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Renal tubular transporters are membrane proteins expressed predominantly in the epithelial cells of the renal proximal tubules. They play a critical role in the secretion and reabsorption of drugs, endogenous compounds, and toxins during renal elimination. These transporters mediate active uptake or efflux of substances across basolateral (blood-facing) and apical (urine-facing) membranes, thus influencing drug pharmacokinetics, efficacy, toxicity, and potential for drug–drug interactions. Inhibition of these transporters can alter drug uptake and excretion, leading to changes in plasma concentrations and potential adverse effects.
Inhibition reduces drug clearance; alters plasma concentration
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