New β-glucan inhibitors as antifungal drugs

Expert Opin Ther Pat. 2011 Oct;21(10):1597-610. doi: 10.1517/13543776.2011.603899. Epub 2011 Jul 25.


Introduction: New classes of synthetic and semi-synthetic β-glucan inhibitors have recently emerged, providing analogs that, in some cases, have been proven to have a high degree of activity against fungi, offering the prospect of alternatives to the commercially available lipopeptide/echinocandin agents caspofungin, micafungin and anidulafungin.

Area covered: This review covers applications disclosing compound classes that include synthetic pyridazinone analogs, bicyclic heteroaryl ring compounds, aniline derivates, and semi-synthetic echinocandin and enfumafungin derivatives. MK-3118 is an analog of the natural product enfumafungin that, in particular, shows promise as it has a spectrum of activity comparable with caspofungin but has the advantageous property of oral bioavailability.

Expert opinion: The diversity of chemical classes in the present review, which have demonstrable activity against β-glucan and the prospect of oral bioavailability, offers hope that safe and effective antifungal drugs will emerge and be commercialized. Of particular note, the Merck compound MK-3118, with solid evidence of efficacy based on preclinical data, has moved into clinical trials.

Publication types

  • Review

MeSH terms

  • Administration, Oral
  • Animals
  • Antifungal Agents / adverse effects
  • Antifungal Agents / pharmacokinetics
  • Antifungal Agents / pharmacology*
  • Biological Availability
  • Drug Design
  • Glycosides / pharmacokinetics
  • Glycosides / pharmacology
  • Humans
  • Mycoses / drug therapy*
  • Mycoses / microbiology
  • Patents as Topic
  • Triterpenes / pharmacokinetics
  • Triterpenes / pharmacology
  • beta-Glucans / antagonists & inhibitors*


  • Antifungal Agents
  • Glycosides
  • Triterpenes
  • beta-Glucans
  • ibrexafungerp