Drug Discovery using Natural Products – Optimization Studies of Inhibitors of Glucan Synthesis as Anti-Fungal Agents

Drug Discovery and Development, Life Sciences, Pharmaceutical,
  • October 31, 2013

Inhibition of b-1,3-glucan synthesis is the mechanism of action of the echinocandin class of natural products and has been shown to result in clinically effective therapy for important fungal pathogens including azole resistant Candida spp. and invasive Aspergillus spp. Infection.

This presentation will outline the chemical modifications of the lipopeptide pneumocandin which led to the discovery and clinical introduction of Cancidas® as an important advance in anti-fungal therapy. A new class of b-1,3-glucan synthesis inhibitor, the triterpene enfumafungin, was recently disclosed which displays broad spectrum (Candida and Aspergillus spp.) antifungal (AF) activity. Importantly, derivatives of enfumafungin were discovered that show good oral bioavailability and have robust anti-fungal activity in mouse models of disseminated disease when delivered orally.

The talk will outline the steps taken to transform a complex natural product with poor ‘druggability’ features into an orally available agent suitable for clinical investigations.

Keywords:

Speakers

Mike Peel, Ph.D., Executive Director Discovery Research, SCYNEXIS, Inc.

Michael Peel joined SCYNEXIS in July 2002 and currently serves as the head of the Discovery Research Division with responsibility for the contract medicinal chemistry group. Prior to joining SCYNEXIS Dr. Peel was at Glaxo/GlaxoWellcome and GSK where he ran a number of drug discovery projects targeting inflammation and oncology in addition to leading a central Kinase Chemistry Team. Dr. Peel received degrees in Chemistry from the University of Sheffield and carried out post-Doctoral studies at Wayne State University.

James Balkovec, Ph.D., Principal and Owner, ChemTract LLC

James Balkovec joined Merck & Co in 1987 as a senior chemist in the infectious disease area and advanced to a position of Senior Director Medicinal Chemistry . Dr. Balkovec led multiple programs with groups of over 30 people and has led or been a key representative on multidisciplinary project teams to guide compounds into development and through Phase IIb. Dr. Balkovec has an expertise in infectious diseases (anti-bacterials, anti-fungals) and has also worked in cardiovascular, metabolic, inflammatory and fibrosis disease areas. Dr. Balkovec received degrees in Chemistry from Universities of Pittsburgh and Wisconsin and performed post-doctoral studies at Columbia University.

Who Should Attend?

The presentation will be of interest to medicinal chemists, particularly those working on performing studies on natural products or large molecular weight compounds with features not typically associated with good drug-like properties.

The information will also be useful for scientists with an interest in anti-fungal drug discovery.

Xtalks Partners

SCYNEXIS

SCYNEXIS, Inc. is a premier drug discovery and development company headquartered in Research Triangle Park, North Carolina. SCYNEXIS delivers innovative solutions to solve the toughest problems in drug discovery and development for our Pharmaceutical, global health and life science partners. Our contract research and development services include Discovery Research, Integrated Pharmaceutical Solutions and Integrated Parasitology. The SCYNEXIS Discovery Research division’s integrated chemistry, DMPK and biology expertise spans across multiple therapeutic areas and has successfully delivered preclinical and clinical drug candidates for our customers.

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