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- Please note
- The information presented here is NOT A COMPLETE LIST of OATP inducers, inhibitors, and substrates
- Not all drug interactions are clinically significant. Potential drug interactions should be researched, and medication changes should only be made after consulting a health professional.
- ACRONYMS AND DEFINITIONS
- CYP - Cytochrome P450
- OATP - Organic anion transporting polypeptide
- Substrate - a drug that is metabolized by a certain enzyme is a substrate of that enzyme
- ORGANIC ANION TRANSPORTING POLYPEPTIDE (OATP)
- Overview
- OATP is sometimes referred to by its gene name, "SLCO - 1A2, 1B1, 1B3, ..."
- OATP is a family of transport molecules located in cell membranes (not to be confused with OAT1, OAT2, OAT3, etc. which are another family of transporters)
- OATP molecules transport drugs from the bloodstream into cells (influx) so that they can be metabolized. OATP molecules transport drugs that have a negative charge (anions).
- Currently, eleven different OATPs have been discovered
- Two of the polypeptides (OATP1B1, OATP1B3) have been studied extensively, and two (OATP2B1, OATP1A2) have very limited data. The other polypeptides are not well characterized.
- 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 - increase the activity of OATP (no OATP inducers have been discovered)
- Inhibitors - block the action of OATP
- When OATP inhibitors are taken with other medications that are transported by OATP, they can alter the elimination of that medication
- Drugs may be transported by OATP and also inhibit it at the same time
- Competitive inhibition
- If two drugs are transported by OATP, they may "compete" for it, and this can alter the elimination of one or both of the drugs
- Compounded interactions
- When a person is taking three or more drugs, the potential for compounded interactions exists
- Example:
- Drug A is metabolized by CYP2D6, and it is transported by OATP
- Drug B inhibits CYP2D6. Drug C inhibits OATP.
- When Drug A is taken with Drug B, its elimination is partially decreased, but it is not significant
- When Drug A is taken with Drug B and Drug C, its elimination is decreased substantially and the interaction becomes significant
- Genetic factors
- OATP is coded for by a gene called SLCO
- Since individuals vary in their genetic makeup, their SLCO gene may vary also
- Some people have SLCO genes that produce OATP molecules that are less effective
- Genetic variations in the SLCO gene can affect how an individual eliminates a drug
- 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-documented while many are not
- Factors that can make drug interactions challenging
- New drugs
- When a new drug is being developed, the FDA requires that it be tested for drug interactions with a small number of medications that are known to have significant interactions
- Obviously, there is no way to test a medication in every possible drug combination that may occur. This means most drugs come to market with incomplete drug interaction profiles.
- After a medication is prescribed to a large number of people, other drug interactions are inevitably discovered
- Research
- Much of the research involving drug metabolism and drug interactions occurs in vitro meaning in a lab, or outside of the human body
- Animal models and cell cultures are often used to test drugs for metabolic pathways and interactions
- Findings from in vitro experiments do not always translate into what actually happens in the human body (in vivo)
- Evolving information
- Drug metabolism is an evolving field of medicine and pharmacology
- Researchers are just beginning to understand all the different systems that are involved in how the body metabolizes and eliminates drugs
- Cell transport systems (ex. p-glycoprotein, OAT, etc.) are a relatively new area of pharmacology and information about how these systems affect drug elimination is evolving
- 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 significant
- Always consult your physician or pharmacist before changing your medication if you are concerned about a possible drug interaction
- 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