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177Lu-AKIR001
- Development stage
- Unknown
- Lead developer
- Akiram Therapeutics
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Gamma Emitters → Radiopharmaceuticals, Monoclonal Antibodies → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
177Lu-DOTA-LDC (also known as 177Lu-AKIR001 or [177Lu]Lu-DOTA-AKIR001) is a targeted radiopharmaceutical developed by Akiram Therapeutics. It consists of a proprietary humanized monoclonal antibody (AKIR001, an affinity-matured derivative of the parental UU-40 antibody) that targets CD44v6, a cell-surface glycoprotein overexpressed in various aggressive solid tumors, including anaplastic thyroid cancer (ATC), head and neck squamous cell carcinoma (HNSCC), non-small cell lung cancer (NSCLC), and gynecological cancers. The antibody is conjugated via a DOTA chelator to the beta-emitting radioisotope lutetium-177 (177Lu). Upon binding to CD44v6-expressing tumor cells, the radiopharmaceutical is internalized, delivering localized, cytotoxic ionizing radiation that induces DNA double-strand breaks and cell death, while sparing surrounding healthy tissues. AKIR001 is engineered with LALA (Leu234Ala, Leu235Ala) mutations in its Fc region to minimize Fc-receptor binding, thereby reducing off-target uptake and Fc-mediated toxicities. It is currently in Phase I clinical development for CD44v6-positive advanced solid tumors.
- Other names
- 177Lu-DOTA-LDC177Lu-DOTA-UU-40177Lu-labeled UU-40[177Lu]Lu-AKIR001[177Lu]Lu-DOTA-AKIR001lutetium-177 AKIR001lutetium177 AKIR001lutetium 177 AKIR001
02
Targets
CD44 (CD44 antigen)
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