The development of a novel class of inhibitors for the enzyme autotaxin, that may find use for the treatment of idiopathic pulmonary fibrosis (IPF), was reported by Professor George Kokotos (Department of Chemistry, National and Kapodistrian University of Athens). According to the research data published in the peer-reviewed Journal of Medicinal Chemistry (2018, 61 (8), 3697–3711), such an inhibitor exhibited very promising results in an animal model of bleomycin-induced pulmonary fibrosis, treating the inflammation and restoring various biomarkers, for example the concentration of BALF collagen, to normal levels. Idiopapthic pulmonary fibrosis, with a median survival time between 2 and 5 years from diagnosis, is a great challenge for the development of novel medicinal agents, since no effective treatment exists so far. The important results of the NKUA group are based on the design and synthesis of novel small organic molecules targeting an enzyme that is involved in the production of a bioactive lipid.
The enzymes involved in lipid metabolism as well as the receptors interacting with bioactive lipids constitute an underinvestigated area for the discovery of novel medicines and, as a consequence, lipids are excellent targets for the design and synthesis of novel small molecules exhibiting new mechanisms of pharmacological action. It has to be noticed that the University of Athens holds a patent and currently explores the application of this invention. The global idiopathic pulmonary fibrosis market generated $1,6 billion in 2016, and is projected to reach $3,5 billion by 2023. The novel autotaxin inhibitors open new avenues for the discovery and the development of drugs that may effectively treat chronic inflammatory conditions, including cancer.
