The pleuromutilin antibiotics: a new class for human use

Curr Opin Investig Drugs. 2010 Feb;11(2):182-91.


Pleuromutilins were discovered as natural-product antibiotics in 1950. Tiamulin was the first pleuromutilin compound to be approved for veterinary use in 1979, followed by valnemulin in 1999. It was not until 2007 that retapamulin became the first pleuromutilin approved for use in humans. However, retapamulin is limited to topical application. Recent advances in lead optimization have led to the synthesis of pleuromutilins that combine potent antibacterial activity with favorable pharmaceutical properties, making these compounds suitable for oral and intravenous delivery. Most pleuromutilins have an antibacterial spectrum that spans the common pathogens involved in both skin and respiratory tract infections. Two new pleuromutilins, BC-3205 and BC-7013 (both Nabriva Therapeutics AG), have entered clinical trials. In this review, the key properties of pleuromutilin derivatives, designed primarily through modifications at the C(14) side chain, are presented, and the potential of these compounds in systemic therapy in humans is discussed.

Publication types

  • Historical Article
  • Review

MeSH terms

  • Animals
  • Anti-Bacterial Agents / administration & dosage
  • Anti-Bacterial Agents / history
  • Anti-Bacterial Agents / pharmacology*
  • Clinical Trials as Topic
  • Diterpenes / administration & dosage
  • Diterpenes / history
  • Diterpenes / pharmacology
  • Drug Design*
  • History, 20th Century
  • History, 21st Century
  • Humans
  • Microbial Sensitivity Tests
  • Pleuromutilins
  • Polycyclic Compounds
  • Respiratory Tract Infections / drug therapy
  • Respiratory Tract Infections / microbiology
  • Skin Diseases, Bacterial / drug therapy
  • Skin Diseases, Bacterial / microbiology
  • Structure-Activity Relationship


  • Anti-Bacterial Agents
  • Diterpenes
  • Polycyclic Compounds