Target intelligence / Profile preview

Lutetium 177-labeled DOTA Complex (177Lu-DOTA Complex)

Target
177Lu-DOTA Complex
Molecular classification
Radiopharmaceutical, Metal chelate complex, Somatostatin analog conjugate
01

Overview

Lutetium-177-labeled DOTA complexes are radiopharmaceutical agents designed for targeted cancer therapy. They consist of the radioactive isotope lutetium-177 chelated by DOTA and conjugated to a targeting moiety, typically a somatostatin analog. The complex selectively binds to somatostatin receptors overexpressed on tumor cells, leading to internalization and subsequent beta particle emission, causing DNA damage and cytotoxicity. The most common clinical application is in the treatment of neuroendocrine tumors using Lutetium-177 dotatate (Lutathera).

Other names
Lutetium-177 dotatateLutathera177Lu-DOTATATE177Lu-DOTA-TATEDOTA-TATE/EB-TATE
02

Mechanism of action

Selective binding to somatostatin receptors (SSTR2) on tumor cells, followed by internalization and beta particle-induced DNA damage.

03

Biological functions

Targeted radiotherapySomatostatin receptor bindingDNA damage inductionTumor cell cytotoxicity
04

Disease associations

CancerNeuroendocrine tumors
05

Safety considerations

Radiation exposureBone marrow toxicityKidney toxicity
06

Biomarkers

Somatostatin receptor expression (SSTR2)

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