FFC#17/2018

Drug repurposing for antivirulence therapy against Pseudomonas aeruginosa

FFC#17/2018

Drug repurposing for antivirulence therapy against Pseudomonas aeruginosa

PRINCIPAL INVESTIGATOR

Livia Leoni (Università Roma Tre, Dip. Scienze, Lab. Microbiologie dei microrganismi)

RESEARCHERS

6

CATEGORY

AREA 3 Bronchopulmonary infection

DURATION

1 year

GOAL

€ 31.000 €

RESULTS

Researchers have discovered a new anti-quorum sensing system (anti-pqs) activity in three “old” FDA-approved drugs originally developed for the treatment of diseases different from Pseudomonas aeruginosa (Pa) infection. The anti-virulence activity of each one of the three drugs was tested against a collection of 100 P. aeruginosa strains isolated from CF patients, having different antibiotic resistance profiles. The interaction of the anti-pqs drugs with antibiotics commonly used in CF therapy was studied in Pa liquid and biofilm cultures. The anti-pqs drugs resulted significantly active against a large percentage of CF strains, even if to different extents, and showed no antagonistic effects toward antibiotics. In particular, multidrug-resistant (MDR) strains seemed to be particularly susceptible to one of these drugs, named Clofoctol. Results based also on toxicity and pharmacokinetic considerations support Clofoctol as the most promising anti-virulence drug for repurposing in CF therapy. However, additional confirmatory studies carried out with a larger number of MDR-Pa CF isolates should be carried out before proceeding with further studies in animal infection models. The final aim is to identify a new “old “ drug suitable to be faster transferred to CF patients.

OTHER RESULTS

FFC#1/2023

Tezacaftor, one of the components of Kaftrio, induces an accumulation of dihydroceramides both in vitro and in vivo in animal models

FFC#4/2023

Pseudopaline–aztreonam conjugates exhibited enhanced antimicrobial activity against Pseudomonas aeruginosa compared to aztreonam alone

FFC#10/2023

Several drugs already approved for human use inhibit the growth of P. aeruginosa, its virulence, or its ability to form biofilms in vitro