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[177Lu]Lu-XT381 is a Lutetium-177 labeled radioligand therapy targeting the prostate-specific membrane antigen (PSMA). Developed by Sinotau Pharmaceutical Group (Beijing Xiantong International Pharmaceutical Technology), it is designed for the treatment of PSMA-positive metastatic castration-resistant prostate cancer (mCRPC). The drug consists of a PSMA-targeting ligand (XT381) conjugated to the beta-emitting radioisotope Lutetium-177. Upon binding to PSMA-expressing tumor cells, the compound is internalized, delivering localized ionizing radiation that induces DNA damage and cell death. It is currently being evaluated in Phase Ib/II clinical trials in China for patients who have progressed on next-generation androgen receptor-directed therapies.
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