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111In-bsIC
- Development stage
- Preclinical
- Lead developer
- University of Toronto
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptides, Antibody Fragments → Engineered Antibody Formats → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
111In-bsIC (also referred to as 111In-bsRIC) is a preclinical bispecific radioimmunoconjugate developed by researchers at the University of Toronto for SPECT/CT imaging of HER2 and HER3 heterodimerization in breast cancer. The conjugate is constructed by linking a trastuzumab Fab fragment (which targets HER2) via a polyethylene glycol (PEG) spacer (optimally PEG24) to a thiolated peptide of heregulin-β1 (pHRG, which targets HER3). The resulting bispecific immunoconjugate is derivatized with diethylenetriaminepentaacetic acid (DTPA) and labeled with indium-111 (111In). By targeting both HER2 and HER3, 111In-bsIC exhibits bivalent properties that may allow preferential binding to HER2/HER3 heterodimers, which are potent drivers of tumor growth and resistance to HER2-targeted therapies.
- Other names
- 111In-DTPA-Fab-PEG24-HRG111In-DTPA-Fab-PEG24-pHRG111In-labeled trastuzumab Fab-heregulin bispecific radioimmunoconjugatetrastuzumab Fab-heregulin bispecific radioimmunoconjugate
02
Targets
ERBB3 (Erb-b2 receptor tyrosine kinase 3)ERBB2 (Erb-b2 receptor tyrosine kinase 2)
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