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

doi:10.1016/S0969-8051(02)00310-4

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

Houston Methodist

Research output: Contribution to journal › Article › peer-review

66 Scopus citations

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 language	English (US)
Pages (from-to)	569-573
Number of pages	5
Journal	Nuclear Medicine and Biology
Volume	29
Issue number	5
DOIs	https://doi.org/10.1016/S0969-8051(02)00310-4
State	Published - 2002

Keywords

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

ASJC Scopus subject areas

Cancer Research
Molecular Medicine
Radiology Nuclear Medicine and imaging

Access to Document

10.1016/S0969-8051(02)00310-4

Cite this

@article{f6fbcc1d096f4029851fb7b920a99ee4,

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

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.",

keywords = "Tc(CO)-DTPA-folate, Folate binding protein, Technetium carbonyl, Tumor-targeting",

author = "Trump, \{David P.\} and Mathias, \{Carla J.\} and Zhenfan Yang and Low, \{Philip S.\} and Mary Marmion and Green, \{Mark A.\}",

note = "Funding Information: This work was partially supported by grant RO1-CA70845 awarded by the National Institutes of Health.",

year = "2002",

doi = "10.1016/S0969-8051(02)00310-4",

language = "English (US)",

volume = "29",

pages = "569--573",

journal = "Nuclear Medicine and Biology",

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T1 - Synthesis and evaluation of 99mTc(CO)3-DTPA-folate as a folate-receptor-targeted radiopharmaceutical

AU - Trump, David P.

AU - Mathias, Carla J.

AU - Yang, Zhenfan

AU - Low, Philip S.

AU - Marmion, Mary

AU - Green, Mark A.

N1 - Funding Information: This work was partially supported by grant RO1-CA70845 awarded by the National Institutes of Health.

PY - 2002

Y1 - 2002

N2 - 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.

AB - 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.

KW - Tc(CO)-DTPA-folate

KW - Folate binding protein

KW - Technetium carbonyl

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