Caspofungin Acetate Antifungal API

English name：Caspofungin acetate
CAS number：179463-17-3
Molecular formula: C54H92N10O17
Molecular weight: 1153.38
The EINECS: 605-859-0
Related category: Microbial metabolites; Pharmaceutical raw materials; Anti-infection, small molecule inhibitor; Small molecule inhibitors, natural products; Medical raw materials; Raw materials; Medical raw materials; Pharmaceutical and chemical industry; Echinalbicans antifungal agents :Amines; Heterocycles; Inhibitors; Intermediates & fine Chemicals; Pharmaceuticals; AP! ; Pharmaceutical raw materials; Pharmaceutical raw materials for scientific research; Synthetic antimicrobial drugs; Raw materials; Chemical reagent; Impurity reference; Apis and intermediates; Chemical raw materials; Biological reagent
Mol file:179463-17-3.mol
 

Structural formula:

Carpofungin acetate
Properties Melting Point >105°C(dec.)
Storage condition -20°C
Solubility In water solubility of 15mg/mL (clarified solution)
Morphological powder
Color White to beige
Water solubility H2O:15mg/mL(clearsolution)
InChIKey OGUJBRYAAJYXQP-LLXMLGLCSA-N
 

Intro

Carpofungin acetate is the first antifungal drug in the Echinocins class to receive marketing approval from the U.S. Food and Drug Administration (FDA). It was introduced in 2001 and has been approved for use in adult and pediatric patients (over 3 months).

Use

Carpofungin acetate for injection is indicated for the empiric treatment of neutropenia in adults and children (3 months and older), suspected fungal infections in patients with fever, and aggressive aspergillosis that does not respond to or is not tolerated by other treatments.​ Bacteria) have activity in vitro.

Action mechanism

Carpofungine acetate works with other echinomycin by non-competitive inhibition of the enzyme beta - (1,3) d-glucan synthase, which is a key component of fungal cell wall synthesis; This enzyme is not found in mammalian cells. Carpofungin acetate has fungicidal activity against candida species, including isolates resistant to triazole, and bactericidal activity against aspergillus.

Pharmacological action

Acetate mooring Finn clean a card by GlareaLozoyeChemicalbooknsis fermentation product synthesis of fat half a synthetic peptide (echinocandin) compounds. Carpofungin acetate can facilitate the synthesis of beta (1,3) D-glucan, an essential component of the cell wall of many filamentous fungi and yeast. P(1,3) D-glucan is not present in mammalian cells. In vitro pharmacological studies have shown that carpofungin has antibacterial activity against many pathogenic Aspergillus and candida fungi. At present, there is no established standard drug sensitivity test for the detection of β(1,3) D-glucan synthesis inhibitors. And the results of drug sensitivity tests are not necessarily linked to clinical outcomes. In mice and rats, the LD50 of carpofungin administered intravenously ranges from about 25mg/kg to 50mg/kg. Long-term studies have not been conducted in animals to assess the carcinogenic potential of carpofungin.

In mice and rats, the LD50 of carpofungin administered intravenously ranges from about 25mg/kg to 50mg/kg. Long-term studies have not been conducted in animals to assess the carcinogenic potential of carpofungin. In a series of in vitro studies, carpofungin was not found to be mutagenic or genotoxic. In addition, in bone marrow chromosome tests in mice, no genotoxicity was found at a net intravenous dose of cappofin up to 12.5mg/kg.

Adverse reaction

General situation Fever, headache, abdominal pain, aches, chills

Stomach and intestine Nausea, diarrhea, vomiting

Liver Elevated liver enzyme levels (aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase, direct bilirubin and total bilirubin)

Renal Increased serum creatinine

Blood Anemia (decreased hemoglobin and hematocrit)

Heart tachycardia

Peripheral blood vessel Phlebitis/thrombophlebitis, intravenous infusion complications, redness

Respiratory system dyspnea

Skin Rash, pruritus, sweating

Matters needing attention

Anaphylaxis has been reported during the use of carpofungin acetate. If allergic symptoms occur, treatment with this product should be discontinued and appropriate treatment should be carried out. Adverse Chemicalbook reactions that may be histamine-mediated have been reported, including rash, facial swelling, angioedema, pruritus, warmth, or bronchospasm, and may require discontinued treatment with this product and/or appropriate management.

Medication for pregnant and lactating women

Pregnant woman

There is no clinical data on the use of carpofungin in pregnant women. In rats, when given to mothers at a toxic dose of 5mg/kg per day, carpofengin caused weight loss in fetal rats and increased the incidence of incomplete skull and trunk ossification. In addition, at this dose, the incidence of the middle neck rib was increased in rats. Animal studies have shown that carpofungin can cross the placental barrier. This product should not be used during pregnancy unless absolutely necessary.

Nursing woman

It is not known whether the drug can be excreted by human milk. Therefore, women treated with this product should not breastfeed.

Children's medicine

Results from well-controlled adult studies, pharmacokinetic data from pediatric patients, and data from prospective studies conducted in pediatric patients aged 3 months to 17 years for the following indications (see Indications) support the safety and efficacy of this product in pediatric patients aged 3 months to 17 years:

Empirical treatment for patients with fever, neutropenia and suspected fungal infection.

Treatment of aggressive candidiasis in patients with neutropenia or without neutropenia, including candidiemia.

Treatment of esophageal candidiasis.

To treat patients with aggressive aspergillus disease who are refractory or cannot tolerate other therapies.

Prospective clinical trials on the efficacy and safety of this product have not been fully studied in neonates and infants under 3 months of age.

This product has not been studied in children for endocarditis, osteomyelitis and meningitis caused by candida. This product has also not been studied as an initial treatment for invasive aspergillosis in children.

Medication for elderly patients

Healthy older men and women (65 years or older) had slightly higher net plasma carpofen concentrations (approximately 28% higher AUC) compared with healthy young men. The same age-related effects were also found in the elderly relative to the younger in patients undergoing Chemicalbook or invasive candidiasis treatment. Elderly patients (65 years or older) do not need to adjust their dosage.

Biological activity

Carpofungin acetate (MK-0991, L-743872) is a lipopeptide antifungal β-1, 3-Glucan synthase inhibitor.

Target point

Target Value

β-1,3-glucan synthase

In vitro study

Carpofungin acetate is the first novel antifungal agent, which inhibits the synthesis of β(1,3) -D-glucan, a major component of the cell wall of filamentous fungi. Previous studies have shown that the in vitro activity of carpofungin acetate is tested for antifungal susceptibility to Candida using standard methods, including microdilution or large dilution, established by the 1997 Guidelines of the National Committee for Clinical Clinical Laboratory Standards for various Candida genera, including Candida Krossa. Although it is only approved by the FDA for the treatment of aspergillosis, there is information that many Chemicalbook Candida genera are sensitive to it. The minimum inhibitory concentrations for 90% Candida were as follows: C. Candida albicans 0.5μg/mL(range, 0.25-0.5), C. Smooth candida mu 1.0 g/mL (range, 0.25 2.0), c. tropical candida mu 1.0 g/mL (range, 0.25 1.0), C.​ Candida karensis 2.0μg/mL(range, 0.5-2.0).

Security information

WGK Germany:3

RTECS number: TP8046500

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