Synthesis, biodistribution, and estrogen receptor scintigraphy of indium-111-diethylenetriaminepentaacetic acid-tamoxifen analogue

Ebrahim S. Delpassand; David J. Yang; Sidney Wallace; Abdallah Cherif; Syed M. Quadri; Janet Price; Angela Joubert; Tomio Inoue; Donald A. Podoloff

doi:10.1021/js960049w

Synthesis, biodistribution, and estrogen receptor scintigraphy of indium-111-diethylenetriaminepentaacetic acid-tamoxifen analogue

Ebrahim S. Delpassand, David J. Yang, Sidney Wallace, Abdallah Cherif, Syed M. Quadri, Janet Price, Angela Joubert, Tomio Inoue, Donald A. Podoloff

Nuclear Medicine

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

25 Scopus citations

Abstract

This study was aimed at developing a hydrophilic diethylenetriaminepentaacetic acid-tamoxifen (DTPA-Tam) analogue for use in imaging estrogen receptor positive (ER+) lesions. In rat uterine cytosol, the IC₅₀ of DTPA-Tam conjugate was 1 μM and of tamoxifen, 2 μM. Biodistribution, autoradiography, and radionuclide imaging of ¹¹¹In-DTPA-Tam in breast-tumor-bearing rats showed that tumor-to-tissue ratios increased steadily between 30 min and 48 h. The in vivo response of MCF-7 breast cancer xenografts to tamoxifen and DTPA-Tam in nude mice demonstrated that DTPA-Tam could reduce tumor growth rate. These results indicate that DTPA-Tam, a new hydrophilic ER+ ligand, might be useful in diagnosing ER+ lesions.

Original language	English (US)
Pages (from-to)	553-559
Number of pages	7
Journal	Journal of Pharmaceutical Sciences
Volume	85
Issue number	6
DOIs	https://doi.org/10.1021/js960049w
State	Published - Jun 1996

ASJC Scopus subject areas

Pharmaceutical Science

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@article{efaa12e41a334639925e4b9912491035,

title = "Synthesis, biodistribution, and estrogen receptor scintigraphy of indium-111-diethylenetriaminepentaacetic acid-tamoxifen analogue",

abstract = "This study was aimed at developing a hydrophilic diethylenetriaminepentaacetic acid-tamoxifen (DTPA-Tam) analogue for use in imaging estrogen receptor positive (ER+) lesions. In rat uterine cytosol, the IC50 of DTPA-Tam conjugate was 1 μM and of tamoxifen, 2 μM. Biodistribution, autoradiography, and radionuclide imaging of 111In-DTPA-Tam in breast-tumor-bearing rats showed that tumor-to-tissue ratios increased steadily between 30 min and 48 h. The in vivo response of MCF-7 breast cancer xenografts to tamoxifen and DTPA-Tam in nude mice demonstrated that DTPA-Tam could reduce tumor growth rate. These results indicate that DTPA-Tam, a new hydrophilic ER+ ligand, might be useful in diagnosing ER+ lesions.",

author = "Delpassand, {Ebrahim S.} and Yang, {David J.} and Sidney Wallace and Abdallah Cherif and Quadri, {Syed M.} and Janet Price and Angela Joubert and Tomio Inoue and Podoloff, {Donald A.}",

note = "Funding Information: The authors wish to thank William C. Liu for his excellent technical assistance in the preparation of autoradiographs and Dianne Perez for her clerical support. This work was supported in part by the American Cancer Society (EDT 45A, 1993-1997), the George and Cleo Cook Fund, the John S. Dunn Sr. Foundation, and the Cesare Gianturco Fund.",

year = "1996",

month = jun,

doi = "10.1021/js960049w",

language = "English (US)",

volume = "85",

pages = "553--559",

journal = "Journal of Pharmaceutical Sciences",

issn = "0022-3549",

publisher = "John Wiley and Sons Inc.",

number = "6",

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AU - Delpassand, Ebrahim S.

AU - Yang, David J.

AU - Wallace, Sidney

AU - Cherif, Abdallah

AU - Quadri, Syed M.

AU - Price, Janet

AU - Joubert, Angela

AU - Inoue, Tomio

AU - Podoloff, Donald A.

N1 - Funding Information: The authors wish to thank William C. Liu for his excellent technical assistance in the preparation of autoradiographs and Dianne Perez for her clerical support. This work was supported in part by the American Cancer Society (EDT 45A, 1993-1997), the George and Cleo Cook Fund, the John S. Dunn Sr. Foundation, and the Cesare Gianturco Fund.

PY - 1996/6

Y1 - 1996/6

N2 - This study was aimed at developing a hydrophilic diethylenetriaminepentaacetic acid-tamoxifen (DTPA-Tam) analogue for use in imaging estrogen receptor positive (ER+) lesions. In rat uterine cytosol, the IC50 of DTPA-Tam conjugate was 1 μM and of tamoxifen, 2 μM. Biodistribution, autoradiography, and radionuclide imaging of 111In-DTPA-Tam in breast-tumor-bearing rats showed that tumor-to-tissue ratios increased steadily between 30 min and 48 h. The in vivo response of MCF-7 breast cancer xenografts to tamoxifen and DTPA-Tam in nude mice demonstrated that DTPA-Tam could reduce tumor growth rate. These results indicate that DTPA-Tam, a new hydrophilic ER+ ligand, might be useful in diagnosing ER+ lesions.

AB - This study was aimed at developing a hydrophilic diethylenetriaminepentaacetic acid-tamoxifen (DTPA-Tam) analogue for use in imaging estrogen receptor positive (ER+) lesions. In rat uterine cytosol, the IC50 of DTPA-Tam conjugate was 1 μM and of tamoxifen, 2 μM. Biodistribution, autoradiography, and radionuclide imaging of 111In-DTPA-Tam in breast-tumor-bearing rats showed that tumor-to-tissue ratios increased steadily between 30 min and 48 h. The in vivo response of MCF-7 breast cancer xenografts to tamoxifen and DTPA-Tam in nude mice demonstrated that DTPA-Tam could reduce tumor growth rate. These results indicate that DTPA-Tam, a new hydrophilic ER+ ligand, might be useful in diagnosing ER+ lesions.

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Synthesis, biodistribution, and estrogen receptor scintigraphy of indium-111-diethylenetriaminepentaacetic acid-tamoxifen analogue

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