177LuDOTATATE

177Lu-DOTATATE, also known as lutetium-177 DOTATATE, is a radiopharmaceutical used in peptide receptor radionuclide therapy (PRRT) for neuroendocrine tumors that express somatostatin receptors, particularly the SSTR2 subtype. It combines the somatostatin analog DOTATATE with the beta-emitting radionuclide lutetium-177.

The therapy works by binding to somatostatin receptors on tumor cells and being internalized, delivering targeted radiation to the tumor with the beta particles from Lu-177. The drug also emits gamma photons that allow post-therapy imaging and dosimetry to assess distribution and uptake.

Indications typically include advanced, metastatic, or unresectable gastroenteropancreatic neuroendocrine tumors that show somatostatin receptor expression on imaging, usually confirmed with Ga-68 DOTATATE PET/CT. Treatment is commonly given in multiple cycles, for example four cycles at intervals of about six to eight weeks. Each cycle often delivers around 7.4 GBq, with the total activity tailored to the patient.

Administration and safety require consideration of renal protection and monitoring. Before therapy, receptor expression is confirmed by diagnostic imaging; during treatment, an amino acid infusion is used to reduce renal radiation exposure, and hematologic and renal function are regularly monitored. Common side effects include nausea, fatigue, and transient decreases in blood cell counts; kidney toxicity and rare long-term risks such as myelodysplastic syndrome may occur.

Regulatory status: Lutathera is approved in several regions for unresectable or metastatic somatostatin receptor-positive gastroenteropancreatic neuroendocrine tumors. The therapy highlights the broader use of radiopharmaceuticals to provide targeted, systemic treatment for select tumor types.