contezolid

has antibacterial activity; structure in first source

Also Known As:

4(1H)-Pyridinone, 2,3-dihydro-1-(2,3,6-trifluoro-4-((5S)-5-((3-isoxazolylamino)methyl)-2-oxo-3-oxazolidinyl)phenyl)-; 5-((isoxazol-3-ylamino)methyl)-3-(2,3,5-trifluoro-4-(4-oxo-3,4-dihydropyridin-1(2H)-yl)phenyl)oxazolidin-2-one; MRX-I compound

Networked: 29 relevant articles (4 outcomes, 7 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- 1-Ring Heterocyclic Compounds
  - Azoles: 2138
    - Oxazoles: 89
      - Oxazolidinones: 316
        contezolid: 29
  - Pyridines: 88
    - Pyridones: 14
      - contezolid: 29

Experts

1.	Yuan, Hong: 5 articles (01/2022 - 01/2019)
2.	Cao, Guoying: 4 articles (01/2022 - 01/2019)
3.	Chen, Yuancheng: 4 articles (01/2022 - 01/2019)
4.	Guo, Beining: 4 articles (01/2022 - 01/2019)
5.	Wu, Jufang: 4 articles (01/2022 - 01/2019)
6.	Wu, Xiaojie: 4 articles (01/2022 - 01/2019)
7.	Yu, Jicheng: 4 articles (01/2022 - 01/2019)
8.	Zhang, Jing: 4 articles (01/2022 - 01/2019)
9.	Wu, Hailan: 3 articles (01/2022 - 01/2019)
10.	Wu, Junzhen: 3 articles (01/2022 - 01/2019)

Related Diseases

1.	Infections 01/01/2019 - "Contezolid is a well-tolerated treatment option for MRSA infection, including at supratherapeutic doses up to 1600 mg. " 01/01/2019 - "To our knowledge, this is the first PK study to predict that a dosing regimen of 800 mg q12h of oral contezolid is sufficient for treating MRSA infection, with a MIC of ≤4 mg/L. " 01/01/2021 - "In general, contezolid may have potential benefits to treat the infections caused by MRSA and VRE pathogens." 01/01/2019 - "PK/PD analysis and Monte Carlo simulations predicted that 800 mg q12h of oral contezolid would be efficacious against MRSA infection, with a MIC of ≤4 mg/L (probability of target attainment, >90%; cumulative fraction of response, >90%). " 09/01/2021 - "Contezolid is also undergoing clinical development for acute bacterial skin and skin structure infections (ABSSSI) in the USA, and for diabetic foot infections. "
2.	Soft Tissue Infections 07/01/2022 - "Contezolid in complicated skin and soft tissue infection." 01/01/2022 - "Clinical Pharmacology and Utility of Contezolid in Chinese Patients with Complicated Skin and Soft-Tissue Infections." 10/28/2022 - "A Phase III multicentre, randomized, double-blind trial to evaluate the efficacy and safety of oral contezolid versus linezolid in adults with complicated skin and soft tissue infections-authors' response." 10/28/2022 - "Comment on: A Phase III multicentre, randomized, double-blind trial to evaluate the efficacy and safety of oral contezolid versus linezolid in adults with complicated skin and soft tissue infections." 01/01/2022 - "This study aimed to build a population pharmacokinetic (PopPK) model for contezolid tablet (MRX-I) in healthy subjects and adults with complicated skin and soft-tissue infections (cSSTIs) to further evaluate the efficacy and safety of contezolid and recommend the optimal dosing regimen based on pharmacokinetic/pharmacodynamic (PK/PD) analysis. "
3.	Multidrug-Resistant Tuberculosis (Drug-Resistant Tuberculosis) 05/17/2022 - "Prospects of contezolid (MRX-I) against multidrug-resistant tuberculosis and extensively drug-resistant tuberculosis." 11/15/2023 - "Pre-clinical and clinical safety studies suggest it may be less toxic than linezolid, making contezolid a potential candidate to replace linezolid in the treatment of drug-resistant tuberculosis. "
4.	Tuberculosis (Tuberculoses) 08/01/2023 - "tuberculosis, and were close to the estimated serum unbound fraction of contezolid (10%), suggesting that unbound contezolid has high CSF permeability." 01/01/2023 - "Rare tuberculosis in recipients of allogeneic hematopoietic stem cell transplantation successfully treated with contezolid-a typical case report and literature review." 10/18/2022 - "While contezolid is an attractive drug candidate with potent antimycobacterial activity and low toxicity, the occurrence of mutations in Mce3R should be considered when designing combination therapy using contezolid for treating tuberculosis." 01/01/2023 - "Clinical Utility of Contezolid-Containing Regimens in 25 Cases of Linezolid-Intolerable Tuberculosis Patients." 11/15/2023 - "We evaluated the dose-ranging activity of contezolid, alone and in combination with bedaquiline and pretomanid, and compared it with linezolid at similar doses, in an established BALB/c mouse model of tuberculosis. "
5.	Thrombocytopenia (Thrombopenia) 01/01/2022 - "Contezolid demonstrated significant lower incidence of leucopenia (0.3% versus 3.4%) and thrombocytopenia (0% versus 2.3%) than linezolid. " 01/01/2023 - "During anti-TB treatment, the patient had a poor response to linezolid-containing regimen, and developed side effects such as gingival bleeding and thrombocytopenia, so the administration was switched to contezolid. " 01/01/2023 - "Contezolid, a novel oxazolidinone antibiotic, may improve drug-related thrombocytopenia in clinical antibacterial treatment." 01/01/2023 - "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. "

Related Drugs and Biologics

1.	Oxazolidinones (2 Oxazolidone)
2.	Anti-Bacterial Agents (Antibiotics)
3.	Linezolid (Zyvox)
4.	Prodrugs
5.	tedizolid phosphate
6.	Tablets
7.	Vancomycin
8.	Methicillin (Metin)
9.	Anti-Infective Agents (Microbicides)
10.	Albumins

Related Therapies and Procedures

1.	Intravenous Administration
2.	Oral Administration
3.	Injections
4.	Therapeutics
5.	Hematopoietic Stem Cell Transplantation