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已发表论文
替加环素的群体药代动力学及其对个体化治疗优化的影响：系统综述
Authors Dai A, Zheng F, Liu J, Chen Q, Zhou Z, Yu L , Yu Z , Guan Y
Received 14 July 2025
Accepted for publication 7 November 2025
Published 11 November 2025 Volume 2025:19 Pages 10045—10060
DOI https://doi.org/10.2147/DDDT.S553622
Checked for plagiarism Yes
Review by Single anonymous peer review
Peer reviewer comments 2
Editor who approved publication: Professor Anastasios Lymperopoulos
Anran Dai,1 Feiyue Zheng,1 Jieqiong Liu,1 Qianping Chen,2 Zhou Zhou,3 Lingyan Yu,4,5 Zhenwei Yu,1,5 Yan Guan1
1Department of Pharmacy, Sir Run Run Shaw Hospital, Zhejiang University School of Medicine, Hangzhou, People’s Republic of China; 2School of Basic Medicine and Clinical Pharmacy, China Pharmaceutical University, Nanjing, People’s Republic of China; 3Department of Pharmacy, Nanjing First Hospital, Nanjing Medical University, Nanjing, People’s Republic of China; 4Department of Pharmacy, The Second Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou, People’s Republic of China; 5Research Center for Clinical Pharmacy, College of Pharmaceutical Science, Zhejiang University, Hangzhou, People’s Republic of China
Correspondence: Zhenwei Yu, Department of Pharmacy, Sir Run Run Shaw Hospital, Zhejiang University School of Medicine, 3 rd East Qingchun Road, Hangzhou, 310016, People’s Republic of China, Email yzw_srrsh@zju.edu.cn
Background: Tigecycline, owing to its broad-spectrum antimicrobial activity, has emerged as an important option in the treatment of infections. However, its optimal dosing strategy remains controversial in clinical practice. Recent studies have provided valuable insights into the population pharmacokinetics (PopPK) of tigecycline. This review aims to synthesize the current literature to offer theoretical guidance for individualized clinical management.
Methods: A systematic search of PopPK studies on tigecycline published from inception to April 2025 was conducted in the PubMed and Web of Science databases. The pharmacokinetics of tigecycline in different populations were systematically reviewed following the PRISMA (Preferred Reporting Items for Systematic Reviews and Meta-Analyses) guidelines.
Results: 16 studies were included, of which 11 focused on critically ill populations (such as those with severe infections, sepsis, renal replacement therapy, multi-drug resistant Gram-negative infections, and impaired liver function, etc). The majority of studies (12/16) adopted a two-compartment model, with the typical parameter ranges as follows: clearance (CL) 3.09– 25.2 L/h, intercompartmental clearance (Q) 31.9– 85.1 L/h, central volume of distribution (V1) 30.9– 162 L, and peripheral volume of distribution (V2) 87.9– 1030 L. This systematic analysis suggested that covariates influencing tigecycline pharmacokinetics were primarily classified into three categories: hepatic function indicators, renal function markers, and body weight-related parameters. All included models underwent internal validation.
Conclusion: Based on the existing evidence, it is recommended to use high-dose tigecycline (100mg, q12h) for drug-resistant bacterial infections, cSSI and VAP, and consider combination therapy. Individualized dose adjustment should be based on liver function and the degree of drug resistance of the pathogen, without considering renal function. The application of other covariates and the model needs to be further verified.
Keywords: tigecycline, population pharmacokinetics, model, covariate, NONMEM
1Department of Pharmacy, Sir Run Run Shaw Hospital, Zhejiang University School of Medicine, Hangzhou, People’s Republic of China; 2School of Basic Medicine and Clinical Pharmacy, China Pharmaceutical University, Nanjing, People’s Republic of China; 3Department of Pharmacy, Nanjing First Hospital, Nanjing Medical University, Nanjing, People’s Republic of China; 4Department of Pharmacy, The Second Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou, People’s Republic of China; 5Research Center for Clinical Pharmacy, College of Pharmaceutical Science, Zhejiang University, Hangzhou, People’s Republic of China
Correspondence: Zhenwei Yu, Department of Pharmacy, Sir Run Run Shaw Hospital, Zhejiang University School of Medicine, 3 rd East Qingchun Road, Hangzhou, 310016, People’s Republic of China, Email yzw_srrsh@zju.edu.cn
Background: Tigecycline, owing to its broad-spectrum antimicrobial activity, has emerged as an important option in the treatment of infections. However, its optimal dosing strategy remains controversial in clinical practice. Recent studies have provided valuable insights into the population pharmacokinetics (PopPK) of tigecycline. This review aims to synthesize the current literature to offer theoretical guidance for individualized clinical management.
Methods: A systematic search of PopPK studies on tigecycline published from inception to April 2025 was conducted in the PubMed and Web of Science databases. The pharmacokinetics of tigecycline in different populations were systematically reviewed following the PRISMA (Preferred Reporting Items for Systematic Reviews and Meta-Analyses) guidelines.
Results: 16 studies were included, of which 11 focused on critically ill populations (such as those with severe infections, sepsis, renal replacement therapy, multi-drug resistant Gram-negative infections, and impaired liver function, etc). The majority of studies (12/16) adopted a two-compartment model, with the typical parameter ranges as follows: clearance (CL) 3.09– 25.2 L/h, intercompartmental clearance (Q) 31.9– 85.1 L/h, central volume of distribution (V1) 30.9– 162 L, and peripheral volume of distribution (V2) 87.9– 1030 L. This systematic analysis suggested that covariates influencing tigecycline pharmacokinetics were primarily classified into three categories: hepatic function indicators, renal function markers, and body weight-related parameters. All included models underwent internal validation.
Conclusion: Based on the existing evidence, it is recommended to use high-dose tigecycline (100mg, q12h) for drug-resistant bacterial infections, cSSI and VAP, and consider combination therapy. Individualized dose adjustment should be based on liver function and the degree of drug resistance of the pathogen, without considering renal function. The application of other covariates and the model needs to be further verified.
Keywords: tigecycline, population pharmacokinetics, model, covariate, NONMEM