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Introduction: lefamulin and pharmacokinetic/pharmacodynamic rationale to support the dose selection of lefamulin
Lefamulin is the first semisynthetic pleuromutilin being developed for oral and intravenous administration. The drug selectively inhibits prokaryotic ribosomal protein synthesis by binding to the peptidyl transferase centre via four H-bonds and other interactions, resulting in an ‘induced fit’ that...
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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Oxford University Press
2019
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6449571/ https://www.ncbi.nlm.nih.gov/pubmed/30949709 http://dx.doi.org/10.1093/jac/dkz084 |
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author | Rodvold, Keith A |
author_facet | Rodvold, Keith A |
author_sort | Rodvold, Keith A |
collection | PubMed |
description | Lefamulin is the first semisynthetic pleuromutilin being developed for oral and intravenous administration. The drug selectively inhibits prokaryotic ribosomal protein synthesis by binding to the peptidyl transferase centre via four H-bonds and other interactions, resulting in an ‘induced fit’ that tightens the binding pocket around lefamulin. This unique mechanism of action has been associated with a low probability of cross-resistance to other antimicrobial classes commonly used to treat community-acquired bacterial pneumonia (CABP). This Supplement, entitled ‘Pharmacokinetic and pharmacodynamic analyses and dose rationale for lefamulin, a novel pleuromutilin antibiotic, for the treatment of community-acquired bacterial pneumonia’, is intended to be a valuable resource for both clinicians and researchers. It provides the essential pharmacokinetic and pharmacodynamic data on lefamulin that were used to support the optimal dose selection of lefamulin for the safe and effective treatment of CABP in adults. |
format | Online Article Text |
id | pubmed-6449571 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | Oxford University Press |
record_format | MEDLINE/PubMed |
spelling | pubmed-64495712019-04-09 Introduction: lefamulin and pharmacokinetic/pharmacodynamic rationale to support the dose selection of lefamulin Rodvold, Keith A J Antimicrob Chemother Supplement Papers Lefamulin is the first semisynthetic pleuromutilin being developed for oral and intravenous administration. The drug selectively inhibits prokaryotic ribosomal protein synthesis by binding to the peptidyl transferase centre via four H-bonds and other interactions, resulting in an ‘induced fit’ that tightens the binding pocket around lefamulin. This unique mechanism of action has been associated with a low probability of cross-resistance to other antimicrobial classes commonly used to treat community-acquired bacterial pneumonia (CABP). This Supplement, entitled ‘Pharmacokinetic and pharmacodynamic analyses and dose rationale for lefamulin, a novel pleuromutilin antibiotic, for the treatment of community-acquired bacterial pneumonia’, is intended to be a valuable resource for both clinicians and researchers. It provides the essential pharmacokinetic and pharmacodynamic data on lefamulin that were used to support the optimal dose selection of lefamulin for the safe and effective treatment of CABP in adults. Oxford University Press 2019-04 2019-04-05 /pmc/articles/PMC6449571/ /pubmed/30949709 http://dx.doi.org/10.1093/jac/dkz084 Text en © The Author(s) 2019. Published by Oxford University Press on behalf of the British Society for Antimicrobial Chemotherapy. http://creativecommons.org/licenses/by-nc/4.0/ This is an Open Access article distributed under the terms of the Creative Commons Attribution Non-Commercial License (http://creativecommons.org/licenses/by-nc/4.0/), which permits non-commercial re-use, distribution, and reproduction in any medium, provided the original work is properly cited. For commercial re-use, please contact journals.permissions@oup.com |
spellingShingle | Supplement Papers Rodvold, Keith A Introduction: lefamulin and pharmacokinetic/pharmacodynamic rationale to support the dose selection of lefamulin |
title | Introduction: lefamulin and pharmacokinetic/pharmacodynamic rationale to support the dose selection of lefamulin |
title_full | Introduction: lefamulin and pharmacokinetic/pharmacodynamic rationale to support the dose selection of lefamulin |
title_fullStr | Introduction: lefamulin and pharmacokinetic/pharmacodynamic rationale to support the dose selection of lefamulin |
title_full_unstemmed | Introduction: lefamulin and pharmacokinetic/pharmacodynamic rationale to support the dose selection of lefamulin |
title_short | Introduction: lefamulin and pharmacokinetic/pharmacodynamic rationale to support the dose selection of lefamulin |
title_sort | introduction: lefamulin and pharmacokinetic/pharmacodynamic rationale to support the dose selection of lefamulin |
topic | Supplement Papers |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6449571/ https://www.ncbi.nlm.nih.gov/pubmed/30949709 http://dx.doi.org/10.1093/jac/dkz084 |
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