Table 1.
List of the major OATs and OATPs frequently implicated in drug therapy
This list includes the representative substrates; the endogenous probes used for the assessment of the transporter function in vivo and the risk for drug-drug interactions are underlined; comprehensive lists covering endogenous and exogenous substrates are available in previous reviews (1, 19, 21, 46, 151–154).
| Protein name (gene name) | Location | Example substrates |
|---|---|---|
| OAT1 (SLC22A6) | Kidney, brain, placenta, muscle; basolateral | Endogenous: α-ketoglutarate, urate, prostaglandin E2, taurine |
| Exogenous: adefovir, cidofovir, acyclovir, methotrexate, pravastatin, ciprofloxacin, chlorothiazide, ochratoxin A | ||
| OAT2 (SLC22A7) | Liver, kidney; basolateral | Endogenous: cGMP, creatinine, prostaglandin E2 |
| Exogenous: irinotecan, 5-fluorouracil, acyclovir, ganciclovir | ||
| OAT3 (SLC22A8) | Kidney, choroid plexus, testis; basolateral | Endogenous: estrone sulfate, bile acids, creatinine, prostaglandin E2, glycochenodeoxycholate-3-O-sulfate (GCDCA-S), 6β-hydroxyl cortisol |
| Exogenous: benzylpenicillin, cimetidine, ranitidine, famotidine, methotrexate, cidofovir, valacyclovir, sitagliptin, pravastatin | ||
| OAT4 (SLC22A11) | Kidney (apical), placenta (basolateral) | Endogenous: dehydroepiandrosterone sulfate, urate, estrone sulfate, prostaglandin E2 |
| Exogenous: indomethacin, tetracycline, ochratoxin A, methotrexate, olmesartan, levocetirizine | ||
| OATP1B1 (SLCO1B1) | Liver (basolateral) | Endogenous: estrone sulfate, estradiol 17β-glucuronide, dehydroepiandrosterone sulfate, coproporphyrin I and III (CPI and CPIII), GCDCA-S, unconjugated and conjugated bilirubin (UCB and CB) |
| Exogenous: bosentan, daunorubicin, fexofenadine, pitavastatin, atorvastatin, rosuvastatin, rifampicin, darunavir, mycrocystin | ||
| OATP1B3 (SLCO1B3) | Liver (basolateral) | Endogenous: cholecystokinin-8, CPI, CPIII, GCDCA-S, UCB, and CB |
| Exogenous: paclitaxel, pitavastatin, atorvastatin, rosuvastatin, rifampicin, telmisartan, mycophenolic acid, glucuronide | ||
| OATP1A2 (SLCO1A2) | Liver (cholangiocytes), brain capillary, kidney, retinal epithelium | Endogenous: estrone sulfate, retinoids, prostaglandin E2 |
| Exogenous: imatinib, fexofenadine, methotrexate, statins, microcystin | ||
| OATP2B1 (SLCO2B1) | Liver, intestine | Endogenous: estrone sulfate, dehydroepiandrosterone sulfate, prostaglandin E2 |
| Exogenous: glibenclamide, statins, fexofenadine, atenolol, montelukast |