Recent Patents on Anti-Infective Drug Discovery

Dieter Kabelitz  
Institute of Immunology
Universitätsklinikum Schleswig-Holstein
Campus Kiel
Arnold-Heller-Straße 3
Kiel, D-24105
Germany

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Medical Claims and Current Applications of the Potent Echinocandin Antifungals

Author(s): Leif Smith and Shi-En Lu

Affiliation: Mississippi State University, Department of Biological Sciences and Department of Basic Sciences at the College of Veterinary Medicine, Mississippi State, Mississippi 39762; USA.

Keywords: Echinocandins, cilofungin, caspofungin, micafungin, anidulafungin, production, structure, pharmacokinetics

Abstract:

Echinocandins are an interesting group of antifungals that were originally discovered in the early 1970s. They are a group of lipopeptides produced by fungi which consists of a large number of structural analogs of echinocandin B, the first echinocandin to be structurally characterized. All clinically used echinocandins are produced semi-synthetically. The cyclic peptide nuclear core is retained while the acyl chain is replaced to minimize toxicity and expand their spectrum of activity. It was not until 2002 with the introduction of caspofungin (Cancidas) into the clinics that their true worth was realized. Since the introduction of caspofungin, two other echinocandins, micafungin (Mycamine) and anidulafungin (Eraxis) have been introduced. They all function by inhibiting an enzyme unique for fungal cell wall production, which presumably accounts for their minimal side-effects. In this review, topics pertaining to their production, structural diversity, and use in the clinic along with the recent patents are discussed.

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Article Details

VOLUME: 5
ISSUE: 1
Page: [58 - 63]
Pages: 6
DOI: 10.2174/157489110790112563