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Endocrine · Reference monograph

Long-acting synthetic somatostatin analogue

Reference compound — not available from Purity Peptides. Shown for research context.

Overview

Octreotide (SMS 201-995) is a synthetic cyclic octapeptide analogue of somatostatin, developed at Sandoz and first described by Wilfried Bauer and colleagues in 1982. By preserving the core pharmacophore of somatostatin, the Phe-Trp-Lys-Thr sequence, within a smaller ring containing D-amino acids and a C-terminal threoninol, its designers produced a molecule far more resistant to enzymatic degradation than the native hormone.

Octreotide is an approved prescription medicine for acromegaly and for symptoms associated with certain neuroendocrine tumours, including carcinoid tumours and VIPomas, in the United States, Europe and elsewhere. Its selectivity for somatostatin receptor subtype 2 made it the template for radiolabelled ligands that transformed neuroendocrine tumour imaging, from indium-111 pentetreotide scintigraphy to gallium-68 DOTA-peptide PET. Long-acting microsphere formulations were later introduced. In research, octreotide is a standard SSTR2 agonist used in studies of growth hormone hypersecretion, neuroendocrine tumour biology, receptor internalisation and theranostic ligand design. The PROMID trial examined its antiproliferative potential in midgut neuroendocrine tumours.

Mechanism studied

  1. Octreotide
  2. SSTR2 / SSTR5
  3. GH & hormone secretion ↓
  4. IGF-1 ↓

Octreotide binds SSTR2 with high affinity, SSTR5 with moderate affinity and SSTR3 with lower affinity, and has negligible affinity for SSTR1 and SSTR4. Through Gi/o coupling it inhibits adenylyl cyclase, reduces calcium influx and activates potassium channels, suppressing exocytosis of growth hormone from somatotroph adenomas and of hormones and amines from neuroendocrine tumour cells. Reduced growth hormone output lowers hepatic IGF-1 production. Antiproliferative effects observed in experimental models involve phosphatase activation, growth arrest and possibly inhibition of angiogenesis. After binding, octreotide drives rapid SSTR2 internalisation, a property exploited by radiolabelled analogues to concentrate signal within tumour cells.

Research highlights

  • 01Developed at Sandoz and described in 1982 as the first clinically viable somatostatin analogue.
  • 02Radiolabelled derivatives, including indium-111 pentetreotide and gallium-68 DOTATOC, became foundational tools in receptor imaging.
  • 03The PROMID trial examined time to tumour progression in midgut neuroendocrine tumours, supporting antiproliferative research.
  • 04Long-acting microsphere formulations made octreotide a reference case in sustained peptide release science.
  • 05Open questions include mechanisms of resistance in somatotroph adenomas and the role of SSTR2 expression heterogeneity.

Latest published research

10,265 papers on PubMed →

  1. Double emulsions enable in situ generation of permeation enhancers for oral delivery of macromolecules

    Pohlit H et al. · Journal of colloid and interface science · 2026 Dec 15 · PMID 42385442

  2. Congenital hyperinsulinism as part of a multisystem disease caused by a compound heterozygous variant in the YARS1 gene

    Bolmasova A et al. · JCEM case reports · 2026 Dec · PMID 42891076

  3. Self-assembly of sodium caprate in simulated intestinal fluids and with a therapeutic peptide: A small-angle neutron scattering study

    Akter S et al. · International journal of pharmaceutics: X · 2026 Dec · PMID 42662504

  4. Octreotide mitigates cisplatin-induced nephrotoxicity through coordinated modulation of the miR-34a/SIRT1 axis and downstream apoptotic, inflammatory, and fibrotic pathways

    Ghoneim ME et al. · Life sciences · 2026 Nov 15 · PMID 42753908

  5. Efficacy of octreotide in preventing lymphedema after radical, modified radical, and partial mastectomy with axillary lymphadenectomy

    Challa S et al. · Journal of plastic, reconstructive & aesthetic surgery : JPRAS · 2026 Nov · PMID 42748551

  6. Structural control and resilience in the oxytocin molecular graph: A graph-theoretic framework for critical atom and bond identification with comparative validation across cyclic peptides

    K ND et al. · Journal of molecular graphics & modelling · 2026 Nov · PMID 42580195

  7. The Diagnosis and Management of Hepatorenal Syndrome: A Comprehensive Update for the Intensivist

    Teixeira JP et al. · Journal of intensive care medicine · 2026 Nov · PMID 40473434

  8. Octreotide-modified pH-responsive nanocomposites for ultrasound imaging-guided chemo-photothermal therapy of prostate cancer

    Sun R et al. · Nanoscale · 2026 Oct 27 · PMID 42944769

Live feed from PubMed (NCBI) for “Octreotide”, updated 2026-10-30. Listing a paper is not an endorsement of its findings.

Registered studies

327 on ClinicalTrials.gov →

From the public ClinicalTrials.gov registry for “Octreotide”, updated 2026-10-30. Shown for research context only; Purity Peptides products are not for human use.

Key references

  1. [1]Manufacturer's prescribing information — FDA / EMA / ANVISA
  2. [2]PubMed — reviews on octreotide and acromegaly

FAQ

  • Octreotide is shorter, containing eight amino acids instead of fourteen, includes D-amino acids and has a modified C-terminus. These features greatly extend its half-life and focus its activity on SSTR2 and SSTR5, unlike native somatostatin, which binds all five subtypes.

  • Many neuroendocrine tumours express abundant SSTR2. Linking octreotide or its relatives to radionuclides creates ligands that bind and internalise in these tumours, allowing visualisation by scintigraphy or PET. This approach also underpins theranostic research pairing diagnostic and radionuclide variants.

  • Octreotide is an approved prescription medicine in many countries for acromegaly and for symptoms associated with certain neuroendocrine tumours. It is supplied here only as a research reference material for laboratory investigation of somatostatin receptor pharmacology.

FOR RESEARCH USE ONLY.Not for human or veterinary use. Not intended to diagnose, treat, cure, or prevent any disease.

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