Anidulafungin

한글명:Anidulafungin

카스 번호166663-25-8

상품명:Anidulafungin

CBNumberCB71120054

분자식C58H73N7O17

포뮬러 무게1140.24

MOL 파일166663-25-8.mol

화학적 성질

녹는점	>196°C (subl.)
끓는 점	1477.0±65.0 °C(Predicted)
밀도	1.47±0.1 g/cm3(Predicted)
저장 조건	under inert gas (nitrogen or Argon) at 2-8°C
용해도	DMSO(약간 용해됨, 가열), 메탄올(약간 용해됨)
산도 계수 (pKa)	9.86±0.26(Predicted)
물리적 상태	고체
물리적 상태	단단한 모양
색상	흰색에서 옅은 베이지까지

그림문자(GHS)

Anidulafungin 화학적 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 While the first member of this class, cilofungin, was withdrawn due to toxicity associated with the formulation vehicle, anidulafungin follows the successful introduction of caspofungin and micafungin.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.
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.
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.
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
C_max 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.

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