Tucatinib Inhibits Renal Transporters OCT2 and MATE Without Impacting Renal Function in Healthy Subjects.
Topletz-Erickson AR, Lee AJ, Mayor JG, Rustia EL, Abdulrasool LI, Wise AL, Dailey B, DeChenne S, Walker LN, Alley SC, Endres CJ.
Topletz-Erickson AR, et al.
J Clin Pharmacol. 2021 Apr;61(4):461-471. doi: 10.1002/jcph.1750. Epub 2020 Sep 28.
J Clin Pharmacol. 2021.
PMID: 32989831
Free PMC article.
Clinical Trial.
In vitro, tucatinib inhibited OCT2-, MATE1-, and MATE2-K-mediated transport of metformin, with IC(50) values of 14.7, 0.340, and 0.135 M, respectively. ...Renal function was assessed by measuring glomerular filtration rate (GFR; based on iohexol plasma clearance) and endog …
In vitro, tucatinib inhibited OCT2-, MATE1-, and MATE2-K-mediated transport of metformin, with IC(50) values of 14.7, 0.340, and 0.13 …