TABLE 2

Involvement of intestinal transporters for drug absorption (see also references contained in Tsuji and Tamai, 1996 )


Transporter

Substrate

Reference
abst or ibat Ileal sodium-dependent bile acid transporter Taurocholate Schneider et al. 1995; Craddock et al., 1998
Pept1 Oligopeptide transporter 1 Aminocephalosporins, β-amino lactam antibiotics (cyclacillin, cephalexin, cephradine), acetylcholinesterase inhibitors (benazepril, quinapril), bestatin, renin inhibitors Fei et al., 1994
Mct1 Monocarboxylic acid transporter 1 Lactate and pyruvate transport (simple aryl and alkyl acids)
Oatp3 Intestinal organic anion transporting polypeptide 3 Taurocholate, estrone sulfate Walters et al., 2000
NPT1 Sodium-dependent phosphate tranporter 1 Fosfomycin, foscarnet Tsuji and Tamai, 1989
OCT1 Organic cation transporter 1 Spermine, spermidine
Folic acid transporter Methotrexate
CNT Nucleoside transporters N1 (purine) and N2 (pyrimidine) Zidovudine, stavudine, thymidine, ribavirin, allopurinol, 5-fluorouracil
Amino acid carrier d- and l-Methionine, l-methyldopa, baclofen, taurine, alanine
MDR1 or Pgp Multidrug resistance protein 1 or P-glycoprotein Daunomycin, rhodamine 123, verapamil, diltiazem, colchicine, digoxin, quinidine, vincristine, etoposide β-blockers (sotalol, pafenolol, celiprolol, tanilol)
Mrp2 Multidrug resistance-associated protein 2 Glutathione conjugates, glucuronide conjugates, leukotriene C4, vincristine Gotoh et al., 2000; Mottino et al., 2000
BCRP Breast cancer resistance protein Topotecan, mitoxantrone, anthracyclines Doyle et al., 1998; Zamber et al., 2003
Mrp3

Rost et al., 2002