Synthesis and evaluation of 99mTc(CO)3-DTPA-folate as a folate-receptor-targeted radiopharmaceutical

David P. Trump, Carla J. Mathias, Zhenfan Yang, Philip S. Low, Mary Marmion, Mark A. Green

Research output: Contribution to journalArticle

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Abstract

A folate-receptor-targeted 99mTc-radiopharmaceutical, [99mTc]Tc(CO)3DTPA-folate, was prepared by heating [99mTc]Tc(CO)3(H2O)3+ in an aqueous solution of the previously reported DTPA-folate conjugate. The radiotracer was HPLC purified (> 98% radiochemical purity) and evaluated in vitro and in vivo as an agent for targeting folate-receptor-positive cells. [99mTc]Tc(CO)3DTPA-folate experienced high, folate-receptor-specific uptake in human KB tumor cells. Intravenous administration of [99mTc]Tc(CO)3DTPA-folate to athymic mice bearing KB cell tumor xenografts resulted in 99mTc tumor uptake of 1.8 ± 0.5 and 3.3 ± 0.2%ID/g (n = 3) at 30 minutes and 4 hours post-injection, respectively. Tumor uptake was reduced when folic acid was co-administered with the intravenous [99mTc]Tc(CO)3DTPA-folate, consistent with radiopharmaceutical localization being mediated by the folate receptor.

Original languageEnglish (US)
Pages (from-to)569-573
Number of pages5
JournalNuclear Medicine and Biology
Volume29
Issue number5
DOIs
StatePublished - Jul 2 2002

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Keywords

  • Folate binding protein
  • Tc(CO)-DTPA-folate
  • Technetium carbonyl
  • Tumor-targeting

ASJC Scopus subject areas

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

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