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177Lu-DOTA-M5A
- Development stage
- Preclinical
- Lead developer
- Uppsala University
- 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-M5A is a preclinical-stage therapeutic radiopharmaceutical (radioimmunotherapy) consisting of the humanized anti-carcinoembryonic antigen (CEA/CEACAM5) monoclonal antibody hT84.66-M5A (M5A) conjugated via a DOTA chelator to the beta-emitting radionuclide lutetium-177 (177Lu). Developed by researchers at Uppsala University and the Beckman Research Institute of the City of Hope, the agent is designed to target CEA-expressing solid tumors, particularly colorectal cancer. Upon binding to CEA on the surface of tumor cells, the conjugate is internalized, and the localized emission of beta particles from 177Lu induces DNA damage and subsequent apoptosis in the cancer cells. Preclinical studies have evaluated 177Lu-DOTA-M5A as a monotherapy and in combination with the HSP90 inhibitor onalespib or PD-1 immune checkpoint blockade, demonstrating enhanced anti-tumor efficacy and prolonged survival in animal models.
- Other names
- 177Lu-labeled hT84.66-M5A177Lu-labeled M5ALu-177-DOTA-M5ALu177-DOTA-M5ALu 177-DOTA-M5A[177Lu]Lu-DOTA-M5Alutetium (177Lu) DOTA-M5Alutetium-177 DOTA-M5Alutetium177 DOTA-M5Alutetium 177 DOTA-M5A
02
Targets
CEACAM5 (Carcinoembryonic antigen related cell adhesion molecule 5)
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