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HTK01169 is a novel radiopharmaceutical ligand designed for the targeted radionuclide therapy of prostate cancer. It is a derivative of the established PSMA-617 molecule, modified with an albumin-binding motif, N-[4-(p-iodophenyl)butanoyl]-Glu, to extend its circulatory half-life. By binding to serum albumin, the drug remains in the blood longer, which increases the cumulative uptake and radiation dose delivered to tumors expressing prostate-specific membrane antigen (PSMA). Labeled with the beta-emitting radioisotope lutetium-177 (177Lu), HTK01169 acts as a targeted radionuclide therapy. Preclinical studies have demonstrated that 177Lu-HTK01169 delivers a significantly higher radiation dose to PSMA-expressing tumors compared to 177Lu-PSMA-617, leading to enhanced treatment efficacy in tumor xenograft models.
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