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227th-trastuzumab
- Development stage
- Phase 1
- Lead developer
- Bayer
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
227th-trastuzumab is a **radiopharmaceutical antibody-drug conjugate** consisting of the monoclonal antibody trastuzumab covalently linked to the alpha-emitting radionuclide thorium-227 via a chelator. It is designed to target and bind to HER2 (receptor tyrosine-protein kinase erbB-2), which is overexpressed in certain cancers such as breast and gastric carcinoma. Upon binding to HER2-positive cancer cells, it delivers highly localized cytotoxic alpha radiation, causing double-stranded DNA breaks and cell death with limited damage to surrounding healthy tissue. The mechanism further includes **antibody-dependent cell-mediated cytotoxicity (ADCC)**. Developed for targeted alpha therapy, its current focus is on advanced HER2-positive breast cancer and other HER2-expressing malignancies[1][2][4].
- Brand names
- 227Th-Trastuzumab corixetan
- Other names
- HER2-targetted thorium conjugate-BayerHER-2-targetted thorium conjugate-BayerHER 2-targetted thorium conjugate-Bayer
02
Targets
ERBB2 (Erb-b2 receptor tyrosine kinase 2)
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