Clinically Relevant Transporter DDIs
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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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