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Caspofungin

Caspofungin
Caspofungin.svg
Clinical data
Pronunciation KAS-poe-FUN-jin
Trade names Cancidas
AHFS/Drugs.com Monograph
License data
Pregnancy
category
  • C
Routes of
administration
Intravenous
ATC code J02AX04 (WHO)
Legal status
Legal status
  • ℞ (Prescription only)
Pharmacokinetic data
Bioavailability 100% (intravenous use only)
Protein binding ~97%
Metabolism Hepatic
Biological half-life 9–11 hours
Excretion Urine (41%), feces (35%)
Identifiers
Synonyms

(4R,5S)-5-[(2-Aminoethyl)amino]-N2-(10,12-dimethyltetradecanoyl)-
4-hydroxy-L-ornithyl-L-threonyl-trans-4-hydroxy-L-prolyl-(S)-4-hydroxy-4-(p-hydroxyphenyl)-L-threonyl-threo-3-hydroxy-L-ornithyl-trans-3-hydroxy-L-proline cyclic (6→1)-peptide

1-[(4R,5S)-5-[(2-Aminoethyl)amino]-N2-(10,12-dimethyl-1-oxotetradecyl)-4-hydroxy-L-ornithine]-5-[(3R)-3-hydroxy-L-ornithine] pneumocandin B0
CAS Number 179463-17-3 YesY
PubChem (CID) 468682
DrugBank DB00520 YesY
ChemSpider 13180298 YesY
UNII VUW370O5QE YesY
KEGG D07626 N
ChEBI CHEBI:474180 YesY
ChEMBL CHEMBL499808 YesY
Chemical and physical data
Formula C52H88N10O15
Molar mass 1093.31 g/mol
3D model (Jmol) Interactive image
 NYesY (what is this?)

(4R,5S)-5-[(2-Aminoethyl)amino]-N2-(10,12-dimethyltetradecanoyl)-
4-hydroxy-L-ornithyl-L-threonyl-trans-4-hydroxy-L-prolyl-(S)-4-hydroxy-4-(p-hydroxyphenyl)-L-threonyl-threo-3-hydroxy-L-ornithyl-trans-3-hydroxy-L-proline cyclic (6→1)-peptide

Caspofungin (INN) (brand name Cancidas worldwide) is a lipopeptide antifungal drug from Merck & Co., Inc. discovered by James Balkovec, Regina Black and Frances A. Bouffard. It is a member of a new class of antifungals termed the echinocandins. It works by inhibiting the enzyme (1→3)-β-D-glucan synthase and thereby disturbing the integrity of the fungal cell wall. Caspofungin was the first inhibitor of fungal (1→3)-β-D-glucan synthesis to be approved by the United States Food and Drug Administration. Caspofungin is administered intravenously.

Caspofungin has been effective in treating fungal infections caused by Aspergillus and Candida species. The following represents MIC susceptibility for a few medically significant organisms.

Caspofungin acetate for injection was originally approved by both the Food and Drug Administration (FDA), in the U.S., and the EMEA, in Europe, in 2001.

Its currently approved therapeutic indications by both organisations include the empirical therapy of presumed fungal infections in febrile, neutropenic adult patients and for salvage therapy in patients treatment of invasive aspergillosis in adult patients whose disease is refractory to, or who are intolerant of, other antifungal agents (i.e., conventional or lipid formulations of amphotericin B and/or itraconazole). Additionally, the FDA approval includes indication for the treatment of candidemia and some specific Candida infections (intra-abdominal abscesses, peritonitis, pleural cavity infections, and esophagitis) and the EMEA approval includes indication for the treatment of general invasive candidiasis in adult patients.


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