. Author manuscript; available in PMC: 2012 Apr 13.

Published in final edited form as: Nat Rev Drug Discov. 2010 Mar;9(3):215–236. doi: 10.1038/nrd3028

Table 1.

SLC transporters of emerging clinical importance in the absorption and disposition of drugs

Transporter/ alias (Gene)	Selected substrates	Selected inhibitors	Organs/cells	Comments
OATP1B1/O ATP-C, OATP2, LST- 1 (SLCO1B1)	Bromosulphophthalein, oestrone-3-sulphate, oestradiol-17β-glucuronide, statins^, repaglinide^, valsartan, olmesartan^*, bilirubin glucuronide, bilirubin, bile acids	Saquinavir, ritonavir^, lopinavir^, rifampicin^, cyclosporine^	Hepatocytes (sinusoidal)	• Has a role in disposition and excretion • Has clinically relevant polymorphisms • Has a role in clinical drug–drug interactions
OATP1B3/O ATP-8 (SLCO1B3)	Bromosulphophthalein, cholecysto kinin 8, statins^, digoxin, fexofenadine, telmisartan glucuronide, telmisartan^, valsartan, olmesartan, oestradiol-17- β-glucuronide, bile acids	Rifampicin^, cyclosporine^, ritonavir, lopinavir^*	Hepatocytes (sinusoidal)	• Has a role in disposition and excretion
OAT1 (SLC22A6)	Para-aminohippurate, adefovir, cidofovir, zidovudine^, lamivudine^, zalcitabine^, acyclovir^, tenofovir^, ciprofloxacin^, methotrexate^*	Probenecid^*, novobiocin	Kidney proximal tubule, placenta	• Has a role in disposition and excretion Has a role in clinical drug–drug interactions
OAT3 (SLC22A8)	Oestrone-3-sulphate, non- steroidal anti-inflammatory drugs, cefaclor, ceftizoxime, furosemide^, bumetanide^	Probenecid^*, novobiocin	Kidney proximal tubule, choroid plexus, blood–brain barrier	• Has a role in disposition and excretion • Has a role in clinical drug–drug interactions
OCT2 (SLC22A2)	N-Methylpyridinium, tetraethylammonium, metformin^, pindolol, procainamide, ranitidine amantadine, amiloride, oxaliplatin, varenicline^	Cimetidine^, pilsicainide, cetirizine^, testosterone, quinidine	Kidney proximal tubule, neurons	• Has a role in disposition and excretion • Has clinically relevant genetic polymorphisms • Has a role in clinical drug–drug interactions
OATP1A2/O ATP-A (SLCO1A2)	Oestrone-3-sulphate, dehydroepiandrosterone sulphate, fexofenadine^, bile salts, methotrexate, bromosulphophthalein, ouabain, digoxin, levofloxacin, statins^	Naringin, ritonavir, lopinavir, saquinavir, rifampicin^*	Brain capillaries endothelia, cholangiocyte s, distal nephron	• Has role in disposition and excretion
OATP2B1/O ATP-B (SLCO2B1)	Oestrone-3-sulphate, bromosulphophthalein, taurocholate, ^*statins, fexofenadine, glyburide, taurocholate	Rifampicin, cyclosporine^*	Hepatocytes (sinusoidal), endothelia	• Has a role in disposition and excretion • Has a role in clinical drug–drug interactions
OCT1 (SLC22A1)	Tetraethylammonium, N- methylpyridinium, metformin^*, oxaliplatin	Quinine, quinidine, disopyramide	Hepatocytes (sinusoidal), intestinal enterocytes	• Has a role in disposition and excretion • Has clinically relevant genetic polymorphisms • Has a role in clinical drug–drug interactions
PEPT1 (SLC15A1)	Glycylsarcosine, cephalexin, cefadroxil, bestatin, valacyclovir, enalapril, aminolevulinic acid, captopril, dipeptides, tripeptides	Glycyl-proline	Intestinal enterocytes, kidney proximal tubule	• Has a role in absorption, disposition and excretion • Has a role in clinical drug–drug interactions
PEPT2 (SLC15A2)	Glycylsarcosine, cephalexin, cefadroxil, bestatin, valacyclovir, enalapril, aminolevulinic acid, captopril, dipeptides, tripeptides	Zofenopril, fosinopril	Kidney proximal tubule, choroid plexus, lung	• Has a role in excretion MATE1
(SLC47A1)	Metformin, N- methylpyridinium, tetraethylammonium	Quinidine, cimetidine, procainamide	Kidney proximal tubule, liver (canalicular membrane), skeletal muscle	• Has a role in disposition and excretion • Has a role in clinical drug–drug interactions
MATE2-K (SLC47A2)	Metformin, N- methylpyridinium, tetraethylammonium	Cimetidine, quinidine, pramipexole	Kidney proximal tubule	• Has a role in disposition and excretion

Can potentially be used for in vivo (clinical) studies.