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[177Lu]Lu-BQ7876 is an investigational radioligand therapy (RLT) developed by the Tomsk National Research Medical Center of the Russian Academy of Sciences for the treatment of prostate cancer. It consists of a urea-based small molecule ligand, BQ7876, which incorporates a DOTA chelator to securely bind the beta-emitting radioisotope lutetium-177 (177Lu). The compound specifically targets prostate-specific membrane antigen (PSMA), a protein highly overexpressed on the surface of metastatic castration-resistant prostate cancer (mCRPC) cells. Upon binding and internalization, the 177Lu isotope delivers localized ionizing radiation, leading to DNA double-strand breaks and subsequent apoptosis of the tumor cells. A Phase 1 clinical trial is currently evaluating its safety, dosimetry, and biodistribution in patients with prostate cancer.
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