A New Potent Angiogenesis Inhibitor, FR-118487

  • Otsuka, Takanao (Exploratory Research Laboratories, Fujisawa Pharmaceutical Co. Ltd.) ;
  • Ohkawa, Takehiko (Exploratory Research Laboratories, Fujisawa Pharmaceutical Co. Ltd.) ;
  • Shibata, Toshihiro (Exploratory Research Laboratories, Fujisawa Pharmaceutical Co. Ltd.) ;
  • Oku, Teruo (Exploratory Research Laboratories, Fujisawa Pharmaceutical Co. Ltd.) ;
  • Okuhara, Masakuni (Exploratory Research Laboratories, Fujisawa Pharmaceutical Co. Ltd.) ;
  • Terano, Hiroshi (Exploratory Research Laboratories, Fujisawa Pharmaceutical Co. Ltd.) ;
  • Kohsaka, Masanobu (Exploratory Research Laboratories, Fujisawa Pharmaceutical Co. Ltd.) ;
  • Imanaka, Hiroshi (Exploratory Research Laboratories, Fujisawa Pharmaceutical Co. Ltd.)
  • Published : 1991.10.01

Abstract

A new angiogenesis inhibitor, FR-118487 was obtained by chemical modification of FR-111142 which was isolated from the fermentation products of Scolecobasidium arenarium F-2015. The antiangiogenic activity of FR-118487 was compared with that of the parent compound, FR-111142. In the endothelial cell proliferation test in vitro and the angiogenesis in the chick embryo chorioal-lantoic membrane assay, FR-118487 had about 5∼10 times stronger antiangiogenic activities than FR-111142. In addition, FR-118487 inhibited the angiogenesis in the rabbit corneal assay and suppressed the solid tumor growth in mice. These findings showed that FR-118487 would be a unique antiangiogenic agent with promising antitumor activity.

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