A Novel Class of Orally Active Antifungal Beta-1,3-D-Glucan Synthase Inhibitors

Ref ID: 18675

Author:

Todd A. Black, PhD – Director/ Site Lead

Author address:

Merck Res. Labs., Kenilworth, NJ.

Full conference title:

52nd Annual ICAAC

Date: 9 September 2014

Abstract:

Echinocandin antifungals inhibit β -1,3 -D- glucan synthase activity, which is required for cell wall synthesis in both yeast and mold pathogens. Fungicidal activity against multiple species of Candida has made the echinocandins agents of choice for treating candidemia and invasive candidiasis in immunosuppressed patients, while potent activity against Aspergillus provides effective therapy for aspergillosis. The fungal specificity of the β -1,3 -D- glucan synthase target has manifest in favorable clinical features for the class including low adverse event rates and minimal drug-drug interactions, particularly relative to the azole-class of antifungals. The primary limitation of the echinocandins is the availability of only parentral formulations. Currently, Merck is investigating novel classes of glucan synthase inhibitors that have the potential to provide oral dosing regimens. Data on the discovery and current development status of these programs will be discussed.

Abstract Number: 1871

Conference Year: 2012

Link to conference website: NULL

New link: NULL

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