Indium-111-DTPA-folate as a potential folate-receptor-targeted radiopharmaceutical

Carla J. Mathias, Susan Wang, David J. Waters, John J. Turek, Philip S. Low, Mark A. Green

Research output: Contribution to journalArticle

128 Scopus citations

Abstract

Indium-111-labeled diethylenetriamine pentaacetic acid (DTPA)-folate was evaluated as a radiopharmaceutical for targeting tumor-associated folate receptors. Methods: Athymic mice were subcutaneously inoculated with ~1.8 x 106 folate receptor-positive KB (human nasopharyngeal carcinoma) cells, yielding 0.2- to 0.6-g tumors in 15 days, at which time 111In-DTPA- folate, 111In-DTPA or 111In-citrate was administered by intravenous injection. Results: The 111In-DTPA-folate conjugate afforded marked tumor- specific 111In deposition in vive using this mouse model. The involvement of the folate receptor in mediating tumor uptake of 111In-DTPA-folate was demonstrated by the blocking of tumor uptake by coadministration of free relic acid (intravenous). The 111In-DTPA-folate also shows folate receptor-mediated uptake and retention in the kidneys, presumably reflecting radiotracer binding to folate receptors of the proximal tubules. In control experiments, the 111In-citrate radiopharmaceutical precursor was also shown to afford significant tumor uptake of 111In, but with much poorer tumor-to-background tissue contrast than that obtained with 111In-DTPA- folate. Unconjugated 111In-DTPA showed no tumor affinity. Conclusion: Indium-111-DTPA-folate appears suitable as a radiopharmaceutical for targeting tumor-associated folate receptors.

Original languageEnglish (US)
Pages (from-to)1579-1585
Number of pages7
JournalJournal of Nuclear Medicine
Volume39
Issue number9
StatePublished - Sep 1 1998

Keywords

  • Folate receptor
  • Indium-111-diethylenetriamine pentaacetic acid folate
  • Tumor targeting

ASJC Scopus subject areas

  • Radiology Nuclear Medicine and imaging

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    Mathias, C. J., Wang, S., Waters, D. J., Turek, J. J., Low, P. S., & Green, M. A. (1998). Indium-111-DTPA-folate as a potential folate-receptor-targeted radiopharmaceutical. Journal of Nuclear Medicine, 39(9), 1579-1585.