Target intelligence / Profile preview

Lutetium-177 chelate (^177Lu chelate)

Target
^177Lu chelate
Molecular classification
Other (Radioisotope-labeled chelate complex)
01

Overview

A radiolabeled lutetium-177 chelate is a chemical complex in which the radioactive isotope lutetium-177 (^177Lu) is stably attached via a chelator (ligand) to a biomolecule that targets specific cell-surface markers, commonly used in radiopharmaceutical therapy for cancer. The chelated radionuclide delivers beta (therapeutic) and gamma (imaging) radiation directly to tumor-expressing cells, sparing normal tissue due to its short path length. These complexes are not biological targets themselves but are radiotherapeutic agents directed to disease-associated targets—typified in FDA-approved agents like ^177Lu-dotatate for neuroendocrine tumors and ^177Lu-PSMA-617 for prostate cancer[1][2][3][4][5][6]. For structured databases and precision medicine applications, the entry should refer to the final biological target of the ligand (e.g., "Somatostatin receptor" for ^177Lu-dotatate or "Prostate-specific membrane antigen" for ^177Lu-PSMA-617). The current name, "Radiolabeled lutetium-177 chelate," is chemically descriptive but biologically underspecified and not unique to a specific target.

Other names
Lutetium-177-labeled chelate^177Lu chelateradiolabeled ^177Lu complexlutetium-177 radiopharmaceutical
02

Mechanism of action

Delivers beta and gamma radiation to ligand-targeted cells, causing DNA damage and apoptosis in tumor cells via local emission[1][2][3][5]

03

Biological functions

Radiotherapeutic payload deliveryImaging agent (theranostics)
04

Disease associations

Cancer (especially neuroendocrine tumors, metastatic castration-resistant prostate cancer[1][2][4][6])
05

Safety considerations

Hematologic toxicity (bone marrow suppression)Nephrotoxicity (renal function monitoring required)Xerostomia, dry mouth (especially with PSMA ligands)Radiation exposure to non-target tissue[4][1]
06

Interacting drugs

Lutetium-177 dotatate (Lutathera)

2 more in the full profile.

07

Biomarkers

Expression of target molecules (e.g., somatostatin receptor, PSMA) as assessed by PET/SPECT imaging[4][6]

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