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Eravacycline

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https://www.readbyqxmd.com/read/28893690/new-agents-for-the-treatment-of-infections-with-gram-negative-bacteria-restoring-the-miracle-or-false-dawn
#1
REVIEW
H Wright, R A Bonomo, D L Paterson
BACKGROUND: Antibiotic resistance in Gram-negative resistance has developed without a commensurate response in the successful development of antibiotic agents, though recent progress has been made. AIMS: This review aims to provide a summary of the existing evidence on efficacy, spectrum of activity and the development of resistance of new agents that have been licensed or have completed advanced clinical trials and that possess activity against resistant Gram-negative organisms...
October 2017: Clinical Microbiology and Infection
https://www.readbyqxmd.com/read/28705668/in-vitro-activity-of-the-novel-fluorocycline-eravacycline-against-carbapenem-non-susceptible-acinetobacter-baumannii
#2
Harald Seifert, Danuta Stefanik, Joyce A Sutcliffe, Paul G Higgins
The activity of eravacycline was compared with anti-Acinetobacter reference antimicrobials against carbapenem non-susceptible Acinetobacter baumannii isolates associated with an acquired OXA or up-regulation of the intrinsic OXA-51-like enzyme. Antimicrobial susceptibility testing was performed by broth microdilution of 286 non-duplicate, carbapenem non-susceptible A. baumannii isolates to eravacycline, amikacin colistin, doxycycline, imipenem, levofloxacin, meropenem, minocycline, sulbactam, tigecycline, and tobramycin...
July 10, 2017: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/28559729/biosynthesis-of-oxytetracycline-by-streptomyces-rimosus-%C3%A2-past-present-and-future-directions-in-the-development%C3%A2-of-tetracycline-antibiotics
#3
REVIEW
Hrvoje Petković, Tadeja Lukežič, Jagoda Šušković
Natural tetracycline (TC) antibiotics were the first major class of therapeutics to earn the distinction of 'broad-spectrum antibiotics' and they have been used since the 1940s against a wide range of both Gram-positive and Gram-negative pathogens, mycoplasmas, intracellular chlamydiae, rickettsiae and protozoan parasites. The second generation of semisynthetic tetracyclines, such as minocycline and doxycycline, with improved antimicrobial potency, were introduced during the 1960s. Despite emerging resistance to TCs erupting during the 1980s, it was not until 2006, more than four decades later, that a third--generation TC, named tigecycline, was launched...
March 2017: Food Technology and Biotechnology
https://www.readbyqxmd.com/read/28505331/antimicrobial-susceptibility-of-clinical-isolates-of-neisseria-gonorrhoeae-to-alternative-antimicrobials-with-therapeutic-potential
#4
P R S Lagacé-Wiens, H J Adam, N M Laing, M R Baxter, I Martin, M R Mulvey, J A Karlowsky, D J Hoban, G G Zhanel
Background: The prevalence of MDR Neisseria gonorrhoeae is increasing globally and represents a public health emergency. Development and approval of new anti-gonococcal agents may take years. As a concurrent approach to developing new antimicrobials, the laboratory and clinical evaluation of currently licensed antimicrobials not widely used for the treatment of gonorrhoea may provide new options for the treatment of gonococcal infections. Objectives: To determine the in vitro activity of nine alternative, currently licensed and late-development antimicrobials with the potential to treat gonococcal infections against 112 clinical isolates of N...
August 1, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28416552/in-vivo-pharmacodynamic-target-assessment-of-eravacycline-against-escherichia-coli-in-a-murine-thigh-infection-model
#5
Miao Zhao, Alexander J Lepak, Karen Marchillo, Jamie VanHecker, David R Andes
Eravacycline is a novel fluorocycline antibiotic with potent activity against a broad range of pathogens, including strains with tetracycline and other drug resistance phenotypes. The goal of the studies was to determine which pharmacokinetic/pharmacodynamic (PK/PD) parameter and magnitude best correlated with efficacy in the murine thigh infection model. Six Escherichia coli isolates were utilized for the studies. MICs were determined using CLSI methods and ranged from 0.125 to 0.25 mg/liter. A neutropenic murine thigh infection model was utilized for all treatment studies...
July 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28333250/the-complexity-of-minocycline-serum-protein-binding
#6
Jian Zhou, Brian T Tran, Vincent H Tam
Objectives: Serum protein binding is critical for understanding the pharmacology of antimicrobial agents. Tigecycline and eravacycline were previously reported to have atypical non-linear protein binding; the percentage of free fraction decreased with increasing total concentration. In this study, we extended the investigation to other tetracyclines and examined the factors that might impact protein binding. Methods: Different minocycline concentrations (0.5-50 mg/L) and perfusion media (saline, 0...
June 1, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28002943/a-divergent-route-to-eravacycline
#7
Wu-Yan Zhang, Qinglin Che, Scott Crawford, Magnus Ronn, Nicholas Dunwoody
A convergent route to eravacycline (1) has been developed by employing Michael-Dieckmann cyclization between enone 3 and a fully built and protected left-hand piece (LHP, 2). After construction of the core eravacycline structure, a deprotection reaction was developed, allowing for the isoxazole ring opening and global deprotection to be achieved in one pot. The LHP is synthesized from readily available 4-fluoro-3-methylphenol in six steps featuring a palladium-catalyzed phenyl carboxylation in the last step...
January 6, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/27851857/assessing-the-efficacy-and-safety-of-eravacycline-vs-ertapenem-in-complicated-intra-abdominal-infections-in-the-investigating-gram-negative-infections-treated-with-eravacycline-ignite-1-trial-a-randomized-clinical-trial
#8
Joseph Solomkin, David Evans, Algirdas Slepavicius, Patrick Lee, Andrew Marsh, Larry Tsai, Joyce A Sutcliffe, Patrick Horn
Importance: Eravacycline is a novel, fully synthetic fluorocycline antibiotic of the tetracycline class with in vitro activity against clinically important gram-negative, gram-positive aerobic, and facultative bacteria including most of those resistant to cephalosporins, fluoroquinolones, β-lactam/β-lactamase inhibitors, multidrug resistant strains and carbapenem-resistant Enterobacteriaceae, and most anaerobic pathogens. Objective: To evaluate the efficacy and safety of eravacycline compared with ertapenem in adult hospitalized patients with complicated intra-abdominal infections (cIAIs)...
March 1, 2017: JAMA Surgery
https://www.readbyqxmd.com/read/27550359/eravacycline-is-active-against-bacterial-isolates-expressing-the-polymyxin-resistance-gene-mcr-1
#9
LETTER
Corey Fyfe, Gabrielle LeBlanc, Brianna Close, Patrice Nordmann, Jacques Dumas, Trudy H Grossman
No abstract text is available yet for this article.
November 2016: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/27400643/the-antibiotic-pipeline-for-multi-drug-resistant-gram-negative-bacteria-what-can-we-expect
#10
REVIEW
Matthew E Falagas, Andreas D Mavroudis, Konstantinos Z Vardakas
INTRODUCTION: A real concern in the medical community is the increasing resistance of bacteria, especially that of Gram-negative types. New antibiotics are currently under clinical development, promising to tackle severe infections caused, especially, by multi-drug resistant (MDR) bacteria and broaden the armamentarium of clinicians. AREAS COVERED: We searched PUBMED and GOOGLE databases. Combinations of already approved β-lactams or monobactams with new β-lactamase inhibitors [imipenem-cilastatin/MK-7655 (relebactam), meropenem/RPX7009 (vaborbactam), ceftaroline/avibactam, aztreonam/avibactam], new β-lactams (S-649266, BAL30072), aminoglycosides (plazomicin), quinolones (finafloxacin) and tetracyclines (eravacycline) were included in the review...
August 2016: Expert Review of Anti-infective Therapy
https://www.readbyqxmd.com/read/27384881/role-of-newer-and-re-emerging-older-agents-in-the-treatment-of-infections-caused-by-carbapenem-resistant-enterobacteriaceae
#11
Joshua T Thaden, Jason M Pogue, Keith S Kaye
Antimicrobial resistance has been identified by the World Health Organization as "one of the three greatest threats to human health." Gram negative bacteria in particular drive this alarming trend. Carbapenem-resistant Enterobacteriaceae (CRE) such as Escherichia coli, Klebsiella pneumoniae, and Enterobacter species are of particular importance as they are associated with poor clinical outcomes and are common causes for a variety of infections including bacteremia, urinary tract infection, intra-abdominal infections and pneumonia...
May 19, 2017: Virulence
https://www.readbyqxmd.com/read/27353265/antibacterial-efficacy-of-eravacycline-in-vivo-against-gram-positive-and-gram-negative-organisms
#12
Marguerite L Monogue, Abrar K Thabit, Yukihiro Hamada, David P Nicolau
Members of the tetracycline class are frequently classified as bacteriostatic. However, recent findings have demonstrated an improved antibacterial killing profile, often achieving ≥3 log10 bacterial count reduction, when such antibiotics have been given for periods longer than 24 h. We aimed to study this effect with eravacycline, a novel fluorocycline, given in an immunocompetent murine thigh infection model over 72 h against two methicillin-resistant Staphylococcus aureus (MRSA) isolates (eravacycline MICs = 0...
August 2016: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/27353264/eravacycline-pharmacokinetics-and-challenges-in-defining-humanized-exposure-in-vivo
#13
Abrar K Thabit, Marguerite L Monogue, David P Nicolau
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...
August 2016: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/27353166/in-vitro-susceptibility-of-%C3%AE-lactamase-producing-carbapenem-resistant-enterobacteriaceae-cre-to-eravacycline
#14
COMPARATIVE STUDY
Yunliang Zhang, Xiaoyan Lin, Karen Bush
Eravacycline is a novel, fully synthetic fluorocycline antibiotic of the tetracycline class being developed for the treatment of complicated urinary tract infections and complicated intra-abdominal infections. Eravacycline has activity against many key Gram-negative pathogens, including Enterobacteriaceae resistant to carbapenems, cephalosporins, fluoroquinolones and β-lactam/β-lactamase inhibitor combinations, including strains that are multidrug-resistant. Carbapenem-resistant Enterobacteriaceae (CRE) isolates from 2010 to 2013 (n=110) were characterized for carbapenemase genes by PCR and sequencing...
August 2016: Journal of Antibiotics
https://www.readbyqxmd.com/read/27044556/in-vitro-activity-of-eravacycline-against-carbapenem-resistant-enterobacteriaceae-and-acinetobacter-baumannii
#15
David M Livermore, Shazad Mushtaq, Marina Warner, Neil Woodford
Eravacycline and comparators were tested against carbapenem- and tigecycline-resistant Enterobacteriaceae and Acinetobacter isolates received at the United Kingdom's national reference laboratory. Eravacycline MICs correlated closely with those of tigecycline but mostly were around 2-fold lower; both molecules retained full activity against isolates with high-level tetracycline and minocycline resistance. MIC90s of eravacycline and tigecycline were raised ca. 2-fold for carbapenem-resistant Enterobacteriaceae compared with carbapenem-susceptible controls, probably reflecting subsets of isolates with increased efflux...
June 2016: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/27043373/development-of-a-platform-for-the-discovery-and-practical-synthesis-of-new-tetracycline-antibiotics
#16
REVIEW
Fan Liu, Andrew G Myers
Tetracyclines have proven to be safe and effective antibiotics over decades but to date all approved members of the class have been discovered and manufactured by chemical modification of fermentation products, which greatly limits the number of new structures that can be explored as future medicines. This review summarizes research leading to the development of a platform synthetic technology that enabled the discovery of the clinical candidate eravacycline, as well as other promising new tetracycline antibiotics, and provides the basis for a practical route for their manufacture...
June 2016: Current Opinion in Chemical Biology
https://www.readbyqxmd.com/read/27005457/new-drugs-for-the-treatment-of-complicated-intra-abdominal-infections-in-the-era-of-increasing-antimicrobial-resistance
#17
REVIEW
Ling-Shan Syue, Yen-Hsu Chen, Wen-Chien Ko, Po-Ren Hsueh
The continuing increase in multidrug-resistant organisms (MDROs) worldwide has created new challenges in treating complicated intra-abdominal infections (cIAIs). A number of novel antimicrobial agents have been developed against resistant pathogens. To target extended-spectrum β-lactamase (ESBL)-producing pathogens, novel β-lactam antibiotics, such as ceftolozane/tazobactam, ceftazidime/avibactam, aztreonam/avibactam, imipenem/relebactam and S-649266, are antimicrobial alternatives for cIAIs. Two new drugs, eravacycline and plazomicin, have activity against Klebsiella pneumoniae carbapenemase (KPC)-producing K...
April 2016: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/26871402/new-therapeutic-options-for-respiratory-tract-infections
#18
REVIEW
Matteo Bassetti, Elda Righi, Alessia Carnelutti
PURPOSE OF REVIEW: The progressive increase of respiratory tract infections caused by multidrug-resistant organisms (MDROs) has been associated with delays in the prescription of an adequate antibiotic treatment and increased mortality, representing a major concern in both community and hospital settings. When infections because of methicillin-resistant Staphylococcus aureus (MRSA) are suspected, vancomycin still represents the first choice, although its efficacy has been recently questioned in favor of new drugs, reported to provide better clinical outcomes...
April 2016: Current Opinion in Infectious Diseases
https://www.readbyqxmd.com/read/26863149/review-of-eravacycline-a-novel-fluorocycline-antibacterial-agent
#19
REVIEW
George G Zhanel, Doris Cheung, Heather Adam, Sheryl Zelenitsky, Alyssa Golden, Frank Schweizer, Bala Gorityala, Philippe R S Lagacé-Wiens, Andrew Walkty, Alfred S Gin, Daryl J Hoban, James A Karlowsky
Eravacycline is an investigational, synthetic fluorocycline antibacterial agent that is structurally similar to tigecycline with two modifications to the D-ring of its tetracycline core: a fluorine atom replaces the dimethylamine moiety at C-7 and a pyrrolidinoacetamido group replaces the 2-tertiary-butyl glycylamido at C-9. Like other tetracyclines, eravacycline inhibits bacterial protein synthesis through binding to the 30S ribosomal subunit. Eravacycline demonstrates broad-spectrum antimicrobial activity against Gram-positive, Gram-negative, and anaerobic bacteria with the exception of Pseudomonas aeruginosa...
April 2016: Drugs
https://www.readbyqxmd.com/read/26796653/new-and-emerging-antibiotics-for-complicated-intra-abdominal-infections
#20
Cheryl R Durand, Mohammad Alsharhan, Kristine C Willett
The purpose of this review is to evaluate the efficacy and safety of ceftazidime/avibactam and ceftolozane/tazobactam in patients with complicated intra-abdominal infections (cIAI), and review eravacycline and other agents in the pipeline for management of cIAI. The increasing incidence of multidrug resistant strains of bacteria has led to the need for additional antibiotics with activity against these organisms. There are 2 newly approved antibiotics, ceftazidime/avibactam and ceftolazane/tazobactam for treatment of cIAI...
January 19, 2016: American Journal of Therapeutics
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