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dotatate
- Development stage
- Approved
- Lead developer
- Advanced Accelerator Applications
- Modality
- Alpha Emitters → Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta Emitters → Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Small Molecules, Peptides
- Administration
- Intravenous
01
Overview
Dotatate is a synthetic octreotide analog peptide that acts as a high-affinity agonist for somatostatin receptors—especially somatostatin receptor subtype 2 (SSTR2)—which are overexpressed in many neuroendocrine tumors. Dotatate is used as the active component in radiopharmaceuticals such as gallium Ga 68 dotatate and lutetium Lu 177 dotatate. When labeled with gallium-68 (^68Ga), it serves as a PET imaging agent for localizing SSTR-positive neuroendocrine tumors in adults and children. When labeled with lutetium-177 (^177Lu), it is used therapeutically to deliver targeted radiation to these tumors (peptide receptor radionuclide therapy or PRRT). The mechanism involves binding to SSTR2 on tumor cells followed by internalization of the radiolabeled peptide; this allows either imaging or targeted cytotoxicity depending on the isotope used[1][2][3][5][6].
- Brand names
- NetspotLutathera
- Other names
- gallium Ga 68 dotatatelutetium Lu 177 dotatate
02
Targets
SSTR2 (Somatostatin receptor type 2)
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