עמידות לאנטיביוטיקה במיוחד על ידי חיידקים גראם שליליים כמעט יצר מצב כמו משבר. האנטיביוטיקה החדשה Zosurabalpin (RG6006) מראה הבטחות. הוא נמצא יעיל נגד חיידקים גראם-שליליים CRAB עמידים לתרופות במחקרים פרה-קליניים.
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 אַנְטִיבִּיוֹטִיקָה 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 אנטיביוטי התנגדות.
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 אַנְטִיבִּיוֹטִיקָה. There is an urgent need for an effective אנטיביוטי against CARB as mortality rate is high (about 40%-60%) which attributed largely to lack of an effective אנטיביוטי. A progress towards this goal has been reported.
Scientists have identified a novel class of אַנְטִיבִּיוֹטִיקָה 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) הוא אנטיביוטי candidate belonging to ‘tethered macrocyclic peptides (MCPs)’ class. In pre-קליני 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 אנטיביוטי-resistance mechanism of CARB suggesting זוסורבלפין יש פוטנציאל.
Hence, human קליני trials have been initiated to check for safety and efficacy זוסורבלפין בטיפול בזיהומים פולשניים הנגרמים על ידי CRAB.
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הפניות:
- Zampaloni, C., Mattei, P., Bleicher, K. et al. A novel אנטיביוטי class targeting the lipopolysaccharide transporter. Nature (2024). https://doi.org/10.1038/s41586-023-06873-0
- האוסר ס., ואח' 2023. Activity of the Novel Antibiotic Zosurabalpin (RG6006) against קליני 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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