Eravacycline pharmacokinetics and challenges in defining humanized exposure in vivo

Abrar K. Thabit, Marguerite L. Monogue, David P. Nicolau

Research output: Contribution to journalArticle

16 Scopus citations

Abstract

We assessed the pharmacokinetic profile of eravacycline, a novel antibiotic of the tetracycline class, and determined the dose in an immunocompetent murine thigh infection model that would provide free-drug exposure similar to that observed in humans after the administration of 1 mg/kg intravenously (i.v.) every 12 h (q12h). Eravacycline demonstrated a nonlinear protein-binding profile. The 2.5-mg/kg i.v. q12h dose in mice resulted in an area under the concentration-time curve for the free, unbound fraction of the drug of 1.64 mg·h/liter, which closely resembles the human exposure level.

Original languageEnglish (US)
Pages (from-to)5072-5075
Number of pages4
JournalAntimicrobial agents and chemotherapy
Volume60
Issue number8
DOIs
StatePublished - Aug 2016
Externally publishedYes

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)
  • Infectious Diseases

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