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Drug uptake transporter

Gene  name Protein  name Expression / Localization Substrates endogenous Substrates exogenous
SLC10A1 NTCP liver, pancreas bile acid, ES, DHEA-S BSP
SLC10A2 ASBT kidney, ileum, bile, small intestine bile acids, taurocholate dimeric bile acid analogues, benzothiazepine derivates
SLC10A6 SOAT1 testis, placenta, pancreas, heart, lung, liver, spleen, small intestine, colon ES, DHEA­-S, PREG-S,
bile acid sulfate
SLC13A3 NaDC-3 kidney, liver, pancreas, brain, placenta succinate, citrate,
SLC15A1 PEPT1 intestine, kidney di-, and tripeptids cefadroxil, amoxicillin, enalapril
SLC15A2 PEPT2 Kidney, lung, brain,
bronchial epithelium
di-, and tripeptids cefadroxil, amoxicillin, fosinopril
SLC22A1 OCT1 liver, kidney organic cations acyclovir, amantadine,
desipramine, ganciclovir, metformin
SLC22A2 OCT2 kidney, brain organic cations amantadine, cimetidine, memantine
SLC22A3 OCT3 kidney, liver, skeletal muscle, placenta, heart, lung, brain organic cations cimetidine
SLC22A4 OCTN1 kidney, skeletal muscle, placenta, prostata organic cations ergothioneine
SLC22A5 OCTN2 skeletal muscle, kidney, heart, brain organic cations L-carnitin
SLC22A6 OAT1 kidney, placenta, brain organic anions penicillin, torasemid, acyclovir, methotrexate, zidovudine, PAH
SLC22A7 OAT2 liver, kidney


bumetanide, cyclothiazide, methotrexate, diclofenac, indomethacin, mefenamate
SLC22A8 OAT3 kidney, liver, brain, skeletal muscle, developing bone organic anions, ES,
cimetidine, methotrexate, zidovudine, PAH
SLC22A11 OAT4 kidney,  placenta organic anions, ES,
SLC47A1 MATE1 liver, kidney organic cations TEA, MPP, metformin
SLC47A2 MATE2-K kidney organic cations TEA, MPP, metformin
SLCO1A2 OATP1A2 brain, kidney, liver ES,
fexofenadine, oubain, tauroursodeoxycholate
SLCO2A1 OATP2A1 ubiquitous prostaglandin prostaglandin-E2
SLCO1B1 OATP1B1 liver bile salts, taurocholate, ES BSP, benzylpenicillin, pravastatin, rosuvastatin, rifampicin, methotrexate
SLCO1B3 OATP1B3 liver bile salts, taurocholate BSP, fluvastatin, pravastatin, pitavastatin, methotrexan
SLCO2B1 OATP2B1 liver, kidney, intestine,
brain, placenta, heart
pravastatin, fexofenadine, atorvastine

BSP = sulfobromophthalein
DHEA-S = dehydroepiandrosterone-sulfate
MPP = 1-methyl-4-phenylpyridinium
PAH = para-aminohippuric acid
PREG-S = pregnenolone sulfate
TEA = tetraethylammonium



New validated products:

  • MRP2
  • roct1


2nd German Pharm-Tox Summit
Heidelberg, Germany
March 06-09, 2017

19th Barrier- and

Bad Herrenalb, Germany
May 15-17, 2017

14th European ISSX Meeting
Köln, Germany

June 26- 29, 2017

2nd Symposium on Transporters in Drug Discovery
London, UK
May 15-16, 2017

Münster Transporttage 2017
Münster, Germany
October 21 – 22, 2017


Guidance for Industry (FDA and EMA)