Nintedanib in idiopathic pulmonary fibrosis.
Idiopathic pulmonary fibrosis (IPF) conveys a median survival of 3 years and until recently has lacked effective therapies. Nintedanib, an orally available, small-molecule tyrosine kinase inhibitor with selectivity for vascular endothelial growth factor (VEGF), platelet-derived growth factor (PDGF) and fibroblast growth factor (FGF) receptors has recently been shown, in two pivotal phase III studies, to effectively slow IPF disease progression. Consequently, nintedanib was given accelerated approval by the FDA in October 2014 for the treatment of IPF. This monograph explores the preclinical rationale for the antifibrotic role of nintedanib and provides an overview of the available data on pharmacokinetics, efficacy and safety.
Centre for Injury and Tissue Repair, University College London, London, UK.
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Woodcock
Centre for Injury and Tissue Repair, University College London; NIHR Respiratory Biomedical Research Unit, Royal Brompton Hospital; Fibrosis Research Group, National Heart and Lung Institute, Imperial College, London, UK. t.maher@imperial.ac.uk.
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Maher
D002986:Clinical Trials as Topic; D005346:Fibroblast Growth Factors / Q000378:metabolism; D006801:Humans; D054990:Idiopathic Pulmonary Fibrosis / Q000188:drug therapy* / Q000378:metabolism; D007211:Indoles / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D015394:Molecular Structure; D010982:Platelet-Derived Growth Factor / Q000378:metabolism; D047428:Protein Kinase Inhibitors / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors; D016896:Treatment Outcome; D042461:Vascular Endothelial Growth Factor A / Q000378:metabolism
D007211:Indoles; D010982:Platelet-Derived Growth Factor; D047428:Protein Kinase Inhibitors; C467484:VEGFA protein, human; D042461:Vascular Endothelial Growth Factor A; D005346:Fibroblast Growth Factors; D011505:Protein-Tyrosine Kinases; C530716:nintedanib
Acute exacerbations; Clinical trials; Therapeutics; Usual interstitial pneumonia