Drug intelligence / Profile preview

212Pb-PSMA

Development stage
Preclinical
Lead developer
Orano Med
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Alpha Emitters → Radiopharmaceuticals, Beta-minus Emitters → Radiopharmaceuticals, Peptides
Administration
Intravenous
01

Overview

212Pb-PSMA is a targeted alpha therapy (TAT) radiopharmaceutical developed by Orano Med for the treatment of prostate cancer. It comprises a peptide ligand designed to bind with high affinity to the prostate-specific membrane antigen (PSMA), a protein significantly overexpressed on the surface of prostate cancer cells. The peptide is conjugated to lead-212 (212Pb), a radioisotope that acts as an in vivo generator of alpha particles. Upon binding to PSMA and subsequent internalization into the cancer cell, the decay of 212Pb releases high-energy alpha radiation. This radiation causes complex, difficult-to-repair double-strand DNA breaks, leading to cell death. This targeted approach is intended to maximize therapeutic efficacy against tumor cells while minimizing exposure and damage to surrounding healthy tissues.

Other names
Lead-212-PSMALead212-PSMALead 212-PSMA212Pb-labeled PSMA-targeting peptide
02

Targets

PSMA (Prostate-specific membrane antigen)DNA

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