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Micafungin (trade name Mycamine) is an echinocandin antifungal drug developed by Astellas Pharma. It inhibits the production of beta-1,3-glucan, an essential component of fungal cell walls. Micafungin is administered intravenously. It received final approval from the U.S. Food and Drug Administration on March 16, 2005, and gained approval in the European Union on April 25, 2008.

Indications

Micafungin is indicated for the treatment of candidemia, acute disseminated candidiasis, Candida peritonitis, abscesses and esophageal candidiasis. Since January 23, 2008, micafungin has been approved for the prophylaxis of Candida infections in patients undergoing hematopoietic stem cell transplantation (HSCT).

Micafungin works by way of concentration-dependent inhibition of 1,3-beta-D-glucan synthase resulting in reduced formation of 1,3-beta-D-glucan, which is an essential polysaccharide comprising one-third of the majority of Candida spp. cell walls. This decreased glucan production leads to osmotic instability and thus cellular lysis. ^[1] ^[2]

Contraindications

Known hypersensitivity to micafungin or any other ingredient contained in the formulation is a contraindication for its use.

Dosage

For the treatment of candidemia, acute disseminated candidiasis, Candida peritonitis and abscesses, the dosage of micafungin is 100 mg once daily. For the treatment of esophageal candidiasis, the dosage is 150 mg once daily. For prophylaxis of Candida infections in HSCT recipients, the dosage is 50 mg once daily.

The metabolism of micafungin occurs hepatically as the drug molecule is a substrate of CYP3A4; a liver enzyme. Precautions should be taken with regards to dosing, as micafungin also inhibits its own clearance via weak CYP3A4 inhibition. ^[3] ^[4]

Dosage forms

Micafungin is a natural antifungal product derived from other fungi as a defense mechanism for competition of nutrients, etc. More specifically, micafungin is derived from FR901379, and is produced by Coleophoma empetri. ^[5] ^[6]

Mycamine 50mg for intravenous (IV) infusion (manufacturer Astellas)
Mycamine 100mg for IV infusion (manufacturer Astellas)
Brand names in countries other than the US may vary.

References

^ Pappas PG, Rotstein CM, Betts RF, et al, “Micafungin vVersus Caspofungin for Treatment of Candidemia and Other Forms of Invasive Candidiasis,” Clin Infect Dis, 2007, 45(7):883-93. [PubMed 17806055]
^ Pettengell K, Mynhardt J, Kluyts T, et al, “Successful Treatment of Oesophageal Candidiasis by Micafungin: A Novel Systemic Antifungal Agent,” Aliment Pharmacol Ther, 2004, 20(4):475-81. [PubMed 15298643]
^ Carver PL, “Micafungin,” Ann Pharmacother, 2004, 38(10):1707-21. [PubMed 15340133]
^ Kohno S, Masaoka T, Yamaguchi H, et al, “A Multicenter, Open-Label Clinical Study of Micafungin (FK463) in the Treatment of Deep-Seated Mycosis in Japan,” Scand J Infect Dis, 36(5):372-9
^ The Journal of Antibiotics (2009) 62, 27-35
^ Fujie, Akihiko, Discovery of Micafungin (FK463): A novel antifungal derived from a novel product lead. Fermentation Research Laboratories, Astellas Pharma Inc., 5-2-6-Tokodai, Tsukuba, Ibaraki 300-2698, japan. Pure Appl. Chem, Vol. 79, No. 4, pp. 603-614, 2007

External links

Mycamine website, run by Astellas Pharma US
Mycamine Prescribing Information
Gregory Eschenauer, Daryl D DePestel, and Peggy L Carver: Comparison of echinocandin antifungals. Ther Clin Risk Manag 2007, 3(1): 71–97.

UpToDate Contents

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1. エキノカンジンの薬理学 pharmacology of echinocandins
2. 口腔咽頭および食道カンジダ症の治療 treatment of oropharyngeal and esophageal candidiasis
3. HIV感染患者における侵襲性肺アスペルギルス症の診断および治療 diagnosis and treatment of invasive pulmonary aspergillosis in hiv infected patients
4. 成人におけるカンジダ菌血症および侵襲性カンジダ症 treatment of candidemia and invasive candidiasis in adults
5. 血液悪性腫瘍を有する成人における侵襲性真菌感染症予防 prophylaxis of invasive fungal infections in adults with hematologic malignancies

English Journal

Calcium-Mediated Induction of Paradoxical Growth following Caspofungin Treatment Is Associated with Calcineurin Activation and Phosphorylation in Aspergillus fumigatus.

Juvvadi PR1, Muñoz A2, Lamoth F3, Soderblom EJ4, Moseley MA4, Read ND2, Steinbach WJ5.
Antimicrobial agents and chemotherapy.Antimicrob Agents Chemother.2015 Aug;59(8):4946-55. doi: 10.1128/AAC.00263-15. Epub 2015 Jun 8.
The echinocandin antifungal drug caspofungin at high concentrations reverses the growth inhibition of Aspergillus fumigatus, a phenomenon known as the "paradoxical effect," which is not consistently observed with other echinocandins (micafungin and anidulafungin). Previous studies of A. fumigatus re
PMID 26055379

Altered Micafungin Pharmacokinetics in Intensive Care Unit Patients.

Lempers VJ1, Schouten JA2, Hunfeld NG3, Colbers A1, van Leeuwen HJ4, Burger DM1, Verweij PE5, Pickkers P6, Brüggemann RJ7.
Antimicrobial agents and chemotherapy.Antimicrob Agents Chemother.2015 Aug;59(8):4403-9. doi: 10.1128/AAC.00623-15. Epub 2015 May 11.
Micafungin is considered an important agent for the treatment of invasive fungal infections in the intensive care unit (ICU). Little is known on the pharmacokinetics of micafungin. We investigated micafungin pharmacokinetics (PK) in ICU patients and set out to explore the parameters that influence m
PMID 25963988

Isavuconazole, micafungin, and 8 comparator antifungal agents' susceptibility profiles for common and uncommon opportunistic fungi collected in 2013: temporal analysis of antifungal drug resistance using CLSI species-specific clinical breakpoints and proposed epidemiological cutoff values.

Pfaller MA1, Rhomberg PR2, Messer SA2, Jones RN2, Castanheira M2.
Diagnostic microbiology and infectious disease.Diagn Microbiol Infect Dis.2015 Aug;82(4):303-13. doi: 10.1016/j.diagmicrobio.2015.04.008. Epub 2015 Apr 29.
The in vitro activities of isavuconazole, micafungin, and 8 comparator antifungal agents were determined for 1613 clinical isolates of fungi (1320 isolates of Candida spp., 155 of Aspergillus spp., 103 of non-Candida yeasts, and 35 non-Aspergillus molds) collected during a global survey conducted in
PMID 25986029

Japanese Journal

Endotoxin does not alter the pharmacokinetics of micafungin, but it impairs biliary excretion of micafungin via multidrug resistance-associated protein 2 (ABCC2/Mrp2) in rats

NODA Takayuki,ABE Fumie,UEYAMA Jun,KATO Miki,KATOH Miki,NADAI Masayuki,SAITO Hiroko,HASEGAWA Takaaki
Journal of infection and chemotherapy : official journal of the Japan Society of Chemotherapy 17(2), 207-213, 2011-04-01
NAID 10028171423

急速に進行し菌球様陰影を呈した肺Aspergillus niger症の1例

齋藤雅俊,四宮祥平,北楯祥子,高原豊,山谷淳代,小島好司,藤本由貴,及川卓,中川研,土原一真,井口晶晴,長内和弘,栂博久
気管支学 : 日本気管支研究会雑誌 33(1), 33-37, 2011-01-25
症例.63歳,男性.3カ月前より乾性咳嗽を自覚し近医受診,間質性肺炎の診断で2カ月前からプレドニゾロン30mg/日の内服を開始された.1カ月前から咳嗽の増悪と全身倦怠感があり当院紹介となった.受診時38℃台の発熱と低酸素血症を認め,両側上肺野に吸気終末cracklesを聴取した.採血では核の左方移動を伴うWBC上昇と炎症反応上昇を認め,アスペルギルス抗原が陽性であった.画像上は両側上葉に空洞形成と …
NAID 110008460780

FKS2遺伝子内変異による Micafungin 低感受性 Candida glabrata が検出された1例

乾佐知子,中村竜也,田辺公一,大野秀明,小池千裕,奥田和之,中田千代,藤本弘子,大倉ひろ枝,宮崎義継,高橋伯夫
感染症学雑誌 : 日本伝染病学会機関誌 : the journal of the Japanese Association for Infectious Diseases 85(1), 49-53, 2011-01-20
NAID 10028048310

Related Pictures

★リンクテーブル★

リンク元	「ミカファンギン」
拡張検索	「micafungin sodium」

「ミカファンギン」

Micafungin
Systematic (IUPAC) name
	{5-[(1S,2S)-2-[(3S,6S,9S,11R,15S,18S,20R,21R,24S,25S,26S)-3-[(1R)-2-carbamoyl-1-hydroxyethyl]-11,20,21,25-tetrahydroxy-15-[(1R)-1-hydroxyethyl]-26-methyl-2,5,8,14,17,23-hexaoxo-18-[(4-{5-[4-(pentyloxy)phenyl]-1,2-oxazol-3-yl}benzene)amido]-1,4,7,13,16,22-hexaazatricyclo[22.3.0.09,13]heptacosan-6-yl]-1,2-dihydroxyethyl]-2-hydroxyphenyl}oxidanesulfonic acid
Clinical data
Trade names	Mycamine
AHFS/Drugs.com	monograph
Licence data	EMA:Link, US FDA:link
Pregnancy cat.	C
Legal status	℞ Prescription only
Routes	Intravenous
Pharmacokinetic data
Protein binding	99.8%
Metabolism	Via catechol-O-methyltransferase pathway
Half-life	11–17 hours
Excretion	40% feces, <15% urine
Identifiers
CAS number	235114-32-6
ATC code	J02AX05
PubChem	CID 477468
DrugBank	DB01141
ChemSpider	21106351
UNII	R10H71BSWG
KEGG	D02465
ChEMBL	CHEMBL1201351
Chemical data
Formula	C56H71N9O23S
Mol. mass	1270.28 g/mol
	InChI InChI=1S/C56H71N9O23S/c1-4-5-6-17-86-32-14-11-28(12-15-32)39-21-33(63-87-39)27-7-9-29(10-8-27)49(75)58-34-20-38(70)52(78)62-54(80)45-46(72)25(2)23-65(45)56(82)43(37(69)22-41(57)71)60-53(79)44(48(74)47(73)30-13-16-36(68)40(18-30)88-89(83,84)85)61-51(77)35-19-31(67)24-64(35)55(81)42(26(3)66)59-50(34)76/h7-16,18,21,25-26,31,34-35,37-38,42-48,52,66-70,72-74,78H,4-6,17,19-20,22-24H2,1-3H3,(H2,57,71)(H,58,75)(H,59,76)(H,60,79)(H,61,77)(H,62,80)(H,83,84,85)/t25-,26-,31+,34-,35-,37+,38+,42-,43-,44-,45-,46-,47-,48-,52+/m0/s1 ; Key:PIEUQSKUWLMALL-NFGJWQNFSA-N ;
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　　[★]

英: micafungin, MCFG
化: ミカファンギンナトリウム micafungin sodium
商: ファンガード
関: 抗真菌薬

抗真菌薬

キャンディン系

作用機序

1,3-β-D-glucanの合成を非競合的に阻害

薬理作用

カンジダ属：殺菌的
アスペルギルス属：静菌的：発芽抑制及び伸長抑制作用

用量

アスペルギルス症：1日1回50-150mg iv
侵襲性カンジダ症：1日1回100-150mg iv

スペクトラム

無効

酵母様真菌：Cryptococcus neoformans
糸状真菌：Zygomyetes spp., Fusarium spp.

相互作用

少ない
ミカファンギン血中濃度↓：EFV、NFV、NVP、リファマイシン系、フェニトイン、カルバマゼピン

副作用

少ない。

「micafungin sodium」

　　[★] ミカファンギン。ミカファンギンナトリウム

[0] Pappas PG, Rotstein CM, Betts RF, et al, “Micafungin vVersus Caspofungin for Treatment of Candidemia and Other Forms of Invasive Candidiasis,” Clin Infect Dis, 2007, 45(7):883-93. [PubMed 17806055]

[1] Pettengell K, Mynhardt J, Kluyts T, et al, “Successful Treatment of Oesophageal Candidiasis by Micafungin: A Novel Systemic Antifungal Agent,” Aliment Pharmacol Ther, 2004, 20(4):475-81. [PubMed 15298643]

[2] Carver PL, “Micafungin,” Ann Pharmacother, 2004, 38(10):1707-21. [PubMed 15340133]

[3] Kohno S, Masaoka T, Yamaguchi H, et al, “A Multicenter, Open-Label Clinical Study of Micafungin (FK463) in the Treatment of Deep-Seated Mycosis in Japan,” Scand J Infect Dis, 36(5):372-9

[4] The Journal of Antibiotics (2009) 62, 27-35

[5] Fujie, Akihiko, Discovery of Micafungin (FK463): A novel antifungal derived from a novel product lead. Fermentation Research Laboratories, Astellas Pharma Inc., 5-2-6-Tokodai, Tsukuba, Ibaraki 300-2698, japan. Pure Appl. Chem, Vol. 79, No. 4, pp. 603-614, 2007

匿名

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案内

案内

micafungin