Table 1.
Drug-metabolizing enzymes (DMEs) and transporters that are involved in ADME processes of pharmacokinetics.
| Organs or tissues | Cell types | Subcellular localization | DMEs/transporters for drugs |
|---|---|---|---|
| Intestine | Intestinal epithelial cells (enterocytes) | Apical (luminal) membrane | OATPs, PEPT1, ASBT, MCT1, MDR1, BCRP, MRP2 |
| Inside the cell | Phase I DMEs: mainly CYPs | ||
| Phase II DMEs: UGT, SULT, and GST | |||
| Basolateral (abluminal) membrane | OCT1, OSTα/γ, MRP1, MRP3 | ||
| Liver | Hepatocytes | Basolateral (sinusoidal) membrane | OATPs, NTCP, OCT1, OAT2/7, OSTα/γ, MRP3, MRP4, MRP6 |
| Inside the cell | Phase I DMEs: mainly CYPs | ||
| Phase II DMEs: UGT, SULT, and GST | |||
| Apical (canalicular) membrane | MDR1, BCRP, MRP2, BSEP, MATE1 | ||
| Kidney | Renal tubular epithelial cells | Basolateral membrane | OCT2, OAT1-3, OATP4C1, OSTα/γ, MRP3 |
| Apical membrane | OAT4, PEPT1/2, OCTN1/2, MDR1, BCRP, MRP2/4, MATE1, MATE2-K |
ASBT: apical sodium dependent bile acid transporter; CYPs: cytochrome P450s; BCRP: breast cancer resistance protein; BSEP: bile salt export pump; DMEs: drug-metabolizing enzymes; GST: glutathione-S-transferase; MATE: multidrug and toxin extrusion protein; MCT: monocarboxylic acid transporter; MDR1: multidrug resistance protein 1 (P-glycoprotein; P-gp); MRP: multidrug resistance-associated protein; NTCP: sodium dependent cotransporting polypeptide; OAT: organic anion transporter; OATPs: organic anion transporting polypeptides; OCT: organic cation transporter; OSTα/γ: heteromeric organic solute transporter; OCTN: organic cation/carnitine transporter; PEPT: peptide transporter; SULT: sulfotransferase; UGT: uridine 5′-diphosphate-glucuronosyltransferase.