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English synonyms : Anidulafungin
CAS number : 166663-25-8
Molecular formula : C58H73N7O17
Molecular weight :1140.24
EINECS number: 658-060-4
Related categories:
Antifungal; Microbial metabolites; Pharmaceutical intermediates; Anti-infection; Small molecule inhibitors, natural products; Inhibitor; Pharmaceutical raw materials; Pharmaceutical raw materials; Pharmaceutical and chemical industry; Raw materials; Medical Chemicalbook raw materials; Pharmaceutical raw materials; Medical raw materials; Antifungals; API; Inhibitors; Chemical intermediates; Raw materials; Household chemicals; Chemical raw materials; Chemical reagent
Structural formula:
The net nature of anifen
Melting point:> 196 C (subl.)
Boiling point: 1477.0 ± 65.0 C (Predicted)
Density: 1.47±0.1g/cm3 (Predicted)
Storage conditions: underinertgChemicalbookas (nitrogenorArgon) at2-8 C
Solubility: DMSO (microsoluble, heated), methanol (microsoluble)
Acicidity coefficient (pK a): 9.86 ± 0.26 (Predicted)
Form: solid
Color: white to light brown
Antifungal
Aifin was developed and developed by Lilly and applied for patent, and then transferred to Vicuron. In September 2005, the company was acquired by Pfizer, which acquired the product to continue the shortage of fungal line products after the expiration of the antifungal drug fluconazole patent. In 2006, the product was approved for listing through FDA review. Fungal infection especially candida infection is a common factor of hospital acquired blood infection, the mortality rate after infection is about 40%, triazole drugs especially fluconazole has long been regarded as a candida and other fungal infections, gold Chemicalbook fungin is the first proven efficacy in clinical studies than fluconazole drugs. Anifengin is an echinocandin antifungal drug, similar products are micarfengin, caspofungin, used for the treatment of esophageal candidiasis, Candida bacteremia and other species of Candida infections, including peritonitis and abdominal abscess, studies confirmed its strong in vitro and in vivo antifungal activity, and no cross-resistance. Fenjing antifungal antibiotics have become an important drug in the clinical treatment of systemic fungal infections, and these drugs have the advantages of high antibacterial activity and low adverse reactions.
Property
Aniffin, at a boiling point of 1477℃ and 847℃ at 760mmHg, belongs to amphotericin B derivative. The solid form is white powder, easy to decompose, insoluble in water, slightly soluble in ethanol and soluble in dimethyl sulfoxide.
Indication
Anifennet is used for candidiasis septicemia, oropharyngeal and esophageal candidiasis, abdominal abscess caused by Candida, and Candida peritonitis, and Aspergillus infection.
Pharmacokinetics
In the echinocandin class. Anifengin is unique. Its transformation through a series of biotransformations. Slow degradation in plasma, but not in metabolism. More than 90% of anifenennet is slowly chemically degraded in the blood and is treated by nonspecific peptidases to form ring-opening products. Anifen net t1 / 2 is about 24h, while its degradation Chemicalbook product, t1 / 2, is about 4d. Net protein degradation is not metabolized by the cytochrome P450 enzyme system, and very few drugs or degradation products are found in the urine. Aifen net degradation products are excreted from feces through bile. No dose adjustment is required in patients with any degree of hepatic impairment or in patients with renal dysfunction.
Pharmacological action
Anifenfungin is an echinocandin antifungal drug with the same mechanism of action of "caspofungin". It has antibacterial activity against Candida and Aspergillus, and is not effective against Cryptococcus, fusaria, and Trichospora.
Usage and dosage
Intravenous administration.
1. Candida septicemia, intraperitoneal disseminated candidiasis and peritonitis: 200mg on the first day, and 100mg once a day thereafter. Course of Chemicalbook was continued until at least 14 days after the last positive culture.
2. Esophageal candidiasis: 100mg on the first day, 50mg after each time, once a day. The course lasted at least 14 days and at least 7 days after resolution of symptoms.
3. Oroopharyngeal Candida infection (HIV infected): fluconazole resistance, 100mg on the first day, 50mg thereafter, once a day.
Bioactivity
Anidulafungin (LY303366), a derivative of echinocandin that inhibits the activity of glucan synthase, is used as an antifungal agent.
Target spot
Target Value
glucan synthase
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MSDS information
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