Tucatinib Inhibits Renal Transporters OCT2 and MATE Without Impacting Renal Function in Healthy Subjects

• Published in: Journal of clinical pharmacology Vol. 61; no. 4; pp. 461 - 471
• Main Authors: Topletz‐Erickson, Ariel R., Lee, Anthony J., Mayor, JoAl G., Rustia, Evelyn L., Abdulrasool, Layth I., Wise, Amanda L., Dailey, Ben, DeChenne, Sharon, Walker, Luke N., Alley, Stephen C., Endres, Christopher J.
• Format: Journal Article
• Language: English
• Published: England 01.04.2021
• Subjects: Adolescent; Adult; Aged; Animals; Antineoplastic Agents - pharmacology; Biological Transport - drug effects; Creatinine - blood; Cross-Over Studies; Dogs; Female; Glomerular Filtration Rate; Healthy Volunteers; HEK293 Cells; Humans; Inhibitory Concentration 50; Madin Darby Canine Kidney Cells; Male; MATE; metformin; Metformin - pharmacokinetics; Middle Aged; OCT2; Organic Cation Transport Proteins - antagonists & inhibitors; Organic Cation Transporter 2 - antagonists & inhibitors; Oxazoles - pharmacology; pharmacokinetics; Pyridines - pharmacology; Quinazolines - pharmacology; Receptor, ErbB-2 - antagonists & inhibitors; renal function; tucatinib; Young Adult; pharmacokinetics; metformin; renal function; tucatinib; MATE; OCT2

Tucatinib is a potent tyrosine kinase inhibitor selective for human epidermal growth factor receptor 2 (HER2) approved by the US Food and Drug Administration for the treatment of HER2‐positive metastatic breast cancer and in development for other HER2‐positive solid tumors. Modest, reversible serum...