Direct Tc-99m labeling of Herceptin (trastuzurnab) by Tc-99m(I) tricarbonyl ion

作者:Chen Wan Jou; Yen Chao Liang; Lo Su Tang; Chen Kuo Ting; Lo Jem Mau*
来源:Applied Radiation and Isotopes, 2008, 66(3): 340-345.
DOI:10.1016/j.apradiso.2007.09.007

摘要

By simply incubating Herceptin (trastuzumab) with [Tc-99m(CO)(3)(OH2)(3)](+) ion in saline, a significant yield of Tc-99m-labeled trastuzumab was found to be achievable. The effective labeling may be based on that trastuzumab is inherent with endogenous histidine group to which Tc-99m(I) tricarbonyl ion can be strongly bound. For practical Tc-99m labeling processing, trastuzumab was purified beforehand from the commercial product, Herceptin (Genentech) via size exclusion chromatography to remove the excipient, a-histidine and a high-labeled yield could be obtained by incubating the purified trastuzumab with [Tc-99m(CO)(3)(OH2)(3)](+). Retention of bioactivity of the Tc-99m(I)-labeled trastuzumab was validated using a cell binding test.