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lutetium-177-dota-trastuzumab
- Development stage
- Preclinical
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
Lutetium-177-dota-trastuzumab is an investigational radiopharmaceutical composed of the monoclonal antibody trastuzumab conjugated via a DOTA chelator to the beta-emitting radioisotope lutetium-177. It specifically targets human epidermal growth factor receptor 2 (HER2) overexpressed on certain tumor cells. Trastuzumab binds to extracellular domains of HER2, and the lutetium-177 delivers localized cytotoxic radiation, resulting in DNA damage and cell death. This approach aims to treat HER2-positive cancers, including gastric cancers, and is designed to bypass mechanisms of resistance to standard trastuzumab therapy. Proof-of-concept studies have demonstrated durability and enhanced efficacy, particularly when combined with statins, in trastuzumab-resistant models[5].
- Other names
- 177Lu-DOTA-trastuzumab[177Lu]Lu-DOTA-trastuzumab
02
Targets
DNAERBB2 (Erb-b2 receptor tyrosine kinase 2)
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