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Endocrine · Reference monograph

Multi-receptor somatostatin analogue for Cushing's disease and acromegaly

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

Overview

Pasireotide (SOM230) is a synthetic cyclohexapeptide somatostatin analogue developed by Novartis. It was designed to mimic the broader receptor profile of native somatostatin more closely than first-generation analogues, binding with high affinity to four of the five somatostatin receptor subtypes and showing particularly strong affinity for SSTR5.

This multi-receptor profile is important because corticotroph adenomas, the pituitary tumours responsible for Cushing's disease, express SSTR5 more prominently than SSTR2, making them relatively unresponsive to octreotide and lanreotide. Pasireotide was approved by the FDA in 2012 for Cushing's disease, becoming the first pituitary-directed medicine for that condition, and a long-acting formulation was later approved for acromegaly. It is an approved prescription medicine in the US and EU. A characteristic finding in clinical research has been hyperglycaemia, reflecting SSTR5's role in islet and incretin biology. For researchers, pasireotide is a key tool for SSTR5 pharmacology, ACTH secretion studies, corticotroph adenoma biology and glucose-handling research.

Mechanism studied

  1. Pasireotide
  2. SSTR1/2/3/5
  3. ACTH & GH ↓
  4. Cortisol & IGF-1

Pasireotide binds SSTR1, SSTR2, SSTR3 and SSTR5, with its highest affinity at SSTR5, considerably higher than that of octreotide. Through Gi/o coupling it inhibits adenylyl cyclase and calcium-dependent exocytosis. In corticotroph adenoma cells, SSTR5 activation suppresses ACTH secretion and pro-opiomelanocortin expression, reducing adrenal cortisol output. In somatotroph adenomas, combined SSTR2 and SSTR5 activity suppresses growth hormone and downstream IGF-1. Hyperglycaemia arises because SSTR5 and SSTR2 activation reduces insulin secretion from beta cells and lowers incretin hormone release, while glucagon suppression is comparatively modest. Pasireotide also produces less SSTR2 internalisation than octreotide, a sign of distinct signalling bias.

Research highlights

  • 01Designed by Novartis as SOM230 to reproduce the multi-receptor binding profile of native somatostatin.
  • 02Approved by the FDA in 2012 for Cushing's disease and later for acromegaly in a long-acting form.
  • 03Studies of corticotroph adenomas revealed predominant SSTR5 expression, explaining the selectivity rationale.
  • 04Mechanistic studies in healthy volunteers linked pasireotide-associated hyperglycaemia to reduced insulin and incretin secretion.
  • 05Open questions include predictors of response in Cushing's disease and the significance of its distinct receptor trafficking profile.

Latest published research

843 papers on PubMed →

  1. Cost-effectiveness of pasireotide long-acting release in acromegaly: a systematic literature review and methodology assessment

    Gilis-Januszewska A et al. · Journal of medical economics · 2026 Dec · PMID 41518621

  2. Beyond the catalytic site: Voxilaprevir and Pasireotide as repurposed therapeutics for conformational inhibition of ADAR1

    Bahena-Culhuac E et al. · Journal of molecular graphics & modelling · 2026 Nov · PMID 42372606

  3. New and emerging pharmacological treatment options for acromegaly: a 2026 update

    Wildemberg LE et al. · Expert opinion on pharmacotherapy · 2026 Oct 21 · PMID 42878008

  4. Should radiotherapy be repositioned in the contemporary management of acromegaly?

    di Filippo L et al. · Pituitary · 2026 Oct 16 · PMID 42888334

  5. Personalised acromegaly treatment: implementing precision medicine in the Gulf States

    Elhadd T et al. · Frontiers in endocrinology · 2026 · PMID 42947680

  6. Predictors of in vitro response to somatostatin and dopamine receptor-targeted treatments are lacking in clinically non-functioning pituitary tumors

    Campana C et al. · Journal of neuroendocrinology · 2026 Oct · PMID 42785810

  7. Comparative Efficacy and Safety of Octreotide, Lanreotide, and Pasireotide in Autosomal Dominant Polycystic Kidney Disease and Polycystic Liver Disease: A Network Meta-Analysis With Real-World Evidence From the FDA Adverse Event Reporting System Database

    Mei Z et al. · Clinical and translational gastroenterology · 2026 Oct 1 · PMID 42476150

  8. Recurrent Cushing's disease due to postoperative seeding of tumor cells in the sphenoid sinus: a case report with review of the literature

    Matsuda T et al. · Endocrine journal · 2026 Oct 1 · PMID 42270362

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

Registered studies

87 on ClinicalTrials.gov →

From the public ClinicalTrials.gov registry for “Pasireotide”, 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]Colao et al., 2012 — N Engl J Med 366:914–924

FAQ

  • Corticotroph adenomas in Cushing's disease express SSTR5 abundantly, and glucocorticoid excess downregulates SSTR2 in these cells. First-generation analogues that act mainly at SSTR2 therefore have limited effect, while pasireotide's strong SSTR5 affinity enables suppression of ACTH secretion in research models.

  • SSTR5 and SSTR2 on pancreatic beta cells and intestinal L- and K-cells mediate inhibition of insulin and incretin secretion. Pasireotide suppresses these pathways more than it suppresses glucagon, shifting glucose balance upward. This makes pasireotide a useful tool in glucose-handling research.

  • Pasireotide is an approved prescription medicine in the United States and European Union for Cushing's disease and acromegaly. Rights to the product were transferred from Novartis to Recordati. It is supplied here strictly as a research reference compound.

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

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