Micafungin

Micafungin C화학적 특성, 용도, 생산

개요

Micafungin, the second member of the echinocandin class of antifungal agents was launched in Japan for the parenteral treatment of various fungal infections caused by Aspergillus and Candida spp. such as fungaemia and respiratory and gastrointestinal mycoses. This water-soluble semisynthetic cyclic lipopeptide is synthesized by acylation with (5-(4- pentyloxyphenyl)isoxazol-3-yl)benzoate of the cyclic peptide nucleus (FR-179642).obtained by enzymatic cleavage of the naturally occurring echinocandin FR-901379, derived from the fungus Coleophoma empedri Micafungin acts by inhibiting the synthesis of 1,3-beta-glucan, an essential polysaccharide of the cell wall of many pathogenic fungi. Micafungin has a marked fungicidal effect on almost all species of Candida, including fluconazole-resistant spp. C. albicans, C. glabrata, C. Krusei, C. parapsilosis and C. tropicalis and a fungistatic effect on a range of Aspergillus species including A. flaws, A. fumigates and A. terreus. Like caspofungin, micafungin is inactive against Cryptococcus neoformans, and the emerging pathogen Trichosporon cutaneum and Fusarium solani. Micafungin has proved highly effective in mouse models of Cancfidiasis and Aspergillus infections (including those using an amphotericin B- and itraconazole-resistant isolate of A. fumigatus). In phase I studies, micafungin had linear pharmacokinetics with an elimination half-life ranging from 11.7 to 15.2 h after injection and was well tolerated.

용도

Micafungin is a semi-synthetic cyclic lipopeptide belonging to the echinocandin class that was reported in 1999 from Fujisawa in Japan. Unlike other marketed semi-synthetic derivatives in this class, micafungin is not derived from echinocandin but rather from FR901379 which contains a phenolic sulphate to enhance aqueous solubility, a serious limitation in the class. Micafungin 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 700 citations.

정의

ChEBI: A cyclic hexapeptide echinocandin antibiotic which exerts its effect by inhibiting the synthesis of 1,3-beta-D-glucan, an integral component of the fungal cell wall. It is used as the sodium salt for the treatment of invas ve candidiasis, and of aspergillosis in patients who are intolerant of other therapy.

Antimicrobial activity

It is active against Aspergillus spp., Candida spp. and the cyst form of Pn. jirovecii. Resistance has rarely been reported.

Pharmaceutical Applications

A semisynthetic lipopeptide derived from a fermentation product of Coleophoma empetri. Formulated as the monosodium salt for intravenous infusion.

Pharmacokinetics

C_max 50 mg 1-h infusion: c. 5 mg/L 1 h post infusion
Plasma half-life: 11–15 h
Volume of distribution: 0.4 L/kg
Plasma protein binding: 99%
Blood concentrations increase in proportion to dosage. Unlike anidulafungin and caspofungin, a loading dose is not required.
Distribution
The drug is widely distributed, the highest concentrations being found in the liver. Levels in the CSF and urine are negligible.
Metabolism and excretion
It is metabolized by the liver and the three inactive metabolites are excreted in the feces (70%). Less than 1% of a dose is eliminated as unchanged drug in the urine. No dosage adjustment is required in patients with severe renal impairment or mild to moderate hepatic impairment. The effect of severe hepatic impairment on micafungin pharmacokinetics has not been studied. Micafungin is not cleared by hemodialysis.

Clinical Use

Candidemia and certain invasive forms of candidosis
Esophageal candidosis
Prophylaxis of Candida infections in hematopoietic stem cell transplant (HSCT) recipients

부작용

Occasional histamine-mediated infusion-related reactions, injection site reactions and transient abnormalities of liver enzymes have been reported. Isolated cases of significant hepatic or renal dysfunction, hepatitis, or liver or renal failure have also been described.

Micafungin 준비 용품 및 원자재

원자재

준비 용품

Micafungin 공급 업체

공급자	전화	이메일	국가	제품 수	이점
AFINE CHEMICALS LIMITED	0571-85134551	info@afinechem.com	CHINA	15377	58
Shaanxi Haibo Biotechnology Co., Ltd	+undefined18602966907	qinhe02@xaltbio.com	China	1000	58
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21691	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
AB PharmaTech,LLC	323-480-4688		United States	989	55
career henan chemical co	+86-0371-86658258	sales@coreychem.com	China	29914	58
Standardpharm Co. Ltd.	86-714-3992388	overseasales1@yongstandards.com	United States	14336	58
Chongqing Chemdad Co., Ltd	+86-023-61398051 +8613650506873	sales@chemdad.com	China	39916	58
Shanghai Yingrui Biopharma Co.,Ltd	21-33585366	export01@shyrchem.com	CHINA	1320	58

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