GLPG-1837

GLPG-1837 (ABBV-974) is a potent, orally available CFTR potentiator with EC50 of 3 nM and 339 nM on F508del and G551D CFTR, respectively; shows enhanced efficacy on CFTR mutants harboring Class III mutations compared to Ivacaftor.Cystic Fibrosis, Phase 2 Clinical (In Vitro) :GLPG1837 is a potent CFTR potentiator, with EC50s of 3 nM and 339 nM for F508del and G551D CFTR, respectively. GLPG1837 increases the conductivity of the G551D CFTR channel with obtained potency of 181 nM. GLPG1837 is reversible CFTR potentiator, with a the apparent affinity within a range of 0.2~2 μM.