PK Transporters

ASBT

Apical-Sodium-dependent Bile acid Transporter

Apical Membrane Absorptive Transporter (from intestinal lumen (gut) into enterocytes)

Substrates are Bile Acids

PEPT1

Oligopeptide Transporter 1

Apical Membrane Absorptive Transporter (from intestinal lumen (gut) into enterocytes)

Di-peptides or tri-peptides

Proton coupled (so activity impacted by pH)

Apical Membrane Efflux Transporters (Intestine)

Enterocyte back in gut (intestinal lumen)

MDR1 (Multidrug Resistance Protein 1) AKA Pgp (P-glycoprotein).

MRP2 (Multidrug Resistance Protein 2)

BCRP (Breast Cancer Resistance Protein)

Apical Membrane Influx Transporters (Intestine)

Gut (intestinal lumen) into enterocyte

ASBT (bile acids) and PEPT1 (tripeptides)

Sinusoidal Influx Transporters (Liver)

Blood into liver cells

NTCP: bile acids and statins

OATP: bile acids, bilirubin, statins, anions, ACE inhibitors and HIV protease inhibitors

MCT2: small CAs

OAT2: p-aminohippuric acid. Inhibited by probenecid

OCT1: metformin and cimetidine

Canalicular Efflux Transporters (Liver)

Liver cell into bile

MDR1 (Pgp): digoxin, verapamil, quinidine, cyclosporine

MRP2: conjugates (glutathione, sulfates, glucuronide)

BCRP: sulfate conjugates and anti-cancer drugs (topotecan, mitoxantrone)

BSEP: bile acids and statins. Effluxes the things brought in by NTCP

MATE: cimetidine, metformin. Effluxes the things brought in by OCT1