Caspofungin acetate

개요Caspofungin is the first in a new class of antifungal agents named echinocandin to be launched in the US for the parenteral treatment of invasive aspergillosis in patients refractory to, or intolerant of other antifungal therapies such as amphotericin-B1 lipid formulation of amphotericin-B and/or itraconazole. Caspofungin is a water soluble, stable, aza-substituted semisynthetic derivative of pneumocandin B, a fermentation product of the fungus Zalerion arboricola. Since fungi and humans are both eukaryotes, new antifungal agents must focus on fungus-specific targets in order to minimize potential toxicity in the human host. In this respect, the lipopeptide caspofungin, inhibits the synthesis of 1,3-beta- D-glucans present only in the fungal cell wall, which leads to the specific lysis of the pathogenic cells. The compound is fungicidal rather than fungistatic, an unusual feature among antifungal agents. Caspofungin has activity in vitro and in vivo against a range of Candida species (including azole and amphotericin B resistant Candida) and also against Aspergillus, an important pathogen which is not susceptible to fluconazole. Caspofungin was generally more active than amphotericin B, flucytosine, fluconazole and itraconazole against Candida species. Cryptococcus is not susceptible to caspofungin. Caspofungin has a half-life in human beings around 10 hours. Unlike the azoles, caspofungin does not inhibit cytochrome P450. The drug has been given intravenously with loading dose of 70 rag, followed by 50 mg daily to be effective in invasive aspergillosis refractory to prior antifungal therapy. Most of the side effects were mild and comprised fever, thrombophlebitis, headache, nausea, rash and flushing.

용도Caspofungin Diacetate is an impurity of Caspofungin Acetate(C184900) which is an echinocandin that inhibits the synthesis of β (1,3)-D-glucan, an integral component of the fungal cell wall. An antifungal drug used in the treatment of invasive fungal infections.