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samarium-153-DOTA-TATE
- Development stage
- Preclinical
- Lead developer
- SCK CEN
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptides
- Administration
- Intravenous
01
Overview
samarium-153-DOTA-TATE (also known as [153Sm]Sm-DOTA-TATE) is a preclinical-stage therapeutic radiopharmaceutical (radioligand therapy) being developed for the treatment of somatostatin receptor-positive (SSTR-positive) tumors, such as gastroenteropancreatic neuroendocrine tumors (GEP-NETs). It consists of the somatostatin analogue DOTA-TATE labeled with the beta- and gamma-emitting radionuclide samarium-153 (153Sm). The DOTA-TATE peptide selectively binds to somatostatin receptor type 2 (SSTR2) overexpressed on tumor cells, facilitating internalization of the complex. Once internalized, the emission of beta particles and Auger/conversion electrons from the decay of 153Sm delivers localized cytotoxic radiation to destroy tumor cells, while its gamma emission allows for SPECT imaging. The high-specific-activity samarium-153 used in this conjugate is produced via neutron activation followed by mass separation, overcoming previous limitations of low specific activity.
- Other names
- [153Sm]Sm-DOTA-TATE153Sm-DOTA-TATE153Sm-DOTATATEsamarium (153Sm) dotatatesamarium-153-DOTATATEsamarium153-DOTATATEsamarium 153-DOTATATE
02
Targets
SSTR2 (Somatostatin receptor type 2)
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