Eravacycline (TP-434) Is Efficacious in Animal Models of Infection
| Autor: | Trudy H. Grossman, Denene Lofland, Andrew M. Slee, Joyce A. Sutcliffe, Timothy M. Murphy |
|---|---|
| Rok vydání: | 2015 |
| Předmět: |
Staphylococcus aureus
Neutropenia medicine.drug_class Antibiotics Microbial Sensitivity Tests Biology medicine.disease_cause Microbiology Mice chemistry.chemical_compound Streptococcus pneumoniae medicine Animals Pharmacology (medical) Escherichia coli Pharmacology Mice Inbred BALB C Lung Pyelonephritis Linezolid Staphylococcal Infections Eravacycline Anti-Bacterial Agents Disease Models Animal Treatment Outcome Infectious Diseases medicine.anatomical_structure Thigh chemistry Tetracyclines Streptococcus pyogenes Female |
| Zdroj: | Antimicrobial Agents and Chemotherapy. 59:2567-2571 |
| ISSN: | 1098-6596 0066-4804 |
| DOI: | 10.1128/aac.04354-14 |
| Popis: | Eravacycline is a novel broad-spectrum fluorocycline antibiotic being developed for a wide range of serious infections. Eravacycline was efficacious in mouse septicemia models, demonstrating 50% protective dose (PD 50 ) values of ≤1 mg/kg of body weight once a day (q.d.) against Staphylococcus aureus , including tetracycline-resistant isolates of methicillin-resistant S. aureus (MRSA), and Streptococcus pyogenes . The PD 50 values against Escherichia coli isolates were 1.2 to 4.4 mg/kg q.d. In neutropenic mouse thigh infection models with methicillin-sensitive S. aureus (MSSA) and S. pyogenes , eravacycline produced 2 log 10 reductions in CFU at single intravenous (i.v.) doses ranging from 0.2 to 9.5 mg/kg. In a neutropenic mouse lung infection model, eravacycline administered i.v. at 10 mg/kg twice a day (b.i.d.) reduced the level of tetracycline-resistant MRSA in the lung equivalent to that of linezolid given orally (p.o.) at 30 mg/kg b.i.d. At i.v. doses of 3 to 12 mg/kg b.i.d., eravacycline was more efficacious against tetracycline-resistant Streptococcus pneumoniae in a neutropenic lung infection model than linezolid p.o. at 30 mg/kg b.i.d. Eravacycline showed good efficacy at 2 to 10 mg/kg i.v. b.i.d., producing up to a 4.6 log 10 CFU reduction in kidney bacterial burden in a model challenged with a uropathogenic E. coli isolate. Eravacycline was active in multiple murine models of infection against clinically important Gram-positive and Gram-negative pathogens. |
| Databáze: | OpenAIRE |
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