Renal Barrier
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SOLVO’s Renal Barrier package consists of in vitro tools to study transporter-mediated drug elimination through the kidney.
Renal proximal and distal tubules carry out specialized directional transport of various solutes.Transporters in the kidney mediate the secretion or reabsorption of many compounds and thereby influence the plasma levels of their substrates. A wide range of efflux and uptake transporters are expressed in the renal epithelial cells to regulate the excretion and the reabsorption of endogenous and exogenous organic anions, cations, peptides and nucleosides that include various kinds of drugs and their metabolites.
P-gp, BCRP, MRP2 and MRP4 primarily localize to the apical (luminal) membrane of renal epithelial cells, while MRP1, MRP3 and MRP6 have been shown to be expressed on the basolateral membrane.
Members of the OATP, OCT, OAT, ENT, and OST transporter families have been identified in the basolateral membrane of proximal tubule cells. Numerous uptake transporters including peptide transporters are present on the luminal membrane of proximal tubule cells and were shown to be responsible for the tubular re-absorption of peptide-like drugs such as beta-lactam antibiotics across the brush-border membranes. The reabsorbtion process results in lower renal clearance than expected based on glomerular filtration. Furthermore, the uptake process might result in increased concentration of drugs in the cytoplasm of proximal tubular cells leading to toxic effects in the kidney. Screening the interaction of test drugs with ABC efflux and uptake transporters is an excellent way to predict active transport involved in their renal elimination.
Transporters in the Human Renal Barrier
Localization of efflux and uptake transporters in the kidney proximal tubules
Transporters in the Rodent Renal Barrier
Screening strategy
- Specific transporter interactions can be characterized with ABC efflux and uptake transporter assays that might shed light on the pharmacokinetics of the test compound in the kidney proximal tubules.
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