RLT Basics

"Radiopharmaceutical therapies, including radioligand therapies (RLTs), are a rapidly evolving class of cancer therapeutics that use radioactive compounds to deliver cytotoxic radiation directly to cancer cells. RLTs combine a radioactive compound with a targeting agent that binds to specific proteins found on cancer cells. Once bound, high-energy radiation is delivered directly to the cancer cells while avoiding surrounding healthy cells, offering a highly localized, tumor-specific approach to treatment (see Sidebar 57). As of June 30, 2025, FDA has approved two RLTs— lutetium-177 dotatate (Lutathera) for neuroendocrine tumors in 2018 and lutetium-177 vipivotide tetraxetan (Pluvicto) for metastatic prostate cancer in 2022 (see Applying Precision to Radiation Therapy)."