Lutetium Lu 177 dotatate
Also known as: 177Lu-DOTATATE, 177Lu‑DOTA‑Tyr³‑Octreotate, 177Lu‑DOTATATE, Lu-177 DOTATATE, Lu‑177 dotatate, Lutathera, OPS201-Lu177, PRRT
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Summary
Lu‑177 DOTATATE (Lutathera) is an intravenously administered radiolabeled peptide used for peptide receptor radionuclide therapy (PRRT) of somatostatin‑receptor positive gastroenteropancreatic neuroendocrine tumors.
Mechanism of Action
Binds high‑affinity somatostatin receptor subtype 2 (SSTR2) on neuroendocrine tumor cells, is internalized, and delivers β‑particle radiation from ¹⁷⁷Lu to induce DNA damage and cell death.
Routes of Administration
Goals & Uses
- Treatment of somatostatin receptor-positive GEP-NETsOncology / Neuroendocrine Tumor ManagementHigh
- Symptom control in functional NETsSymptom ManagementModerate
- Symptom controlPalliativeModerate
- Treatment of GEP‑NETOncologyHigh
- Objective tumor response / tumor shrinkageOncology / Tumor ResponseModerate
- Treatment of other SSTR2-positive tumors (off-label/investigational)Oncology / Investigational UseLow
- Improvement of progression-free survival in NETsOncology / Disease ControlHigh
Contraindications
- Known hypersensitivity to peptide or DOTA chelateAllergyHigh
- Previous maximum radiation dose to critical organs (kidneys, bone marrow)Radiation OncologyHigh
- Severe renal impairment (eGFR <30 mL/min)RenalModerate
- PregnancyPopulationHighPotential fetal risk or insufficient safety data
- Severe renal impairment (eGFR <30 mL/min/1.73m²)RenalHigh
- BreastfeedingPopulationHighPotential transfer into breast milk or insufficient safety data
- Hypersensitivity to dotatate or Lu-177 componentsAllergy / ImmunologyHigh
Adverse Effects
- renal toxicityRenalUncommon
- HepatotoxicityHepaticUncommonLiver injury or dysfunction
- Myelosuppression (thrombocytopenia, anemia, lymphopenia)HematologicCommon
- Hepatotoxicity (elevated transaminases)HepaticUncommon
- Nausea/vomitingGastrointestinalCommon
- Nephrotoxicity / renal impairmentRenalUncommon
- Nausea and vomitingGastrointestinalCommon
- FatigueGeneralCommonLow energy or tiredness
- Radiation-induced myelodysplastic syndrome / acute leukemiaHematologic / Secondary MalignancyRare
- Hematologic toxicity (thrombocytopenia, neutropenia)HematologicCommon
Drug Interactions
- Myelosuppressive agents (chemotherapy, immunosuppressants)Moderate
- Long-acting somatostatin analogues (e.g., octreotide LAR)Moderate
- Aminoglycoside antibioticsModerate
- Nephrotoxic agents (e.g., aminoglycosides, NSAIDs, cisplatin)High
- Short-acting somatostatin analogues (e.g., octreotide SC)High
- Other radiopharmaceuticalsModerate
Population Constraints
- Patients with moderate renal impairment (eGFR 30-60 mL/min/1.73m²)RenalRelative
- Pediatric patientsAgeRelative
- Male patients with female partners of childbearing potentialReproductiveRelative
- Elderly with compromised marrow reserveAgeRelative
- Pregnant womenReproductiveAbsolute
- Patients with significant bone marrow involvement or prior myelotoxic therapyHematologicRelative
- Women of childbearing potentialReproductiveRelative
Regulatory Status
- European UnionApprovedApproved: SSTR‑positive gastroenteropancreatic NETsEMA centralized procedure
- United StatesApprovedApproved: Somatostatin receptor‑positive gastroenteropancreatic neuroendocrine tumorsFDA label includes G1–G2 NETs
- United KingdomApprovedApproved: SSTR‑positive gastroenteropancreatic NETsMHRA approval
FDA approved (2018) for G1–G2 gastroenteropancreatic NETs; EMA approval 2017; UK MHRA approval 2018.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Lutetium Lu 177 dotatate?
Lu‑177 DOTATATE (Lutathera) is an intravenously administered radiolabeled peptide used for peptide receptor radionuclide therapy (PRRT) of somatostatin‑receptor positive gastroenteropancreatic neuroendocrine tumors.
What is Lutetium Lu 177 dotatate used for?
Lutetium Lu 177 dotatate is educationally associated with: Treatment of somatostatin receptor-positive GEP-NETs, Symptom control in functional NETs, Symptom control, Treatment of GEP‑NET, Objective tumor response / tumor shrinkage, Treatment of other SSTR2-positive tumors (off-label/investigational), Improvement of progression-free survival in NETs. Educational only — not medical advice.
How is Lutetium Lu 177 dotatate administered?
Recorded routes of administration: Intravenous.
What are the potential side effects of Lutetium Lu 177 dotatate?
Reported adverse effects include: renal toxicity, Hepatotoxicity, Myelosuppression (thrombocytopenia, anemia, lymphopenia), Hepatotoxicity (elevated transaminases), Nausea/vomiting, Nephrotoxicity / renal impairment, Nausea and vomiting, Fatigue, Radiation-induced myelodysplastic syndrome / acute leukemia, Hematologic toxicity (thrombocytopenia, neutropenia). This list is not exhaustive — consult a qualified clinician.
Who should avoid Lutetium Lu 177 dotatate?
Recorded contraindications: Known hypersensitivity to peptide or DOTA chelate, Previous maximum radiation dose to critical organs (kidneys, bone marrow), Severe renal impairment (eGFR <30 mL/min), Pregnancy, Severe renal impairment (eGFR <30 mL/min/1.73m²), Breastfeeding, Hypersensitivity to dotatate or Lu-177 components. Consult a qualified clinician before use.