Edotreotide

Summary

Edotreotide (DOTA-TOC) is a cyclic octapeptide somatostatin analogue conjugated to the chelator DOTA, enabling radiolabeling for peptide receptor radionuclide therapy (PRRT) and diagnostic imaging. As 90Y-edotreotide (90Y-DOTATOC), it has been used in PRRT for somatostatin receptor-positive neuroendocrine tumors. The 68Ga-labeled form is used for PET imaging. SomaKit TOC (68Ga-labeled) is approved in the EU for PET imaging of somatostatin receptor-positive neuroendocrine tumors.

Mechanism of Action

Edotreotide (DOTA-TOC) is a somatostatin analogue that binds with high affinity to somatostatin receptors (particularly SSTR2) overexpressed on neuroendocrine tumors. When chelated with radiometals (e.g., 90Y, 68Ga, 111In), it delivers targeted radionuclide therapy or enables diagnostic imaging of receptor-expressing tumors.

Routes of Administration

Goals & Uses

• Detection of paraganglioma and pheochromocytomaDiagnostic / ImagingModerate
• PET imaging of somatostatin receptor-positive neuroendocrine tumorsDiagnostic / ImagingHigh
• Peptide receptor radionuclide therapy (PRRT) of NETsOncology / TherapyModerate
• Tumor staging and restaging of neuroendocrine tumorsDiagnostic / ImagingHigh

Contraindications

• Severe renal impairment (for 90Y-DOTATOC therapy)Organ ImpairmentHigh
• PregnancyPopulationHighPotential fetal risk or insufficient safety data
• BreastfeedingPopulationHighPotential transfer into breast milk or insufficient safety data
• Hypersensitivity to edotreotide or somatostatin analoguesAllergy / HypersensitivityHigh

Adverse Effects

• Injection site reactionsLocalUncommon
• Radiation-induced secondary malignancyOncologicRare
• Nausea and vomitingGastrointestinalCommon
• MyelosuppressionHematologicUncommon
• Transient hormonal effects (hypoglycemia, flushing)EndocrineUncommon
• NephrotoxicityRenalUncommon

Drug Interactions

• Chemotherapy agents causing myelosuppressionModerate
• Long-acting somatostatin analogues (octreotide LAR, lanreotide)Moderate
• Nephrotoxic agents (aminoglycosides, NSAIDs, cisplatin)High

Population Constraints

• Patients with bone marrow compromiseHematologicRelative
• Pediatric patientsAgeRelative
• Patients with renal impairmentOrgan ImpairmentRelative
• Elderly patientsAgeRelative

Regulatory Status

• European UnionApprovedApproved: PET imaging of somatostatin receptor-positive gastroenteropancreatic neuroendocrine tumors (GEP-NETs) in adults (as SomaKit TOC, 68Ga-edotreotide)SomaKit TOC received EMA approval in 2016. 90Y-edotreotide for PRRT is not separately approved but used in clinical practice.
• United StatesInvestigational68Ga-DOTATOC has been available under IND at select centers; FDA approval is held by 68Ga-DOTATATE (Netspot) and 177Lu-DOTATATE (Lutathera), not edotreotide specifically.
• United KingdomApprovedApproved: PET imaging of somatostatin receptor-positive NETs (SomaKit TOC, post-Brexit recognition of EMA approval)Recognized following EMA approval; MHRA status aligns with EU for SomaKit TOC.

SomaKit TOC (68Ga-edotreotide, 68Ga-DOTATOC) received EMA approval in 2016 for PET imaging of somatostatin receptor-positive neuroendocrine tumors. In the US, 68Ga-DOTATOC has been used under IND/NDA pathways; 68Ga-DOTATATE (a related but distinct compound) holds FDA approval. 90Y-edotreotide is used investigationally for PRRT in various jurisdictions.

Evidence & Sources

No sources recorded yet.