Edotreotide yttrium Y-90
Also known as: 90Y-DOTATOC, DOTA-Tyr3-octreotide Y-90, DOTA‑(D‑Phe1)‑Tyr3‑Octreotide, DOTATOC, Edotreotide, OctreoTher, SOM230 radiolabeled analogue (distinct), Y-90 DOTA-TOC, Y-90 edotreotide
Source Edotreotide yttrium Y-90 at Peptiology
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Summary
Edotreotide yttrium (90Y‑DOTATOC) is a radiolabeled somatostatin analogue used in peptide‑receptor radionuclide therapy (PRRT) for somatostatin‑receptor‑positive tumours, especially neuroendocrine tumours (NETs), gastro‑enteropancreatic NETs, pheochromocytomas and paragangliomas. The compound is administered intravenously and delivers high‑energy beta radiation from yttrium‑90 to tumour cells that express the sst2 receptor, aiming to halt tumour growth and induce tumour regression.
Mechanism of Action
90Y‑DOTATOC consists of the somatostatin analogue DOTATOC linked to the beta‑emitter yttrium‑90. The peptide binds with high affinity to somatostatin receptor subtype 2 (sst2) on tumour cells, is internalised, and the yttrium‑90 decay emits penetrating beta particles that cause DNA double‑strand breaks and cell death within the tumour while sparing surrounding tissue.
What the Research Shows
Clinical experience with 90Y‑DOTATOC derives from phase I/II series, retrospective cohorts and a recent meta‑analysis. In 30 patients treated with escalating activities, 23% achieved partial or complete tumour reduction and 64% had stable disease, with low acute toxicity up to 2.59 GBq per cycle (Paganelli 2001). A systematic review of 213 patients with pheochromocytoma or paraganglioma reported a pooled disease‑control rate of 0.76 for 90Y‑PRRT (Marretta 2023). Larger reviews of NETs note objective response rates of 20‑28% overall and 28‑38% in gastro‑enteropancreatic NETs, with disease stabilisation in more than half of patients (Nisa 2011; Kjaer 2015). Dosimetry‑guided administration in a prospective phase‑2 trial showed highly variable renal doses, prompting activity adjustments in 85% of patients (Menda 2018). Across studies, renal toxicity is dose‑limiting, while bone‑marrow suppression is less frequent.
Reported Benefits
Evidence indicates that 90Y‑DOTATOC can achieve objective tumour shrinkage in roughly one‑quarter of treated patients and disease stabilisation in the majority, translating into meaningful disease‑control rates (0.76–0.83) across tumour types. PRRT also provides symptomatic relief in hormone‑secreting tumours and has been associated with a survival benefit in NET cohorts, although the latter is based on non‑randomised data. The high‑energy beta emission permits treatment of larger lesions that may be less responsive to lower‑energy isotopes.
Limitations of the Evidence
Most data come from small, single‑centre or retrospective series; randomised controlled trials are lacking. Renal toxicity limits the cumulative activity that can be delivered, and dosimetry varies widely between patients, complicating standardised dosing. Comparative effectiveness versus the newer 177Lu‑DOTATATE remains uncertain, with some reports suggesting lower toxicity for the latter. Long‑term outcomes and quality‑of‑life impacts are incompletely characterised.
Safety Considerations
Acute reactions are rare; studies report no immediate adverse events up to 2.59 GBq per cycle. Transient lymphocytopenia and occasional grade II renal toxicity after cumulative doses have been observed. Grade 3‑4 kidney toxicity occurs in about 1.5 % of patients and severe bone‑marrow suppression in roughly 9.5 %, usually reversible with supportive care. Renal protection (e.g., amino‑acid infusion) is recommended to mitigate nephrotoxicity.
How It Is Administered
90Y‑DOTATOC is given intravenously, typically in three treatment cycles spaced 6–8 weeks apart. Activity per cycle has ranged from ~3 GBq to 4.4 GBq in adult studies, with dose adjustments based on patient‑specific renal dosimetry. Amino‑acid infusion is commonly used during administration to protect the kidneys.
Routes of Administration
Goals & Uses
- Symptom control in functional NETsSymptom ManagementModerate
- Tumor downsizing prior to surgeryOncologyModerate
- Treatment of somatostatin receptor-positive neuroendocrine tumorsOncologyHigh
- Neuroendocrine tumor therapyOncologyModerate
- Metastatic paraganglioma / pheochromocytomaOncologyLow
Contraindications
- Hepatic decompensation / liver metastases >70% liver replacementHepaticModerate
- Severe renal impairmentOrganHighKidney function concerns
- PregnancyPopulationHighPotential fetal risk or insufficient safety data
- BreastfeedingPopulationHighPotential transfer into breast milk or insufficient safety data
- Hypersensitivity to DOTA-TOC or somatostatin analoguesImmunologicHigh
- Severe bone marrow suppressionHematologicHigh
Adverse Effects
- Myelosuppression (thrombocytopenia, leukopenia)HematologicCommon
- Nausea/vomitingGastrointestinalCommon
- Hematologic toxicity (anemia, thrombocytopenia, leukopenia)HematologyCommon
- Nausea and vomitingGastrointestinalCommon
- FatigueGeneralCommonLow energy or tiredness
- Radiation-induced hepatotoxicityHepaticUncommon
- Secondary myelodysplastic syndrome / leukemiaHematologicRare
- NephrotoxicityRenalUncommon
Drug Interactions
- Nephrotoxic agents (e.g., aminoglycosides, NSAIDs)Moderate
- Nephrotoxic agents (aminoglycosides, NSAIDs, contrast agents)High
- Myelosuppressive chemotherapyModerate
- Long-acting somatostatin analogues (octreotide LAR, lanreotide)Moderate
Population Constraints
- Patients with prior external beam radiation to kidneys or bone marrowPrior TherapyRelative
- Pediatric patientsAgeRelative
- Elderly patients (>70 years)AgeRelative
- Patients with renal impairment (GFR <40 mL/min)RenalRelative
Regulatory Status
- European UnionInvestigationalUsed under clinical trial protocols for NETs.
- United StatesUnapprovedAvailable only via IND for research.
- United KingdomUnknownPost-Brexit regulatory status uncertain; likely available through specialist centers on named-patient or compassionate use basis.
Approved in Switzerland and used under various national regulatory frameworks in Europe. Not FDA-approved in the United States; Lutathera (Lu-177 DOTATATE) is the FDA-approved PRRT. EMA approval status has been complex; OctreoTher was approved in Switzerland and used under compassionate/named-patient programs across Europe.
Evidence & Sources
- Journal ArticleModerateMarretta AL, et al.2023-01-01T00:00:00.000000Z
- Journal ArticleModeratePaganelli G, et al.2001-01-01T00:00:00.000000Z
- Journal ArticleModerateKjaer A, Knigge U2015-01-01T00:00:00.000000Z
- Journal ArticleModerateBodei L, et al.2009-01-01T00:00:00.000000Z
- Journal ArticleModerateMenda Y, et al.2018-01-01T00:00:00.000000Z
- Journal ArticleModerateNisa L, Savelli G, Giubbini R2011-01-01T00:00:00.000000Z
Frequently Asked Questions
What types of tumours can be treated with 90Y‑DOTATOC?
It is indicated for tumours that express somatostatin receptor subtype 2, most commonly neuroendocrine tumours of the gastrointestinal tract, pancreas, bronchial system, as well as pheochromocytomas and paragangliomas.
How does 90Y‑DOTATOC differ from 177Lu‑DOTATATE?
Both target sst2, but yttrium‑90 emits higher‑energy beta particles with deeper tissue penetration, which may be advantageous for larger lesions. 177Lu emits lower‑energy betas and is reported to have slightly less renal toxicity, though head‑to‑head trials are limited.
What are the main side effects to watch for?
The principal concerns are renal toxicity, which is dose‑limiting, and bone‑marrow suppression. Acute allergic‑type reactions are uncommon. Protective amino‑acid infusions are used to reduce kidney exposure.
Is the treatment curative?
Current evidence supports disease control and tumour reduction in a subset of patients, but cure is rare. PRRT is generally used to prolong survival, alleviate symptoms, and stabilize disease in advanced, inoperable cases.
Can dosing be personalised?
Yes. Recent studies using 90Y‑DOTATOC PET/CT and bremsstrahlung SPECT/CT allow patient‑specific renal dosimetry, leading to activity adjustments in most patients to stay within safe kidney dose limits.
What is Edotreotide yttrium Y-90?
Edotreotide yttrium (90Y‑DOTATOC) is a radiolabeled somatostatin analogue used in peptide‑receptor radionuclide therapy (PRRT) for somatostatin‑receptor‑positive tumours, especially neuroendocrine tumours (NETs), gastro‑enteropancreatic NETs, pheochromocytomas and paragangliomas. The compound is administered intravenously and delivers high‑energy beta radiation from yttrium‑90 to tumour cells that express the sst2 receptor, aiming to halt tumour growth and induce tumour regression.
What is Edotreotide yttrium Y-90 used for?
Edotreotide yttrium Y-90 is educationally associated with: Symptom control in functional NETs, Tumor downsizing prior to surgery, Treatment of somatostatin receptor-positive neuroendocrine tumors, Neuroendocrine tumor therapy, Metastatic paraganglioma / pheochromocytoma. Educational only — not medical advice.
How is Edotreotide yttrium Y-90 administered?
Recorded routes of administration: Intravenous.
What are the potential side effects of Edotreotide yttrium Y-90?
Reported adverse effects include: Myelosuppression (thrombocytopenia, leukopenia), Nausea/vomiting, Hematologic toxicity (anemia, thrombocytopenia, leukopenia), Nausea and vomiting, Fatigue, Radiation-induced hepatotoxicity, Secondary myelodysplastic syndrome / leukemia, Nephrotoxicity. This list is not exhaustive — consult a qualified clinician.
Who should avoid Edotreotide yttrium Y-90?
Recorded contraindications: Hepatic decompensation / liver metastases >70% liver replacement, Severe renal impairment, Pregnancy, Breastfeeding, Hypersensitivity to DOTA-TOC or somatostatin analogues, Severe bone marrow suppression. Consult a qualified clinician before use.