GLPG1837

GLPG1837 is an orally available small molecule and a potent cystic fibrosis transmembrane conductance regulator (CFTR) potentiator developed for the treatment of cystic fibrosis (CF), particularly targeting Class III mutations such as G551D, S1251N, and other gating mutations. As a CFTR potentiator, GLPG1837 enhances the function of defective CFTR protein by increasing the probability that the chloride channel remains open, thereby facilitating chloride ion transport across epithelial cell membranes. This mechanism is similar to that of other known potentiators like ivacaftor (VX-770). The drug was developed by Galapagos in collaboration with AbbVie and underwent Phase 1 and Phase 2 clinical trials in patients with specific CFTR mutations. Although it demonstrated safety and efficacy in early studies, development for cystic fibrosis was discontinued after Phase 2 trials.

Other names

N-(3-carbamoyl-5,5,7,7-tetramethyl-4,7-dihydro-5H-thieno[2,3-c]pyran-2-yl)-1H-pyrazole-3-carboxamide1654725-02-6