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SOME ABC DRUG TRANSPORTERS

Compiled By Jessica Oesterheld, M.D.

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 GeneMedRx. This metabolism-based drug interaction software predicts response to medication combinations with optional input of genetic variations.

Last Update: May 22, 2009
Click here for a print version

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

 

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