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A somatostatin analog with broad receptor coverage and high SSTR5 affinity.
Also known as: Signifor
Part of the Foundational & therapeutic peptides cluster
Overview
Pasireotide is a synthetic cyclohexapeptide somatostatin analog with roughly 40-fold greater affinity for somatostatin receptor 5 than earlier analogs. This broader receptor profile underlies its approval for Cushing's disease and acromegaly. Content here is educational only.
Source & context
Biological / chemical source: Synthetic cyclohexapeptide analog of somatostatin
Primary research or clinical context: Approved for Cushing's disease and acromegaly
Broadened receptor profile
Where octreotide and lanreotide act mainly through SSTR2, pasireotide engages SSTR1, 2, 3 and especially SSTR5. Targeting SSTR5 lets it suppress ACTH secretion in corticotroph tumors, which is why it is used in Cushing's disease.
Design trade-offs
The wider receptor coverage that gives pasireotide its distinct indication also alters its metabolic effect on glucose regulation compared with older analogs. It is a frequently cited example of how receptor-subtype selectivity shapes a peptide drug's clinical niche.
Sequence
One-letter sequence commonly cited for Pasireotide (educational; isoforms and modifications may differ):
XXWKYF
X = non-canonical residue (Residue 1 is hydroxyproline; residue 2 is 2-phenylglycine; tyrosine residue at position 5 is phenylmethylated). X marks a non-canonical residue — see the structure block below. (Plotted as alanine on the wheel.)
Residues plotted ~100° apart around an α-helix — clustering of one color reveals an amphipathic face.
Structure & chemistry
Molecular identity & reference confidence
Source-supported reference
Reference values are taken from the cited molecular record or curated profile. A database match is not independent laboratory verification; modifications, counter-ions, and formulations can change the measured mass.
- Molecular form
- Pasireotide (source record; form not independently established)
- Species
- Not established by this molecular identity audit
- Termini (N / C)
- Not specified / Not specified
Average reference mass
Reference policy updated: 2026-10-05
- IUPHAR/BPS source snapshot · 2026-10-01
- PubChem molecular record · 2026-10-01
- Molecular formula
- C58H66N10O9
- Average reference mass
- ≈ 1,047.2
- Status
- Approved medicine in at least one jurisdiction (IUPHAR record)
Residue 1 is hydroxyproline; residue 2 is 2-phenylglycine; tyrosine residue at position 5 is phenylmethylated
- PubChem CID: 9941444
- IUPHAR ligand: 2018
- DrugBank: DB06663
- CAS RN: 396091-73-9
- UNII: 98H1T17066
Chemistry values: IUPHAR/BPS Guide to Pharmacology, PubChem · fetched 2026-10-01.
Clinical development snapshot
ClinicalTrials.gov lists 86 registered studies with “Pasireotide” as an intervention (snapshot 2026-10-01). A registry footprint is not evidence of efficacy or approval.
| NCT | Title | Phase | Status | Updated |
|---|---|---|---|---|
| NCT05928390 | Pasireotide s.c. in Patients With Post-Bariatric Hypoglycaemia | Phase 2 | active not recruiting | 2026-09-17 |
| NCT06784752 | Study to Evaluate the Efficacy and Safety of [177Lu]Lu-DOTA-TATE in Patients With Grade 1 and Grade 2 Advanced | Phase 3 | recruiting | 2026-09-11 |
| NCT06295952 | A Study of Pasireotide in People With Prolactinoma | Phase 2 | recruiting | 2026-03-04 |
| NCT07312643 | Study in Healthy Subjects to Investigate the Relative Bioavailability and Safety of Pasireotide After Single S | Phase 1 | completed | 2026-02-04 |
| NCT03972488 | Study to Evaluate the Efficacy and Safety of Lutathera in Patients With Grade 2 and Grade 3 Advanced GEP-NET | Phase 3 | active not recruiting | 2026-01-21 |
| NCT02713776 | Reduction by Pasireotide of the Effluent Volume in High-output Enterostomy in Patients Refractory to Usual Med | Phase 2 | completed | 2025-12-19 |
Pasireotide — reconstitution calculator
Enter how much peptide is in the vial and how much diluent (e.g. bacteriostatic water) is added. The tool returns the resulting solution concentration — and, for any amount you type, the volume it corresponds to. This is educational arithmetic, not a dosing recommendation.
Reference form: Pasireotide (source record; form not independently established)Average reference mass: 1,047.2 Da
Enter an amount to see the volume it corresponds to.
Educational concentration mathematics only. This tool does not recommend a dose, amount, or protocol, and nothing here is medical advice. Many peptides are not authorized by Health Canada for human use — see our reconstitution and bacteriostatic-water guides for context.
FAQ about Pasireotide
What is Pasireotide?+
Pasireotide is a synthetic cyclohexapeptide somatostatin analog with roughly 40-fold greater affinity for somatostatin receptor 5 than earlier analogs. This broader receptor profile underlies its approval for Cushing's disease and acromegaly. Content here is educational only.
What Canadian product status is recorded for Pasireotide?+
Canadian product status for Pasireotide has not been verified in this profile. No verified record here does not mean no authorization exists. Status depends on the product, formulation and use; consult Health Canada's product records.
What is the typical length of Pasireotide?+
Pasireotide is commonly described as approximately 6 amino acids (Somatostatin analog).
Related peptides
References & further reading
- 1.McKeage (2015). Pasireotide in Acromegaly: A Review. Drugs
- 2.Mondin et al. (2025). Real-life data on pasireotide in monotherapy or combined in active Cushing's disease. Front Endocrinol (Lausanne)
- 3.Gadelha et al. (2022). Pituitary acting drugs: cabergoline and pasireotide. Pituitary
- 4.Cuevas-Ramos et al. (2016). Pasireotide: a novel treatment for patients with acromegaly. Drug Des Devel Ther
- 5.Silverstein (2016). Hyperglycemia induced by pasireotide in patients with Cushing's disease or acromegaly. Pituitary
- 6.Wildemberg et al. (2016). Pasireotide for the treatment of acromegaly. Expert Opin Pharmacother
- 7.Samson (2016). Management of Hyperglycemia in Patients With Acromegaly Treated With Pasireotide LAR. Drugs
- 8.Feelders et al. (2012). Pasireotide. Nat Rev Drug Discov
- 9.PubChem — compound summary for Pasireotide (CID 9941444)
- 10.Wikipedia — Pasireotide