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| Pronunciation | /ˌkæspoʊˈfʌndʒɪn/KAS-poh-FUN-jin |
| Trade names | Cancidas |
| Other names | (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]: 185 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[2] |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a615001 |
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| Routes of administration | Intravenous |
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| Bioavailability | 100% (intravenous use only) |
| Protein binding | ~97% |
| Metabolism | Peptide hydrolysis,N-acetylation[4] |
| Eliminationhalf-life | 9–11 hours |
| Excretion | Kidney (41%),feces (35%) |
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| Chemical and physical data | |
| Formula | C52H88N10O15 |
| Molar mass | 1093.331 g·mol−1 |
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Caspofungin (INN;[1][5] brand nameCancidas) is alipopeptideantifungal drug fromMerck & Co., Inc.[6] It is a member of a class of antifungals termed theechinocandins.[medical citation needed] It works by inhibiting theenzyme(1→3)-β-D-glucan synthase and thereby disturbing the integrity of the fungalcell wall.[medical citation needed]
Caspofungin was the first inhibitor of fungal (1→3)-β-D-glucan synthesis to be approved by the United States Food and Drug Administration.[7] Caspofungin is administeredintravenously.[2] Caspofungin is a therapeutic alternative on theWorld Health Organization's List of Essential Medicines.[8]
Caspofungin acetate for injection was initially approved by both the USFood and Drug Administration (FDA), and theEuropean Medicines Agency (EMA) in 2001.[citation needed]
Its approved therapeuticindications by both organizations include the empirical therapy of presumed fungal infections in febrile,neutropenic adults and for salvage therapy in people treatment of invasiveaspergillosis in adults whose disease is refractory to, or who are intolerant of, other antifungal agents (i.e., conventional or lipid formulations ofamphotericin B and/oritraconazole).[medical citation needed] Additionally, the FDA approval includes indication for the treatment ofcandidemia and some specificCandida infections (intra-abdominal abscesses,peritonitis,pleural cavity infections, andesophagitis) and the EMA approval includes indication for the treatment of generalinvasive candidiasis in adults.[medical citation needed]
The mean duration of therapy in previous studies was 34 days.[medical citation needed] Some people were even healed by a one-day treatment. However, a few people were treated for as long as 162 days and tolerated the drug well, indicating that longtime use may be indicated and tolerated favourably in complicated cases of aspergillosis. Generally, the duration of treatment is dictated by the severity of the disease, the clinical response, and the improvement of immunocompetence in immunocompromised people.[medical citation needed]
About 36% of patients refractory to other therapies responded well to caspofungin therapy, while even 70% of patients intolerant to other therapies were classified as responders. Direct comparative studies to other drugs in the treatment of invasive aspergillosis have so far not been undertaken.[medical citation needed]
Caspofungin has been effective in treating fungal infections caused byAspergillus andCandida species. It is a member of the echinocandin family, a new class of antifungal agents with broad spectrum of activity against all Candida species. In comparison to treatment with eitherfluconazole oramphotericin B, all three drugs in this class have been demonstrated to be highly effective or superior in well-defined clinical settings including invasive Candida infections, Candida oesophagitis and candidaemia. Higherminimum inhibitory concentration (MIC) of these agents has been observed against C. parapsilosis and C. guilliermondii.[9]
In a few patients with infections caused byCandida albicans, mutants with reduced sensitivity to caspofungin have been noticed, but is currently still rare. The mechanism is probably a point mutation in the (1→3)-β-D-glucan synthase gene.[10] There are no data regarding development of resistance in other fungi thanC. albicans.[medical citation needed]
The following summarizes MIC susceptibility for a few medically significant organisms.[11]
Caspofungin has been shown in animal studies to have embryotoxic properties.[medical citation needed] The drug is found in the milk of lactating rats, but it is not known whether this is seen in humans.[medical citation needed]
Caspofungin is FDA approved for people aged three months and older.[2] Dosing is based on body surface area (BSA) as calculated by the Mosteller formula.[12]
Compared to amphotericin B, caspofungin seems to have a relatively low incidence of side effects. In clinical studies and postmarketing reports, the side effects seen in 1% or more of the patients were as follows:[medical citation needed]
Additionally, infrequent cases of symptomatic liver damage, peripheral edema and swelling, andhypercalcemia have been seen.[medical citation needed]
The concomitant use of caspofungin andciclosporin in healthy volunteers led to a more frequent increase of liver enzymes (ALT=SGPT andAST=SGOT) than noted with cyclosporine alone.[medical citation needed]
Reactions due to histamine release (rash, facial swelling, pruritus, sensation of warmth) have been seen.[medical citation needed] Known hypersensitivity to caspofungin acetate or any other ingredient contained in the formulation contraindicate its use.[medical citation needed]
Caspofungin is semisynthesized frompneumocandin B0, a fermentation product ofGlarea lozoyensis.[7]
Caspofungin is slowly metabolized by peptide hydrolysis andN-acetylation in liver. Therefore, in case of liver impairment the dose needs to be reduced. Caspofungin also undergoes spontaneous chemical degradation to an open-ring peptide compound, L-747969. Additional metabolism involves hydrolysis into constitutive amino acids and their derivatives, including dihydroxyhomotyrosine andN-acetyl-dihydroxyhomotyrosine.[2]
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