Dalbavancin exposure in vitro selects for dalbavancin-non-susceptible and vancomycin-intermediate strains of methicillin-resistant Staphylococcus aureus.


Journal

Clinical microbiology and infection : the official publication of the European Society of Clinical Microbiology and Infectious Diseases
ISSN: 1469-0691
Titre abrégé: Clin Microbiol Infect
Pays: England
ID NLM: 9516420

Informations de publication

Date de publication:
Jun 2021
Historique:
received: 08 05 2020
revised: 13 08 2020
accepted: 21 08 2020
pubmed: 1 9 2020
medline: 26 8 2021
entrez: 1 9 2020
Statut: ppublish

Résumé

Dalbavancin is a lipoglycopeptide active against methicillin-resistant Staphylococcus aureus (MRSA). Its long half-life (8.5-16 days) allows for once-weekly or single-dose treatments but could prolong the mutant selection window, promoting resistance and cross-resistance to related antimicrobials such as vancomycin. The objective of this study was to evaluate the capacity of post-distributional pharmacokinetic exposures of dalbavancin to select for resistance and cross-resistance in MRSA. We simulated average, post-distributional exposures of single-dose (1500 mg) dalbavancin (fCmax 9.9 μg/mL, β-elimination t Dalbavancin was bactericidal against most strains for days 1-4 before regrowth of less susceptible subpopulations occurred. Isolates with eight-fold increases in dalbavancin MIC were detected as early as day 4 but increased 64-128-fold in all models by day 28. Vancomycin and daptomycin MICs increased 4-16-fold, exceeding the susceptibly breakpoints for both antibiotics; β-lactam MICs generally decreased by two-to eight-fold, suggesting a dalbavancin-β-lactam seesaw effect, but increased by eight-fold or more in certain isolates. Resistant isolates carried mutations in a variety of genes, most commonly walKR, apt, stp1, and atl. In our in vitro system, post-distributional dalbavancin exposures selected for stable mutants with reduced susceptibility to dalbavancin, vancomycin, and daptomycin, and generally increased susceptibility to β-lactams in all strains of MRSA tested. The clinical significance of these findings remains unclear, but created an opportunity to genotype a unique collection of dalbavancin-resistant strains for the first time. Mutations involved genes previously associated with vancomycin intermediate susceptibility and daptomycin non-susceptibility, most commonly walKR-associated genes.

Identifiants

pubmed: 32866650
pii: S1198-743X(20)30508-5
doi: 10.1016/j.cmi.2020.08.025
pmc: PMC7914275
mid: NIHMS1634068
pii:
doi:

Substances chimiques

Anti-Bacterial Agents 0
Teicoplanin 61036-62-2
Vancomycin 6Q205EH1VU
dalbavancin 808UI9MS5K

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

910.e1-910.e8

Subventions

Organisme : NIAID NIH HHS
ID : R01 AI136979
Pays : United States
Organisme : NIAID NIH HHS
ID : R21 AI132994
Pays : United States

Informations de copyright

Copyright © 2020 European Society of Clinical Microbiology and Infectious Diseases. Published by Elsevier Ltd. All rights reserved.

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Auteurs

Brian J Werth (BJ)

Department of Pharmacy, School of Pharmacy, University of Washington, Seattle, WA, USA. Electronic address: bwerth@uw.edu.

Nathaniel K Ashford (NK)

Department of Pharmacy, School of Pharmacy, University of Washington, Seattle, WA, USA.

Kelsi Penewit (K)

Department of Laboratory Medicine, School of Pharmacy, University of Washington, Seattle, WA, USA.

Adam Waalkes (A)

Department of Laboratory Medicine, School of Pharmacy, University of Washington, Seattle, WA, USA.

Elizabeth A Holmes (EA)

Department of Laboratory Medicine, School of Pharmacy, University of Washington, Seattle, WA, USA.

Dylan H Ross (DH)

Department of Medicinal Chemistry, School of Pharmacy, University of Washington, Seattle, WA, USA.

Tianwei Shen (T)

Department of Medicinal Chemistry, School of Pharmacy, University of Washington, Seattle, WA, USA.

Kelly M Hines (KM)

Department of Medicinal Chemistry, School of Pharmacy, University of Washington, Seattle, WA, USA; University of Georgia, Department of Chemistry, Athens, GA, USA.

Stephen J Salipante (SJ)

Department of Laboratory Medicine, School of Pharmacy, University of Washington, Seattle, WA, USA.

Libin Xu (L)

Department of Medicinal Chemistry, School of Pharmacy, University of Washington, Seattle, WA, USA.

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Classifications MeSH