Evidence Grade A — Regulatory approved. 9240 published studies. 237 registered clinical trials.
Medically reviewed by a licensed medical professional
Loading...
Octreotide is a medication that mimics somatostatin — a natural hormone that acts as a brake on many other hormones in the body. It is used for conditions caused by hormone overproduction, including acromegaly (excess growth hormone) and hormone-secreting neuroendocrine tumours. Available as a short-acting injection (Sandostatin), a monthly depot (Sandostatin LAR), and the first-ever oral somatostatin tablet (Mycapssa), it has one of the longest track records of any peptide medication — over 35 years.
Octreotide is also known by these brand and alternate names:
9,240 published studies: 6928 human, 945 animal, 816 in-vitro, 1667 reviews
Octreotide is marketed as Sandostatin (approved 1988), Sandostatin LAR monthly depot (approved 1998), and Mycapssa oral capsules (approved June 2020 — the first oral somatostatin analogue). It is used for acromegaly, carcinoid syndrome, VIPomas, and gastroenteropancreatic neuroendocrine tumours (GEP-NETs).
The PROMID trial demonstrated that octreotide LAR significantly delayed tumour progression in patients with neuroendocrine tumours of the midgut, establishing somatostatin analogues as a standard treatment for these cancers. The approval of Mycapssa as an oral formulation was a significant advance for patients who had been receiving monthly injections for years. Octreotide has been on the market for over 35 years and has one of the longest safety track records of any peptide medication.
Your body produces somatostatin as a natural 'off switch' for many hormones — it tells the pituitary gland to stop releasing growth hormone, tells the gut to slow hormone secretion, and reduces blood flow to the digestive organs. Octreotide mimics this effect but lasts much longer than the natural hormone (hours rather than minutes). It is particularly effective at suppressing growth hormone in acromegaly and reducing hormone secretion from neuroendocrine tumours, which relieves symptoms like severe flushing and diarrhoea.
Octreotide's evidence base is extensive. The PROMID trial demonstrated that monthly octreotide LAR significantly delayed tumour progression in patients with neuroendocrine tumours of the midgut, establishing somatostatin analogues as a standard first-line treatment for these cancers. For acromegaly, octreotide normalises growth hormone levels in approximately 50-65% of patients. The approval of Mycapssa (oral octreotide capsules) in 2020 was a significant advance for patients who had been receiving monthly injections for years, though the oral form is currently approved only for acromegaly patients already stable on injectable octreotide. Key limitations include gallstone formation (affecting up to 63% of long-term users) and blood sugar elevation. Lanreotide (Somatuline Depot) is considered clinically equivalent and offers home self-injection.
PeptideTrace tracks 237 registered clinical trials for Octreotide sourced from ClinicalTrials.gov.
Vatalanib and Octreotide in Treating Patients With Progressive Neuroendocrine Tumors
A Multicenter Placebo-Controlled Dose Titration Study to Evaluate the Efficacy and Safety of Sandostatin (SMS 201-995) in the Treatment of Patients With Acquired Immunodeficiency Related Diarrhea
A Multicenter Placebo-Controlled Double Blind Study to Evaluate the Efficacy and Safety of Sandostatin ( SMS 201-995 ) in Patients With Acquired Immunodeficiency Related Diarrhea Who Were Either "Responders" or "Non-Responders" in a Prior Placebo-Controlled Double-Blind Sandostatin Study.
Single Dose Pharmacodynamic and Pharmacokinetic Study of DG3173
Intranasal Delivery of Octreotide for Treatment of Diabetic Macular Edema
FDA ORIG 1
FDA SUPPL 1
FDA SUPPL 2
FDA SUPPL 3
FDA SUPPL 4
FDA SUPPL 5
FDA SUPPL 7
Health Canada Market Authorisation
FDA SUPPL 10
FDA SUPPL 6
FDA SUPPL 15
FDA ORIG 1
FDA ORIG 1
FDA SUPPL 19
FDA SUPPL 18
FDA SUPPL 21
FDA SUPPL 23
FDA ORIG 1
FDA SUPPL 1
FDA SUPPL 25
FDA SUPPL 2
FDA SUPPL 13
FDA SUPPL 11
FDA SUPPL 5
FDA SUPPL 27
FDA SUPPL 3
FDA ORIG 1
FDA SUPPL 29
FDA SUPPL 28
FDA SUPPL 30
FDA SUPPL 32
FDA SUPPL 33
FDA SUPPL 34
FDA SUPPL 35
FDA SUPPL 25
FDA SUPPL 5
FDA SUPPL 6
FDA SUPPL 2
FDA SUPPL 8
FDA SUPPL 6
FDA SUPPL 36
FDA SUPPL 43
FDA SUPPL 5
FDA SUPPL 7
FDA SUPPL 28
FDA ORIG 1
FDA SUPPL 41
FDA SUPPL 46
FDA SUPPL 10
FDA SUPPL 13
FDA SUPPL 11
FDA SUPPL 16
FDA SUPPL 14
FDA SUPPL 9
FDA SUPPL 13
FDA SUPPL 32
FDA SUPPL 35
FDA SUPPL 33
FDA ORIG 1
FDA SUPPL 47
FDA ORIG 1
FDA SUPPL 6
FDA SUPPL 49
FDA SUPPL 21
FDA SUPPL 18
FDA ORIG 1
EMA Marketing Authorisation
FDA ORIG 1
Octreotide is a synthetic cyclic octapeptide (8 amino acids) somatostatin analogue that retains the critical pharmacophore (Phe-Trp-Lys-Thr) of native somatostatin-14. Its half-life of 1.5–2 hours (versus ~3 minutes for native somatostatin) enables therapeutic use. Available as immediate-release SC injection, long-acting IM depot (LAR), and oral capsules.
Octreotide binds with high affinity to somatostatin receptors SST2 and SST5 (with lower affinity for SST3). Activation of these Gi-coupled receptors inhibits secretion of growth hormone, glucagon, insulin, gastrin, vasoactive intestinal peptide (VIP), secretin, and other GI/pancreatic hormones. It also exerts antiproliferative effects on neuroendocrine tumor cells via cell cycle arrest and apoptosis induction.
Octreotide is marketed as Sandostatin (SC, approved 1988), Sandostatin LAR (IM depot, approved November 1998, monthly), and Mycapssa (oral capsules using TPE technology, approved June 26, 2020—the first oral somatostatin analogue). Indications include acromegaly, carcinoid syndrome/VIPomas, and GEP-NETs. The PROMID trial demonstrated octreotide LAR significantly prolonged median PFS in midgut NETs (14.3 months vs 6.0 months placebo; HR 0.34; P<0.001). In acromegaly, GH normalization is achieved in 39–75% and IGF-1 normalization in 55–88%. Biliary abnormalities occur in approximately 63% of patients.
Linaclotide is marketed as Linzess (approved August 2012). It is taken as a daily oral capsule on an empty stomach, at least 30 minutes before the first meal. The recommended dose is 290 mcg for IBS-C and 72 or 145 mcg for chronic constipation. In clinical trials, approximately 34% of IBS-C patients met the composite improvement endpoint compared to 17% on placebo. Diarrhoea is the most common side effect (approximately 20%) and the leading reason for discontinuation. Linaclotide has a boxed warning against use in children under 6 years due to deaths in young mice, though no such events have been reported in humans. It competes with plecanatide (which targets the same pathway) and other IBS-C treatments.
Elamipretide (Forzinity) was approved by the FDA for Barth syndrome based on the TAZPOWER trial. The randomised crossover phase (12 patients) did not meet its primary endpoints, but the open-label extension (168 weeks) demonstrated durable improvements in walking distance and muscle strength that formed the basis for approval. Barth syndrome affects approximately 1 in 300,000–400,000 births. A larger Phase III trial in primary mitochondrial myopathy (218 patients, MMPOWER-3) did not meet its primary endpoint, and the drug was not approved for that broader indication. Elamipretide remains approved exclusively for Barth syndrome. See also SS-31 (#158) for the research compound context.
Glucagon has been available as an emergency injection since the 1960s and remains the standard rescue treatment for severe hypoglycaemia. Recent innovation has focused on making it easier to administer in emergencies. Baqsimi, approved in 2019, was the first needle-free option as a nasal powder. Gvoke, also approved in 2019, eliminated the need to mix and reconstitute the medication before injection — a significant advance since severe hypoglycaemia often impairs the ability to follow complex preparation steps. Dasiglucagon (Zegalogue), a next-generation stable liquid glucagon approved in 2021, further improved on the convenience of rescue administration. Beyond emergency rescue, glucagon's receptor is now a major research target — dual and triple agonists combining glucagon receptor activity with GLP-1 (such as survodutide and retatrutide) are in advanced clinical trials for obesity and metabolic disease.
Evidence Reviews
Timelines
Regulatory Status
Deep Dives
This content is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional before making decisions about your health.
