109906
论文已发表
注册即可获取德孚的最新动态
IF 收录期刊
- 3.4 Breast Cancer (Dove Med Press)
- 3.2 Clin Epidemiol
- 2.6 Cancer Manag Res
- 2.9 Infect Drug Resist
- 3.7 Clin Interv Aging
- 5.1 Drug Des Dev Ther
- 3.1 Int J Chronic Obstr
- 6.6 Int J Nanomed
- 2.6 Int J Women's Health
- 2.9 Neuropsych Dis Treat
- 2.8 OncoTargets Ther
- 2.0 Patient Prefer Adher
- 2.2 Ther Clin Risk Manag
- 2.5 J Pain Res
- 3.0 Diabet Metab Synd Ob
- 3.2 Psychol Res Behav Ma
- 3.4 Nat Sci Sleep
- 1.8 Pharmgenomics Pers Med
- 2.0 Risk Manag Healthc Policy
- 4.1 J Inflamm Res
- 2.0 Int J Gen Med
- 3.4 J Hepatocell Carcinoma
- 3.0 J Asthma Allergy
- 2.2 Clin Cosmet Investig Dermatol
- 2.4 J Multidiscip Healthc
已发表论文
康泽立（Contezolid）用于超高龄人群：通过药代动力学洞察平衡疗效与安全性
Authors Liu T, Liang B, Liu B, Huang D, Zhang N, Fang X, Li H , Cai Y
Received 16 July 2025
Accepted for publication 27 October 2025
Published 11 November 2025 Volume 2025:20 Pages 1963—1973
DOI https://doi.org/10.2147/CIA.S554322
Checked for plagiarism Yes
Review by Single anonymous peer review
Peer reviewer comments 2
Editor who approved publication: Prof. Dr. Nandu Goswami
Tingting Liu,1,* Beibei Liang,2,* Bing Liu,3,* Dengfeng Huang,2 Na Zhang,2 Xiangqun Fang,1 Hongxia Li,1 Yun Cai2
1Department of Pulmonary and Critical Care Medicine, The Second Medical Center and National Clinical Research Center for Geriatric Diseases, Chinese PLA General Hospital, Beijing, 100853, People’s Republic of China; 2Center of Medicine Clinical Research, Department of Pharmacy, Medical Supplies Center, The First Medical Center of Chinese PLA General Hospital, Beijing, 100853, People’s Republic of China; 3Department of Adult Cardiac Surgery, The Sixth Medical Center of Chinese PLA General Hospital, Beijing, 100853, People’s Republic of China
*These authors contributed equally to this work
Correspondence: Yun Cai, Email caicai_hh@126.com Hongxia Li, Email lhxia301@126.com
Background: Contezolid is a new oxazolidinone antibacterial agent, and its pharmacokinetic (PK) characteristics and safety in super-elderly patients remain poorly understood.
Methods: Contezolid PK parameters were analyzed in enrolled super-elderly patients (≥ 80 years), with systematic assessment of steady-state profiles and adverse events.
Results: Thirteen super-elderly patients (mean age: 94.9 ± 4.8 years) were included in the study. The plasma concentrations of contezolid peaked at 2– 3h post administration. Both Cmax and AUC0-t exhibited dose-dependent increases across regimens (400 mg q24h, 400 mg q12h, and 800 mg q12h). When receiving a dosage of 800 mg q12h, super-elderly patients demonstrated comparable Cmax (20.32 vs 26.45 mg/L), AUC0-t (97.80 vs 90.38 h·mg/L), and clearance (9.08 vs 10.20 L/h) values to those of healthy adults but prolonged Tmax (2.67 vs 0.57 h) and shorter t1/2 values (2.33 vs 4.84 h). For pathogens with a minimum inhibitory concentration (MIC) ≤ 1 mg/L, 400 mg of contezolid q12h resulted in a > 90% probability of target attainment (PTA), whereas doubling the dose to 800 mg q12h resulted in a PTA > 90% against pathogens with MICs of 2– 4 mg/L. Contezolid was well tolerated, with mild gastrointestinal adverse reactions (vomiting, n=2) and elevated AST (n=1), γ-GT (n=2), and lipase (n=1) levels. According to a self-controlled analysis of 9 patients who switched from linezolid to contezolid, the incidence of thrombocytopenia was significantly lower when taking contezolid (11.1% vs 77.8%).
Conclusion: Contezolid has comparable PKs in super-elderly and healthy adults. While a dosage of 400 mg q12h is sufficient for pathogens with MICs ≤ 1 mg/L, a higher dosage of 800 mg q12h is recommended for higher MICs (2– 4 mg/L), with both doses demonstrating favorable safety.
Clinical Trial Registration Number: ChiCTR2200056377; 4/2/2022.
Keywords: contezolid, super-elderly patients, pharmacokinetics, optimal dose regimens, safety
1Department of Pulmonary and Critical Care Medicine, The Second Medical Center and National Clinical Research Center for Geriatric Diseases, Chinese PLA General Hospital, Beijing, 100853, People’s Republic of China; 2Center of Medicine Clinical Research, Department of Pharmacy, Medical Supplies Center, The First Medical Center of Chinese PLA General Hospital, Beijing, 100853, People’s Republic of China; 3Department of Adult Cardiac Surgery, The Sixth Medical Center of Chinese PLA General Hospital, Beijing, 100853, People’s Republic of China
*These authors contributed equally to this work
Correspondence: Yun Cai, Email caicai_hh@126.com Hongxia Li, Email lhxia301@126.com
Background: Contezolid is a new oxazolidinone antibacterial agent, and its pharmacokinetic (PK) characteristics and safety in super-elderly patients remain poorly understood.
Methods: Contezolid PK parameters were analyzed in enrolled super-elderly patients (≥ 80 years), with systematic assessment of steady-state profiles and adverse events.
Results: Thirteen super-elderly patients (mean age: 94.9 ± 4.8 years) were included in the study. The plasma concentrations of contezolid peaked at 2– 3h post administration. Both Cmax and AUC0-t exhibited dose-dependent increases across regimens (400 mg q24h, 400 mg q12h, and 800 mg q12h). When receiving a dosage of 800 mg q12h, super-elderly patients demonstrated comparable Cmax (20.32 vs 26.45 mg/L), AUC0-t (97.80 vs 90.38 h·mg/L), and clearance (9.08 vs 10.20 L/h) values to those of healthy adults but prolonged Tmax (2.67 vs 0.57 h) and shorter t1/2 values (2.33 vs 4.84 h). For pathogens with a minimum inhibitory concentration (MIC) ≤ 1 mg/L, 400 mg of contezolid q12h resulted in a > 90% probability of target attainment (PTA), whereas doubling the dose to 800 mg q12h resulted in a PTA > 90% against pathogens with MICs of 2– 4 mg/L. Contezolid was well tolerated, with mild gastrointestinal adverse reactions (vomiting, n=2) and elevated AST (n=1), γ-GT (n=2), and lipase (n=1) levels. According to a self-controlled analysis of 9 patients who switched from linezolid to contezolid, the incidence of thrombocytopenia was significantly lower when taking contezolid (11.1% vs 77.8%).
Conclusion: Contezolid has comparable PKs in super-elderly and healthy adults. While a dosage of 400 mg q12h is sufficient for pathogens with MICs ≤ 1 mg/L, a higher dosage of 800 mg q12h is recommended for higher MICs (2– 4 mg/L), with both doses demonstrating favorable safety.
Clinical Trial Registration Number: ChiCTR2200056377; 4/2/2022.
Keywords: contezolid, super-elderly patients, pharmacokinetics, optimal dose regimens, safety