Micafungin (FK463)
(Synonyms: 米卡芬净; 咪克芬净; FK463) 目录号 : GC32244
Micafungin Sodium (FK463, Mycamine) is an inhibitor of 1, 3-beta-D-glucan synthesis, used as an antifungal drug.
Cas No.:235114-32-6
Sample solution is provided at 25 µL, 10mM.
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Micafungin Sodium (FK463, Mycamine) is an inhibitor of 1, 3-beta-D-glucan synthesis, used as an antifungal drug.
Micafungin is an antifungal agent that does not inhibit bacteria. Although micafungin does not inhibit the bacteria directly, it does promote the survival of G. mellonella[1]. Micafungin inhibits biofilm formation by impeding 1,3-β-D-glucan synthesis in Candida albicans[2].
[1] Fuchs BB, et al. Mycopathologia. 2016, 181(1-2):17-25. [2] Kissoyan KA, et al. Biofouling. 2016, 32(7):779-86.
| Cas No. | 235114-32-6 | SDF | |
| 别名 | 米卡芬净; 咪克芬净; FK463 | ||
| Canonical SMILES | O=C([C@](NC(C(NC([C@@](C[C@@H](O)C1)([H])N1C2=O)=O)[C@H](O)[C@H](C3=CC(OS(=O)(O)=O)=C(O)C=C3)O)=O)([H])[C@H](O)CC(N)=O)N4[C@@](C(N[C@@H]([C@@H](C[C@@H](C(NC2[C@H](O)C)=O)NC(C5=CC=C(C6=NOC(C7=CC=C(OCCCCC)C=C7)=C6)C=C5)=O)O)O)=O)([H])[C@@H](O)[C@@H](C)C4 | ||
| 分子式 | C56H71N9O23S | 分子量 | 1270.27 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.7872 mL | 3.9362 mL | 7.8723 mL |
| 5 mM | 0.1574 mL | 0.7872 mL | 1.5745 mL |
| 10 mM | 0.0787 mL | 0.3936 mL | 0.7872 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Micafungin (FK463), alone or in combination with other systemic antifungal agents, for the treatment of acute invasive aspergillosis
J Infect 2006 Nov;53(5):337-49.PMID:16678903DOI:10.1016/j.jinf.2006.03.003.
Background: Micafungin (FK463) is a new lipopeptide compound (echinocandin) with activity against Aspergillus and Candida species. This study evaluated the safety and efficacy of micafungin in patients with proven or probable invasive aspergillosis (IA). Methods: A multinational, non-comparative study was conducted to examine proven or probable (pulmonary only) Aspergillus species infection in a wide variety of patient populations. The study employed an open-label design utilizing micafungin alone or in combination with another systemic antifungal agent. Criteria for IA and therapeutic responses were judged by an independent panel. Results: Of the 331 patients enrolled, only 225 met diagnostic criteria for IA as determined by the independent panel and received at least one dose of micafungin. Patients included 98/225 who had undergone hematopoietic stem cell transplantation (HSCT) (88/98 allogeneic), 48 with graft versus host disease (GVHD), and 83/225 who had received chemotherapy for hematologic malignancy. A favorable response rate at the end of therapy was seen in 35.6% (80/225) of patients. Of those only treated with micafungin, favorable responses were seen in 6/12 (50%) of the primary and 9/22 (40.9%) of the salvage therapy group, with corresponding numbers in the combination treatment groups of 5/17 (29.4%) and 60/174 (34.5%) of the primary and salvage treatment groups, respectively. Of the 326 micafungin-treated patients, 183 (56.1%) died during therapy or in the 6-week follow-up phase; 107 (58.5%) deaths were attributable to IA. Conclusions: Micafungin as primary or salvage therapy proved efficacious and safe in high-risk patients with IA, although patient numbers are small in the micafungin-only groups.
Effect of Micafungin (FK463) on Candida albicans adherence to epithelial cells
Chemotherapy 2002 Jul;48(3):148-53.PMID:12138332DOI:10.1159/000064921.
Background: Adherence is considered a major virulence trait of Candida albicans. FK463 is a new investigational intravenous antifungal of the 'candin family' with potent in vitro and in vivo activity against Candida spp. Objective: The aim of the present study was to investigate the effect of Micafungin (FK463) on Candida adherence to epithelial cells of azole-sensitive and azole-resistant C. albicans isolates. Methods: An in vitro assay using microtest plate technology and fluorescence measurement was developed to compare the adherence of C. albicans SC5314 and of paired C. albicans isolates to epithelial cells in the presence and in the absence of FK463. Results: FK463 showed a marked inhibitory effect on the adherence of C. albicans SC5314. The addition of FK463 reduced the adherence of C. albicans SC5314 to 90% of the value of control without drug. A dose-dependent adherence inhibition was observed with FK463 in the range of 10-0.015 microg ml(-1). The comparison of paired C. albicans isolates, either a fluconazole-susceptible and a fluconazole-resistant isolate of one patient, revealed no significant difference in the adherence behavior between azole-susceptible and azole-resistant. Conclusion: Micafungin (FK463) has the capacity to reduce adherence of C. albicans azole-susceptible and azole-resistant strains to epithelial cells.
Micafungin for the treatment of invasive aspergillosis
J Infect 2014 Jun;68(6):507-26.PMID:24480373DOI:10.1016/j.jinf.2014.01.007.
Invasive aspergillosis is a major cause of morbidity and mortality in immunocompromised patients, particularly those with neutropenia and those undergoing bone marrow or stem cell transplants. Micafungin is an echinocandin antifungal drug with activity against all major Candida spp. Currently, Micafungin is indicated for treatment of invasive candidiasis, oesophageal candidiasis and prophylaxis of Candida infection in patients undergoing allogeneic haematopoietic stem cell transplantation or patients who are expected to have neutropenia. Micafungin demonstrates in vitro and in vivo activity against Aspergillus spp. It is currently not licensed to treat Aspergillus infections in the UK or USA. This review summarises the current evidence base surrounding the clinical use of Micafungin in the treatment of invasive aspergillosis to consider the potential role of Micafungin in these patients. There are currently no randomised studies comparing Micafungin with standard antifungal therapy. Prospective non-randomised clinical studies, predominantly performed in Japan, involving 492 patients with aspergillosis and 455 febrile patients with chemotherapy-induced neutropenia suggest that Micafungin may be as effective as comparator antifungal agents. Other clinical evidence is limited to case reports. Further experience in the form of randomised controlled trials is required to establish the exact role of Micafungin in the context of currently available broad-spectrum antifungal agents.
Safety, tolerability, and pharmacokinetics of Micafungin (FK463) in febrile neutropenic pediatric patients
Antimicrob Agents Chemother 2005 Aug;49(8):3317-24.PMID:16048942DOI:10.1128/AAC.49.8.3317-3324.2005.
Micafungin (FK463) is a new parenteral echinocandin. A multicenter, phase I, open-label, sequential-group dose escalation study was conducted to assess the safety, tolerability, and pharmacokinetics of micafungin in neutropenic pediatric patients. A total of 77 patients stratified by age (2 to 12 and 13 to 17 years) received micafungin. Therapy was initiated at 0.5 mg/kg per day and escalated to higher dose levels of 1.0, 1.5, 2.0, 3.0, and 4.0 mg/kg per day. Micafungin was administered within 24 h of initiating broad-spectrum antibacterial antibiotics for the new onset of fever and neutropenia. The most common overall adverse events in the study population were diarrhea (19.5%), epistaxis (18.2%), abdominal pain (16.9%), and headache (16.9%). Nine patients (12%) experienced adverse events considered by the investigator to be possibly related to the study drug. The most common related events were diarrhea, vomiting, and headache, all occurring in two patients each. There was no evidence of a dose-limiting toxicity as defined within the prespecified criteria of this clinical protocol. There was one death during the study due to septic shock. The pharmacokinetic profiles for micafungin over the 0.5- to 4.0-mg/kg dose range demonstrated dose linearity. Clearance, volume of distribution, and half-life remained relatively constant over the dose range and did not change with repeated administration. The overall plasma pharmacokinetic profile was similar to that observed in adults. However, there was an inverse relation between age and clearance. For patients 2 to 8 years old, clearance was approximately 1.35 times that of patients >/=9 years of age. In summary, micafungin over a dosage range between 0.5 and 4.0 mg/kg/day in 77 febrile neutropenic pediatric patients displayed linear pharmacokinetics and increased clearance as a function of decreasing age.
A multicenter, open-label clinical study of Micafungin (FK463) in the treatment of deep-seated mycosis in Japan
Scand J Infect Dis 2004;36(5):372-9.PMID:15287383DOI:10.1080/00365540410020406.
The efficacy and safety of Micafungin (FK463), which is a new lipopeptide antifungal agent of the echinocandin class and is active against both Aspergillus and Candida species, were investigated in patients with deep-seated mycosis in this study. 70 patients were treated with micafungin 12.5-150 mg/d intravenously for up to 56 d. The overall clinical response rates were 60% (6/10) in invasive pulmonary aspergillosis, 67% (6/9) in chronic necrotizing pulmonary aspergillosis, 55% (12/22) in pulmonary aspergilloma, 100% (6/6) in candidemia, and 71% (5/7) in esophageal candidiasis. The response rates for patients with prior antifungal treatment which was considered ineffective or toxic, were similar to rates for patients without prior treatment. Mycological eradication was observed in patients infected with Aspergillus fumigatus, Aspergillus flavus, Aspergillus terreus, Aspergillus niger, Candida albicans, Candida glabrata, or Candida krusei. Adverse events related to micafungin were reported in 21 patients (30%), and there was no dose-related occurrence of any adverse event. It is concluded that treatment with micafungin as monotherapy seems to be effective and safe in patients with deep-seated mycosis.