TABLE 1

Major solute carrier (SLC) drug transporters

Only those SLC drug transporters reviewed in the text are presented.

SLC SubfamilySpeciesTransporter Gene Name
(Protein Name)
Organ with Highest ExpressionaCommon Substrateb
OATPHumanSLCO1A2 or SLCO1A3 (OATP-A or OATP1A2)BrainBromsulfthalein (BSP), methotrexate, enalapril, levofloxacin
SLCO1B1 (OATP1B1)LiverCobimetinib, lovastatin, clotrimazole, valsartan, cyclosporine, rifampicin
SLCO1B3 (OATP1B3)LiverRifampicin, olmesartan, methotrexate, digoxin, pioglitazone
SLCO1B3-SLCO1B7 or LST-3TM12 (OATP1B3-1B7)Liver, breastTaurocholic acid, lithocholic acid, ezetimibe
SLCO2A1 (OATP2A1)LungAlprostadil, latanoprost, iloprost
SLCO2B1 (OATP2B1)LiverAzilsartan, balsalazide, gavestinel, valsartan
SLCO3A1 (OATP3A1)BrainBenzylpenicillin, safinamide, iloprost
SLCO4A1 (OATP4A1)LungLiothyronine, levothyroxine, benzylpenicillin
SLCO4C1 (OATP4C1)KidneyLiothyronine, digoxin, saxagliptin, ouabain
RodentSlco1a1 (Oatp1a1 or Oatp1)Liver, kidneyEstradiol 17beta-d-glucuronide
Slco1a4 (Oatp1a4 or Oatp2)Brain, liver, kidneySulforhodamine-101 (SR-101)
Slco1a5 (Oatp1a5)KidneyFexofenadine, celiprolol
Slco1a6 (Oatp1a6)KidneyTaurocholic acid (TCA)
Slco1b2 (Oatp1b2)LiverPitavastatin
Slc16a2 (Oatp1c1)Liver, kidneySulforhodamine-101 (SR-101), thyroxine (T4)
Slco2a1 (Oatp2a1)Lung, liverPhenolsulfonphthalein
Slco2b1 (Oatp2b1)UbiquitousFexofenadine rosuvastatin
Slco3a1 (Oatp3a1)BrainSodium fluorescein
Slco4c1 (Oatp4c1)Kidney, lungDigoxin
OATHumanSLC22A6 (OAT1)KidneyCimetidine, methotrexate, indomethacin, probenecid, oxytetracycline, hydrochlorothiazide
SLC22A7 (OAT2)LiverOxytetracycline, cimetidine, methotrexate, salicylic acid
SLC22A8 (OAT3)KidneyTaurocholic acid, benzylpenicillin, cimetidine, tetracycline
SLC22A11 (OAT4)KidneyOxytetracycline, aminohippuric acid, methotrexate, relebactam
SLC22A10 (OAT5)LiverNone reported
SLC22A9 (OAT7)LiverEstrone sulfate, dehydroepiandrosterone, butyrate
SLC22A12 (URAT1)KidneyUrate
RodentSlc22a6 (Oat1)KidneySame as SLC22A6
Slc22a7 (Oat2)Liver, kidneySame as SLC22A7
Slc22a8 (Oat3)KidneySame as SLC22A8
Slc22a12 (Urat1)KidneyUrate
OCTHumanSLC22A1 (OCT1)LiverMetformin, levofloxacin, cimetidine, codeine
SLC22A2 (OCT2)KidneyMetformin, cimetidine, cisplatin, quinidine
SLC22A3 (OCT3)Skeletal muscleMetformin, cimetidine, oxaliplatin
RodentSlc22a1 (Oct1)Liver, kidney, intestineSame as SLC22A1
Slc22a2 (Oct2)KidneySame as SLC22A2
OCTNHumanSLC22A5 (OCTN2)Skeletal muscle, kidney, heart, placentaAmphetamine, nicotine, formoterol, colistin, oxaliplatin
RodentSlc22a5 (Octn2)Kidney, liver, testisSame as SLC22A5
LOC303140 (Octn3)TestesAcetylcarnitine
PEPTHumanSLC15A1 (PEPT1)IntestineCephalexin, enalapril, benzylpenicillin
RodentSlc15a1 (Pept1)IntestineSame as SLC15A1
MATEHumanSLC47A1 (MATE1)Adrenal glandMetformin, levofloxacin, cimetidine, cisplatin
SLC47A2 (MATE2 or MATE2-K)KidneyMetformin, cimetidine, cisplatin, quinidine
RodentSlc47a1 (Mate1)Kidney, liverSame as SLC47A1
Slc47a2 (Mate2)TestisSame as SLC47A2
  • aThe information is extracted from the Human Protein Atlas (https://www.proteinatlas.org/) and UniProt (https://www.uniprot.org/).

  • bOnly selected compounds are presented; please refer to the literatures for a more comprehensive list of the substrates (Roth et al., 2012; César-Razquin et al., 2015; Lin et al., 2015; Bhutia et al., 2016; Murray and Zhou, 2017; Rives et al., 2017; Nigam, 2018; Schlessinger et al., 2018; Liu, 2019; Ayka and Şehirli, 2020; Bednarczyk and Sanghvi, 2020; Huang et al., 2020; Koepsell, 2020; Pácha et al., 2021; Pizzagalli et al., 2021; Yang and Shu, 2021).