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Nintedanib: from discovery to the clinic

Gerald J Roth1, Rudolf Binder, Florian Colbatzky

  • 1Department of Medicinal Chemistry; §Department of Drug Metabolism and Pharmacokinetics; ‡Department of Non-Clinical Drug Safety; ∥Department of Translational Medicine and Clinical Pharmacology; ⊥Department of Respiratory Diseases Research; and #Corporate Division Medicine, TA Oncology, Boehringer Ingelheim Pharma GmbH & Co. KG , 88397 Biberach an der Riss, Germany.

Journal of Medicinal Chemistry
|December 5, 2014
PubMed

Insights

Nintedanib, a triple angiokinase inhibitor, effectively treats non-small cell lung cancer (NSCLC), ovarian cancer, and idiopathic pulmonary fibrosis (IPF). This review details its preclinical and clinical development, highlighting significant efficacy in phase III studies.

Area of Science:

  • Pharmacology
  • Oncology
  • Pulmonology

Background:

  • Nintedanib is an oral small-molecule tyrosine kinase inhibitor targeting key pathways in angiogenesis and fibrosis.
  • It inhibits vascular endothelial growth factor receptor (VEGFR), fibroblast growth factor receptor (FGFR), and platelet-derived growth factor receptor (PDGFR) families, among others.

Purpose of the Study:

  • To provide a comprehensive review of nintedanib's preclinical and clinical research.
  • To summarize the drug discovery process and latest clinical trial data for nintedanib.

Main Methods:

  • Literature review of preclinical studies.
  • Analysis of clinical trial data from phase III studies.

Main Results:

  • Nintedanib demonstrated significant efficacy in treating non-small cell lung cancer (NSCLC).
  • Nintedanib showed significant efficacy in treating ovarian cancer.
  • Nintedanib demonstrated significant efficacy in treating idiopathic pulmonary fibrosis (IPF).

Conclusions:

  • Nintedanib is a clinically validated therapeutic agent for NSCLC, ovarian cancer, and IPF.
  • The review consolidates nintedanib's research and development journey, from discovery to clinical application.

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