Table 2.
A list of representative substrates for the solute carrier family 21 (SLCO) transporter OATP1A2. Endogenous substrates are on the right panel. Frequently prescribed drugs that are substrates for OATP1A2 are listed in the middle and left panel. Drugs are clustered by therapeutic class and this list in not exhaustive. Endogenous transport substrates of OATP1A2 include bile acids and linear and cyclic peptides, steroid conjugates, the thyroid hormones T4, T3 and rT3, prostaglandin E2. Pharmacologic and other exogenous transporter substrates for OATP1A2 include antibiotics, synthetic prostaglandins, HIV antivirals, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors (statins), natural product cardiac glycosides, antihistamines, beta adrenergic blocking agents (beta blockers), chemotherapeutics, the synthetic opioid receptor agonists [D-Pen2,D-Pen5]enkephalin (DPDPE) and deltorphin II, certain magnetic resonance imaging contrast agents, and the dye sulfobromophthalein (SBP).
| Endogenous Substrates | Drug Substrates | |
|---|---|---|
| Steroid Hormones: | Antibiotics: | Beta-blockers: |
| DHEA-S Estradiol-17β-glucuronide Estrone-3-sulfate |
Erythromycin Ciprofloxacin Gatifloxacin Rifamycin Levofloxacin/fluoroquinolones Tebipenem Pivoxil |
Acebutolol Atenolol Celiprolol Labetalol Nadolol Sotalol Talinolol |
| Thyroid Hormones: | Prostaglandins: | Chemotherapeutics: |
| Reverse triiodothyronine (rT3) Thyroxine (T4) Triiodothyronine (T3) |
Unaprostone | Methotrexate Imatinib Atrasentan |
| Prostaglandins: | HIV antivirals: | Dyes: |
| Prostaglandin E2 | Darunavir Lopinavir Saquinavir |
Sulfobromophthalein (SBP) |
| Bile Acids: | Statins: | Paralytics: |
| Bilirubin Cholic acid Glycocholate Taurocholate Taurochenodeoxycholate (TCDC) Tauroursodeoxycholate (TUDC) |
Rosuvastatin Atorvostatin Pitavastatin |
Rocuronium |
| Other: | Cardiac Glycosides: | Opiates: |
| linear and cyclic peptides | Ouabain | Deltophorin II DPDPE (synthetic) |
| Antihistamines: | ||
| Fexofenadine | ||