Preparation of 66Ga- and 68Ga-labeled Ga(III)-deferoxamine-folate as potential folate-receptor-targeted PET radiopharmaceuticals

Carla J. Mathias; Michael R. Lewis; David E. Reichert; Richard Laforest; Terry L. Sharp; Jason S. Lewis; Zhen Fan Yang; David J. Waters; Paul W. Snyder; Philip S. Low; Michael J. Welch; Mark A. Green

doi:10.1016/S0969-8051(03)00080-5

Preparation of ⁶⁶Ga- and ⁶⁸Ga-labeled Ga(III)-deferoxamine-folate as potential folate-receptor-targeted PET radiopharmaceuticals

Carla J. Mathias, Michael R. Lewis, David E. Reichert, Richard Laforest, Terry L. Sharp, Jason S. Lewis, Zhen Fan Yang, David J. Waters, Paul W. Snyder, Philip S. Low, Michael J. Welch, Mark A. Green

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Abstract

A folate-receptor-targeting radiopharmaceutical, Ga(III)-deferoxamine-folate (Ga-DF-Folate), was radiolabeled with two positron-emitting isotopes of gallium, cyclotron-produced ⁶⁶Ga (9.5 hour half-life) and generator-produced ⁶⁸Ga (68 minute half-life). The [⁶⁶Ga]Ga-DF-Folate was administered to athymic mice with folate-receptor-positive human KB cell tumor xenografts to demonstrate that microPET mouse tumor imaging is feasible with ⁶⁶Ga, despite the relatively high positron energy of this radionuclide. Using the athymic mouse KB tumor xenograft model, dual-isotope autoradiography was also performed following i.v. co-administration of [¹⁸F]-FDG, a marker of regional metabolic activity, and folate-receptor-targeted [ ¹¹¹In]In-DTPA-Folate. The autoradiographic images of 1 mm tumor sections demonstrate the gross heterogeneity of the KB cell tumor xenograft, as well as subtle disparity in the regional accumulation of the two radiotracers.

Original language	English
Pages (from-to)	725-731
Number of pages	7
Journal	Nuclear Medicine and Biology
Volume	30
Issue number	7
DOIs	https://doi.org/10.1016/S0969-8051(03)00080-5
State	Published - Oct 2003

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Mathias, C. J., Lewis, M. R., Reichert, D. E., Laforest, R., Sharp, T. L., Lewis, J. S., Yang, Z. F., Waters, D. J., Snyder, P. W., Low, P. S., Welch, M. J., & Green, M. A. (2003). Preparation of ⁶⁶Ga- and ⁶⁸Ga-labeled Ga(III)-deferoxamine-folate as potential folate-receptor-targeted PET radiopharmaceuticals. Nuclear Medicine and Biology, 30(7), 725-731. https://doi.org/10.1016/S0969-8051(03)00080-5

@article{c82f3965819f48ca8a33fd3e2ce1b710,

title = "Preparation of 66Ga- and 68Ga-labeled Ga(III)-deferoxamine-folate as potential folate-receptor-targeted PET radiopharmaceuticals",

abstract = "A folate-receptor-targeting radiopharmaceutical, Ga(III)-deferoxamine-folate (Ga-DF-Folate), was radiolabeled with two positron-emitting isotopes of gallium, cyclotron-produced 66Ga (9.5 hour half-life) and generator-produced 68Ga (68 minute half-life). The [66Ga]Ga-DF-Folate was administered to athymic mice with folate-receptor-positive human KB cell tumor xenografts to demonstrate that microPET mouse tumor imaging is feasible with 66Ga, despite the relatively high positron energy of this radionuclide. Using the athymic mouse KB tumor xenograft model, dual-isotope autoradiography was also performed following i.v. co-administration of [18F]-FDG, a marker of regional metabolic activity, and folate-receptor-targeted [ 111In]In-DTPA-Folate. The autoradiographic images of 1 mm tumor sections demonstrate the gross heterogeneity of the KB cell tumor xenograft, as well as subtle disparity in the regional accumulation of the two radiotracers.",

author = "Mathias, {Carla J.} and Lewis, {Michael R.} and Reichert, {David E.} and Richard Laforest and Sharp, {Terry L.} and Lewis, {Jason S.} and Yang, {Zhen Fan} and Waters, {David J.} and Snyder, {Paul W.} and Low, {Philip S.} and Welch, {Michael J.} and Green, {Mark A.}",

note = "Funding Information: This work was supported by grants from the National Cancer Institute of the U.S. Public Health Service (R01-CA70845 and R24 CA86307). ",

year = "2003",

month = oct,

doi = "10.1016/S0969-8051(03)00080-5",

language = "English",

volume = "30",

pages = "725--731",

journal = "Nuclear Medicine and Biology",

issn = "0969-8051",

number = "7",

}

Mathias, CJ, Lewis, MR, Reichert, DE, Laforest, R, Sharp, TL, Lewis, JS, Yang, ZF, Waters, DJ, Snyder, PW, Low, PS, Welch, MJ & Green, MA 2003, 'Preparation of ⁶⁶Ga- and ⁶⁸Ga-labeled Ga(III)-deferoxamine-folate as potential folate-receptor-targeted PET radiopharmaceuticals', Nuclear Medicine and Biology, vol. 30, no. 7, pp. 725-731. https://doi.org/10.1016/S0969-8051(03)00080-5

TY - JOUR

T1 - Preparation of 66Ga- and 68Ga-labeled Ga(III)-deferoxamine-folate as potential folate-receptor-targeted PET radiopharmaceuticals

AU - Mathias, Carla J.

AU - Lewis, Michael R.

AU - Reichert, David E.

AU - Laforest, Richard

AU - Sharp, Terry L.

AU - Lewis, Jason S.

AU - Yang, Zhen Fan

AU - Waters, David J.

AU - Snyder, Paul W.

AU - Low, Philip S.

AU - Welch, Michael J.

AU - Green, Mark A.

N1 - Funding Information: This work was supported by grants from the National Cancer Institute of the U.S. Public Health Service (R01-CA70845 and R24 CA86307).

PY - 2003/10

Y1 - 2003/10

N2 - A folate-receptor-targeting radiopharmaceutical, Ga(III)-deferoxamine-folate (Ga-DF-Folate), was radiolabeled with two positron-emitting isotopes of gallium, cyclotron-produced 66Ga (9.5 hour half-life) and generator-produced 68Ga (68 minute half-life). The [66Ga]Ga-DF-Folate was administered to athymic mice with folate-receptor-positive human KB cell tumor xenografts to demonstrate that microPET mouse tumor imaging is feasible with 66Ga, despite the relatively high positron energy of this radionuclide. Using the athymic mouse KB tumor xenograft model, dual-isotope autoradiography was also performed following i.v. co-administration of [18F]-FDG, a marker of regional metabolic activity, and folate-receptor-targeted [ 111In]In-DTPA-Folate. The autoradiographic images of 1 mm tumor sections demonstrate the gross heterogeneity of the KB cell tumor xenograft, as well as subtle disparity in the regional accumulation of the two radiotracers.

AB - A folate-receptor-targeting radiopharmaceutical, Ga(III)-deferoxamine-folate (Ga-DF-Folate), was radiolabeled with two positron-emitting isotopes of gallium, cyclotron-produced 66Ga (9.5 hour half-life) and generator-produced 68Ga (68 minute half-life). The [66Ga]Ga-DF-Folate was administered to athymic mice with folate-receptor-positive human KB cell tumor xenografts to demonstrate that microPET mouse tumor imaging is feasible with 66Ga, despite the relatively high positron energy of this radionuclide. Using the athymic mouse KB tumor xenograft model, dual-isotope autoradiography was also performed following i.v. co-administration of [18F]-FDG, a marker of regional metabolic activity, and folate-receptor-targeted [ 111In]In-DTPA-Folate. The autoradiographic images of 1 mm tumor sections demonstrate the gross heterogeneity of the KB cell tumor xenograft, as well as subtle disparity in the regional accumulation of the two radiotracers.

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U2 - 10.1016/S0969-8051(03)00080-5

DO - 10.1016/S0969-8051(03)00080-5

M3 - Article

C2 - 14499330

AN - SCOPUS:0141448741

SN - 0969-8051

VL - 30

SP - 725

EP - 731

JO - Nuclear Medicine and Biology

JF - Nuclear Medicine and Biology

IS - 7

ER -

Preparation of ⁶⁶Ga- and ⁶⁸Ga-labeled Ga(III)-deferoxamine-folate as potential folate-receptor-targeted PET radiopharmaceuticals

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