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177Lu-LNC1011 is a novel long-circulating radiopharmaceutical designed for the treatment of metastatic castration-resistant prostate cancer (mCRPC). It is a dansylated amino acid-modified ligand that targets the prostate-specific membrane antigen (PSMA), which is highly expressed in prostate cancer cells. The drug consists of a PSMA-targeting ligand conjugated to the beta-emitting radioisotope lutetium-177 (^177Lu), enabling targeted delivery of ionizing radiation to tumor sites while sparing normal tissues. Preclinical and early clinical studies have demonstrated high tumor uptake, prolonged retention in lesions, rapid clearance from non-target organs, and promising anti-tumor activity with manageable hematological toxicity. The primary mechanism involves delivering cytotoxic radiation directly to PSMA-expressing cancer cells[2][5][3].
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