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Research Paper
99mTc-Tetraethylenepentamine-Folate a New 99mTc Based Folate Derivative for the Detection of Folate Receptor Positive Tumors: Synthesis and Biological Evaluation
Puja Panwar, Vibha Srivastava, Vibha Tandon, Pushpa Mishra, Krishna Chuttani, Rakesh K. Sharma, Ramesh Chandra and Anil K. Mishra
volume 3 | issue 10
october 2004Pages: 995-1001
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A new radiopharmaceutical, 99mTc-Tetraethylenepentamine(TEPA)-Folate has been synthesized introducing TEPA (triethylenepenatamine) to the _-carboxyl group of folic acid. This binds with 99mTc high efficiency at ambient temperature. The resulting 99mTc-N5-folate is stable under physiological conditions at least for 24 hr after radiocomplexation. TEPA is a known open chain pentamine (N5) chelator, its four-nitrogen act as the binding site for 99mTc. The folate membrane receptor binding of the 99mTc-TEPA-Folate by established human tumor cell lines (KB, U-87MG and MDA-MB-468) showed KD in _M range in normal DMEM (10% serum, 10 _M folic acid). The blood kinetic studies showed more than 70% clearance within 5 minutes from the circulation. The KB cell line tumors in mice were readily identifiable in the _ images and revealed major accumulation of radiotracer in liver, kidneys and intestines. High tumor uptake was shown in the tumor bearing nude mice; tumor to blood ratios reached 2.68 ± 0.52 and 5.5 ± 1.47 at 1 and 4 h after post injection respectively. Surviving fractions as obtained in clonogenic assay were 1.02 ± 0.07 and 1.03 ± 0.05 in U-87MG and MDA-MB-468 cell lines respectively. The 99mTc-N5-Folate conjugate have promising utility as a receptor specific radiopharmaceutical for imaging neoplastic tissues known to over express folate-binding protein.
We now provide open access to journal articles published online for one year or more. This article may be downloaded at the following link:
Download PDFIf the document does not open, please right-click on the link (control-click on a Macintosh) and select the option to save the file to disk.