Medical claims and current applications of the potent echinocandin antifungals.
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.
Smith
Leif
L
Mississippi State University, Department of Biological Sciences and Department of Basic Sciences at the College of Veterinary Medicine, Mississippi State, Mississippi 39762, USA. jls859@msstate.edu
Lu
Shi-En
SE
D000818:Animals; D000935:Antifungal Agents / Q000009:adverse effects / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use*; D055808:Drug Discovery; D054714:Echinocandins / Q000009:adverse effects / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use*; D006801:Humans; D015394:Molecular Structure; D009181:Mycoses / Q000188:drug therapy* / Q000382:microbiology; D010330:Patents as Topic; D013329:Structure-Activity Relationship; D016896:Treatment Outcome
D000935:Antifungal Agents; D054714:Echinocandins