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Antimikrobiese weerstand (AMR): 'n nuwe antibiotika Zosurabalpin (RG6006) toon belofte in pre-kliniese proewe

Antibiotiese weerstand veral deur Gram-negatiewe bakterieë het byna 'n krisisagtige situasie geskep. Die nuwe antibiotika Zosurabalpin (RG6006) toon beloftes. Daar is gevind dat dit effektief is teen middel-weerstandige, Gram-negatiewe bakterieë CRAB in pre-kliniese studies.   

Antimicrobial resistance (AMR), driven mainly by the misuse and overuse of antimicrobials, is one of top public health risk.  

Infections by Gram-negative bacteria are particularly concerning. It is not easy for most of antibiotika to cross both inner and outer membranes present in this category of bacteria to enter the bacterial cells to show bactericidal actions. Also, Gram-negative bacteria have accumulated disproportionately high degree of antibiotika weerstand.  

Acinetobacter baumannii is a Gram-negative bacterium. Infection by one of its strains called ‘carbapenem-resistant Acinetobacter baumannii’ (CRAB) is hard to treat using available antibiotika. There is an urgent need for an effective antibiotika against CARB as mortality rate is high (about 40%-60%) which attributed largely to lack of an effective antibiotika. A progress towards this goal has been reported.  

Scientists have identified a novel class of antibiotika namely, tethered macrocyclic peptides (MCPs) which are active against the Gram –ve bacteria A. baumannii including CARB by blocking transport of bacterial lipopolysaccharide from the inner membrane to the outer membrane.  

Zosurabalpin (RG6006) is 'n antibiotika candidate belonging to ‘tethered macrocyclic peptides (MCPs)’ class. In pre-kliniese trials involving in vitro studies and in vivo studies on animal models, Zosurabalpin has been found to be effective against drug-resistant isolates of ‘carbapenem-resistant Acinetobacter baumannii’ (CRAB) from different regions. It successfully overcame antibiotika-resistance mechanism of CARB suggesting Zosurabalpin potensiaal het.  

Hence, human kliniese trials have been initiated to check for safety and efficacy Zosurabalpin in die behandeling van indringende infeksies wat deur KRAB veroorsaak word.  

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Verwysings:  

  1. Zampaloni, C., Mattei, P., Bleicher, K. et al. A novel antibiotika class targeting the lipopolysaccharide transporter. Nature (2024). https://doi.org/10.1038/s41586-023-06873-0 
  2. Hawser S., et al 2023. Activity of the Novel Antibiotic Zosurabalpin (RG6006) against Kliniese Acinetobacter Isolates from China, Open Forum Infectious Diseases, Volume 10, Issue Supplement_2, December 2023, ofad500.1754, https://doi.org/10.1093/ofid/ofad500.1754  

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Umesh Prasad
Umesh Prasad
Wetenskapjoernalis | Stigterredakteur, Scientific European tydskrif

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