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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