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Overview

 
 
 
Due to the high morbidity and mortality associated with infections caused by multidrug-resistant bacteria, such as Staphylococcus aureus, Enterococcus faecalis, Acinetobacter baumannii, Pseudomonas aeruginosa and Klebsiella pneumoniae the discovery of innovative agents with potent activity against these pathogens is the top priority of our anti-infectives research team.
 
 
BAL30072
 
Basilea’s lead molecule BAL30072, is a novel sulfactam antibiotic with a broad coverage of aerobic Gram-negative bacteria, including many of the contemporary problem pathogens such as carbapenem–resistant Pseudomonas aeruginosa and Acinetobacter baumannii. BAL30072 is stable towards many types of beta-lactamases that destroy most of the currently marketed beta-lactam antibiotics, including those of the carbapenem type. It is taken up very readily into bacteria, exploiting essential nutrient uptake systems and is able to circumvent resistance caused by changes in the outer membrane of Gram-negative bacteria. In experimental settings, bacterial resistance towards BAL30072 develops more slowly than it does to other drugs. BAL30072 has shown to be highly compatible with agents used for treating Gram-positive infections and even works synergistically with some agents used for treating Gram-negative infections, such as carbapenems and aminoglycosides
 
 
Exploratory programs
 
Basilea scientists are exploiting their expertise in beta-lactam chemistry to advance research into innovative antibiotics that can resist attack by beta-lactamases and to discover new inhibitors of beta-lactamases that could be used to restore the activity of antibiotics against which bacteria have developed resistance.

Basilea is also pursuing novel macrolides applying expertise developed during the identification and characterization of BAL19403, a macrolide with potent activity against Propionibacterium acnes, including many resistant strains. Further exploratory research projects are focused on finding novel inhibitors that work on targets not exploited by currently marketed antibiotics and should therefore avoid specific resistance mechanisms.


 
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