GLPG-3221

GLPG-3221 is a potent, orally active corrector of CFTR (cystic fibrosis transmembrane conductance regulator), with an EC50 of 105 nM. GLPG-3221 can be uesd for the treatment of cystic fibrosis[1].

Signaling Pathways >> Membrane Transporter/Ion Channel >> CFTR

Research Areas >> Others

GLPG-3221 (1 mg/kg; i.v.) treatment shows the Cl and t1/2 are 0.13 L/h/kg and 3 hours, respectively[1]. GLPG-3221 (1 mg/kg; p.o.)treatment shows the F% value is 53%[1]. Animal Model: Rat[1]  Dosage: 1 mg/kg Administration: i.v. administration (Pharmacokinetic Analysis) Result: The Cl and t1/2 were 0.13 L/h/kg and 3 hours, respectively.

[1]. Scanio MJC, et al.Discovery of ABBV/GLPG-3221, a Potent Corrector of CFTR for the Treatment of Cystic Fibrosis.ACS Med Chem Lett. 2019 Oct 31;10(11):1543-1548.