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Lutetium Lu-177 PSMA-0057 is an investigational radioligand therapy (RLT) developed by Suzhou Ruihe Pharmaceutical Technology for the treatment of prostate-specific membrane antigen (PSMA)-positive metastatic castration-resistant prostate cancer (mCRPC). The drug consists of the beta-emitting radioisotope lutetium-177 conjugated to the PSMA-0057 ligand, which specifically targets PSMA, a protein highly expressed on the surface of prostate cancer cells. Upon binding, the compound is internalized, delivering localized ionizing radiation to induce DNA damage and cell death in tumor cells while minimizing exposure to healthy tissue. It is typically paired with the diagnostic imaging agent Gallium [68Ga] PSMA-0057 as part of a theranostic approach.
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