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Drugs Fut 2021, 46(1): 5
ISSN 0377-8282
Copyright 2021 Clarivate
CCC: 0377-8282
DOI: 10.1358/dof.2021.46.1.3179432
 
 
Afabicin. Enoyl-(acyl-carrier-protein) reductase FabI inhibitor, Antibacterial drug
Saxena, D., Kaul, G., Dasgupta, A., Chopra, S.
 
 
The emergence of resistance to most clinically deployed antibiotics has called for development of new therapeutic agents with novel mechanisms of action. The fatty acid (FASII) biosynthetic pathway of bacteria is relatively an unexploited bacterial target for antimicrobial agents. Afabicin (Debio-1450), previously known as AFN-1720, is an investigational enoyl-[acyl-carrier-protein] reductase FabI inhibitor, currently under clinical development. It is a prodrug of Debio-1452, which is a species-specific, narrow-spectrum antibiotic active against > 5,000 strains of Staphylococcus aureus including methicillin-resistant S. aureus (MRSA) with an MIC90 0.016 mcg/mL. Afabicin is rapidly converted into its active metabolite, Debio-1452. It displays an excellent penetration potential in mice and human studies. Afabicin has displayed good safety and tolerability profiles in clinical studies and is currently under phase II clinical trials in patients with bone or joint infections.


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