1. Academic Validation
  2. In vitro and in vivo antifungal activities of T-2307, a novel arylamidine

In vitro and in vivo antifungal activities of T-2307, a novel arylamidine

  • Antimicrob Agents Chemother. 2008 Apr;52(4):1318-24. doi: 10.1128/AAC.01159-07.
Junichi Mitsuyama 1 Nobuhiko Nomura Kyoko Hashimoto Eio Yamada Hiroshi Nishikawa Makoto Kaeriyama Akiko Kimura Yozo Todo Hirokazu Narita
Affiliations

Affiliation

  • 1 Research Laboratories, Toyama Chemical Co. Ltd., 2-4-1 Shimookui, Toyama 930-8508, Japan. Junichi_Mitsuyama@toyama-chemical.co.jp
Abstract

The in vitro and in vivo Antifungal activities of T-2307, a novel arylamidine, were evaluated and compared with those of fluconazole, voriconazole, micafungin, and amphotericin B. T-2307 exhibited broad-spectrum activity against clinically significant pathogens, including Candida species (MIC range, 0.00025 to 0.0078 microg/ml), Cryptococcus neoformans (MIC range, 0.0039 to 0.0625 microg/ml), and Aspergillus species (MIC range, 0.0156 to 4 microg/ml). Furthermore, T-2307 exhibited potent activity against fluconazole-resistant and fluconazole-susceptible-dose-dependent Candida albicans strains as well as against azole-susceptible strains. T-2307 exhibited fungicidal activity against some Candida and Aspergillus species and against Cryptococcus neoformans. In mouse models of disseminated candidiasis, cryptococcosis, and aspergillosis, the 50% effective doses of T-2307 were 0.00755, 0.117, and 0.391 mg.kg(-1).dose(-1), respectively. This agent was considerably more active than micafungin and amphotericin B against candidiasis and than amphotericin B against cryptococcosis, and its activity was comparable to the activities of micafungin and amphotericin B against aspergillosis. The results of preclinical in vitro and in vivo evaluations performed thus far indicate that T-2307 could represent a potent injectable agent for the treatment of candidiasis, cryptococcosis, and aspergillosis.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-114220
    98.41%, Antifungal Agent