TargetRx Atlas

MRNA basic information

  • mRNA ID:ENST00000221930
  • Gene Name:TGFB1
  • mRNA database:Ensembl
  • mRNA expression :down-regulated
  • mRNA Method:PCR
  • mRNA Pathway:NA
  • Evidence:validated
  • (mRNA-drug)

Drug basic information

  • Drug ID:DB09080
  • Drug Name:Olodaterol
  • Drug Method:down-regulated the gene expression

Disease basic infommation

  • Disease:idiopathic pulmonary fibrosis
  • Tissue:patients tissues

Other information

  • Title:Olodaterol shows anti-fibrotic efficacy in in vitro and in vivo models of pulmonary fibrosis
  • Journal:British Journal of Pharmacology
  • Published:2017
  • PubMed ID:28810065
  • Abstract:Background and purpose:Idiopathic pulmonary fibrosis (IPF) is a fatal respiratory disease characterized by excessive fibroblast activation ultimately leading to scarring of the lungs. Although, the activation of β2-adrenoceptors (β2-AR) has been shown to inhibit pro-fibrotic events primarily in cell lines, the role of β2-adrenoceptor agonists has not yet been fully characterized. The aim of our study was to explore the anti-fibrotic activity of the long-acting β2-adrenoceptor agonist olodaterol in primary human lung fibroblasts (HLF) and in murine models of pulmonary fibrosis. Experimental approach:We assessed the activity of olodaterol to inhibit various pro-fibrotic mechanisms, induced by different pro-fibrotic mediators, in primary HLF from control donors and patients with IPF (IPF-LF). The in vivo anti-fibrotic activity of olodaterol, given once daily by inhalation in either a preventive or therapeutic treatment regimen, was explored in murine models of lung fibrosis induced by either bleomycin or the overexpression of TGF-β1. Key results:In both HLF and IPF-LF, olodaterol attenuated TGF-β-induced expression of α-smooth muscle actin, fibronectin and endothelin-1 (ET-1), FGF- and PDGF-induced motility and proliferation and TGF-β/ET-1-induced contraction. In vivo olodaterol significantly attenuated the bleomycin-induced increase in lung weight, reduced bronchoalveolar lavage cell counts and inhibited release of pro-fibrotic mediators (TGF-?, MMP-9 and tissue inhibitor of metalloproteinase-1). Forced vital capacity was increased only with the preventive treatment regimen. In the TGF-β-overexpressing model, olodaterol additionally reduced the Col3A1 mRNA expression. Conclusion and implications:Olodaterol showed anti-fibrotic properties in primary HLF from control and IPF patients and in murine models of lung fibrosis.
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