.5NRLiu et al., 2012
Amprenavirg7.01.8NR152.51.5NR
  • NR, not reported. Pgp (ABCB1), MRP2 (ABCC2), BCRP (ABCG2).

  • a Unless otherwise indicated, data represent cultured human primary hepatocytes exposed to RIF (≥10 µM) for ≥24 h; phenobarbital (1 mM) for 48 h.

  • b Unless otherwise indicated, data reported as fold-increase in mRNA expression.

  • c Fold-increase in protein expression.

  • d Maximal observed fold-induction (over a concentration range of 0.1–10 µM).

  • e Human liver tissue slices incubated with RIF (10 µM for 16 h) or phenobarbital (50 µM for 24 h).

  • f Hepatocytes incubated with phenobarbital (3.2 mM) for 72 h.

  • g Final concentration of amprenavir was 10 µM.