Lutetium Lu 177 Dotatate
Also known as: Lutathera, 177Lu-DOTATATE, Lu-177 dotatate
A radioactive somatostatin-analog peptide that delivers radiation to neuroendocrine tumors, FDA-approved in 2018 as Lutathera. Prescription drug.
Last updated
Mechanism of Action
Lutetium Lu 177 dotatate links the somatostatin analog peptide Tyr3-octreotate to the chelator DOTA, which holds the radioactive isotope lutetium-177. The peptide binds somatostatin receptor subtype 2, which many well-differentiated neuroendocrine tumors overexpress, and is taken into the tumor cells. Lutetium-177 then emits beta particles with a short tissue range (up to about 2 mm), damaging DNA in the tumor and nearby cells while limiting exposure to distant tissue; it also emits gamma rays that allow imaging.
- Half-life
- ~6.6 days (physical half-life of lutetium-177)
- Administration Routes
- Intravenous
- Research Status
- Clinical
Reported Benefits
- FDA-approved for somatostatin receptor-positive gastroenteropancreatic neuroendocrine tumors in adults and children aged 12 and older
- Prolonged progression-free survival versus high-dose octreotide in the phase 3 NETTER-1 trial (midgut tumors)
- Prolonged progression-free survival as first-line treatment for grade 2-3 tumors in the phase 3 NETTER-2 trial
Potential Side Effects
- Bone marrow suppression (low lymphocytes, platelets, blood counts)
- Nausea and vomiting
- Secondary myelodysplastic syndrome and leukemia
- Kidney and liver toxicity
- Neuroendocrine hormonal crisis and infertility risk
Common Dosing
Given as intravenous infusions by nuclear medicine teams, typically a course of four treatments spaced weeks apart, with an amino acid infusion to protect the kidneys and long-acting octreotide between doses. Activity is measured in GBq/mCi, and patients are first confirmed as somatostatin receptor-positive by imaging. Dosing is set and supervised by the prescribing clinician.
The dosing information above is aggregated from research literature and anecdotal community reports for educational purposes only. It is not a recommendation, prescription, or medical advice. Peptides are sold as research chemicals only and are not intended for human use.
Contraindications
- Pregnancy (can cause fetal harm; radiation exposure)
- Breastfeeding during and after treatment
- Somatostatin receptor-negative tumors are not expected to respond
- View
Phase 3 Trial of (177)Lu-Dotatate for Midgut Neuroendocrine Tumors
2017
- View
[(177)Lu]Lu-DOTA-TATE plus long-acting octreotide versus high‑dose long-acting octreotide for the treatment of newly diagnosed, advanced grade 2-3, well-differentiated, gastroenteropancreatic neuroendocrine tumours (NETTER-2): an open-label, randomised, phase 3 study
2024