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- ACRONYMS AND DEFINITIONS
- CYP - Cytochrome P450
- OATP - Organic anion transporting polypeptide
- ORGANIC ANION TRANSPORTING POLYPEPTIDE (OATP)
- Overview
- Organic anion transporting polypeptide (OATP), sometimes referred to by its gene name SLCO1A2, SLCO1B1, SLCO1B3, etc., is a family of transport molecules located in cell membranes that transport negatively-charged drugs (anions) from the blood into cells (influx) to be metabolized. Currently, eleven different OATPs have been discovered. OATP1B1 and OATP1B3 are the most studied, while OATP2B1 and OATP1A2 have limited data. The remaining polypeptides are not well characterized.
- OATP should not be confused with with OAT1, OAT2, OAT3, etc., which are another family of transporters
- OATPs are located in the following tissues
- OATP1B1 - liver
- OATP1B3 - liver
- OATP2B1 - liver, intestine, kidney, placenta
- OATP1A2 - brain, kidney, liver, intestine [1,2,4]
- OATP drug interactions
- Inducers and Inhibitors
- Inducers - OATP inducers increase transporter activity, decreasing exposure to substrates
- Inhibitors - OATP inhibitors block transporter activity, increasing exposure to substrates
- One drug may inhibit or induce multiple transporters and enzymes (e.g. p-glycoprotein, OATP, CYP3A4)
- Some OATP substrates also simultaneously inhibit the transporter
- Inducers and inhibitors can be subdivided into strong, moderate, or weak, depending on the degree of their effect
- Competitive inhibition
- If two drugs are transported by the same OATP, they may "compete" for the transporter, altering the metabolism of one or both of the drugs
- IMPORTANT POINTS ABOUT DRUG INTERACTIONS
- Drug interactions are challenging
- Information on drug interactions can be difficult to assimilate
- Certain drug interactions and metabolic pathways are well-defined while many are not
- Factors that can make drug interactions challenging
- New drugs
- During drug development, the FDA requires interaction testing with medications that are known to have significant effects on CYP enzymes and transporters. Obviously, there is no way to test a new drug with every medication available, meaning most drugs come to market with incomplete interaction profiles. After the medication is prescribed to a large number of people, other drug interactions are inevitably discovered.
- Research
- Drug research often occurs in a laboratory setting (in vitro) with animals and cell cultures. Findings from these experiments do not always reflect what happens in the human body (in vivo).
- Evolving information
- Drug metabolism is an evolving field, and researchers are just beginning to understand all the different ways the body eliminates medications. Cytochrome P450 enzymes have been studied for a while, but cell transport systems (e.g. p-glycoprotein, OAT) are a relatively new area of pharmacology, and their role in drug elimination has not been completely elucidated.
- Important points
- Not all drug interactions are known or can be predicted
- Good information on possible drug interactions may not be available
- Not all drug interactions are clinically significant, and patients should consult their healthcare provider if they are concerned about a possible interaction
- Drug interaction checkers provide the most efficient and practical way to check for interactions among multiple medications. A free interaction checker is available from Drugs.com (see Drugs.com interactions checker).
- OATP INDUCERS
- No OATP Inducers have been discovered
- OATP INHIBITORS
- OATP inhibitors
- Atazanavir (Reyataz®) - OATP1B1, OATP1B3 [4]
- Clarithromycin (Biaxin®) - OATP1B1, OATP1B3 [1,2]
- Cobicistat (part of Stribild®) - OATP1B1, OATP1B3 [3]
- Cyclosporine (Neoral®, Gengraf®, Sandimmune®) - OATP1B1, OATP1B3 [1,4]
- Daclatasvir (Daklinza™) - OATP1B1, OATP1B3 [3]
- Eltrombopag (Promacta®) - OATP1B1 [4]
- Erythromycin (E-mycin®) - OATP1B1, OATP1B3 [1,2]
- Gemfibrozil (Lopid®) - OATP1B1 [1,4]
- Glecaprevir (Mavyret™) OATP1B1, OATP1B3 [3]
- Ibrexafungerp (Brexafemme®) - OATP1B1, OATP1B3 (in vitro) [3]
- Lopinavir/Ritonavir (Kaletra®) - OATP1B1, OATP1B3 [4]
- Letermovir (Prevymis®) - OATP1B1, OATP1B3 [3]
- Paritaprevir (Viekira Pak™, Technivie™) - OATP1B1, OATP1B3 [3]
- Pibrentasvir (Mavyret™) OATP1B1, OATP1B3 [3]
- Ritonavir/Lopinavir (Kaletra®) - OATP1B1, OATP1B3 [4]
- Sacubitril (Entresto®) - OATP1B1, OATP1B3 (in vitro) [3]
- Saquinavir (Invirase®) - OATP1B1, OATP1B3 [4]
- Simeprevir (Olysio®) - OATP1B1, OATP1B3 [3]
- Telithromycin (Ketek®) - OATP1B1, OATP1B3 [1,2]
- Teriflunomide (Aubagio®) - OATP1B1, OATP1B3 [3]
- Tipranavir (Aptivus®) - OATP1B1 [4]
- Rifampin - OATP1B1, OATP1B3 [1,4]
- Velpatasvir (Epclusa®, Vosevi™) - OATP1B1, OATP1B3, OATP2B1 [3]
- Voclosporin (Lupkynis®) - OATP1B1, OATP1B3 (in vitro) [3]
- Voxilaprevir (Vosevi™) - OATP1B1, OATP1B3 [3]
- OATP SUBSTRATES (DRUGS TRANSPORTED BY OATP)
- OATP substrates
- Atogepant (Qulipta®) - OATP1B1, OATP1B3 [3]
- Atorvastatin (Lipitor®) - OATP1B1, OATP1B3 [3,4]
- Bilirubin - OATP1B1, OATP1B3 [5]
- Bosentan (Tracleer®) - OATP1B1 [4]
- Digoxin (Lanoxin®) - OATP1B3 [4]
- Empagliflozin (Jardiance®) - OATP1B1, OATP1B3 [3]
- Ezetimibe (Zetia®) - OATP1B1 [4]
- Fexofenadine (Allegra®) - OATP1B1, OATP1B3, OATP1A2, OATP2B1 [1,2]
- Fluvastatin (Lescol®) - OATP1B1 [4]
- Glyburide (DiaBeta®) - OATP1B1 [4]
- Glecaprevir (Mavyret™) OATP1B1, OATP1B3 [3]
- Grazoprevir (Zepatier®) - OATP1B1, OATP1B3 [3]
- Irinotecan (Camptosar®) - OATP1B1 [4]
- Letermovir (Prevymis®) - OATP1B1, OATP1B3 [3]
- Lovastatin (Mevacor®) - OATP1B1 [1,2]
- Methotrexate (Rheumatrex®) - OATP1B1, OATP1B3 [4]
- Olmesartan (Benicar®) - OATP1B1, OATP1B3 [4]
- Paritaprevir (Viekira Pak™, Technivie™) - OATP1B1, OATP1B3 [3]
- Pitavastatin (Livalo®) - OATP1B1, OATP1B3 [4]
- Pravastatin (Pravachol®) - OATP1B1, OATP2B1 [4]
- Repaglinide (Prandin®) - OATP1B1 [3,4]
- Rifampin - OATP1B1, OATP1B3 - [4]
- Rifaximin (Xifaxan®) - OATP1A2, OATP1B1, OATP1B3 [3]
- Revefenacin (Yupelri®) - OATP1B1, OATP1B3 [3]
- Rosuvastatin (Crestor®) - OATP1B1, OATP1B3 [4]
- Simvastatin (Zocor®, Zetia®) - OATP1B1 [3,4]
- Thyroxine (Synthroid®, Levoxyl®) - OATP1B1 [4]
- Telmisartan (Micardis®) - OATP1B3 [4]
- Valsartan (Diovan®) - OATP1B1, OATP1B3 [3,4]
- Velpatasvir (Epclusa®, Vosevi™) - OATP1B1, OATP1B3 [3]
- Voxilaprevir (Vosevi™) - OATP1B1, OATP1B3 [3]
- BIBLIOGRAPHY
- 1 - PMID 19785645
- 2 - PMID 21103967
- 3 - Manufacturer's Package Insert
- 4 - FDA drug development and drug interactions - CLICK HERE
- 5 - 23886114