TABLE 1

Selected endogenous and exogenous canalicular ABC transporter substrates

ABCB11ABCC2ABCB1ABCG2ABCB4ABCG5/G8
Endogenous substrates
 Glycocholic acidaBilirubin mono- and diglucuronideaAldosteroneaCholic acidaPhosphatidylcholineaCholesterola
 Taurocholic acidaCholecystokinin-8-sulfateaCholesterolaEstradiol-17β-glucuronidea
 Glycochenodeoxycholic acidaEstradiol-17β-glucuronideaCortisolaEstrone-3-sulfatea
 Taurochenodeoxycholic acidaEstrone-3-sulfateaEstradiol-17β-glucuronideaFolic acid glutamatesa
 Glycodeoxycholic acidaGlutathione disulfideaEstroneaGlycocholic acida
 Taurodeoxycholic acidaHyodeoxycholic acid glucuronideaEthinylestradiolaHemea
 Tauroursodeoxycholic acidaLeukotriene C4aOpioid peptidesaProtoporphyrin IXa
 Taurolithocholate-3-sulfateaProstaglandin E2aShort-chain phospholipidsaTaurocholic acida
Taurolithocholatic acid sulfateaUnconjugated bilirubinaTaurolithocholic acid sulfatea
Tauroursodeoxycholic acida6α-OH-taurocholic acidUratea
6α-OH-taurocholic acid
Exogenous substrates
 Calcein-AMAcetaminophen glucuronideCalcein-AMa4-Methylumbelliferone glucuronideaDigoxina24-Methylene cholesterola
 PravastatinaAcetaminophen glutathioneColchicine4-Methylumbelliferone sulfateaPaclitaxelaBrassicasterola
 TaxolAcetaminophen sulfateDaunorubicinaAlbendazole sulfoxideaVinblastineaCampesterola
 VinblastineAmpicillinDigoxinaAnthracenesa5α-Campestanola
ArseniteaDiltiazemaAnthracyclinesa5α-Cholestanola
Bromosulfophthalein glutathioneaDocetaxelaCamptothecin derivatesa22-Dehydrocholesterola
CadmiumaDoxorubicinaDaunomycinaSitosterola
Carboxydichlorofluorescein-diacetateErythromycinaDinitrophenyl glutathionea5α-Sitostanola
CeftriaxoneEthidium bromideaDoxorubicinaStigmasterola
DibromosulfophthaleinEtoposideaE3040-glucuronide
Dinitrophenyl glutathioneaGramicidin DaHoechst 33342a
Indomethacin glucuronideHoechst 33342aIrinotecan (SN-38 metabolite)a
MethotrexateaIndinavirImatiniba
Morphine glucuronideaIvermectinaLysotracker greena
Mycophenolic acid glucuronideLosartanMethotrexatea
PaclitaxelaMethotrexateaMitoxantronea
Phenobarbital glucuronideMitomycin CaNucleoside analogsa
Phenolphthalein sulfateOpioid peptidesaPheophorbide αa
2-amino-1-methyl-6-phenylimidazo[4,5b]pyridine (PhIP)PaclitaxelaPhIPa
Phytoestrogen glucuronidesRhodamine 123aPitavastatina
PravastatinaRitonaviraRhodamine 123a
ProbenecidaSaquinaviraTopotecana
Resveratrol sulfateaTeniposidea
SulfinpyrazoneaTopotecana
VinblastineaValinomycina
ZincVerapamila
Vinblastinea
Vincristinea
  • a Demonstrated in ABC human transporter studies.