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177Lu-HA-DOTATATE
- Development stage
- Unknown
- Lead developer
- Scintomics
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Gamma Emitters → Radiopharmaceuticals, Peptide-Drug Conjugates → Peptide Conjugates → Peptides
- Administration
- Intravenous, Intra-arterial
01
Overview
177Lu-HA-DOTATATE is a high-affinity therapeutic radiopharmaceutical designed for peptide receptor radionuclide therapy (PRRT) of somatostatin receptor (SSTR)-expressing tumors. It consists of the somatostatin analogue iodo-tyrosine-3-octreotate (HA-TATE) labeled with the beta-emitting radionuclide Lutetium-177 via the macrocyclic chelating agent DOTA. The addition of iodine to the tyrosine residue in HA-TATE significantly enhances its binding affinity for SSTR2 and SSTR5 compared to standard DOTATATE. Upon binding to SSTRs on the cell membrane of neuroendocrine tumors or meningiomas, the radioconjugate is internalized, delivering localized cytotoxic radiation that induces double-stranded DNA breaks and subsequent tumor cell death.
- Other names
- 177Lu-DOTA-3-iodo-Tyr3-octreotate177Lu-high-affinity-DOTATATE[177Lu]Lu-HA-DOTATATElutetium Lu 177 DOTA-3-iodo-Tyr3-octreotatelutetium Lu 177 high-affinity DOTATATE
02
Targets
SSTR2 (Somatostatin receptor type 2)SSTR5 (Somatostatin receptor 5)
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