Tumor detection using 18F-labeled matrix metalloproteinase-2 inhibitor

Shozo Furumoto, Kyoka Takashima, Kazuo Kubota, Tatsuo Ido, Ren Iwata, Hiroshi Fukuda

Research output: Contribution to journalArticlepeer-review

88 Citations (Scopus)


Matrix metalloproteinase-2 (MMP-2) is a key enzyme involved in tumor invasiveness. (2R)-2- [4-(6-[18F]Fluorohex-1-ynyl)-benzenesulfonylamino]-3-methylbutyric acid ([18F]SAV03), a new fluorine-18 labeled MMP-2 inhibitor developed for tumor imaging with PET, was biologically evaluated using in vivo tumor model. Enzymatic MMP-2 assay of SAV03 yielded an IC50 value of 1.9 μM. Biodistribution study of [18F]SAV03 using Ehrlich tumor bearing mice showed that the uptake in tumor was higher than in other organs, except for the liver, small intestine, and bone. When [18F]SAV03M, a methyl ester of [18F]SAV03, was used as a prodrug, the uptake in liver at 30 min after injection decreased by half and that in tumor increased by 2.4 times, compared with [18F]SAV03. Radio-thin-layer chromatographic analysis of [18F]SAV03M metabolites revealed that administered [18F]SAV03M was easily converted to the parent drug in vivo and accumulated in tumor tissue. Thus, [18F]SAV03M is suitable as the prodrug of [18F]SAV03 with potent efficacy. Whole body autoradiography using [18F]SAV03M also indicated tumor-specific accumulation of radioactivity, while higher accumulations in bone and intestinal contents were observed. Our results suggest that [18F]SAV03M could be potentially suitable for tumor imaging with PET.

Original languageEnglish
Pages (from-to)119-125
Number of pages7
JournalNuclear Medicine and Biology
Issue number2
Publication statusPublished - 2003 Feb


  • Autoradiography
  • Fluorine-18
  • Matrix metalloproteinase
  • Matrix metalloproteinase inhibitor
  • Tumor imaging

ASJC Scopus subject areas

  • Molecular Medicine
  • Radiology Nuclear Medicine and imaging
  • Cancer Research


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