Anidulafungin

Anidulafungin 속성

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 While the first member of this class, cilofungin, was withdrawn due to toxicity associated with the formulation vehicle, anidulafungin follows the successful introduction of caspofungin and micafungin.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

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.

Anidulafungin 준비 용품 및 원자재

원자재

준비 용품

Anidulafungin 공급 업체

공급자	전화	이메일	국가	제품 수	이점
ENBRIDGE PHARMTECH CO., LTD.	+8613812269233	tinayang@enbridgepharm.com	China	303	58
AFINE CHEMICALS LIMITED	0571-85134551	info@afinechem.com	CHINA	15377	58
Hebei Mojin Biotechnology Co., Ltd	+8613288715578	sales@hbmojin.com	China	12456	58
shandong perfect biotechnology co.ltd	+86-53169958659; +8618596095638	sales@sdperfect.com	China	294	58
Henan Bao Enluo International TradeCo.，LTD	+86-17331933971 +86-17331933971	deasea125996@gmail.com	China	2503	58
Shanghai Daken Advanced Materials Co.,Ltd	+86-371-66670886	info@dakenam.com	China	15928	58
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21691	55
Hangzhou FandaChem Co.,Ltd.	008657128800458; +8615858145714	fandachem@gmail.com	China	9348	55
Shanghai Yingrui Biopharma Co., Ltd.	+86-21-33585366 - 03@	sales03@shyrchem.com	CHINA	738	60
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32480	60

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