ArticleAntimicrobial agents and chemotherapy2015
Activity of Debio1452, a FabI inhibitor with potent activity against Staphylococcus aureus and coagulase-negative Staphylococcus spp., including multidrug-resistant strains.
Article in Antimicrobial agents and chemotherapy, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed.
- Antibacterial drug discovery: challenges and preclinical promises from synthetic small molecules.Chemical Society reviews · 2026Review
- Model-based quantification of immune response and anti-staphylococcal activity of afabicin in immunocompetent mouse thigh infections to enable predictions of clinical efficacy.Antimicrobial agents and chemotherapy · 2026Article
- Current Trends in Clinical Trials of Prodrugs.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Model-based translation of results from in vitro to in vivo experiments for afabicin activity against Staphylococcus aureus.The Journal of antimicrobial chemotherapy · 2024Article
- An Iterative Approach Guides Discovery of the FabI Inhibitor Fabimycin, a Late-Stage Antibiotic Candidate withACS central science · 2022Article
- Emerging Treatment Options for Acute Bacterial Skin and Skin Structure Infections and Bloodstream Infections Caused byInfection and drug resistance · 2022Review
- Novel Targets for Antimicrobials.Turkish journal of pharmaceutical sciences · 2020Review
- Article
- Emerging Treatment Options for Infections by Multidrug-Resistant Gram-Positive Microorganisms.Microorganisms · 2020Review
- A novel series of enoyl reductase inhibitors targeting the ESKAPE pathogens, Staphylococcus aureus and Acinetobacter baumannii.Bioorganic & medicinal chemistry · 2018Article
- Therapeutic Targets in Chlamydial Fatty Acid and Phospholipid Synthesis.Frontiers in microbiology · 2018Review
- Article
- Clinical Relevance of Type II Fatty Acid Synthesis Bypass in Staphylococcus aureus.Antimicrobial agents and chemotherapy · 2017Article
- Antibiotics in the clinical pipeline at the end of 2015.The Journal of antibiotics · 2017Review
- Article
- A Pathogen-Selective Antibiotic Minimizes Disturbance to the Microbiome.Antimicrobial agents and chemotherapy · 2016Article
- Thiolactomycin-Based Inhibitors of Bacterial β-Ketoacyl-ACP Synthases with in Vivo Activity.Journal of medicinal chemistry · 2016Article
- Initial broth microdilution quality control guidelines for Debio 1452, a FabI inhibitor antimicrobial agent.Antimicrobial agents and chemotherapy · 2015Article
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Authors and funding
5 authors.
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No grant is acknowledged in the PubMed record.
Abstract
Staphylococcus aureus and coagulase-negative staphylococci (CoNS) are responsible for a wide variety of human infections. The investigational antibacterial Debio1450 (previously AFN-1720), a prodrug of Debio1452 (previously AFN-1252), specifically targets staphylococci without significant activity against other Gram-positive or Gram-negative species. Debio1452 inhibits FabI, an enzyme critical to fatty acid biosynthesis in staphylococci. The activity of Debio1452 against CoNS, methicillin-susceptible S. aureus (MSSA), and methicillin-resistant S. aureus (MRSA), including significant clones, was determined. A globally diverse collection of 574 patient isolates from 35 countries was tested that included CoNS (6 species, 103 strains), MSSA (154 strains), MRSA (163 strains), and molecularly characterized strains (including spa-typed MRSA clones; 154 strains). The isolates were tested for susceptibility by CLSI broth microdilution methods against Debio1452 and 10 comparators. The susceptibility rates for the comparators were determined using CLSI and EUCAST breakpoint criteria. All S. aureus and CoNS strains were inhibited by Debio1452 concentrations of ≤ 0.12 and ≤ 0.5 μg/ml, respectively. The MIC50s for MSSA, MRSA, and molecularly characterized MRSA strains were 0.004 μg/ml, and the MIC90s ranged from 0.008 to 0.03 μg/ml. The MICs were higher for the CoNS isolates (MIC50/90, 0.015/0.12 μg/ml). Among S. aureus strains, resistance was common for erythromycin (61.6%), levofloxacin (49.0%), clindamycin (27.6%), tetracycline (15.7%), and trimethoprim-sulfamethoxazole (7.0%). Debio1452 demonstrated potent activity against MSSA, MRSA, and CoNS. Debio1452 showed significantly greater activity overall (MIC50, 0.004 μg/ml) than the other agents tested against these staphylococcal species, which included dominant MRSA clones and strains resistant to currently utilized antimicrobial agents.
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