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Assay Development for High-Throughput Drug Screening Against Mycobacteria
Published on: October 25, 2024
The pleuromutilin antibiotics: a new class for human use
1Nabriva Therapeutics AG, Leberstrasse 20, 1110 Vienna, Austria. Rodger.novak@nabriva.com
Current Opinion in Investigational Drugs (London, England : 2000)
|January 30, 2010
Summary
Pleuromutilin antibiotics, discovered in 1950, are advancing for human systemic therapy. New derivatives show potent activity against common pathogens, suitable for oral and IV delivery.
Area of Science:
- Medicinal Chemistry
- Microbiology
- Pharmacology
Background:
- Pleuromutilins are a class of natural-product antibiotics discovered in 1950.
- Tiamulin (1979) and valnemulin (1999) were approved for veterinary use.
- Retapamulin, approved in 2007, marked the first human pleuromutilin but is limited to topical use.
Observation:
- Recent lead optimization has yielded pleuromutilin derivatives with potent antibacterial activity and favorable pharmaceutical properties.
- These novel compounds are suitable for oral and intravenous administration.
- The antibacterial spectrum of most pleuromutilins covers common pathogens causing skin and respiratory tract infections.
Findings:
- Two new pleuromutilin compounds, BC-3205 and BC-7013, have advanced to clinical trials.
- Modifications, particularly at the C(14) side chain, are key to developing these derivatives.
- These derivatives exhibit potential for systemic therapy in humans.
Implications:
- The development of orally and intravenously deliverable pleuromutilins offers new therapeutic options for bacterial infections.
- These advancements address the limitations of earlier topical-only pleuromutilins.
- Further research and clinical trials are crucial to establish the efficacy and safety of these novel systemic antibiotics.
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