Pentetreotide
Also known as: 111In-DTPA-octreotide, 111In‑pentetreotide, D‑Phe‑Cys‑Phe‑D‑Trp‑Lys‑Thr‑Cys‑Thr‑NH2, In-111 pentetreotide, Indium-111 pentetreotide, OctreoScan
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Summary
Pentetreotide is a synthetic octapeptide somatostatin analogue used primarily as a radiopharmaceutical (e.g., ^111In‑pentetreotide, Octreoscan) for scintigraphic imaging of neuroendocrine tumors and other somatostatin‑receptor expressing lesions.
Mechanism of Action
high‑affinity binding to somatostatin receptor subtype 2 (sst2) and related subtypes, inhibiting hormone secretion and allowing radiolabelled imaging of receptor‑positive tissues
Routes of Administration
Goals & Uses
- Diagnostic imaging of somatostatin‑receptor positive tumorsDiagnosticHigh
- Staging and metastasis detectionOncology / StagingHigh
- Detection of small cell lung cancerDiagnostic OncologyModerate
- Patient selection for somatostatin analogue therapyTheranosticsModerate
- Localization of neuroendocrine tumorsDiagnostic ImagingHigh
- Pheochromocytoma and paraganglioma localizationDiagnostic ImagingModerate
Contraindications
- Severe renal impairmentOrganModerateKidney function concerns
- PregnancyPopulationHighPotential fetal risk or insufficient safety data
- BreastfeedingPopulationModeratePotential transfer into breast milk or insufficient safety data
- Hypersensitivity to pentetreotide or any component of the formulationAllergyHigh
- Hypersensitivity to octreotide or DTPAAllergyHigh
Adverse Effects
- Radiation exposureRadiologicalCommon
- Anaphylaxis / hypersensitivity reactionImmunologicRare
- HypotensionCardiovascularUncommonLow blood pressure
- FlushingVascularUncommonWarmth and redness of the skin
- NauseaGastrointestinalCommonFeeling of sickness or urge to vomit
- Hypoglycemia or hyperglycemiaMetabolicRare
- VomitingGastrointestinalCommonForceful expulsion of stomach contents
- Allergic reaction (rash, urticaria, anaphylaxis)ImmuneRare
- Flushing or warmth sensationVascularCommon
- DiarrheaGastrointestinalUncommonLoose or frequent stools
Drug Interactions
- Renal‑clearing radiopharmaceuticalsLow
- Octreotide (therapeutic)High
- Octreotide or other somatostatin analoguesModerate
- LanreotideHigh
- Total parenteral nutrition (TPN)Low
Population Constraints
- PregnancyReproductive SafetyRelative
- Renal impairmentOrgan ImpairmentRelative
- Pediatric patientsAgeRelative
- Patients with insulinomaEndocrineRelative
Regulatory Status
- European UnionApprovedApproved: diagnostic imaging of neuroendocrine tumors, meningioma detectionAvailable as radiolabelled formulations (e.g., ^68Ga‑pentetreotide) under EU guidelines
- United StatesWithdrawnApproved: diagnostic imaging of somatostatin‑receptor positive tumors (historical)Octreoscan (^111In‑pentetreotide) withdrawn from market in 2020
- United KingdomApprovedApproved: same as EURegulated as a radiopharmaceutical
Approved in many jurisdictions for diagnostic imaging; the ^111In formulation (Octreoscan) was withdrawn from the US market in 2020 but remains available in the EU and other regions.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Pentetreotide?
Pentetreotide is a synthetic octapeptide somatostatin analogue used primarily as a radiopharmaceutical (e.g., ^111In‑pentetreotide, Octreoscan) for scintigraphic imaging of neuroendocrine tumors and other somatostatin‑receptor expressing lesions.
What is Pentetreotide used for?
Pentetreotide is educationally associated with: Diagnostic imaging of somatostatin‑receptor positive tumors, Staging and metastasis detection, Detection of small cell lung cancer, Patient selection for somatostatin analogue therapy, Localization of neuroendocrine tumors, Pheochromocytoma and paraganglioma localization. Educational only — not medical advice.
How is Pentetreotide administered?
Recorded routes of administration: Intravenous.
What are the potential side effects of Pentetreotide?
Reported adverse effects include: Radiation exposure, Anaphylaxis / hypersensitivity reaction, Hypotension, Flushing, Nausea, Hypoglycemia or hyperglycemia, Vomiting, Allergic reaction (rash, urticaria, anaphylaxis), Flushing or warmth sensation, Diarrhea. This list is not exhaustive — consult a qualified clinician.
Who should avoid Pentetreotide?
Recorded contraindications: Severe renal impairment, Pregnancy, Breastfeeding, Hypersensitivity to pentetreotide or any component of the formulation, Hypersensitivity to octreotide or DTPA. Consult a qualified clinician before use.