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Iopofosine I-124 is a phospholipid ether analog radiolabeled with iodine I 124, developed as a diagnostic PET imaging agent for cancer. It selectively accumulates in tumor cells due to decreased activity of phospholipase D (PLD) in malignant cells compared to normal tissue. This selective uptake is facilitated by the drug’s entry through lipid rafts—microdomains overexpressed in cancer cell membranes—which leads to prolonged retention within tumors and enables clear visualization on PET scans. The mechanism allows for high tumor-to-background contrast, particularly useful for brain tumors such as glioma. Preclinical studies have shown broad-spectrum, cancer-selective uptake and retention across multiple animal models. The drug has received orphan drug designation from the FDA as a diagnostic for glioma management[1][2][7].
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