Drug intelligence / Profile preview

[131]I-IAZA

Development stage
Phase 2
Lead developer
University of Alberta
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

[131]I-IAZA is a small molecule radiopharmaceutical developed by the University of Alberta for the detection and potential treatment of hypoxic regions within solid tumors. It consists of iodoazomycin arabinoside (IAZA), a 2-nitroimidazole derivative, labeled with the radioisotope iodine-131. The mechanism of action involves the selective accumulation and trapping of the molecule in hypoxic cells, where it undergoes bioreduction in the absence of oxygen, allowing for visualization via Single-photon emission-computed tomography (SPECT) imaging. This targeting is clinically significant because tumor hypoxia is associated with resistance to conventional chemotherapy and radiation, as well as increased metastatic potential. While primarily investigated as an imaging and dosimetry tool in Phase I/II trials for locally advanced or metastatic solid tumors, the use of iodine-131 also provides a basis for its potential application as an adjunct molecular radiotherapy agent.

Other names
1-alpha-D-(5-[131I]Iodo-5-deoxyarabinofuranosyl)-2-Nitroimidazoleiodoazomycin arabinoside labeled with iodine-131131I-iodoazomycin arabinoside

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