Substrate-dependent effects of molecular-targeted anticancer agents on activity of organic anion transporting polypeptide 1B1

  • Hiroyoshi Koide, Masayuki Tsujimoto, Ai Takeuchi, Miyu Tanaka, Yoko Ikegami, Mayu Tagami, Syoko Abe, Miki Hashimoto, Tetsuya Minegaki, Kohshi Nishiguchi
  • Xenobiotica, November 2017, Taylor & Francis
  • DOI: 10.1080/00498254.2017.1393582

Substrate-dependent effects of molecular-targeted anticancer agents on activity of OATP1B1

What is it about?

We have shown that nilotinib and lenvatinib moderately and strongly inhibited OATP1B1-mediated substrate uptake, respectively. In contrast, afatinib stimulated OATP1B1-mediated uptake of FL and SN-38, ceritinib stimulated that of valsartan, and nintedanib stimulated that of FL and valsartan. In addition, the effects of afatinib, ceritinib and nintedanib on OATP1B1 activity differed markedly depending on the type of substrate. The evaluation of OATP1B1 activity using only a single probe substrate for some molecular-targeted agents may lead to a faulty understanding of their mechanisms of drug interactions.

Why is it important?

Knowledge about the substrate-dependent nature of those interactions will help researchers and clinicians to avoid making incorrect predictions about interactions with molecular-targeted drugs based on single-substrate studies.


Hiroyoshi Koide
Kyoto Yakka Daigaku

I am grateful to the collaborators who cooperated with me. We believe this article will help predict and avoid drug interaction via OATP1B1.

Read Publication

The following have contributed to this page: Hiroyoshi Koide