Selected transport substrates for human OATP family members
| Transporter | Substrates | Reference(s) |
|---|---|---|
| OATP1A2 | Antibiotics (e.g., ciprofloxacin, enoxacin, erythromycin, gatifloxacin, levofloxacin, lomefloxacin, norfloxacin); antihistamines (e.g., fexofenadine); antineoplastic drugs (e.g., imatinib, methotrexate); β-blockers (e.g., acebutolol, atenolol, celiprolol, labetalol, sotalol, talinolol); cardiac glycosides (e.g., ouabain); endothelin-A receptor antagonists (e.g., atrasentan, BQ-123); HIV-1 protease inhibitors (e.g., darunavir, lopinavir, saquinavir); HMG-CoA reductase inhibitors (e.g., pitavastatin, rosuvastatin); neuromuscular blocking agents (e.g., rocuronium); opioid analgesic peptides (e.g., DPDPE); bilirubin; bromosulfophthalein; cholate; deltorphin II; estradiol-17β-glucuronide; estrone-3-sulfate; glycocholate; hydroxyurea; PGE2; reverse T3; taurocholate; taurochenodeoxycholate; tauroursodeoxycholate; T4; T3; metabolite of unoprostone | Roth et al., 2012 |
| OATP1B1 | Angiotensin-converting enzyme inhibitors (e.g., enalapril, temocapril); angiotensin II receptor antagonists (e.g., olmesartan, valsartan); antibiotics (e.g., cefazolin, cefditoren, cefoperazone, rifampicin); antifungal agents (e.g., caspofungin); anti-inflammatory drugs (e.g., mesalazine); antineoplastic agents (e.g., gimatecan, methotrexate); benzylpenicillin; endothelin-A receptor antagonists (e.g., atrasentan, bosentan, BQ-123); HIV-1 protease inhibitors (e.g., darunavir, lopinavir, saquinavir); HMG-CoA reductase inhibitors (e.g., atorvastatin, cerivastatin, fluvastatin, pitavastatin, pravastatin, rosuvastatin, simvastatin acid); loop diuretics (e.g., torasemide); opioid analgesic peptides (e.g., DPDPE); arsenic; bilirubin; bisglucuronosyl bilirubin; bromosulfophthalein; cholate; estradiol-17β-glucuronide; estrone-3-sulfate; fluorescein; glycocholate; glycoursodeoxycholate; hydroxyurea; leukotriene C4; leukotriene E4; monoglyucuronosyl bilirubin; phalloidin; PGE2; taurocholate; tauroursodeoxycholate; thromboxane B2; T4 | Roth et al., 2012 |
| OATP1B3 | Angiotensin-converting enzyme inhibitors (e.g., enalapril); angiotensin II receptor antagonists (e.g., olmestartan, telmisartan, valsartan); antibiotics (e.g., benzylpenicillin, cefadroxil, cefazolin, cefditoren, cefmetazole, cefoperazone, cephalexin, erythromycin, nafcillin, rifampicin); antihistamines (e.g., fexofenadine); antineoplastic drugs (e.g., docetaxel, imatinib, paclitaxel); cardiac glycosides (e.g., digoxin, ouabain); endothelin-A receptor antagonists (e.g., atrasentan, bosentan, BQ-123); HIV-1 protease inhibitors (e.g., saqunavir); HMG-CoA reductase inhibitors (e.g., fluvastatin, pitavastatin, rosuvastatin); nonsteroidal anti-inflammatory drugs (e.g., diclofenac); opioid analgesic peptides (e.g., DPDPE); bilirubin; bromosulfophthalein; cholate; cholecystokinin octapeptide (CCK-8); dehydroepiandrosterone-3-sulfate; deltorphin II; estradiol-17β-glucuronide; estrone-3-sulfate; fluorescein; glutathione; glycocholate; glycoursodeoxycholate; hydroxyurea; leukotriene C4; phalloidin; taurocholate; taurochenodeoxycholate; tauroursodeoxycholate; T4; T3 | Roth et al., 2012 |
| OATP1C1 | Bromosulfophthalein; estradiol-17β-glucuronide; estrone-3-sulfate; thyroid hormones | Pizzagalli et al., 2002; Westholm et al., 2009a,b |
| OATP2A1 | Prostaglandins (e.g., PGE1, PGE2, PGF2α, PGH2, thromboxane B2) | Kanai et al., 1995; Chi and Schuster, 2010 |
| OATP2B1 | Antibiotics (e.g., benzylpenicillin, tebipenem pivoxil); antihistamines (e.g., fexofenadine); anti-inflammatory drugs (e.g., mesalazine); β-blockers (e.g., talinolol); endothelin-A receptor antagonists (e.g., bosentan); HMG-CoA reductase inhibitors (e.g., atorvastatin, fluvastatin, pravastatin, pitavastatin, rosuvastatin); leukotriene receptor antagonists (e.g., monteleukast); aliskiren; bromosulfophthalein; dehydroepiandrosterone-3-sulfate; estrone-3-sulfate; ezetimibe glucuronide; glibenclamide; pregnenolone sulfate; taurocholate; metabolite of unoprostone | Tamai et al., 2001; Kobayashi et al., 2003; Nozawa et al., 2004; Gao et al., 2005; Kopplow et al., 2005; Hirano et al., 2006; Ho et al., 2006; Grube et al., 2006a,b; Noe et al., 2007; Treiber et al., 2007; Oswald et al., 2008; Vaidyanathan et al., 2008; Leuthold et al., 2009; Mougey et al., 2009; Konig et al., 2011 |
| OATP3A1_v1 | Antibiotics (e.g., benzylpenicillin); endothelin-A receptor antagonists (e.g., BQ-123); PGE1; PGE2; T4; vasopressin; estrone-3-sulfate; deltorphin II | Tamai et al., 2000; Huber et al., 2007; Roth et al., 2012 |
| OATP3A1_v2 | Endothelin-A receptor antagonists (e.g., BQ-123); PGE1; PGE2; T4; vasopressin; arachidonic acid | Huber et al., 2007; Roth et al., 2012 |
| OATP4A1 | Antibiotics (e.g., benzylpenicillin); estradiol-17β-glucuronide; estrone-3-sulfate; T4; T3; reverse T3; PGE2; taurocholate; metabolite of unoprostone | Tamai et al., 2000; Fujiwara et al., 2001; Gao et al., 2005 |
| OATP4C1 | Antifolates (e.g., methotrexate); cardiac glycosides (e.g., digoxin, ouabain); cAMP; estrone-3-sulfate; sitagliptin; T4; T3 | Mikkaichi et al., 2004; Chu et al., 2007; Yamaguchi et al., 2010 |
PGE, prostaglandin.