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Anidulafungin

Anidulafungin 구조식 이미지
카스 번호:
166663-25-8
상품명:
Anidulafungin
동의어(영문):
Eraxis;Ecalta;CS-2272;LY 303366;nidulafungin;AN(Local GMP);Anidulafungin;LY 303366, Eraxis;Anidulafungin-d11;An u a ung nidlfi
CBNumber:
CB71120054
분자식:
C58H73N7O17
포뮬러 무게:
1140.24
MOL 파일:
166663-25-8.mol

Anidulafungin 속성

끓는 점
1477.0±65.0 °C(Predicted)
밀도
1.47±0.1 g/cm3(Predicted)
저장 조건
Inert atmosphere,2-8°C
산도 계수 (pKa)
9.86±0.26(Predicted)

안전

Anidulafungin C화학적 특성, 용도, 생산

개요

Anidulafungin, a semi-synthetic derivative of echinocandin B, has been developed and launched as an intravenous treatment for serious fungal infections, such as candidemia, Candida-derived peritonitis, intra-abdominal abscesses, and esophageal candidiasis. As a non-competitive inhibitor of 1,3-b-D-glucan synthase, which is responsible for the formation of glucan polymers, anidulafungin interferes with the cell wall synthesis of most pathogenic fungi. This mode of action is characteristic of the echinocandin class of antifungals. While the first member of this class, cilofungin, was withdrawn due to toxicity associated with the formulation vehicle, anidulafungin follows the successful introduction of caspofungin and micafungin. Compared to the other echinocandins, anidulafungin appears to be more potent (MIC90 ofr0.25 mg/mL for C.albicans, 0.5 mg/mL for C.glabrata, 1 mg/mL for C. krusel and C.tropicalis, 2mg/mL for C.lusitaniae, and 2 mg/mL for Aspergillus spp) and is devoid of significant drug interactions since it is neither an inhibitor nor substrate of the cytochrome P450 isoenzymes. The emergence of the echinocandins circumvents the concern regarding the rising resistance to the azole and amphotericin B antifungals; no cross-resistance is expected because the echinocandins work at the cell wall rather than the cell membrane.

Originator

Eli Lilly (US)

용도

Anidulafungin is a semi-synthetic cyclic lipopeptide belonging to the echinocandin class that was reported in 1995 and commercially developed by Eli Lilly. Anidulafungin inhibits the synthesis of β-(1,3)-D-glucan, an essential component of the cell wall of susceptible fungi and is extensively referenced in the literature with over 400 citations.

용도

nucleoside reverse transcriptase inhibitor (NRTI) for HIV treatment in adults

정의

ChEBI: A semisynthetic echinocandin anti-fungal drug. It is active against Aspergillus and Candida species and is used for the treatment of invasive candidiasis.

상표명

Eraxis (Vicuron).

Antimicrobial activity

It is active against Aspergillus spp., Candida spp. and the cyst stage of Pneumocystis jirovecii. Resistance has not yet been reported.

Pharmaceutical Applications

A semisynthetic lipopeptide derived from a fermentation product of Aspergillus nidulans. Formulated for intravenous infusion.

Pharmacokinetics

Cmax 100 mg 1-h infusion: c. 9 mg/L end infusion
Plasma half-life: 18–27 h
Volume of distribution: 0.6 L/kg
Plasma protein binding: 84%
Blood concentrations increase in proportion to dosage. The steady state is achieved on the first day after a loading dose (twice the daily maintenance dose).
Distribution
Levels in the CSF are negligible.
Metabolism and excretion
Unlike caspofungin and micafungin, anidulafungin is not metabolized by the liver, but undergoes slow non-enzymatic degradation in the blood to a peptide breakdown product which is enzymatically degraded and excreted in the feces and bile. About 30% of a dose is eliminated in the feces, of which less than 10% is unchanged drug. Less than 1% of a dose is excreted in the urine. No dosage adjustment is required in patients with hepatic or renal impairment. Anidulafungin is not cleared by hemodialysis.

Clinical Use

Candidemia and certain invasive forms of candidosis
Esophageal candidosis

부작용

Occasional histamine-mediated infusion-related reactions, injection site reactions and transient abnormalities of liver enzymes have been reported.

Anidulafungin 준비 용품 및 원자재

원자재

준비 용품


Anidulafungin 공급 업체

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공급자 전화 팩스 이메일 국가 제품 수 이점
ENBRIDGE PHARMTECH CO., LTD.
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AFINE CHEMICALS LIMITED
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Henan DaKen Chemical CO.,LTD.
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Hangzhou FandaChem Co.,Ltd.
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Shanghai Yingrui Biopharma Co., Ltd.
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ATK CHEMICAL COMPANY LIMITED
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15950718863
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career henan chemical co
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sales@coreychem.com China 29954 58
TianYuan Pharmaceutical CO.,LTD
+86-755-23284190 13684996853
+86-755-23284190 sales@tianpharm.com CHINA 305 58

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