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Iopofosine I‑131 is a small-molecule phospholipid drug conjugate (PDC) radiopharmaceutical designed for targeted cancer therapy. It consists of a phospholipid ether analog labeled with the radioactive isotope iodine‑131. Upon administration, iopofosine selectively accumulates in tumor cells due to decreased activity of phospholipase D in these cells compared to normal tissue, resulting in prolonged retention and targeted delivery of cytotoxic ionizing radiation directly to malignant cells while sparing healthy tissue. This mechanism enables selective tumor cell killing via DNA damage from beta-emitting radiation. The drug is being developed primarily by Cellectar Biosciences for hematologic malignancies such as relapsed/refractory Waldenstrom’s macroglobulinemia, multiple myeloma, and various pediatric cancers including neuroblastoma and sarcomas. Orphan Drug Designations have been granted for several rare cancers[1][2][3][4][5][7].
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