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177Lu-iPSMA
- Development stage
- Unknown
- Lead developer
- Instituto Nacional de Investigaciones Nucleares
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptides
- Administration
- Intravenous
01
Overview
177Lu-iPSMA is a novel radiopharmaceutical developed by the Instituto Nacional de Investigaciones Nucleares (ININ) in Mexico for the treatment of metastatic castration-resistant prostate cancer (mCRPC). It consists of a small-molecule PSMA inhibitor, iPSMA (DOTA-hydrazinylnicotinoyl-lysine(Nal)-urea-glutamate), labeled with the beta-emitting radioisotope Lutetium-177. The ligand features a unique molecular configuration, including a pyridine ring and a hydrazine group (HYNIC), which provides an additional anchoring site to target the Prostate-Specific Membrane Antigen (PSMA) enzyme. Once bound to PSMA-expressing cancer cells, the compound is internalized, allowing the Lutetium-177 to deliver localized cytotoxic beta radiation (maximum tissue penetration of 2.2 mm), which induces DNA damage and cell death in tumor tissues while minimizing exposure to surrounding healthy cells.
- Other names
- 177Lu-DOTA-HYNIC-iPSMA177Lu-DOTA-HYNIC-Lys(Nal)-urea-gluLutetium (177Lu) iPSMA
02
Targets
PSMA (Prostate-specific membrane antigen)
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