Literature DB >> 31208999

In Vivo Pharmacokinetic/Pharmacodynamic Targets of Levonadifloxacin against Staphylococcus aureus in a Neutropenic Murine Lung Infection Model.

Sachin S Bhagwat1, Hariharan Periasamy2, Swapna S Takalkar2, Rajesh Chavan2, Pavan Tayde2, Amol Kulkarni2, Jaikumar Satav2, Vineet Zope2, Mahesh Patel2.   

Abstract

Levonadifloxacin is a novel benzoquinolizine subclass of fluoroquinolone, active against quinolone-resistant Staphylococcus aureus A phase 3 trial for levonadifloxacin and its oral prodrug was recently completed. The present study identified area under the concentration-time curve for the free, unbound fraction of a drug divided by the MIC (fAUC/MIC) as an efficacy determinant for levonadifloxacin in a neutropenic murine lung infection model. Mean plasma fAUC/MIC requirement for static and 1 log10 kill effects against 9 S. aureus were 8.1 ± 6.0 and 25.8 ± 12.3, respectively. These targets were employed in the selection of phase 3 doses.
Copyright © 2019 American Society for Microbiology.

Entities:  

Keywords:  ABSSSIs; MRSA; levonadifloxacin

Mesh：

Substances：

Year:  2019        PMID： 31208999      PMCID： PMC6658750          DOI： 10.1128/AAC.00909-19

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN： 0066-4804            Impact factor:   5.191


  8 in total

1.  The anti-methicillin-resistant Staphylococcus aureus quinolone WCK 771 has potent activity against sequentially selected mutants, has a narrow mutant selection window against quinolone-resistant Staphylococcus aureus, and preferentially targets DNA gyrase.

Authors:  Sachin S Bhagwat; Lakshmi A Mundkur; Shrikant V Gupte; Mahesh V Patel; Habil F Khorakiwala
Journal:  Antimicrob Agents Chemother       Date:  2006-08-28       Impact factor: 5.191

2.  In vitro activity of the quinolone WCK 771 against recent U.S. hospital and community-acquired Staphylococcus aureus pathogens with various resistance types.

Authors:  Sachin S Bhagwat; Pamela McGhee; Klaudia Kosowska-Shick; Mahesh V Patel; Peter C Appelbaum
Journal:  Antimicrob Agents Chemother       Date:  2008-11-24       Impact factor: 5.191

3.  Intrapulmonary Pharmacokinetics of Levonadifloxacin following Oral Administration of Alalevonadifloxacin to Healthy Adult Subjects.

Authors:  Keith A Rodvold; Mark H Gotfried; Rakesh Chugh; Mugdha Gupta; Ravindra Yeole; Anasuya Patel; Ashima Bhatia
Journal:  Antimicrob Agents Chemother       Date:  2018-02-23       Impact factor: 5.191

4.  Pharmacodynamics of the new fluoroquinolone gatifloxacin in murine thigh and lung infection models.

Authors:  D Andes; W A Craig
Journal:  Antimicrob Agents Chemother       Date:  2002-06       Impact factor: 5.191

Review 5.  Pharmacokinetics and pharmacodynamics of fluoroquinolones in the respiratory tract.

Authors:  R Wise; D Honeybourne
Journal:  Eur Respir J       Date:  1999-07       Impact factor: 16.671

6.  A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.

Authors:  Noel J de Souza; Shrikant V Gupte; Prasad K Deshpande; Vijaya N Desai; Satish B Bhawsar; Ravindra D Yeole; Milind C Shukla; Jacob Strahilevitz; David C Hooper; Bülent Bozdogan; Peter C Appelbaum; Michael R Jacobs; Nitin Shetty; Mahesh V Patel; Rasendrakumar Jha; Habil F Khorakiwala
Journal:  J Med Chem       Date:  2005-08-11       Impact factor: 7.446

7.  Pharmacodynamics of the new des-f(6)-quinolone garenoxacin in a murine thigh infection model.

Authors:  D Andes; W A Craig
Journal:  Antimicrob Agents Chemother       Date:  2003-12       Impact factor: 5.191

8.  In Vivo Pharmacodynamic Target Assessment of Delafloxacin against Staphylococcus aureus, Streptococcus pneumoniae, and Klebsiella pneumoniae in a Murine Lung Infection Model.

Authors:  Alexander J Lepak; David R Andes
Journal:  Antimicrob Agents Chemother       Date:  2016-07-22       Impact factor: 5.191
  8 in total
  1 in total

Review 1.  Levonadifloxacin, a Novel Broad-Spectrum Anti-MRSA Benzoquinolizine Quinolone Agent: Review of Current Evidence.

Authors:  Sachin S Bhagwat; Manohar Nandanwar; Atul Kansagara; Anusuya Patel; Swapna Takalkar; Rajesh Chavan; Hariharan Periasamy; Ravindra Yeole; Prasad K Deshpande; Satish Bhavsar; Ashima Bhatia; Jaishid Ahdal; Rishi Jain; Mahesh Patel
Journal:  Drug Des Devel Ther       Date:  2019-12-24       Impact factor: 4.162
  1 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.