Page data last changed: . Registry refreshes and identity assessments are separate from scientific content review.
An eight-residue cyclic somatostatin mimic with two D-amino acids — one of the most widely used peptide drugs in medicine.
Also known as: Sandostatin · Mycapssa · octreotide acetate · SMS 201-995
Part of the Foundational & therapeutic peptides cluster
Overview
Octreotide is a cyclic eight-amino-acid synthetic analogue of somatostatin (C49H66N10O10S2, ≈1,019 Da) with a D-phenylalanine at position 1, a D-tryptophan at position 4 and a disulfide bridge between its two cysteines. It suppresses growth hormone, thyrotropin and a range of pancreatic and gut hormones. Approved for acromegaly, TSH-secreting pituitary tumours and neuroendocrine tumours, it is available as injection, long-acting depot and — since 2020 — an oral capsule, and radiolabelled forms image somatostatin-receptor-positive tumours.
Source & context
Biological / chemical source: Synthetic analog
Primary research or clinical context: Approved for acromegaly, TSH-secreting pituitary tumours and neuroendocrine tumours; oral formulation (Mycapssa) approved by the FDA in 2020 and the EMA in 2022; also used in nuclear-medicine imaging
What octreotide is
Octreotide is a synthetic octapeptide that mimics somatostatin, the hormone that switches off growth hormone and many gut and pancreatic secretions. Native somatostatin lasts only minutes; octreotide was engineered from its receptor-binding core into a compact, cyclic, protease-resistant molecule that could be used as a medicine (Katz & Erstad, Clinical Pharmacy 1989). Its molecular formula is C49H66N10O10S2 and its average mass about 1,019 Da. It has been in clinical use since the late 1980s and, with 325 registered studies on ClinicalTrials.gov and more than 9,000 PubMed entries, it is among the most thoroughly documented peptide drugs.
Sequence and structure
The selected reference backbone is F-C-F-W-K-T-C-X, where X8 is threoninol, the reduced terminal threonine, rather than an ordinary threonine acid. The reference also carries D-phenylalanine at position 1, D-tryptophan at position 4 and a disulfide bond between Cys2 and Cys7. Those changes turn a fragile hormone fragment into a drug: the D-amino acids resist proteolysis, and the disulfide holds the Phe-Trp-Lys-Thr β-turn that the somatostatin receptor recognises. The chip display shows the backbone; the selected-form note and expanded sequence describe the stereochemistry and modifications.
Mechanism
Like somatostatin, octreotide suppresses secretion of pituitary growth hormone and thyrotropin and decreases release of pancreatic islet hormones including insulin, glucagon and vasoactive intestinal peptide; it also reduces splanchnic blood flow, gastric acid secretion, gastrointestinal motility and pancreatic exocrine function (Katz & Erstad, 1989). That breadth explains its indications — growth-hormone-producing tumours, hormone-secreting neuroendocrine tumours — and its off-label uses in variceal bleeding, chylothorax and hyperinsulinism, where the hormone-suppressing and blood-flow effects are exploited.
Approved uses and formulations
IUPHAR records octreotide's use for growth-hormone-producing tumours, pituitary tumours secreting thyroid-stimulating hormone, and nuclear-medicine imaging of somatostatin-receptor-expressing neuroendocrine tumours. In June 2020 the FDA approved an oral octreotide (Mycapssa) as long-term maintenance for acromegaly patients who had responded to and tolerated injectable octreotide or lanreotide, with an equivalent EMA approval in 2022. A once-monthly subcutaneous depot (CAM2029) has completed phase 3 in acromegaly (NCT04076462), and population pharmacokinetic modelling supports dosing it every four weeks with less daily fluctuation than immediate-release injections (Glatard et al., Clinical Pharmacokinetics 2025).
| Form | Cadence | Status |
|---|---|---|
| Immediate-release injection (subcutaneous / intravenous) | Multiple times daily | Approved since the late 1980s |
| Oral capsule (Mycapssa) | Daily | FDA June 2020; EMA 2022 — acromegaly maintenance |
| Subcutaneous depot (CAM2029) | Every 4 weeks | Phase 3 completed; observational study recruiting |
| Radiolabelled octreotide analogues | Diagnostic | Nuclear-medicine imaging of neuroendocrine tumours |
Off-label evidence: bleeding, chylothorax, hyperinsulinism
A meta-analysis of trials comparing somatostatin or octreotide with placebo or H2 antagonists in variceal bleeding found a significant efficacy advantage but no difference in mortality, and the reviewer concluded the two are at least as effective as other vasoactive treatments with fewer adverse effects (Burroughs, Gut 1994); one trial noted lower mortality than balloon tamponade (Cello & Chan, Digestion 1993). In neonates with congenital or postoperative chylothorax, octreotide is described as a promising approach to reducing drainage when conservative measures fail (Stajich & Ashworth, Neonatal Network 2006). In infants with hyperinsulinism, case reports show octreotide raising glucose sufficiently to avoid pancreatectomy, but the reviewer judged the data inconclusive owing to sample size and design (Barrons, Annals of Pharmacotherapy 1997).
Side effects
Octreotide's adverse effects follow from suppressing hormones broadly: reduced insulin and glucagon secretion, reduced gut motility and pancreatic exocrine output, and reduced growth indices in children (Barrons, 1997). Bradycardia has been reported, including a case of deleterious haemodynamic effects in a non-acromegalic patient, with the authors cautioning that few data exist in populations other than acromegaly (Herrington et al., Pharmacotherapy 1998). Gallstone formation and glucose disturbances are the label-level cautions; they are the prescriber's domain and are not detailed further here.
Octreotide vs lanreotide and pasireotide
Lanreotide is the other first-generation somatostatin analogue, also an octapeptide with D-amino acids, marketed mainly as a monthly depot; pasireotide is a second-generation analogue with broader receptor coverage. Octreotide remains the reference compound because of its record: it is the comparator in the oral and depot development programmes above, and radiolabelled octreotide derivatives underpin somatostatin-receptor imaging. Octreotide-derived delivery and diagnostic nanosystems are an active preclinical field (Fan et al., Journal of Drug Targeting 2023).
A note on veterinary and research use
Octreotide is also used off-label in veterinary medicine; a 2024 retrospective series described its use in 18 dogs with protein-losing enteropathy refractory to standard therapy, with adverse effects in 3 of 18 and clinical improvement in 6 of 12 evaluable dogs (Jablonski et al., Journal of Veterinary Internal Medicine 2024). Octreotide is a prescription medicine; it is not sold as a research peptide in the way growth-hormone secretagogues are. This profile is educational; it is not guidance on obtaining or using any product and it is not medical advice.
Sequence of the selected reference form
Sequence backbone for the reference form: Octreotide free peptide, threoninol terminus. Termini, stereochemistry and modifications are described below.
FCFWKTCX
F1 is D-Phe; W4 is D-Trp; X8 is threoninol (Thr-ol), not an ordinary threonine acid; disulfide Cys2-Cys7.. X marks a noncanonical residue; see the expanded sequence and reference chemistry below.
Analyze sequences in the playground →Structure & chemistry
Molecular identity & reference confidence
Source-supported reference
The selected reference is the cyclic D-Phe1/D-Trp4 octreotide parent with a threoninol terminus. The old CID lacks stereochemistry. The label’s free-peptide mass excludes variable acetate equivalents.
- Molecular form
- Octreotide free peptide, threoninol terminus
- Species
- Synthetic somatostatin analogue; no natural source species applies
- Termini (N / C)
- Free D-phenylalanyl amino terminus / L-threoninol (amino alcohol)
Average reference mass · Molecular identity assessment: 2026-10-05
Reference policy updated: 2026-10-05
- PubChem PUG REST selected parent properties · 2026-10-05
- PubChem selected-parent biologic notation · 2026-10-05
- PubChem selected-parent identifiers with depositor attribution · 2026-10-05
- NIH GSRS independently selected parent record · 2026-10-05
- Official product label chemical description, selected parent distinguished from formulation · 2026-10-05
H-D-Phe-Cys(1)-Phe-D-Trp-Lys-Thr-Cys(1)-Thr-ol
- Molecular formula
- C49H66N10O10S2
- Average reference mass
- ≈ 1,019.3
- Receptors
- Somatostatin receptors (SSTR), acting as a somatostatin mimetic
- Backbone
- Octreotide free peptide, threoninol terminus
- C-terminus
- L-threoninol (amino alcohol)
- Status
- Approved: injectable and depot forms (acromegaly, neuroendocrine tumours); oral octreotide (Mycapssa) FDA-approved June 2020, EMA 2022, for maintenance in acromegaly
- PubChem CID: 448601
- CAS RN: 83150-76-9
- UNII: RWM8CCW8GP
Chemistry values: curated profile, PubChem.
Clinical development snapshot
ClinicalTrials.gov lists 327 registered studies with “Octreotide” as an intervention (snapshot 2026-10-01). A registry footprint is not evidence of efficacy or approval.
| NCT | Title | Phase | Status | Updated |
|---|---|---|---|---|
| NCT00569127 | Octreotide Acetate and Recombinant Interferon Alfa-2b or Bevacizumab in Treating Patients With Metastatic or L | Phase 3 | active not recruiting | 2026-10-01 |
| NCT02019706 | Prospective Evaluation of 68Ga-DOTATATE PET/CT, Octreotide and F-DOPA PET Imaging in Ectopic Cushing Syndrome | Phase 2 | recruiting | 2026-09-28 |
| NCT07583563 | An Observational Study of Octreotide Subcutaneous Depot in Patients With Acromegaly | — | recruiting | 2026-09-25 |
| NCT06441331 | Phase I Trial to Determine the Dose and Evaluate the PK and Safety of Lutetium Lu 177 Edotreotide Therapy in P | Phase 1 | recruiting | 2026-09-25 |
| NCT07842172 | Somatostatin Analogues vs. Observation After Peptide Receptor Radionuclide Therapy (PRRT) in Nonfunctional Neu | Phase 3 | not yet recruiting | 2026-09-25 |
| NCT06930625 | A Study to Assess the Efficacy and Safety of Debio 4126 in Participants With Acromegaly Previously Treated Wit | Phase 3 | recruiting | 2026-09-22 |
Octreotide — 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: Octreotide free peptide, threoninol terminusAverage reference mass: 1,019.3 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.
Change log
Dated observations from the data pipeline (registry flags, trial footprints, identifiers) and editorial reviews of this profile.
- Trials2 registered studies added on ClinicalTrials.gov (now 327).
- EditorialProfile content reviewed and updated by the editorial team.
FAQ about Octreotide
What is Octreotide?+
Octreotide is a cyclic eight-amino-acid synthetic analogue of somatostatin (C49H66N10O10S2, ≈1,019 Da) with a D-phenylalanine at position 1, a D-tryptophan at position 4 and a disulfide bridge between its two cysteines. It suppresses growth hormone, thyrotropin and a range of pancreatic and gut hormones. Approved for acromegaly, TSH-secreting pituitary tumours and neuroendocrine tumours, it is available as injection, long-acting depot and — since 2020 — an oral capsule, and radiolabelled forms image somatostatin-receptor-positive tumours.
What Canadian product status is recorded for Octreotide?+
Canadian product status for Octreotide 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 length of the selected reference form for Octreotide?+
The selected reference form (Octreotide free peptide, threoninol terminus) has 8 residues or residue-derived units in its backbone. Other forms in this family may have a different length.
What is octreotide?+
A synthetic cyclic octapeptide analogue of somatostatin that suppresses growth hormone and gut-hormone secretion. It is approved for acromegaly, TSH-secreting pituitary tumours and neuroendocrine tumours.
What is octreotide's structure?+
Eight backbone positions (FCFWKTCX), where X8 is threoninol, in a ring closed by a Cys–Cys disulfide, with D-Phe at position 1 and D-Trp at position 4. Formula C49H66N10O10S2, mass about 1,019 Da.
Is there an oral octreotide?+
Yes. Mycapssa was approved by the FDA in June 2020 and the EMA in 2022 as maintenance treatment for acromegaly in patients who responded to injectable octreotide or lanreotide.
Octreotide vs lanreotide?+
Both are first-generation somatostatin analogues; lanreotide is usually given as a monthly depot, while octreotide comes as injection, oral capsule and a four-weekly depot in development.
What are octreotide's side effects?+
Effects of broad hormone suppression — glucose changes, reduced gut motility and pancreatic secretion, gallstones — plus reported bradycardia, particularly outside acromegaly.
Is octreotide used for bleeding?+
Off-label, yes: meta-analysis supports efficacy in variceal bleeding comparable to other vasoactive agents with fewer adverse effects, without a mortality difference.
Further reading
- PK conceptsWhy Peptides Have Short Half-Lives (And How Engineers Fix It)Proteases, renal clearance, DPP-4, PEGylation, lipidation, cyclization—educational guide to peptide pharmacokinetics concepts.
- PharmacologyGLP-1 and Incretin Peptide Half-Lives Compared: From 2 Minutes to 8 DaysA sourced table of the plasma half-lives of native GLP-1, exenatide, liraglutide, dulaglutide, semaglutide, tirzepatide, retatrutide, cagrilintide and the newer co-agonists — and the three engineering strategies (DPP-4 resistance, albumin binding, Fc fusion) that stretch minutes into a week.
- Lab practicePeptide Storage & Stability: Lyophilized vs In SolutionEducational guide to storing research peptides—temperature, moisture, freeze-thaw, light, and why lyophilized powders differ from solutions.
- FoundationsWhat Are Research Peptides? A Clear Educational GuideLearn what “research peptides” means, how they differ from approved peptide drugs, quality markers (COA, purity), and how to study them responsibly.
Related peptides
References & further reading
- 1.Stajich et al. (2006). Octreotide. Neonatal Netw
- 2.Jablonski et al. (2024). Use of octreotide for the treatment of protein-losing enteropathy in dogs: Retrospective study of 18 cases. J Vet Intern Med
- 3.Barrons (1997). Octreotide in hyperinsulinism. Ann Pharmacother
- 4.Fan et al. (2023). Octreotide and Octreotide-derived delivery systems. J Drug Target
- 5.Burroughs (1994). Octreotide in variceal bleeding. Gut
- 6.Glatard et al. (2025). Population Pharmacokinetic Analysis of an Octreotide Depot (CAM2029) in the Treatment of Acromegaly. Clin Pharmacokinet
- 7.Katz et al. (1989). Octreotide, a new somatostatin analogue. Clin Pharm
- 8.Cello et al. (1993). Octreotide therapy for variceal hemorrhage. Digestion
- 9.Herrington AM et al. (1998). Octreotide-induced bradycardia. Pharmacotherapy