In vitro Activity of Contezolid Against Methicillin-Resistant Staphylococcus aureus, Vancomycin-Resistant Enterococcus, and Strains With Linezolid Resistance Genes From China

Wang, Siheng; Cai, Chang; Shen, Yingbo; Sun, Chengtao; Shi, Qingxin; Wu, Ningjun; Zheng, Shufang; Qian, Jiao; Zhang, Rong; Zhou, Hongwei

doi:10.3389/fmicb.2021.729900

Cited by 15 publications

(8 citation statements)

References 27 publications

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“… 8 According to a recent study, contezolid exhibited considerable activity in vitro against VRE isolates. 27 In addition to cSSTI, contezolid has also been found to be effective in lung infections, such as pulmonary tuberculosis. 28 , 29 Based on our knowledge, this is the first published report of a patient with VREfm pneumonia who was treated successfully with contezolid.…”

Section: Discussionmentioning

confidence: 99%

Sequential Therapy of Linezolid and Contezolid to Treat Vancomycin-Resistant Enterococcus faecium Pneumonia in a Centenarian Patient: Case Report

Chen¹,

Liu²,

Zhang³

2023

IDR

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Enterococcus faecium ( E. faecium ) is one of the core components of enterococci and causes serious illnesses in the elderly and immunocompromised patients. Due to its adaptive traits and antibiotic resistance, E. faecium has evolved as a worldwide hospital-associated pathogen, especially vancomsycin-resistant Enterococcus faecium (VREfm). Pneumonia caused by VREfm is quite rare in clinical settings, and optimal treatment has not yet been determined. Here, we present a case of nosocomial VREfm pneumonia with lung cavitation following adenovirus infection, which was successfully treated with linezolid and contezolid.

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Section: Discussionmentioning

confidence: 99%

Sequential Therapy of Linezolid and Contezolid to Treat Vancomycin-Resistant Enterococcus faecium Pneumonia in a Centenarian Patient: Case Report

Chen¹,

Liu²,

Zhang³

2023

IDR

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“…Oxazolidinones, including linezolid, contezolid, and tedizolid, are applied as the first-line drug for the antimicrobial treatment of gram-positive bacterial infections. Multiple reports have shown the excellent antibacterial activity of radezolid against the planktonic cells of gram-positive bacteria ( Moellering, 2014 ; Zheng J. et al, 2020 ; Wang et al, 2021 ). A previous study shows that radezolid still has potent antibacterial activity against E. faecalis linezolid non-susceptible strains, with the MIC of radezolid being 2–8 times lower than that of linezolid ( Zheng J. et al, 2020 ).…”

Section: Discussionmentioning

confidence: 99%

Antibacterial and anti-biofilm activity of radezolid against Staphylococcus aureus clinical isolates from China

et al. 2023

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Although the potent antibacterial ability of radezolid against Staphylococcus aureus has been widely reported worldwide, its antibacterial and anti-biofilm activity against the S. aureus clinical isolates from China remains elusive. In this study, the minimum inhibitory concentration (MIC) of radezolid was determined in S. aureus clinical isolates from China using the agar dilution method, and the relationship between radezolid susceptibility and ST distribution was also investigated. The anti-biofilm activity of radezolid against S. aureus was determined by a crystal violet assay and compared with that of linezolid and contezolid. The quantitative proteomics of S. aureus treated with radezolid was analyzed, and the genetic mutations in radezolid-induced resistant S. aureus were determined by whole-genome sequencing. The dynamic changes in transcriptional expression levels of several biofilm-related genes were analyzed by quantitative RT-PCR. Our data showed that radezolid MIC ranged from ≤0.125 to 0.5 mg/L, which was almost 1/4 × MIC of linezolid against S. aureus, indicating the greater antibacterial activity of radezolid than linezolid. The S. aureus clinical isolates with radezolid MICs of 0.5 mg/L were most widely distributed in ST239 of MRSA and ST7 of MSSA. Moreover, the more robust anti-biofilm activity of radezolid with subinhibitory concentrations (1/8 × MIC and 1/16 × MIC) was demonstrated against S. aureus when compared with that of contezolid and linezolid. Genetic mutations were found in glmS, 23S rRNA, and DUF1542 domain-containing protein in radezolid-induced resistant S. aureus selected by in vitro induction of drug exposure. Quantitative proteomic analysis of S. aureus indicated that the global expression of some biofilm-related and virulence-related proteins was downregulated. Quantitative RT-PCR further confirmed that the expressions of some downregulated biofilm-related proteins, including sdrD, carA, sraP, hlgC, sasG, spa, sspP, fnbA, and oatA, were decreased after 12 h and 24 h of exposure to radezolid. Conclusively, radezolid shows robust antibacterial and anti-biofilm activity against S. aureus clinical isolates from China when compared with contezolid and linezolid.

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“…In addition, contezolid had good antibacterial activity against aerobic GPB, especially against the drug-resistant strains of such aerobic Gram-positive cocci as MRSA, penicillin-resistant S. pneumoniae (PRSP), and VRE. Of note, a previous study indicated that contezolid had limited activity against strains carrying linezolid-resistance genes, such as Staphylococcus capitis with the cfr gene and E. faecalis with the optrA gene, and vanA - and vanM- type VRE strains ( Wang et al, 2021a ). Moreover, compared with linezolid, contezolid was active against most non-tuberculous Mycobacterium reference strains, with the exception of Mycobacterium avium and Mycobacterium intracellulare , and pre-exposure to contezolid did not induce drug resistance ( Wilcox, 2005 ; Guo et al, 2021 ).…”

Section: Antibacterial Efficacymentioning

confidence: 99%

Contezolid, a novel oxazolidinone antibiotic, may improve drug-related thrombocytopenia in clinical antibacterial treatment

Liu

Luo

et al. 2023

Front. Pharmacol.

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One of the major limitations in the clinical use of existing oxazolidinone antibiotics is their characteristic adverse reactions, in particular thrombocytopenia. In anti-infective treatment, if patients are suspected of having drug-induced thrombocytopenia, the first step is to immediately discontinue the offending drug. Even in patients with severe infections, the antibacterial drug may need to be changed or the antibacterial treatment may need to be discontinued because thrombocytopenia may have a more serious clinical prognosis. In addition, if the patient needs to continue antibacterial treatment after discharge, the lack of conditions for monitoring platelet levels may also pose hidden dangers to the patient. Contezolid is an orally administered oxazolidinone antibacterial agent approved by the National Medical Products Administration of China in 2021. We found that contezolid may have an improved safety profile with a significantly reduced potential for myelosuppression based on the results of our observational clinical study. In this article, we review the advantages of contezolid as a new oxazolidinone antibiotic and describe three typical clinical cases of patients who experienced drug-induced thrombocytopenia after using linezolid. The platelet levels of these different patients were all significantly improved to varying degrees after initiation of contezolid treatment.

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In vitro Activity of Contezolid Against Methicillin-Resistant Staphylococcus aureus, Vancomycin-Resistant Enterococcus, and Strains With Linezolid Resistance Genes From China

Cited by 15 publications

References 27 publications

Sequential Therapy of Linezolid and Contezolid to Treat Vancomycin-Resistant Enterococcus faecium Pneumonia in a Centenarian Patient: Case Report

Sequential Therapy of Linezolid and Contezolid to Treat Vancomycin-Resistant Enterococcus faecium Pneumonia in a Centenarian Patient: Case Report

Antibacterial and anti-biofilm activity of radezolid against Staphylococcus aureus clinical isolates from China

Contezolid, a novel oxazolidinone antibiotic, may improve drug-related thrombocytopenia in clinical antibacterial treatment

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