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VX-659 + tezacaftor + VX-561
- Development stage
- Phase 2
- Lead developer
- Vertex
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
**VX-659 + tezacaftor + VX-561** is a triple combination investigational therapy for cystic fibrosis (CF), comprising two CFTR correctors (VX-659 and tezacaftor) and one CFTR potentiator (VX-561, a once-daily deuterated ivacaftor). VX-659 and tezacaftor act on different sites of the CFTR protein, improving its processing and trafficking to the cell surface, while VX-561 facilitates the sustained opening of the chloride channel, thus enhancing chloride and sodium ion transport across epithelial surfaces. This combination targets the underlying protein defect in CF caused by Phe508del mutations, and has shown additive clinical efficacy in lung function and sweat chloride reduction, with a safety profile similar to dual combination CFTR modulators. Developed by Vertex Pharmaceuticals, the regimen is intended to treat CF patients with both Phe508del/Phe508del and Phe508del/minimal function genotypes[1][2][3][4].
- Other names
- VX-659 + tezacaftor + VX-561
02
Targets
CFTR (Cystic fibrosis transmembrane conductance regulator)
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