Design, synthesis and biological evaluation of deuterated nintedanib for improving pharmacokinetic properties

9Citations
Citations of this article
29Readers
Mendeley users who have this article in their library.

This article is free to access.

Abstract

Nintedanib is a novel triple angiokinase inhibitor that inhibits three growth factors simultaneously. Deuterated derivatives of nintedanib at certain metabolically active sites were prepared and evaluated in vitro and in vivo. In particular, deuterated compound SKLB-C2202 had significantly improved pharmacokinetic properties compared with nintedanib. These efforts lay the foundation for further investigating the druggability of SKLB-C2202. Deuterated derivatives of nintedanib at certain metabolically active sites were prepared and evaluated in vitro and in vivo. Deuterated compound SKLB-C2202 had significantly improved pharmacokinetic properties compared with nintedanib. Further research is underway.

Cite

CITATION STYLE

APA

Xu, R., Zhan, M., Peng, L., Pang, X., Yang, J., Zhang, T., … Chen, Y. (2015). Design, synthesis and biological evaluation of deuterated nintedanib for improving pharmacokinetic properties. Journal of Labelled Compounds and Radiopharmaceuticals, 58(7), 308–312. https://doi.org/10.1002/jlcr.3299

Register to see more suggestions

Mendeley helps you to discover research relevant for your work.

Already have an account?

Save time finding and organizing research with Mendeley

Sign up for free