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68Ga-HTK03149 is a radiolabeled small molecule positron emission tomography (PET) imaging agent that targets the prostate-specific membrane antigen (PSMA). It is based on the Lys-urea-Aad pharmacophore, where Glu in the original PSMA-targeting motif is replaced with L-2-aminoadipic acid (Aad), resulting in high tumor uptake and significantly reduced off-target accumulation in kidneys and salivary glands compared to earlier agents. This improved biodistribution profile enables clearer imaging of PSMA-expressing tumors, particularly prostate cancer lesions. 68Ga-HTK03149 is used for precise localization of PSMA-positive lesions to guide treatment decisions, especially as part of a theranostic pair with therapeutic agents such as 177Lu-HTK03170. The drug was developed at BC Cancer, Vancouver, Canada[1][2][4][6].
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