Some ABC Drug Transporters

This table is an abridged guide to ABC drug transporters. To appreciate the full benefits of this information, click here to get a free 30-day trial version of YouScript^®. This metabolism-based drug interaction software predicts response to medication combinations with optional input of genetic variations.

Name (Genetics) (Regulation)	Site	Substrates			Inhibitors		Inducers
ABCB1** (P-gp) Tubular Secretion Kidney PXR (pregnane x receptor), CAR (constitutive androstane receptor) C3435T is part of a haplotype involving two polymorphisms C1236T & G2677T- results in increased absorption and decreased excretion of digoxin and fexofenadine.	Apical I, l,K,BBB,P, stem cells Neutral and positively charged hydrophobic	Broad specificity			Cyclosporine Erythromycin Ketoconazole	Quinidine	Rifampin St Johns wort
ABCB4 (MDR3)	L,Apical	Digoxin 16763017 Paclitaxol 16763017 Vinblastine 16763017			Cyclosporine 16763017 Glyburide Funk 2008 Nefazodone Funk 2008	Verapamil 16763017 Vinblastine 16763017
ABCB11 (BSEP) induced by FXR 18433342	L, Apical	Paclitaxel 17323126 Pravastatin 1843334 (not other statins) 18433342 Sulindac 18433342 Vinblastine 18433342			Bosentan 16763017 Cyclosporine 16763017 Glibenclamide 12404239* Rifampin 16763017	Tamoxifen Wang Er-Jia* Troglitazone 16763017 Valinomycin Wang Er-Jui*
ABCC1** (MRP1, ABC29,GS-X) Active reabsorption Kidney, gateway to the stroke brain 18796513	WS, BL, not adult liver But Apical in choroid plexus epithelial cells organic anions hydrophilic	Adefovir CDER Berberine 18691054 Ciprofloxacin 18691054 Cloroquine 18691054 Colchicine ABC website CPT-11 17979652 Cyclophospamide GSH 18691054 Daunorubicin 18433342 Doxorubicin 17979652	Epirubicin 17979652 Etoposide 17979652 Flutamide 18691054 Grepafloxacin 18691054 Idarubicin 18691054 Indinavir 18691054 Irinotecan 18691054 Methotrexate 18691054	Mitoxantrone 17979652 Nelfinavir 18691054 Paclitaxel 18691054 *Glutathione conjugates 17979652 Ritonavir 18691054 Saquinavir 18691054 Vinblastine 17979652 Vincristine 17979652 SN-38 17979652	Benzbromarone 18691054 Cediranib 19255759 Cyclosporine 16364611 Disulfarim 18691054 Glyburide 18691054 Indomethacin 16364611 Lamivudine 18691054 Probenecid 18691054 Ritonavir 18691054	Sulfinpyrazone 16364611 Verapamil 18691054 Zidovudine 18691054 Zosuquidar 18691054	Epirubicin
ABCC2 (MRP2, cMOAT) (cMRP) Canalicular multispecific organic anion transporter PXR,CAR, FXR 18417112 Genetics Dubin-Johnson (increased bilirubin glucuronides) Non-alcholholic fatty liver disease 18926681 Irinotecan levels	Apical, I,L,K transports Phase 2 conjugates and co-transports with Glutathione same distribution in gut Anions with 1 or more neg charges 17722645 FXR, PXR, CAR 17722645	Adefovir 16863439 Ampicillin 16863439 Azithromycin 18624680 Beta-lactam antibiotics Bilirubin glucuronide 18624680 Ceftriaxone 16863439 Cerivistatin FDA Workshop 2008 Cidofovir 16863439 Cisplatin 17979652 CPT-11 17979652 Cyclosporine 18417112 Doxorubicin 1797965 Epirubicin 17979652	Etoposide 17979652 Glibenclamide 18433342 Grepafloxacin 18200507 Indinavir 18417112 Irinotecan 18433342 Lopinavir 18691054 Methotrexate 17979652 Mitoxatrone 16863439 Nelfinavir 16863439 Olmesartan 18691054 Pennicillin G 16863439 Pravastatin 18433342	Probenecid 17722645 Ritonavir 18417112 Saquinavir 18417112 SN-38 17979652 Sulfinpyrazone 17979652 Telmisartan 18838068 Valsartan FDA Workshop Vinblastine 17979652 Vincristine 17979652	Bosanten 18417112 Celecoxib 18417112 Cyclosporine 16316932 Daunorubicin 15822193 Etodolac 18417112 Etoposide 15822193 Furosemide 16364611	Glyburide 18417112 Grapefruit juice 16863439 Ibuprofen 18417112 ?Indomethacin 18417112 16863439 Ketoprofen 18417112 Naproxen 18417112 Orange Juice 16863439 Probenecid 18087819 Progestins 16863439 Sulindac 18417112 Tolmetin 18417112	Benzbromarone 18845662 CBZ 17112801 Clotrimazole 17722645 Diclofenac 18845662 Glucocorticoids 15795103 Phenobarbital 17722645 Rifampin 17722645
ABCC3 (MRP3, MOAT-D, cMOAT-2) Active reabsorb Kidney CAR, PXR 18433342	Basolateral I,L,K Hydrophilic organic anions	Acetaminophen glucuronide 18691054 Etoposide 18691054 Methotrexate 18433342	Tenosposide 18691054 Vincristine 16364611		Etoposide 18691054 Methotrexate 18691054
ABCC4 (MRP4, MOAT-B) Tubular Secretion Kidney Polymorphisms	Apical I, BBB, K choroid plexus, L, BL organic anions hydrophilic	(Adefovir) 18691054 Bumetanide 18417112 Ceftizoxime 18353444 Cefazolin 18353444 Cefotaxime 18353444 Ceftizoxime 19252335 Cidofovir 18417112 DHEAS 18417112 Folinic acid 18353444 Furosemide 17135398	Ganciclovir 18691054 Hydrochlorothiazide 17135398 Imatanib 18483382 Irinotecan 18417112 Lamivudine 17979652 Mercaptopurine 18691054	Methotrexate 17979652 Olmesartan 18353444 (Tenofovir) 18691054 Thioguanine 18691054 Topotecan 17979652 Zalcitabine 18417112 Zidovudine 18691054	Aspirin 18417112 Celecoxib 18353444 Diclofenac 18691054 Dipyridamole 16364611 Etodolac 18417112 Ibuprofen 18417112 Indomethacin 18353444 Ketoprofen 18417112 Losartan 18353444 Methotrexate 18691054	Naproxen 18417112 Piroxicam 18417112 Probenecid 16364611 Rofecoxib 18691054 Sildenafil 18353444 Sulfinpyrazone 18691054 Sulindac 18353444 Verapamil 18417112
ABCC5 (MRP5, MOAT-C, p ABC11)	Skeletonal muscle, CV Both Apical and BL BBB organic anions hydrophilic	Mercaptopruine 17979652 Methotrexate 18691054 Stavudine 18691054	Thioguanine 17979652		Benzbromarone 18691054 Probenecid 16364611 Sildenafil 16364611	Sulfinpyrazone 16364611
ABCC6 (MRP6, MOAT-E, MLP-1. ARA)	BL, L, K organic anions hydrophilic	Actinomycin-D 18691054 Cisplatin 18691054 Daunorubicin 18691054 Doxorubicin 18691054 Etoposide 18691054	Mercaptopurine 16364611 Mitoxantrone 18417112 Teniposide 18691054		Benzbromarone 18691054 Indomethacin 18691054 Probenecid 18691054		Retinoids 17045963
ABCG2 ** (BCRP, MXR, White 2, ABC15,BMDP, ABCP) mitoxantrone-resistance protein Placenta-specific ABC protein Major Factor active secretion in breast ABCG2 34G>A and 421C>A SNPs may be linked to higher intestinal drug absorption, whereas 616C>A may be associated with lower drug absorption. in vitro, higher expression in men 18433342 PXR, CAR	Apical, esp duodenum, jejunum, L, K proximal tubule, Breast, stem cells BL in P-> towards maternal side,BBB, Hydrophilic and Hydrophobicanions CAR, PXR 17722645	Acyclovir AAPS workshop Actinomycin D 18624680 Atorvastatin FDA workshop 2008 Camptotecan AAPS Workshop Ciprofloxacin and other quinolones 18200507 Cimetidine 18433342 Diclofenac 18845662 Dipyridamole 16247709 Daunorubicin 17979652, 18433342 Dehydroepiandrosterone-sulfate 16146333 Doxorubicin 17979652 Enrofloxacin 18200507 Epirubicin 17979652 Erlotinib 18309947 17b-estradiol 18624680 Estrone 18624680 Etoposide 17979652 Flavopiridol 17323126	Fluorouracil 17979652 Gefitinib 17979652 Genistein 18624680 Glyburide 18079276 Imatanib 18483382 Irinotecan 17979652, 18433342 Lamivudine 17979652 Lapatinib 18216274 Methotrexate 17979652 Mitoxantrone 17979652 Nitrofurantoin 18433342 Ofloxacin AAPS workshop Norfloxacin AAPS workshop Pantoprazole 16146333	Pitavastatin 17722645, 18433342 Pravastatin FDA Workshop 2008 Prazosin 17722645 Progesterone 18624680 Riluzole 91469241 Rosuvastatin 18433342 Sulfasalazine CDER, FDA Workshop 2008 SN-38 17979652 Tamoxifen 18624680 Testosterone 18624680 Topotecan 17979652, 18433342 Troglitazone sulfate 18433342 Rosuvastatin CDER Zidovudine 17979652	Chlorpromazine 18834354 Clozapine 18834354 Cyclosporine 16404634 Diethylstilbestrol 16146333 Dipyridamole 16247709 Eroltanib FDA Workshop Gefitinib 16146333 Imatinib 16146333 Itraconazole 17518356 Ketoconazole 17518356 Lapatanib 18216274 Nelfinavir 16146333, 18433342 Nicardipine 15908473 Nitrendipine 15908473 Nitrofurdantoin FDA workshop	Omeprazole 16146333 Paliperidone 18834354 Prazosin Quetiapine 18834354 Reserpine 16146333 Risperidone 18834354 Ritonavir 16146333 Saquinavir 16146333, 18433342 Tacrolimus 16404634 Tamoxifen 16146333	CBZ 17112801 Rifampin 17722645
*Multidrug resistance in Cancer drugs I=Intestine L=liver K=Kidney BBB= Blood Brain Barrier WS= Widespread P=Placenta B=Breast PMID number to look up in PubMed CDER= FDA web site probe or inhibitor or inducer A= apical BL= basolateral