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Drug intelligence / Profile preview
iodine-131-labeled prostate-specific membrane antigen ligand
- Development stage
- Unknown
- Lead developer
- Lantheus
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Gamma Emitters → Radiopharmaceuticals, Small Molecules
- Administration
- Intravenous
01
Overview
Iodine-131-labeled prostate-specific membrane antigen (PSMA) ligands are a class of therapeutic radiopharmaceuticals designed to target and treat prostate cancer cells. These agents consist of a small-molecule ligand (often a glutamate-urea-lysine derivative) that binds with high affinity to the extracellular domain of PSMA, which is overexpressed in prostate cancer, particularly in metastatic and castration-resistant stages. Once bound, the iodine-131 isotope undergoes beta decay, emitting high-energy electrons that cause double-stranded DNA breaks and subsequent apoptosis in the targeted tumor cells. The most prominent candidate in this class is 131I-MIP-1095 (also known as 131I-RPS-001), which has been investigated in clinical trials for metastatic castration-resistant prostate cancer (mCRPC), both as a monotherapy and in combination with androgen receptor signaling inhibitors like enzalutamide.
- Other names
- iodine-131-labeled PSMA ligandiodine131-labeled PSMA ligandiodine 131-labeled PSMA ligand131I-labeled PSMA ligand
02
Targets
PSMA (Prostate-specific membrane antigen)
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