Drug intelligence / Profile preview

Iofolastat I-123

Development stage
Phase 1
Lead developer
Lantheus
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Gamma Emitters → Radiopharmaceuticals, Small Molecules
Administration
Intravenous
01

Overview

Iofolastat I-123 is a radiopharmaceutical small molecule, specifically a radiolabeled glutamate–urea–lysine analogue, designed for molecular imaging of prostate cancer. It selectively binds to the prostate-specific membrane antigen (PSMA), a transmembrane glycoprotein highly expressed on malignant prostate epithelial cells and the neovasculature of various solid tumors. Upon binding PSMA, iofolastat I-123 enables visualization of PSMA-expressing cells using gamma scintigraphy or SPECT imaging due to its iodine‑123 radioisotope label. The drug was developed by Molecular Insight Pharmaceuticals for diagnostic use in detecting metastatic prostate cancer lesions in bone and soft tissue[1][3][4][7].

Brand names
Trofex
Other names
iofolastat (123I)IOFOLASTAT I 123iofolastat I123
02

Targets

PSMA (Prostate-specific membrane antigen)

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