Significance of OAT2 and OCT2 in creatinine clearance: Mechanistic evaluation using freshly-prepared human primary renal proximal tubule cells

Our results obtained with primary hPTCs indicate that OCT2/MATE (versus OAT2) play a major role in the active renal secretion of creatinine. Quantitative pharmacokinetic models should therefore focus on OCT2/MATE when describing serum creatinine and creatinine clearance modulation by inhibitor drugs and genotype- or disease-related activity changes. The present study highlights the utility of freshly isolated hPTCs to support solute carrier phenotyping to enable the functional assessment of renal transport mechanisms.