Target intelligence / Profile preview

Lutetium(3+) ion (Lu3+)

Target
Lu3+
Molecular classification
Lanthanide, Metal ion, Radionuclide
01

Overview

Lutetium(3+) ion, particularly in its radioactive isotope form Lutetium-177, is a trivalent lanthanide metal utilized as a therapeutic payload in radiopharmaceutical medicine. It is not a biological target itself, such as a receptor or enzyme; rather, it serves as the cytotoxic component of targeted therapies for various cancers (PubChem CID 104842). In clinical applications, the ion is typically chelated to a ligand that targets specific biomarkers, such as Somatostatin Receptors (SSTR) in neuroendocrine tumors or Prostate-Specific Membrane Antigen (PSMA) in prostate cancer. Upon localization at the tumor site, Lutetium-177 undergoes beta-minus decay, delivering localized ionizing radiation that results in catastrophic DNA damage and subsequent apoptosis of the malignant cells (NCI Drug Dictionary). This approach allows for the high-precision treatment of metastatic disease while minimizing exposure to surrounding healthy tissues due to the relatively short penetration depth of the emitted beta particles. Lutetium-based radiopharmaceuticals, such as Lutathera and Pluvicto, have become standard-of-care options for patients with advanced, treatment-resistant malignancies (FDA, 2018; 2022).

Other names
Lutetium ionLutetium-177177LuLutetium(III) cationLu(III)
02

Mechanism of action

Lutetium-177 is a beta-emitting radionuclide that induces cell death by releasing high-energy electrons (beta particles) during its decay to Hafnium-177. These particles travel a short distance (average 0.67 mm) to cause ionizing radiation-induced double-stranded DNA breaks and the formation of reactive oxygen species within the target-expressing cells and their immediate vicinity (FDA, 2018; 2022; NCI Drug Dictionary).

03

Biological functions

No endogenous biological functionExogenous therapeutic payloadMimics calcium in physiological pathways
04

Disease associations

Metastatic castration-resistant prostate cancer (mCRPC)Gastroenteropancreatic neuroendocrine tumors (GEP-NETs)Advanced malignancies
05

Safety considerations

Myelosuppression (anemia, leukopenia, thrombocytopenia)NephrotoxicityRadiation-induced secondary malignanciesXerostomia (dry mouth)Fatigue
06

Interacting drugs

Lutetium Lu 177 dotatate (Lutathera)

4 more in the full profile.

07

Biomarkers

Prostate-Specific Membrane Antigen (PSMA) expressionSomatostatin Receptor Type 2 (SSTR2) expressionGallium-68 DOTATATE PET/CT uptakeGallium-68 PSMA-11 PET/CT uptakeSerum Prostate-Specific Antigen (PSA)Chromogranin A

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