Skip to main content
Log in

Micafungin

  • Adis Drug Profile
  • Published:
Drugs Aims and scope Submit manuscript

Abstract

  • ▴ Micafungin, an echinocandin antifungal agent with a novel mechanism of action, inhibits β-(l,3)-D-glucan synthase interfering with fungal cell wall synthesis. It shows excellent antifungal activity against a broad range of Candida spp., including azole-resistant strains, and Aspergillus spp. in in vitro and animal studies.

  • ▴ In HIV-positive patients, intravenous micafungin 50–150 mg/day dose-dependently eradicated endoscopically confirmed oesophageal candidiasis, with micafungin 100 and 150 mg/day being more effective than micafungin 50 mg/day and as effective as fluconazole 200 mg/day in a double-blind trial.

  • ▴ In nonblind trials, micafungin (monotherapy or combination therapy) was effective against invasive aspergillosis, candidiasis and candidaemia in paediatric and adult patients with newly diagnosed or refractory infections.

  • ▴ Micafungin 50 mg/day provided significantly better antifungal prophylaxis than fluconazole 400 mg/ day in 882 haematopoietic stem cell transplant recipients in a randomised, double-blind trial. Respective overall success rates were 80% and 73.5%.

  • ▴ Micafungin is generally well tolerated. Adverse events were not dose- or infusion-related with micafungin 12.5–900 mg/day; no histamine-like reactions occurred. Micafungin was as well tolerated as fluconazole, with numerically fewer micafungin recipients discontinuing treatment (4.2% vs 7.2%).

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Fig. 1
Fig. 2
Fig. 3

Similar content being viewed by others

References

  1. Arathoon EG. Clinical efficacy of echinocandin antifungals. Curr Opin Infect Dis 2001 Dec; 14(6): 685–91

    Article  PubMed  CAS  Google Scholar 

  2. O’Grady NP, Alexander M, Dellinger EP, et al. Guidelines for the prevention of intravascular catheter-related infections. MMWR 2002; 51(RR10): 1–26

    PubMed  Google Scholar 

  3. Graybill JR. Hitting a new target with echinocandins: why chase something else? Curr Opin Invest Drug 2001; 2(4): 468–71

    CAS  Google Scholar 

  4. Groll AH, Walsh TJ. FK-463 Fujisawa Pharmaceutical Co Ltd. Curr Opin Anti-Infect Invest Drugs 2000; 2(4): 405–12

    CAS  Google Scholar 

  5. Nishiyama Y, Uchida K, Yamaguchi H. Morphological changes of Candida albicans induced by micafungin (FK463), a water-soluble echinocandin-like lipopeptide. J Electron Microsc (Tokyo) 2002; 51(4): 247–55

    Article  CAS  Google Scholar 

  6. Rex JH, Pfaller MA, Walsh TJ, et al. Antifungal susceptibility testing: practical aspects and current challenges. Clin Microbiol Rev 2001; 14(4): 643–58

    Article  PubMed  CAS  Google Scholar 

  7. Müller FM, Kurzai O, Hacker J, et al. Effect of the growth medium on the in vitro antifungal activity of micafungin (FK-463) against clinical isolates of Candida dubliniensis. J Antimicrob Chemother 2001 Nov; 48(5): 713–5

    Article  PubMed  Google Scholar 

  8. Tomishima M, Ohki H, Yamada A, et al. FK463, a novel water-soluble echinocandin lipopeptide: synthesis and antifungal activity [letter]. J Antibiot (Tokyo) 1999 Jul; 52(7): 674–6

    Article  CAS  Google Scholar 

  9. Mikamo H, Sato Y, Tamaya T. In vitro antifungal activity of FK463, a new water-soluble echinocandin-like lipopeptide. J Antimicrob Chemother 2000 Sep; 46(3): 485–7

    Article  PubMed  CAS  Google Scholar 

  10. Laverdiere M, Hoban D, Restieri C, et al. In vitro activity of three new triazoles and one echinocandin against Candida bloodstream isolates from cancer patients. J Antimicrob Chemother 2002 Jul; 50(1): 119–23

    Article  PubMed  CAS  Google Scholar 

  11. Tawara S, Ikeda F, Maki K, et al. In vitro activities of a new lipopeptide antifungal agent, FK463, against a variety of clinically important fungi. Antimicrob Agents Chemother 2000 Jan; 44(1): 57–62

    Article  PubMed  CAS  Google Scholar 

  12. Ostrosky-Zeichner L, Rex JH, Pappas PG, et al. Antifungal susceptibility survey of 2,000 bloodstream Candida isolates in the United States. Antimicrob Agents Chemother 2003 Oct; 47(10): 3149–54

    Article  PubMed  CAS  Google Scholar 

  13. Uchida K, Nishiyama Y, Yokota N, et al. In vitro antifungal activity of a novel lipopeptide antifungal agent, FK463, against various fungal pathogens. J Antibiot (Tokyo) 2000 Oct; 53(10): 1175–81

    Article  CAS  Google Scholar 

  14. Nakai T, Uno J, Ikeda F, et al. In vitro antifungal activity of micafungin (FK463) against dimorphic fungi: comparison of yeast-like and mycelial forms. Antimicrob Agents Chemother 2003 Apr; 47(4): 1376–81

    Article  PubMed  CAS  Google Scholar 

  15. Stevens DA. Drug interaction in vitro between a polyene (AmBisone; Ambi) and an echinocandin (FK463; FK) vs. Aspergillus species. Proceedings of the 39th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1999 Sep 26–30; San Francisco, 543

  16. Ostrosky-Zeichner L, Matar M, Paetznick VL, et al. In-vitro synergy testing of anidulafungin (AFG) and micafungin (MFG) in combination with amphotericin B (AMB) against Aspergillus spp. and Fusarium spp. [abstract no. M-1816] Proceedings of the 42nd Interscience Conference on Antimicrobial Agents and Chemotherapy; 2002 Sep 27–30; San Diego

  17. Manavathu EK, Ganesan LT, Cutright PH, et al. In vitro antifungal activity of voriconazole in two-drug combination with micafungin, caspofungin and amphotericin B [abstract no. J-125]. Proceedings of the 41st Interscience Conference on Antimicrobial Agents and Chemotherapy; 2001 Dec 16–19; Chicago

  18. Chiou CC, Mavrogiorgos N, Tillem E, et al. Synergy, pharmacodynamics, and time-sequenced ultrastructural changes of the interaction between nikkomycin Z and the echinocandin FK463 against Aspergillus fumigatus. Antimicrob Agents Chemother 2001 Dec; 45(12): 3310–21

    Article  PubMed  CAS  Google Scholar 

  19. O’Shaughnessy EM, Peter J, Walsh TJ. In vitro additive and synergistic effect of two echinocandins, caspofungin and micafungin with voriconazole against Aspergillus fumigatus [abstract no. M-856]. Proceedings of the 42nd Interscience Conference on Antimicrobial Agents and Chemotherapy; 2002 Sep 27–30; San Diego

  20. Ernst EJ, Roling EE, Petzold CR, et al. In vitro activity of micafungin (FK-463) against Candida spp.: microdilution, time-kill, and postantifungal-effect studies. Antimicrob Agents Chemother 2002 Dec; 46(12): 3846–53

    Article  PubMed  CAS  Google Scholar 

  21. Manavathu EK, Ramesh MS, Baskaran I, et al. A comparative study of the post-antifungal effect (PAFE) of amphotericin B, triazoles and echinocandins on Aspergillus fumigatus and Candida albicans. J Antimicrob Chemother 2004 Feb; 53(2): 386–9

    Article  PubMed  CAS  Google Scholar 

  22. Kuhn DM, George T, Chandra J, et al. Antifungal susceptibility of Candida biofilms: unique efficacy of amphotericin B lipid formulations and echinocandins. Antimicrob Agents Chemother 2002 Jun; 46(6): 1773–80

    Article  PubMed  CAS  Google Scholar 

  23. Borg-Von Zepelin M, Zaschke K, Gross U, et al. Effect of micafungin (FK463) on Candida albicans adherence to epithelial cells. Chemotherapy 2002 Jul; 48(3): 148–53

    Article  PubMed  CAS  Google Scholar 

  24. Maesaki S, Hossain MA, Miyazaki Y, et al. Efficacy of FK463, a (l,3)-beta-D-glucan synthase inhibitor, in disseminated azole-resistant Candida albicans infection in mice. Antimicrob Agents Chemother 2000 Jun; 44(6): 1728–30

    Article  PubMed  CAS  Google Scholar 

  25. Ikeda F, Wakai Y, Matsumoto S, et al. Efficacy of FK463, a new lipopeptide antifungal agent, in mouse models of disseminated candidiasis and aspergillosis. Antimicrob Agents Chemother 2000 Mar; 44(3): 614–8

    Article  PubMed  CAS  Google Scholar 

  26. Warn PA, Sharp A, Morrissey G, et al. In vivo activity of micafungin in a persistently neutropenic murine model of disseminated infection caused by Candida tropicalis. J Antimicrob Chemother 2002 Dec; 50(6): 1071–4

    Article  PubMed  CAS  Google Scholar 

  27. Warn PA, Morrissey G, Morrissey J, et al. Activity of micafungin (FK463) against an itraconazole-resistant strain of Aspergillus fumigatus and a strain of Aspergillus terreus demonstrating in vivo resistance to amphotericin B. J Antimicrob Chemother 2003; 51: 913–9

    Article  PubMed  CAS  Google Scholar 

  28. Luque JC, Clemons KV, Stevens DA. Efficacy of micafungin alone or in combination against systemic murine aspergillosis. Antimicrob Agents Chemother 2003 Apr; 47(4): 1452–5

    Article  PubMed  CAS  Google Scholar 

  29. Matsumoto S, Wakai Y, Nakai T, et al. Efficacy of FK463, a new lipopeptide antifungal agent, in mouse models of pulmonary aspergillosis. Antimicrob Agents Chemother 2000 Mar; 44(3): 619–21

    Article  PubMed  CAS  Google Scholar 

  30. Kohno S, Maesaki S, Iwakawa J, et al. Synergistic effects of combination of FK463 with amphotericin B: enhanced efficacy in murine model of invasive pulmonary aspergillosis [abstract no. 1686]. Proceedings of the 40th Interscience Conference on Antimicrobial Agents and Chemotherapy; 2000 Sep 17–20; Toronto

  31. Petraitis V, Petraitiene R, Groll AH, et al. Comparative anti-fungal activities and plasma pharmacokinetics of micafungin (FK463) against disseminated candidiasis and invasive pulmonary aspergillosis in persistently neutropenic rabbits. Antimicrob Agents Chemother 2002 Jun; 46(6): 1857–69

    Article  PubMed  CAS  Google Scholar 

  32. Ito M, Nozu R, Kuramochi T, et al. Prophylactic effect of FK463, a novel antifungal lipopeptide, against Pneumocystis carinii infection in mice. Antimicrob Agents Chemother 2000 Sep; 44(9): 2259–62

    Article  PubMed  CAS  Google Scholar 

  33. Tawara S, Nakai T, Matsumoto K, et al. Effect of micafungin and caspofungin on histamine release, blood pressure and heart rate in rats [abstract no. 29]. Proceedings of the 12th Annual Focus on Fungal Infections Meeting; 2002 Mar 14–16; Phoenix

  34. Groll AH, Mickiene D, Petraitis V, et al. Compartmental pharmacokinetics and tissue distribution of the antifungal echinocandin lipopeptide micafungin (FK463) in rabbits. Antimicrob Agents Chemother 2001 Dec; 45(12): 3322–7

    Article  PubMed  CAS  Google Scholar 

  35. Suzuki S, Terakawa M, Yokobayashi F, et al. Pharmacokinetics of FK463, a novel water-soluble echinocandin-like lipopeptide, in animals [abstract no. F-144]. Proceedings of the 38th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1998 Sep 24–27; San Diego, 269

  36. Azuma J, Yamamoto I, Ogura M, et al. Phase I study of FK463, a new antifungal agent, in healthy adult male volunteers [abstract no. F-146]. Proceedings of the 38th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1998 Sep 24–27; San Diego, 269

  37. Townsend R, Terakawa M, Bekersky I. PK/disposition of 14C/ FK463, a novel echinocandin antifungal, in male volunteers [abstract]. J Clin Pharmacol 2000 Sep; 40: 1048

    Google Scholar 

  38. Mukai T, Ohkuma T, Nakahara K, et al. Pharmacokinetics of FK463, a novel echinocandin analogue, in elderly and non-elderly subjects [abstract]. Proceedings of the 41st Interscience Conference on Antimicrobial Agents and Chemotherapy; 2001 Dec 15–19; Chicago

  39. Townsend R, Hebert M, Wisemandle W, et al. Concomitant pharmacokinetics (PK) of micafungin, an echinocandin antifungal, and tacrolimus in healthy volunteers [abstract]. Proceedings of the 31st Annual Meeting of the American College of Clinical Pharmacology; 2002 Sep 21–23; San Francisco

  40. Townsend R, Hebert M, Wisemandle W, et al. Concomitant pharmacokinetics (PK) of micafungin, an echinocandin antifungal, and cyclosporine in healthy volunteers [abstract]. Proceedings of the 31st Annual Meeting of the American College of Clinical Pharmacology; 2002 Sep 21–23; San Francisco

  41. Townsend R, Bekersky I, Buell DN, et al. Pharmacokinetic (PK) evaluation of echinocandin FK463 in pediatric and adult patients [abstract no. 024]. Proceedings of the 11th Focus on Fungal Infections Meeting; 2001 Mar 14–16; Washington, DC

  42. Heresi GP, Gertsmann DR, Blumer JL, et al. Pharmacokinetic, safety, and tolerance study of micafungin (FK463) in premature infants [abstract]. Proceedings of the Pediatric Academic Societies Annual Meeting; 2003 May 3–6; Seattle

  43. Hiemenz J, Cagnoni P, Simpson D, et al. Maximum tolerated dose and pharmacokinetics of FK463 in combination with fluconazole for the prophylaxis of fungal infections in adult bone marrow or peripheral stem cell transplant patients [abstract]. Proceedings of the 39th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1999 Sep 26–30; San Francisco, 576

  44. Townsend R, Terakawa M, Bekersky I. Pharmacokinetics of FK463, a novel echinocandin antifungal, in bone marrow or peripheral stem cell transplant patients [abstract]. J Clin Pharmacol 2000 Sep; 40: 1049

    Google Scholar 

  45. Townsend R, Hebert M, Dessimoz M, et al. Pharmacokinetics (PK) of micafungin, an echinocandin antifungal, in subjects with severe renal dysfunction [abstract]. Proceedings of the 31st Annual Meeting of the American College of Clinical Pharmacology; 2002 Sep 21–23; San Francisco

  46. Townsend R, Hebert M, Dessimoz M, et al. Pharmacokinetics (PK) of micafungin, an echinocandin antifungal, in subjects with moderate hepatic dysfunction (MHD) [abstract]. Proceedings of the 31st Annual Meeting of the American College of Clinical Pharmacology; 2002 Sep 21–23; San Francisco

  47. Seibel N, Schwartz C, Arrieta A, et al. A phase I study to determine the safety and pharmacokinetics of FK463 (echinocandin) in febrile neutropenic pediatric patients [abstract no. 18]. Proceedings of the 40th Interscience Conference on Antimicrobial Agents and Chemotherapy; 2000 Sep 17–20; Toronto

  48. Kohno S, Masaoka T, Yamaguchi H. A multicenter, open-label clinical study of FK463 in patients with deep mycosis in Japan [abstract]. Proceedings of the 41st Interscience Conference on Antimicrobial Agents and Chemotherapy; 2001 Dec 16–19; Chicago

  49. Kontoyiannis DP, Buell D, Frisbee-Hume S, et al. Initial experience with FK-463 for the treatment of candidemia in cancer patients [abstract no. J-1629]. Proceedings of the 41st Interscience Conference on Antimicrobial Agents and Chemotherapy; 2001 Dec 16–19; Chicago, 394

  50. Ullmann AJ, Van Burik JA, McSweeney P, et al. An open phase II study of the efficacy of micafungin (FK463) alone and in combination for the treatment of invasive aspergillosis (IA) in adults and children [abstract no. 0400]. Clin Microbiol Infect 2003; 9 (6)

  51. Ratanatharathorn V, Flynn P, Van Burik J-A, et al. Micafungin in combination with systemic antifungal agents in the treatment of refractory aspergillosis (RA) in bone marrow transplant (BMT) patients [abstract no. 2472]. Proceedings of the 44th Annual Meeting of the American Society of Hematology; 2002 Dec 6–10; Philadelphia

  52. De Wet NTE, Llanos-Cuentas A, Suleiman H, et al. Micafungin (FK463) dose response and comparison with fluconazole in oesophageal candidiasis [abstract no. M-1754]. Proceedings of the 43rd Interscience Conference on Antimicrobial Agents and Chemotherapy; 2003 Sep 14–17; Chicago

  53. Pettengell K, MynhardtJ, Kluyts T, et al. A multicenter study of the echinocandin antifungal FK463 for the treatment of esophageal candidiasis in HIV positive patients [abstract]. Proceedings of the 40th Interscience Conference on Antimicrobial Agents and Chemotherapy; 2000 Sep 17–20; Toronto, 371

  54. Pettengell K, MynhardtJ, Kluyts T, et al. A multicenter study to determine the minimal effective dose of FK463 for the treatment of esophageal candidiasis in HIV-positive patients [abstract]. Proceedings of the 39th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1999 Sep 26–29; San Francisco, 567

  55. Suleiman J, Delia Negra M, Llanos-Cuentas A, et al. Open label study of micafungin in the treatment of esophageal candidiasis (EC) [abstract no. M-892]. Proceedings of the 42nd Conference on Antimicrobial Agents and Chemotherapy; 2002 Sep 27–30; San Diego

  56. Powles R, Sirohi B, Chopra R, et al. Assessment of maximum tolerated dose and pharmacokinetics of FK463 in neutropenic patients after haematopoietic stem cell transplantation [abstract]. Blood 2001 Nov 16; 98 (Pt 2): 361

    Google Scholar 

  57. Powles R, Sirohi B, Chopra R, et al. Use of FK 463, a novel echinocandin analog in patients undergoing stem cell transplantation (SCT) for hematologic malignancies, a matched pair comparison of biochemical toxicity with historical controls [abstract]. Bone Marrow Transplant 2002 Mar; 29 Suppl. 2: S247

    Google Scholar 

  58. Anaissie E, Kontoyiannia D, Raffali J, et al. Micafungin (MCFG), an echinocandin antifungal agent for the treatment of new and refractory candidemia [abstract no. P-35]. Proceedings of the 13th Annual Focus on Fungal Infections Meeting; 2003 Mar 19–21; Maui (HI)

  59. Van Burik J, Ratanatharathorn V, Lipton J, et al. Randomized, double-blind trial of micafungin (MI) versus fluconazole (FL) for prophylaxis of invasive fungal infections in patients (pts) undergoing hematopoietic stem cell transplant (HSCT), NIAID/BAMSG protocol 46 [abstract no. M-1238]. Proceedings of the 42nd Interscience conference on Antimicrobial Agents and Chemotherapy; 2002 Sep 27–30; San Diego

  60. Kemper M, Weinstein A, Frame D, et al. Incidence and consequences of nephrotoxicity in HSCT treated with empiric amphotericin, micafungin or no anti-fungal agent [abstract no. P-49]. Proceedings of the 13th Annual Focus on Fungal Infections Meeting; 2003 Mar 19–21; Maui (HI)

  61. Fujisawa Pharmaceutical Co., Ltd. Funguard® for infusion 50mg. Funguard® for infusion 75mg [prescribing information]. Japan: Fujisawa Pharmaceutical Co. Ltd, 2003

    Google Scholar 

  62. Japanese premium for micafungin. Scrip 2002 Dec; 2806: 22

  63. Fujisawa Healthcare Inc. Fujisawa Healthcare, Inc. submits NDA for new antifungal product [online]. Available from URL: http://www.fujisawa.com [Accessed 2002 Aug 8]

  64. Fujisawa GmbH. Fujisawa GmbH submits new antifungal drug in Europe [online]. Available from URL: http://www.fujisawaeurope.com [Accessed 2003 Mar 1]

Download references

Author information

Authors and Affiliations

Authors

Corresponding author

Correspondence to Lesley J. Scott.

Rights and permissions

Reprints and permissions

About this article

Cite this article

Jarvis, B., Figgitt, D.P. & Scott, L.J. Micafungin. Drugs 64, 969–982 (2004). https://doi.org/10.2165/00003495-200464090-00004

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.2165/00003495-200464090-00004

Keywords

Navigation