Abstract：
:Tigecycline is highly active against various drug-resistant bacteria. The US Food and Drug Administration (FDA) recently issued a black box warning for tigecycline owing to an associated increase in all-cause mortality. Clinical breakpoints of antibiotics are vital in susceptibility testing of pathogens for the selection of antibiotic therapy; however, no consensus exists between different committees on the clinical breakpoints of tigecycline. Of note, tigecycline exhibits atypical non-linear plasma protein binding (PPB) behaviour, and the pivotal probability of target attainment (PTA) analysis for the determination of clinical breakpoints did not account for the PPB of tigecycline. In this work, the PTA analysis was performed with consideration of atypical non-linear PPB behaviour of tigecycline. A model describing atypical non-linear PPB was developed and validated. Monte Carlo simulations were performed to determine the target ratio of area under the free drug concentration-time curve to minimum inhibitory concentration (fAUC/MIC) for Escherichia coli and, subsequently, PTA analyses were performed. The target fAUC/MIC ratio for E. coli was determined as 2.05, whilst the target AUC/MIC ratio was 6.96. The PTA analyses suggest a lower clinical breakpoint of tigecycline against E. coli. This finding suggests that there is a need to revisit the current clinical breakpoints of tigecycline.
journal_name
Int J Antimicrob Agentsjournal_title
International journal of antimicrobial agentsauthors
Singh RSP,Mukker JK,Drescher SK,Deitchman AN,Derendorf Hdoi
10.1016/j.ijantimicag.2016.12.008subject
Has Abstractpub_date
2017-04-01 00:00:00pages
449-455issue
4eissn
0924-8579issn
1872-7913pii
S0924-8579(17)30047-Xjournal_volume
49pub_type
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journal_title：International journal of antimicrobial agents
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journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
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pub_type： 杂志文章
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journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
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journal_title：International journal of antimicrobial agents
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journal_title：International journal of antimicrobial agents
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