Abstract
The article provides a comparison of the theoretically calculated and experimentally determined yield of the reaction 176Lu (n, �A)177Lu. Also, it provides the results of the studies on lutetium-177 labeling of a non-peptide antagonist of gonadotropin-releasing hormone (GnRH) elagolix (ELA) associated with a chelating DOTA (DOTAELA). The synthesized DOTAELA complex was labeled with the 177Lu isotope.177Lu was produced by the reaction (n, �A) using the enriched LuCl3 target at the reactor WWR�CK. Production of 177Lu by the (n, �A) reaction from the enriched 176Lu target achieved by irradiation for 17 days. All stages of the complex preparation were evaluated by paper chromatography. The optimal technological parameters for the synthesis of the complex 177Lu-DOTAELA are: pH - 4.5, 90-100 �aC and 40 min. The obtained optimal parameters made it possible to produce a labeled complex of 177Lu�CDOTAELA with a radiochemical yield of �Y 95%.
Highlights
In women in many countries of the world, including Kazakhstan, breast cancer (BC) is the most common malignant neoplasm
Triple negative breast cancer (TNBC) comprises about 8–20% of all breast tumors; it is more common in women up to 50 years of age before menopause, with early menarche, the first pregnancy at a younger age, a short period of breastfeeding, and a high body mass index
TNBC is characterized by a lack of expression of estrogen, progesterone and HER-2 receptors, which is characterized by an aggressive course, metastatic disease and reduction of life expectancy; the maximum risk of recurrence occurs during the first three years after surgical treatment [2,3,4]
Summary
In women in many countries of the world, including Kazakhstan, breast cancer (BC) is the most common malignant neoplasm. Elagolix is the first of a new class of GnRH inhibitors that have been designated as the second generation due to their non-peptide nature and oral bioavailability. In this regard, a DOTAELA molecule was synthesized, consisting of an elagolix bound to a chelating DOTA molecule via an ethylenediamine bridge to allow labeling with isotopes such as lutetium-177 and gallium-68.The substance has no analogues in the treatment of triple negative breast cancer and is the first in this field [6,7,8]. The depth of 177Lu penetration into the tissue is equal to 2 mm, which is advantageous, especially for small metastases [9]. It can be used as an alternative to 131I or as an addition to 90Y
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