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Lutetium Lu-177 LNC1003 (also known as [177Lu]Lu-LNC1003 or 177Lu-PSMA-EB-01) is a novel, clinical-stage, prostate-specific membrane antigen (PSMA)-targeted radioligand therapy (RLT) developed by Yantai Lannacheng Biotechnology (a subsidiary of Yantai Dongcheng Pharmaceutical). The drug consists of a high-affinity PSMA-targeting ligand conjugated to an Evans blue (EB) moiety, which is chelated to the beta-emitting radioisotope lutetium-177 (177Lu). The EB moiety reversibly binds to circulating serum albumin, significantly extending the blood circulation half-life of the radioconjugate. This albumin-binding strategy enhances tumor uptake and retention while reducing renal clearance, potentially allowing for lower therapeutic doses and fewer treatment cycles compared to conventional PSMA-targeted radioligands like 177Lu-PSMA-617. Lutetium Lu-177 LNC1003 is currently being evaluated in Phase 1 clinical trials for the treatment of patients with PSMA-positive metastatic castration-resistant prostate cancer (mCRPC).
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