Pulmonary

In vitro and mouse studies identified a hydroxamic acid-based ENPP2 inhibitor that could help treat pulmonary fibrosis. Chemical synthesis and in vitro testing in enzymatic activity assays of hydroxamic acid analogs yielded a compound that inhibited mouse ENPP2 with an IC₅₀ of 60 nM. In a mouse model of pulmonary fibrosis, the compound decreased the number of fibrotic lesions and vascular permeability in the lung, the number of inflammatory cells in bronchoalveolar lavage fluid, collagen levels in the lung and bronchoalveolar lavage fluid compared with vehicle. Next steps could include testing the compound in additional models of pulmonary fibrosis.

Galapagos N.V. has the ENPP2 inhibitor GLPG1690 in Phase II testing to treat idiopathic pulmonary fibrosis (IPF) and Phase I testing to treat chronic obstructive pulmonary disease (COPD) and other pulmonary diseases...