Caspofungin acetate

Bezeichnung:Caspofungin acetate

CAS-Nr179463-17-3

Englisch Name:Caspofungin acetate

CBNumberCB51120146

SummenformelC54H92N10O17

Molgewicht1153.38

MOL-Datei179463-17-3.mol

Caspofungin acetate physikalisch-chemischer Eigenschaften

Schmelzpunkt	>105°C (dec.)
storage temp.	-20°C
Löslichkeit	H2O: soluble15mg/mL (clear solution)
Aggregatzustand	powder
Farbe	white to beige
InChIKey	OGUJBRYAAJYXQP-LLXMLGLCSA-N

Sicherheit

WGK Germany	3
RTECS-Nr.	TP8046500

Gefahreninformationscode (GHS)

Caspofungin acetate Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Caspofungin 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.
Beschreibung
Caspofungin is an antifungal compound that is classified as an echinocandin, as it acts by noncompetititvely inhibiting the enzyme 1,3-β glucan synthase and preventing the synthesis of glucan in the fungal cell wall. It is effective against disseminated or invasive aspergillosis and candidiasis in mice. Caspofungin has a 50% minimum effective concentration against Aspergillus spp. of 0.015 μg/ml. It does not antagonize other antifungal compounds, like amphotericin B, and, in some cases, may show additive or synergistic activity.
Chemische Eigenschaften
White Solid
Originator
Merck & Co (US)
Verwenden
Calcium antagonist, coronary vasodilator, anti-inflammatory, analgesic
Verwenden
Caspofungin 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.
Verwenden
Caspofungin acetate is a semi-synthetic analogue of pneumocandin B0 with improved water solubility, a significant limitation in the development of the echinocandin class as pharmaceuticals. Caspofungin acetate acts by inhibiting the synthesis of β-(1,3)-D-glucan, an essential component of the cell wall of susceptible fungi.
Definition
ChEBI: The diacetate salt of caspofungin. It is used for the treatment of invasive candidiasis, and of aspergillosis in patients who are refractory to, or intolerant of, other therapy.
Trademarks
Cancidas (Merck).
Biochem/physiol Actions
Caspofungin is an echinocandin antifungal that inhibits 1,3-β-D-glucan synthase, which is required for cell wall synthesis, thereby disturbing the integrity of the fungal cell wall.
Veterinary Drugs and Treatments
Caspofungin has potential for treating invasive aspergillosis or disseminated candidal infections in companion animals although little, if any, information on its use in dogs or cats is available.

Caspofungin acetate Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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