Synonyms: ABBV/GLPG-3221 | compound 19 [PMID: 31749908]
Compound class:
Synthetic organic
Comment: ABBV-3221(GLPG-3221) is a novel cystic fibrosis transmembrane conductance regulator (CFTR) corrector that is being developed in a collaboration between AbbVie and Galapagos for the treatment of cystic fibrosis [2]. It was designed to provide improved clinical efficacy when used in a triple combination with a CFTR potentiator and a second, but mechanistically distinct, corrector molecule. ABBV-3221 enhances channel activity by increasing pore opening whilst the channel's two nucleotide-binding domains are dimerized [1].
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References |
1. Levring J, Terry DS, Kilic Z, Fitzgerald G, Blanchard SC, Chen J. (2023)
CFTR function, pathology and pharmacology at single-molecule resolution. Nature, 616 (7957): 606-614. [PMID:36949202] |
2. Scanio MJC, Searle XB, Liu B, Koenig JR, Altenbach R, Gfesser GA, Bogdan A, Greszler S, Zhao G, Singh A et al.. (2019)
Discovery of ABBV/GLPG-3221, a Potent Corrector of CFTR for the Treatment of Cystic Fibrosis. ACS Med Chem Lett, 10 (11): 1543-1548. [PMID:31749908] |