title: Micafungin sodium (FK-463).
abstract: FK-463 (micafungin) represents the latest development candidate in a novel chemical class of echinocandin lipopeptide antifungal compounds. This agent has potent in vitro and experimental in vivo activity against a variety of pathogenic Candida species (yeasts) and Aspergillus fumigatus (filamentous fungus). This compound has favorable pharmacokinetics and a unique mode of action that makes it active against fungal isolates resistant to established antifungal agents, particularly the triazole agent fluconazole. Single- and multiple-dose phase I studies in normal human volunteers and phase II clinical trials in patients have been completed, with the compound being generally well tolerated and efficacious against infections caused by Candida and Aspergillus species. Published information on the in vitro and experimental in vivo activity, experimental and human pharmacokinetics, and clinical trial data of this new antifungal, echinocandin-like lipopeptide are summarized in this monograph.
authors.affiliation: Regulatory Affairs-International, Merck Research Laboratories, Rahway, New Jersey 07065-0900, USA. robert_fromling@merck.com
authors.forename: Robert A
authors.initials: RA
authors.lastname: Fromtling
mesh_terms: D000818:Animals; D000935:Antifungal Agents / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use*; D002986:Clinical Trials as Topic; D054714:Echinocandins; D005658:Fungi / Q000187:drug effects*; D006801:Humans; D055666:Lipopeptides; D008074:Lipoproteins / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use*; D000077551:Micafungin; D009181:Mycoses / Q000188:drug therapy* / Q000382:microbiology; D010456:Peptides, Cyclic / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use*
chemical_list: D000935:Antifungal Agents; D054714:Echinocandins; D055666:Lipopeptides; D008074:Lipoproteins; D010456:Peptides, Cyclic; D000077551:Micafungin