• The Korean Journal of Nuclear Medicine
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• v.34 no.5
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• pp.410-417
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• 2000

Purpose: Idoxifene is currently entering phase II clinical trials for the treatment of advanced breast cancer. The radiolabeled idoxifene using $[^{123}I]$ provides an opportunity for clinical pharmacology with single photon emission computed tomography (SPECT). The purpose of this study was to prepare radiolabeled idoxifene using $[^{123}I]$ and to determine its cell uptake of breast cancer cell line. Materials and Methods: With a view to evaluating new anticancer drugs, we are investigating the novel antiestrogen pyrrolidino-4-iodotamoxifen (idoxifene). $[^{123}I]$Idoxifene has been prepared in no-carrier-added form using a tributyl stannylated precursor which has been synthesized by means of (2-chloroethoxy)benzene with (${\pm}$)-2-phenylbutanoic acid on the basis of previously reported standard methods. The biodistribution and dynamic behavior of the compound were investigated using the comparative breast cancer cell line, MCF-7 (estrogen receptor-positive) and MDA-MB-468 (non-estrogen receptor). Results and Conclusion: Acylation of (2-chloroethoxy)benzene with (${\pm}$)-2-phenylbutanoic acid gave the versatile ketone (81%) which reacted with 1,4-diiodobenzene to give triphenylethylene as a mixture of E and Z geometric isomers, which were separated by the recrystallization in ethanol. The E-isomer was treated with pyrrolidine to give idoxifene (67%). In order to incorporate radioactive iodine into the 4-position, the 4-stannylated precursor was prepared (30%). The yield of radioiodination was 90-92% with a high radiochemical purity greater than 98%. The ratio of tumor uptake of the breast cancer cell line between MCF-7 and MDA-MB-468 was about 1.7.

• The Korean Journal of Nuclear Medicine
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• v.36 no.6
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• pp.325-332
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• 2002

Purpose: Human Na+/I- symporter (hNIS) is known to be expressed in many tissues other than thyroid gland. The breast cancer cells are one of them and the possibility of radioiodine therapy in treatment of the breast cancer may be suggested. We investigated the expression rate of hNIS and the relationship between the expression of hNIS and the finding of 99mTc-MIBI scintimammographv in the breast cancer Materials and Methods: Surgically proved 56 patients with breast cancer were the subjects of this study The expression of hNIS were evaluated by immunohistochemistry and the results were compared to the findings of 99m7c-MIBI scintimammography. Results: Overall expression rate of hNIS was 41.1% in 56 patients. According to the pathologic diagnosis, it was 42.9% in 49 patients with invasive ductal carcinoma and 28.6% in the 7 patients with ductal carcinoma in situ. The expression rate of hNIS in the 41 cases with a focal increased uptake at he breast lesion on 99m7c-MIBI sointimammogram was 31.7%. That in the 15 cases without any abnormal uptake on the scan was significantly higher(65.7%, p<0.05). Conclusion: The expression rate of hNIS in the patients with breast cancer was not so high. The rate was higher in the patients with no increased uptake at the breast lesion on 99m7c-MIBI scintimammography.