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CTT1403 is a PSMA-targeted radiotherapeutic agent designed for the treatment of metastatic castration-resistant prostate cancer (mCRPC). It consists of a phosphoramidate peptidomimetic that binds irreversibly to prostate-specific membrane antigen (PSMA) and is labeled with the radionuclide lutetium-177 (^177Lu). The molecule also incorporates an albumin-binding motif, which extends its circulation half-life and enhances tumor uptake. This targeted delivery allows for concentrated beta radiation therapy to PSMA-expressing cancer cells while minimizing off-target toxicity. Preclinical studies demonstrated significant tumor growth inhibition and increased survival in animal models. Phase I clinical trials have shown favorable safety profiles, effective tumor targeting, and early evidence of therapeutic efficacy in patients with advanced prostate cancer[1][5][7].
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