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177Lu-EBRGD is a targeted radiotherapeutic agent developed by Molecular Targeting Technologies, Inc. (MTTI) through an exclusive license from the National Institutes of Health (NIH). The compound is designed to treat integrin-expressing malignancies, including glioblastoma multiforme (GBM) and non-small cell lung cancer (NSCLC). Its structure incorporates a Lutetium-177 radioisotope, an RGD (Arg-Gly-Asp) peptide sequence, and an Evans Blue (EB) derivative. The RGD peptide specifically targets integrin αvβ3, which is frequently overexpressed on tumor cells and angiogenic blood vessels. The Evans Blue moiety facilitates reversible binding to endogenous serum albumin, which serves as a carrier to extend the drug's blood circulation time and enhance its accumulation within the tumor microenvironment. This albumin-binding strategy allows for higher therapeutic doses to be delivered to the tumor with reduced frequency and lower overall toxicity compared to standard RGD radiopharmaceuticals.
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