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Antimicrobial Agents and Chemotherapy, January 2000, p. 57-62, Vol. 44, No. 1
0066-4804/0/$04.00+0
Copyright © 2000, American Society for Microbiology. All rights reserved.

In Vitro Activities of a New Lipopeptide Antifungal Agent, FK463, against a Variety of Clinically Important Fungi

Shuichi Tawara,1 Fumiaki Ikeda,1,* Katsuyuki Maki,1 Yoshihiko Morishita,1 Kazumi Otomo,1 Noriko Teratani,1 Toshio Goto,1 Masaki Tomishima,2 Hidenori Ohki,2 Akira Yamada,2 Koji Kawabata,2 Hisashi Takasugi,2 Kazuo Sakane,2 Hirokazu Tanaka,2 Fumio Matsumoto,3 and Shogo Kuwahara4

Medicinal Biology Research Laboratories1 and Medicinal Chemistry Research Laboratories,2 Fujisawa Pharmaceutical Co., Ltd., 1-6, 2-Chome Kashima, Yodogawa-ku, Osaka 532-8514, Kanagawa Prefectural Nursing and Hygienic School Hospital, 1-6, Shiomidai, Isogo-ku, Yokohama 235-0022,3 and Toho University School of Medicine, 21-16, 5-Chome Ohmori Nishi, Ohta-ku, Tokyo 143-8540,4 Japan

Received 3 May 1999/Returned for modification 26 July 1999/Accepted 11 October 1999

The in vitro antifungal activity and spectrum of FK463 were compared with those of amphotericin B, fluconazole, and itraconazole by using a broth microdilution method specified by National Committee for Clinical Laboratory Standards document M27-A (National Committee for Clinical Laboratory Standards, Wayne, Pa., 1997). FK463 exhibited broad-spectrum activity against clinically important pathogens including Candida species (MIC range, less-or-equivalent 0.0039 to 2 µg/ml) and Aspergillus species (MIC range, less-or-equivalent 0.0039 to 0.0313 µg/ml), and its MICs for such fungi were lower than those of the other antifungal agents tested. FK463 was also potently active against azole-resistant Candida albicans as well as azole-susceptible strains, and there was no cross-resistance with azoles. FK463 showed fungicidal activity against C. albicans, i.e., a 99% reduction in viability after a 24-h exposure at concentrations above 0.0156 µg/ml. The minimum fungicidal concentration (MFC) assays indicated that FK463 was fungicidal against most isolates of Candida species. In contrast, the MFCs of FK463 for A. fumigatus isolates were much higher than the MICs, indicating that its action is fungistatic against this species. FK463 had no activity against Cryptococcus neoformans, Trichosporon species, or Fusarium solani. Neither the test medium (kind and pH) nor the inoculum size greatly affected the MICs of FK463, while the addition of 4% human serum albumin increased the MICs for Candida species and A. fumigatus more than 32 times. Results from preclinical in vitro evaluations performed thus far indicate that FK463 should be a potent parenteral antifungal agent.

* Corresponding author. Mailing address: Department of Infectious Diseases, Medicinal Biology Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., 1-6, 2-Chome, Kashima, Yodogawa-Ku, Osaka 532-8514, Japan. Phone: 81-6-6390-1158. Fax: 81-6-6304-5367. E-mail: fumiaki_ikeda{at}po.fujisawa.co.jp.

Antimicrobial Agents and Chemotherapy, January 2000, p. 57-62, Vol. 44, No. 1
0066-4804/0/$04.00+0
Copyright © 2000, American Society for Microbiology. All rights reserved.


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