Clinically Relevant Transporter DDIs

The following charts show a partial list of compounds that have been implicated in transporter-based clinically relevant drug-drug interactions as either a substrate or inhibitor.


P-gp

 
Transporter Perpetrators/Inhibitors Victims/Substrates
P-gp Clarithromycin
Cyclosporine
Erythromycin
Itraconazole
Quinidine
Ritonavir
Telithromycin
Verapamil
Aliskiren
Digoxin
Docetaxel
Fexofenadine
Paclitaxel
Ritonavir
Talinolol
Vinblastine










 

BCRP

 
Transporter Perpetrators/Inhibitors Victims/Substrates
BCRP Elacridar (GF120918) Pitavastatin
Rosuvastatin
Topotecan






 

OATP1B1

 
Transporter Perpetrators/Inhibitors Victims/Substrates
OATP1B1 Atazanavir
Clarithromycin
Cyclosporine
Gemfibrozil
Glibenclamide
Lopinavir
Rifampin
Bosentan
Cerivastatin
Pravastatin
Rifampin
Rosuvastatin
Simvastatin
Valsartan








 


OATP1B3

 
Transporter Perpetrators/Inhibitors Victims/Substrates
OATP1B3 Atazanavir
Clarithromycin
Cyclosporine
Gemfibrozil
Lopinavir
Rifampin
Bosentan
Paclitaxel
Pravastatin
Rifampin
Rosuvastatin
Valsartan





 




OATP2B1

 
Transporter Perpetrators/Inhibitors Victims/Substrates
OATP2B1 Cyclosporine
Gemfibrozil
Quercetin
Grapefruit juice
Orange juice
Aliskiren
Atorvastatin
Pravastatin
Pitavastatin
Rosuvastatin





 



OATP1A2

 
Transporter Perpetrators/Inhibitors Victims/Substrates
OATP1A2 Verapamil
Naringin
Quercetin
Grapefruit juice
Orange juice
Atenolol
Celiprolol
Ciprofloxacin
Fexofenadine
Pravastatin






 


OAT1

 
Transporter Perpetrators/Inhibitors Victims/Substrates
OAT1 Indomethacin
Mycophenolate
Olmesartan
Probenecid
Adefovir
Captopril
Cidofovir
Furosemide





 


OAT3

 
Transporter Perpetrators/Inhibitors Victims/Substrates
OAT3 Gemfibrozil
Indomethacin
Mycophenolate
Olmesartan
Probenecid
Salicylate
Benzylpenicillin
Cefotiam
Furosemide
Methotrexate
Olmesartan
Pravastatin







 


OCT2

 
Transporter Perpetrators/Inhibitors Victims/Substrates
OCT2 Bisoprolol
Carvedilol
Cimetidine
Procainamide
Ranitidine
Trimethoprim
Amatadine
Cimetidine
Cisplatin
Lamivudine
Metformin
Ranitidine







 


MATE1

 
Transporter Perpetrators/Inhibitors Victims/Substrates
MATE1 Cimetidine
Pyrmethamine
Quinidine
Rapamycin
Cephalexin
Cimetidine
Metformin
Procainamide





 
 
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ABC (Efflux) Transporters
SLC (Uptake) Transporters
 
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