Studies conducted since the late 1990s show substantial activity of selected citrus flavonoids as cystic fibrosis transmembrane conductance regulator (CFTR) membrane protein activators. Aimed at reinvigorating fundamental and applied research on citrus flavonoids for the treatment of mucoviscidosis, the thesis of this work is that aptly formulated citrus flavonoids hold significant potential for developing a multitarget treatment of cystic fibrosis combining in a single treatment antimicrobial, anti‐inflammatory, CFTR‐stimulating, and immunomodulatory properties, as required by a genetic disease eventually causing chronic lung inflammation and bacterial infection reinforcing each other.