177Lu-rhPSMA-10.1

177Lu-rhPSMA-10.1 is a novel radiohybrid prostate-specific membrane antigen (PSMA)-targeted radiopharmaceutical therapy. It consists of the beta-emitting radioisotope lutetium-177 conjugated to the radiohybrid PSMA ligand rhPSMA-10.1. The 'radiohybrid' (rh) nature of the ligand allows for the same molecule to be labeled with either a diagnostic radioisotope (such as Fluorine-18) or a therapeutic one (such as Lutetium-177), facilitating a theranostic approach. The drug is designed to bind specifically to PSMA, which is highly overexpressed on the surface of prostate cancer cells. Upon binding, the drug is internalized, and the lutetium-177 delivers targeted ionizing radiation to the tumor cell, causing DNA damage and cell death while sparing surrounding healthy tissue. It is currently being investigated by M.D. Anderson Cancer Center in clinical trials for various stages of prostate cancer, including high-risk localized disease (the Nautilus Trial) and metastatic castration-resistant prostate cancer (mCRPC).

Other names

lutetium Lu 177 rhPSMA-10.1177Lu-radiohybrid PSMA-10.1