VX-809 (Lumacaftor) 936727-05-8

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Molecular Weight:

452.41 VX-809 (Lumacaftor) acts to correct CFTR mutations common in cystic fibrosis by increasing mutant CFTR (F508del-CFTR) maturation,EC50 of 0.1 μM. Phase 3.

Biological Activity

VX-809 acts at the level of the ER to allow a fraction of the
F508del-CFTR to adopt a properly folded form, to exit the ER and
mobilize to the cell surface for normal functioning. In Fischer rat
thyroid (FRT) cells expressing F508del-CFTR, VX-809 treatment
significantly improves F508del-CFTR maturation by 7.1 fold with an EC50
of 0.1 μM, and enhances F508del-CFTR-mediated chloride transport by
approximately 5 fold with EC50 of 0.5 μM, while VRT-768 has higher EC50
values of 7.9 μM and 16 μM, respectively.


In HEK-293 cells expressing
F508del-CFTR, VX-809 (3 μM) treatment increases F508del-CFTR exit from
the ER by 6 fold, reaching levels comparable to 34% of CFTR. In primary
human bronchial epithelial (HBE) cells with F508del-CFTR mutation,
VX-809 increases CFTR maturation and enhances chloride secretion with
EC50 of 350 nM and 81 nM, respectively, more efficacious than Corr-4a
and VRT-325.


F508del-CFTR corrected by VX-809 exhibits single-channel
open probability of 0.39 similar to normal CFTR of 0.40. Unlike VX-770,
VX-809 is not a CFTR potentiator, as acute addition of VX-809 has no
effect on F508del-CFTR function.


In contrast to VRT-325 and Corr-4a,
VX-809 does not improve the processing of the normal or mutant forms of
hERG or P-gp, as well as other disease-causing mislocalized Proteins,
including α1-antitrypsin Z mutant (E342K-α1-AT) or N370S-β-glucosidase,
suggesting that VX-809 is specific for CFTR. VX-809 in combination with
VRT-325 or Corr-4a has additive effect on CFTR-mediated chloride
transport in cultured F508del-HBE.

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Product Categories : Transmembrane Transporters > CFTR Inhibitor