Comparative <i>in vitro</i> potency and kill curve activity of tedizolid and linezolid against Gram-positive bacteria isolated from Chinese hospitalized patients in 2013–2016

Wang, Shan; Li, Yun; Xue, Feng; Liu, Jian; Yang, Weiwei; Zhang, Jia; Glenschek-Sieberth, Martin; Lyu, Yuan

doi:10.1080/1120009x.2019.1623968

Cited by 2 publications

(2 citation statements)

References 27 publications

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“…A two-compartment model with sigmoidal absorption and linear elimination was developed that successfully described the plasma disposition kinetics when applied to the pooled data from seven clinical studies (phase I-III) [10]. Neither a clinically important covariate nor ethnic differences affected the PK disposition significantly [11][12][13][14]. The PK characteristics are shown in Table 1.…”

Section: Pk Profile In Healthy Subjectsmentioning

confidence: 99%

“…Its moderate activity against anaerobes particularly against Bacteroides fragilis (MIC 90 of 1 mg/L) can be exploited to treat mixed aerobic and anaerobic infection [67]. Tedizolid expresses good activity against several clinically relevant respiratory pathogens such as PRSP (MIC 90 of 0.25 mg/L) and PSSP (MIC 90 of 0.125-0.25 mg/L) and has a clinical potential to treat respiratory infections [12,35,49,68].…”

Section: Antimicrobial Spectrummentioning

confidence: 99%

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Pharmacokinetics and Pharmacodynamics of Tedizolid

2022

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Tedizolid is an oxazolidinone antibiotic with high potency against Gram-positive bacteria and currently prescribed in bacterial skin and skin-structure infections. The aim of the review was to summarize and critically review the key pharmacokinetic and pharmacodynamic aspects of tedizolid. Tedizolid displays linear pharmacokinetics with good tissue penetration. In in vitro susceptibility studies, tedizolid exhibits activity against the majority of Gram-positive bacteria (minimal inhibitory concentration [MIC] of ≤ 0.5 mg/L), is four-fold more potent than linezolid, and has the potential to treat pathogens being less susceptible to linezolid. Area under the unbound concentration-time curve (fAUC) related to MIC (fAUC/MIC) was best correlated with efficacy. In neutropenic mice, fAUC/MIC of ~ 50 and ~ 20 induced bacteriostasis in thigh and pulmonary infection models, respectively, at 24 h. The presence of granulocytes augmented its antibacterial effect. Hence, tedizolid is currently not recommended for immunocompromised patients. Clinical investigations with daily doses of 200 mg for 6 days showed non-inferiority to twice-daily dosing of linezolid 600 mg for 10 days in patients with acute bacterial skin and skin-structure infections. In addition to its use in skin and skin-structure infections, the high pulmonary penetration makes it an attractive option for respiratory infections including Mycobacterium tuberculosis. Resistance against tedizolid is rare yet effective antimicrobial surveillance and defining pharmacokinetic/pharmacodynamic targets for resistance suppression are needed to guide dosing strategies to suppress resistance development.

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Section: Pk Profile In Healthy Subjectsmentioning

confidence: 99%

Section: Antimicrobial Spectrummentioning

confidence: 99%

Pharmacokinetics and Pharmacodynamics of Tedizolid

2022

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Determination of Tedizolid in Bacterial Growth Medium Mueller-Hinton Broth by High-Performance Liquid Chromatography and Its Application to an In Vitro Study in the Hollow-Fiber Infection Model

et al. 2021

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Pharmacokinetic/pharmacodynamic (PKPD) studies of anti-infectives are frequently performed in in vitro infection models where accurate quantification of antibiotic concentrations in bacterial growth media is crucial to establish PK/PD relationships. Here, a sensitive and rapid high-performance liquid chromatography (HPLC) method was developed to quantify tedizolid (TDZ) in the bacterial growth medium Mueller-Hinton broth (MHB). Matrix components were separated by direct protein precipitation with methanol (1:1). The chromatographic separation was carried out in a Dionex Ultimate 3000 HPLC system using an Accucore® C-18 RPMS HPLC column (2.6 µm, 100 × 2.1 mm) using isocratic elution with 25% acetonitrile and 75% of 0.1% formic acid. The lower limit of quantification was 0.03 mg/L when measured at 300 nm. Following relevant European Medicine Agency guidelines, the method was successfully validated for linearity, selectivity, recovery, inter- and intra-day precision, and accuracy and stability. When applied to in vitro PKPD studies, the method successfully quantified a range of TDZ concentration (Cmin, 0.09-Cmax, 0.65 mg/L) in MHB. The analyzed concentrations were in line with the planned PK profiles. The application of the developed method to quantify TDZ in MHB in in vitro PKPD studies is warranted.

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Comparative in vitro potency and kill curve activity of tedizolid and linezolid against Gram-positive bacteria isolated from Chinese hospitalized patients in 2013–2016

Cited by 2 publications

References 27 publications

Pharmacokinetics and Pharmacodynamics of Tedizolid

Pharmacokinetics and Pharmacodynamics of Tedizolid

Determination of Tedizolid in Bacterial Growth Medium Mueller-Hinton Broth by High-Performance Liquid Chromatography and Its Application to an In Vitro Study in the Hollow-Fiber Infection Model

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