GLPG-1837

Description: GLPG1837 (also known as ABBV-974) is a novel, potent and reversible CFTR (cystic fibrosis transmembrane conductance regulator) potentiator with EC50s of 3 nM and 339 nM for F508del and G551D CFTR, respectively. Cystic fibrosis (CF) is caused by mutations in the gene for the cystic fibrosis transmembrane conductance regulator (CFTR). With the discovery of Ivacaftor and Orkambi, it has been shown that CFTR function can be partially restored by administering one or more small molecules. These molecules aim at either enhancing the amount of CFTR on the cell surface (correctors) or at improving the gating function of the CFTR channel (potentiators).

References: J Med Chem. 2018 Feb 22; 61(4):1425-1435.