What is it about?

Thein vitrometabolic stability and transport mechanism of TM-25659, a novel TAZmodulator, was investigated in human hepatocytes and human liver microsomes (HLMs) based onthe preferred hepatobiliary elimination in rats. In addition, thein vitrotransport mechanism andtransporter-mediated drug–drug interactions were evaluated using oocytes and MDCKII cellsoverexpressing clinically important drug transporters.

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Why is it important?

OATP1B1, OATP1B3, P-gp and MRP2 might be major transporters responsible for the pharmacokineticsand drug–drug interaction of TM-25659, although their contribution toin vivopharmacokinetics needsto be further investigated

Perspectives

understandingthe drug uptake and efflux transporters as well asdrug metabolizing enzymes that are responsiblefor the pharmacokinetics and drug response arecritical for new drug development.

Professor Im-Sook Song
Kyungpook National University

Read the Original

This page is a summary of: Transport characteristics and transporter-based drug-drug interactions of TM-25659, a novel TAZ modulator, Biopharmaceutics & Drug Disposition, December 2013, Wiley,
DOI: 10.1002/bdd.1883.
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