Preclinical development and commercial exploitation of Autotaxin inhibitors, a novel pharmaceutical target in the pathogenesis of pulmonary fibrosis and chronic inflammation (ΑΤΧ)


Autotaxin (ATX, ENPP2) is a secreted glycoprotein present in the majority of biological fluids, which catalyzes the production of lysophosphatidic acid (LPA). LPA, a bioactive phospholipid, is implicated in a wide range of functions through the existence of 6 GPCR cognate receptors (LPAR1-6), which are expressed in all body cells at different ratios. Published studies from the BSRC Fleming laboratories indicated ΑΤΧ as a possible prediction biomarker and drug target in chronic inflammatory diseases, such as idiopathic pulmonary fibrosis (IPF). IPF is a chronic, gradual and, often, deadly disease of unknown aetiology in urgent need for the development of new treatments, which has lately attracted the pharmaceutical industry interest. Genetic and pharmacological studies have shown the decisive role of ΑΤΧ in IPF pathogenesis and provided the proof of principle for the clinical trials of phase III of an ATX inhibitor.
In this context, BSRC Fleming, National and Kapodistrian University of Athens and UNIPHARMA have created a drug discovery pipeline towards the discovery of novel inhibitors against the catalytic function of ΑΤΧ. The goals and expected results of the project include the discovery of novel ATX inhibitors with improved characteristics and ADMET properties, as well as the registration and commercial exploitation of the relative intellectual property.
Co-financed by the European Regional Development Fund of the European Union and Greek national funds