Antibiotikumokkal szembeni rezisztencia különösen a Gram-negatív baktériumok által szinte válságszerű helyzetet teremtett. A Zosurabalpin (RG6006) új antibiotikum ígéretes. A preklinikai vizsgálatok során hatékonynak találták a gyógyszerrezisztens, Gram-negatív baktériumok CRAB ellen.
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 antibiotikumok 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 antibiotikum ellenállás.
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 antibiotikumok. There is an urgent need for an effective antibiotikum against CARB as mortality rate is high (about 40%-60%) which attributed largely to lack of an effective antibiotikum. A progress towards this goal has been reported.
Scientists have identified a novel class of antibiotikumok 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) egy antibiotikum candidate belonging to ‘tethered macrocyclic peptides (MCPs)’ class. In pre-klinikai 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 antibiotikum-resistance mechanism of CARB suggesting Zosurabalpin van potenciálja.
Hence, human klinikai trials have been initiated to check for safety and efficacy Zosurabalpin CRAB által okozott invazív fertőzések kezelésében.
***
Referenciák:
- Zampaloni, C., Mattei, P., Bleicher, K. et al. A novel antibiotikum 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 Klinikai 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
***
