Lutetium Lu177 Edotreotide
Also known as: 177Lu-DOTATOC, 177Lu-edotreotide, 177Lu‑EDOT, ITM-11, Lu-177-DOTA-Tyr3-octreotide, Lu‑177‑DOTA‑TOC, Lu‑177‑edotreotide, Lutathera (related, distinct: DOTATATE), OctreoTher
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Summary
Lu‑177 edotreotide is a DOTA‑conjugated somatostatin analogue labeled with the β‑emitting radionuclide lutetium‑177, used experimentally for peptide receptor radionuclide therapy (PRRT) of SSTR2‑positive neuroendocrine tumours.
Mechanism of Action
high‑affinity binding to somatostatin receptor subtype 2 (SSTR2) on neuroendocrine tumor cells, delivering β‑particle radiation from ¹⁷⁷Lu to induce DNA damage and cell death
Routes of Administration
Goals & Uses
- treatment of metastatic gastroenteropancreatic neuroendocrine tumoursOncologyHigh
- Palliation of symptoms in functional NETsSymptom ManagementModerate
- Tumor response and disease control in midgut NETsOncologyHigh
- Treatment of other SSTR2-expressing tumors (paraganglioma, pheochromocytoma, meningioma)Oncology / InvestigationalLow
- Treatment of somatostatin receptor-positive GEP-NETsOncology / Neuroendocrine Tumor ManagementHigh
- palliation of hormone‑related symptomsSymptom ControlModerate
Contraindications
- Prior maximum cumulative radiation dose to kidneysRadiation DosimetryHigh
- Severe renal impairment (eGFR <30 mL/min)RenalModerate
- Severe renal impairment (GFR <30 mL/min)Renal FunctionHigh
- PregnancyPopulationHighPotential fetal risk or insufficient safety data
- BreastfeedingPopulationHighPotential transfer into breast milk or insufficient safety data
- Severe bone marrow suppressionHematologicHigh
Adverse Effects
- renal toxicityRenalUncommon
- Myelosuppression (thrombocytopenia, leukopenia, anemia)HematologicCommon
- Nausea/vomitingGastrointestinalCommon
- Nausea and vomitingGastrointestinalCommon
- FatigueGeneralCommonLow energy or tiredness
- Radiation-induced hepatotoxicityHepaticRare
- haematologic toxicity (thrombocytopenia, neutropenia)HematologicCommon
- Secondary myelodysplastic syndrome / leukemiaHematologicRare
- NephrotoxicityRenalUncommon
Drug Interactions
- concomitant nephrotoxic agents (e.g., aminoglycosides, NSAIDs)Moderate
- Myelosuppressive chemotherapyHigh
- Long-acting somatostatin analogues (octreotide LAR, lanreotide)Moderate
- Nephrotoxic drugs (aminoglycosides, NSAIDs, cisplatin)High
Population Constraints
- Pediatric patientsAgeRelative
- Children (<18 y)AgeRelative
- Elderly patients (>75 years)AgeRelative
- Elderly (>75 y)AgeRelative
- Patients with renal impairmentOrgan ImpairmentRelative
- Patients with extensive bone marrow involvement by tumorDisease CharacteristicsRelative
Regulatory Status
- European UnionInvestigationalclinical trial phase III (EurA) as of 2024
- United StatesInvestigationalunder IND for PRRT of SSTR2‑positive NETs
- United KingdomUnknownUsed in specialized centers; regulatory approval status in UK post-Brexit requires verification with MHRA.
The FDA approved lutetium Lu-177 edotreotide (OCREOTIDE-based DOTA conjugate; brand: PluvictoTM is a different compound; edotreotide as therapeutic known as ITM-11) in 2024 for GEP-NETs. Distinct from lutetium Lu-177 dotatate (Lutathera). 177Lu-edotreotide (DOTATOC) is approved in some jurisdictions; regulatory status varies by exact formulation and jurisdiction.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Lutetium Lu177 Edotreotide?
Lu‑177 edotreotide is a DOTA‑conjugated somatostatin analogue labeled with the β‑emitting radionuclide lutetium‑177, used experimentally for peptide receptor radionuclide therapy (PRRT) of SSTR2‑positive neuroendocrine tumours.
What is Lutetium Lu177 Edotreotide used for?
Lutetium Lu177 Edotreotide is educationally associated with: treatment of metastatic gastroenteropancreatic neuroendocrine tumours, Palliation of symptoms in functional NETs, Tumor response and disease control in midgut NETs, Treatment of other SSTR2-expressing tumors (paraganglioma, pheochromocytoma, meningioma), Treatment of somatostatin receptor-positive GEP-NETs, palliation of hormone‑related symptoms. Educational only — not medical advice.
How is Lutetium Lu177 Edotreotide administered?
Recorded routes of administration: Intravenous.
What are the potential side effects of Lutetium Lu177 Edotreotide?
Reported adverse effects include: renal toxicity, Myelosuppression (thrombocytopenia, leukopenia, anemia), Nausea/vomiting, Nausea and vomiting, Fatigue, Radiation-induced hepatotoxicity, haematologic toxicity (thrombocytopenia, neutropenia), Secondary myelodysplastic syndrome / leukemia, Nephrotoxicity. This list is not exhaustive — consult a qualified clinician.
Who should avoid Lutetium Lu177 Edotreotide?
Recorded contraindications: Prior maximum cumulative radiation dose to kidneys, Severe renal impairment (eGFR <30 mL/min), Severe renal impairment (GFR <30 mL/min), Pregnancy, Breastfeeding, Severe bone marrow suppression. Consult a qualified clinician before use.