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XTR008 (177Lu-PSMA-I&T) is a therapeutic radiopharmaceutical developed by Sinotau Pharmaceutical Group for the treatment of prostate cancer. It consists of the PSMA-I&T (Imaging and Therapy) ligand, a small molecule peptidomimetic that specifically targets Prostate-Specific Membrane Antigen (PSMA), labeled with the beta-emitting radioisotope Lutetium-177. PSMA is highly overexpressed on the surface of prostate cancer cells, particularly in metastatic castration-resistant prostate cancer (mCRPC). Upon binding to the extracellular domain of PSMA, the radioligand is internalized into the cell, where the Lutetium-177 delivers localized ionizing radiation, causing double-stranded DNA breaks and subsequent cell death. Sinotau is currently evaluating XTR008 in Phase 3 clinical trials in China as a targeted radioligand therapy for patients with mCRPC.
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