TABLE 3

Established mathematical models of parent and metabolites obtained from SCH-based data

Drugs and MetabolitesRemarksReferences
Terfenadine∼15% as BEI, kefflux > > kbile in rat SCHsTurncliff et al. (2006)
Fexofenadine∼15% as BEI, kefflux > kbile in rat SCHs
TroglitazoneMinimum biliary excretion in rat SCHsLee et al. (2010)
Troglitazone glucuronide∼50% as BEI, kefflux > kbile in rat SCHs
Troglitazone sulfate∼20% as BEI, kefflux < kbile in rat SCHs
PafuramidineRapidly metabolized in rat and human SCHsYan et al. (2011, 2012)
Furamidine (active form of pafuramidine)kefflux > > kbile in rat and human SCHs
CPD-0868Rapidly metabolized in rat SCHsYan et al. (2011)
CPD-0801 (active form of CPD-0868)kefflux > > kbile in rat SCHs
Mycophenolic acid (MPA)Rapidly metabolized in human SCHsMatsunaga et al. (2014)
MPA phenyl-glucuronide (MPAG)∼40% as BEI, kefflux > kbile in human SCHs
BosentanMinimum biliary excretion in human SCHsMatsunaga et al. (2016)
Ro 48-5033kefflux = kbile in human SCHs
Ro 47-8634kefflux = kbile in human SCHs
Ro 64-1056kefflux = kbile in human SCHs
  • BEI, biliary excretion index; CPD-0801, 2,5-bis (5-amidino)-2-pyridyl furan; CPD-0868, 2,5-bis [5-(N-methoxyamidino)-2-pyridyl] furan; kbile, biliary excretion rate from cells to bile canaliculi; kefflux, efflux rate from cells to buffer; OCT1, organic cation transporter 1.