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Nintedanib: from discovery to the clinic.

Abstract：

:Nintedanib (BIBF1120) is a potent, oral, small-molecule tyrosine kinase inhibitor, also known as a triple angiokinase inhibitor, inhibiting three major signaling pathways involved in angiogenesis. Nintedanib targets proangiogenic and pro-fibrotic pathways mediated by the VEGFR family, the fibroblast growth factor receptor (FGFR) family, the platelet-derived growth factor receptor (PDGFR) family, as well as Src and Flt-3 kinases. The compound was identified during a lead optimization program for small-molecule inhibitors of angiogenesis and has since undergone extensive clinical investigation for the treatment of various solid tumors, and in patients with the debilitating lung disease idiopathic pulmonary fibrosis (IPF). Recent clinical evidence from phase III studies has shown that nintedanib has significant efficacy in the treatment of NSCLC, ovarian cancer, and IPF. This review article provides a comprehensive summary of the preclinical and clinical research and development of nintedanib from the initial drug discovery process to the latest available clinical trial data.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Roth GJ,Binder R,Colbatzky F,Dallinger C,Schlenker-Herceg R,Hilberg F,Wollin SL,Kaiser R

doi

10.1021/jm501562a

subject

Has Abstract

pub_date

2015-02-12 00:00:00

pages

1053-63

issue

3

eissn

0022-2623

issn

1520-4804

journal_volume

58

pub_type

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