Title : Inhibitory effects of vandetanib on creatinine transport via renal organic cation transporter OCT2.

Pub. Date : 2021 Mar 1

PMID : 33296710






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1 European Journal of Pharmaceutical Sciences: PHASCI-D-20-01517R2Inhibitory effects of vandetanib on creatinine transport via renal organic cation transporter OCT2. vandetanib solute carrier family 22 member 2 Homo sapiens
2 We examined the interaction of vandetanib with the human organic cation transporter 2 (hOCT2) stably expressed in human embryonic kidney (HEK) 293 cells. vandetanib solute carrier family 22 member 2 Homo sapiens
3 We examined the interaction of vandetanib with the human organic cation transporter 2 (hOCT2) stably expressed in human embryonic kidney (HEK) 293 cells. vandetanib solute carrier family 22 member 2 Homo sapiens
4 Vandetanib inhibited the uptake of creatinine mediated by hOCT2 in a dose-dependent manner. vandetanib solute carrier family 22 member 2 Homo sapiens
5 The IC50 value for vandetanib inhibition of creatinine uptake by hOCT2 was 3.7 +- 1.0 muM (average +- SE of three separate experiments). vandetanib solute carrier family 22 member 2 Homo sapiens
6 Vandetanib showed markedly higher affinity for hOCT2 than cimetidine and trimethoprim. vandetanib solute carrier family 22 member 2 Homo sapiens
7 These results suggest that hOCT2 may play a crucial role in elevating the serum creatinine levels, as well as increasing the risk of renal impairment during vandetanib administration. vandetanib solute carrier family 22 member 2 Homo sapiens