[111In]In-DOTA-TCO-trastuzumab

[111In]In-DOTA-TCO-trastuzumab is a radiolabeled monoclonal antibody designed for imaging and potentially therapy of HER2-positive cancers. It consists of trastuzumab, a recombinant humanized IgG1 antibody targeting the human epidermal growth factor receptor 2 (HER2), conjugated with DOTA (a chelator for radiometals) and trans-cyclooctene (TCO). This construct is radiolabeled with Indium-111, a gamma-emitting isotope used for single-photon emission computed tomography (SPECT) imaging. The TCO moiety enables bioorthogonal click chemistry, allowing for click-cleavable strategies to enhance tumor-to-background imaging contrast. After binding to HER2 on tumor cells and internalization, the complex can be selectively cleared from non-target tissues using a tetrazine trigger, leaving radioactivity predominantly in the tumor. This approach enables sensitive and specific detection of HER2-positive tumors and has potential as a theranostic agent, especially for personalized cancer management, primarily in breast and other HER2-expressing malignancies[5][6].

Other names

Indium-111 DOTA-TCO-trastuzumabIndium111 DOTA-TCO-trastuzumabIndium 111 DOTA-TCO-trastuzumab111In-DOTA-TCO-trastuzumab