Resistência a antibióticos particularmente por bactérias Gram-negativas quase criou uma situação semelhante a uma crise. O novo antibiótico Zosurabalpin (RG6006) mostra-se promissor. Verificou-se que é eficaz contra bactérias Gram-negativas resistentes a medicamentos CRAB em estudos pré-clínicos.
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 antibióticos 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 antibiótico resistência.
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 antibióticos. There is an urgent need for an effective antibiótico against CARB as mortality rate is high (about 40%-60%) which attributed largely to lack of an effective antibiótico. A progress towards this goal has been reported.
Scientists have identified a novel class of antibióticos 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.
Zosuralpina (RG6006) é um antibiótico candidate belonging to ‘tethered macrocyclic peptides (MCPs)’ class. In pre-clínico 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 antibiótico-resistance mechanism of CARB suggesting Zosurbalpina tem potencial.
Hence, human clínico trials have been initiated to check for safety and efficacy Zosurbalpina no tratamento de infecções invasivas causadas por CRAB.
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Referências:
- Zampaloni, C., Mattei, P., Bleicher, K. et al. A novel antibiótico class targeting the lipopolysaccharide transporter. Nature (2024). https://doi.org/10.1038/s41586-023-06873-0
- Hawser S., et al 2023. Activity of the Novel Antibiotic Zosurabalpin (RG6006) against Clínico 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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