Lutetium-177 dotatate (Lutathera)
Overview
A radiolabeled somatostatin analog consisting of the peptide DOTA-Tyr3-octreotate chelated to the beta-emitting radioisotope lutetium-177. Lutathera binds with high affinity to somatostatin receptor subtype 2 (SSTR2), which is overexpressed on neuroendocrine tumor cells, delivering targeted radiation therapy directly to tumor cells while sparing surrounding normal tissue. This peptide receptor radionuclide therapy (PRRT) approach combines receptor-targeted delivery with cytotoxic radiation.
Key Research Findings
FDA-approved in 2018 for somatostatin receptor-positive gastroenteropancreatic neuroendocrine tumors (GEP-NETs). NETTER-1 trial showed 79% reduction in risk of disease progression or death vs. high-dose octreotide (Strosberg et al., NEJM, 2017). Overall response rate of 18% with disease control rate of 82%. Nephrotoxicity and myelosuppression are principal dose-limiting toxicities.
Intravenous
FDA Approved
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