DRUG TRANSPORTERS IN THE INTESTINE - Drug Transporters: Molecular Characterization and Role in Drug Disposition - page 501

TABLE 16.1. Well-Studied Drug Transporters in the Intestine
Symbol Alias Subcellular Localization Substrates

ABC Subfamily B ABCB1 MDR1, Pgp Apical membrane of

enterocytes 17

Anti-cancer drugs: paclitaxel 45 , vinblastine 70

Anti-HIV drugs: saquinavir 71
Immunosuppressants: tacrolimus 72
Antihistamine drugs: fexofenadine 73
Cardiovascular drugs: Digoxin 46

Subfamily C ABCC1 MRP1 Basolateral membrane

of crypt cells 16

Anticancer drugs: Doxorubicin 74 ,
Daunomycin, 62 vincristine 63

ABCC2 MRP2, CMOAT Apical membrane Anticancer drugs: PEITC, 75 EGCG, 76

etoposide 77
Anti-HIV drugs: saquinaivir 78

ABCC3 MRP3 Basolateral

membrane 79

Apical membrane 80 Anticancer drugs: Topotecan, 57 mitoxantrone 81

Subfamily G ABCG2 BCRP, MXR, ABCP

Anti-HIV drugs: saquinavir 36
Antihistamine drugs: fexofenadine 73

SLC SLCO subfamily SLCO1A2 OATP, OATP1, OATP-A Unknown

Apical membrane 82 Lipid-lowering drugs: pravastatin 82

SLCO2B1 OATP-B

SLC15A subfamily SLC15A1 PEPT1 Apical membrane of

villus epithelial
cells 83

Cephalosporins, penicillins,
angiotensin-converting enzyme (ACE)
inhibitors, antiviral drugs (see review 84 )