Abstract
Contezolid is a novel oxazolidinone, which exhibits potent activity against gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus (VRE), and penicillin-resistant Streptococcus pneumoniae (PRSP). In this study, the in vitro activity of contezolid was compared with linezolid (LZD), tigecycline (TGC), teicoplanin (TEC), vancomycin (VA), daptomycin (DAP), and florfenicol (FFC) against MRSA and VRE strains isolated from China. Contezolid revealed considerable activity against MRSA and VRE isolates with MIC90 values of 0.5 and 1.0 μg/mL, respectively. For VRE strains with different resistance genotypes, including vanA- and vanM-type strains, contezolid did not exhibit significantly differential antibacterial activity. Furthermore, the antimicrobial activity of contezolid is similar to or slightly better than that of linezolid against MRSA and VRE strains. Subsequently, the activity of contezolid was tested against strains carrying linezolid resistance genes, including Staphylococcus capitis carrying cfr gene and Enterococcus faecalis carrying optrA gene. The results showed that contezolid exhibited similar antimicrobial efficacy to linezolid against strains with linezolid resistance genes. In general, contezolid may have potential benefits to treat the infections caused by MRSA and VRE pathogens.
Highlights
Increasing resistance to antibiotics in gram-positive cocci is a major concern of health care
The objective of this study was to evaluate the in vitro activity of contezolid relative to that of other comparator antimicrobial agents against methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus (VRE), and strains carrying linezolid resistance genes using clinical isolates collected from China
The antimicrobial activity of contezolid was explored in strains carrying linezolid resistance genes. Both against S. capitis with cfr gene and E. faecalis with optrA gene, contezolid showed similar Minimum inhibitory concentrations (MICs) distributions to linezolid (Table 4). These results demonstrated that contezolid displayed limited activity against strains carrying linezolid resistance genes
Summary
Increasing resistance to antibiotics in gram-positive cocci is a major concern of health care. The emergence of multidrug-resistant (MDR) bacteria leads to a decline in the treatment options. The World Health Organization (WHO) published a list of antibiotic-resistant “priority pathogens” in 2017 (Asokan et al, 2019). Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus (VRE) are of particular concern since they are responsible for several severe infections. MRSA exhibits resistance to most available antibiotics, including fluoroquinolones and peptides, aminoglycosides, macrolides, and tetracycline (Osei Sekyere and Mensah, 2020). Novel antibacterial agents are urgently needed to treat infectious diseases caused by MDR gram-positive pathogens
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