The objective of this study was the facile preparation of ¹⁷⁷Lu-CHX-A’’-DTPA-Trastuzumab injection for breast cancer therapy. Trastuzumab conjugated with CHX-A’’-DTPA-NCS was radiolabeled with ¹⁷⁷Lu in>95% radiochemical purity. In vitro studies in SKBR3 and MDA-MB-453 cells confirmed specificity of ¹⁷⁷Lu-CHX-A’’- DTPA-Trastuzumab to HER2 positive cells. The radioimmunoconjugate showed good immunoreactivity, in vitro stability in saline and Kd of 1.01 ± 0.13 nM in SKBR3 cells. Clearance of ¹⁷⁷Lu-CHX-A’’-DTPA-Trastuzumab in Swiss mice was predominantly through the hepatobiliary route with minimal bone uptake.