Octreotide

What is octreotide?

Octreotide is a synthetic peptide that mimics somatostatin, a natural inhibitory hormone. It is a regulator-approved prescription medicine, first approved by the FDA in 1988 (Sandostatin), and is given as an injection, a long-acting depot or — in the US — an oral capsule.

Identity

Octreotide belongs to the same class as lanreotide and pasireotide, which are different molecules with different receptor profiles. It should not be confused with native somatostatin (14 or 28 amino acids, short half-life), or with radiopharmaceuticals built on the octreotide scaffold — edotreotide (DOTATOC), oxodotreotide (DOTATATE; 177Lu-dotatate is Lutathera), 111In-pentetreotide (OctreoScan) and 68Ga-DOTATATE — which are separate medicines or diagnostics.

How it works

Octreotide binds mainly to somatostatin receptor 2 (SSTR2) and also SSTR5. Through these receptors it lowers growth hormone and IGF-1 in acromegaly and reduces hormone secretion from neuroendocrine tumours, which eases diarrhoea and flushing. The oral capsule (Mycapssa) uses a permeation enhancer; octreotide is not an ordinary orally absorbed peptide.

Approved uses and evidence

• Acromegaly: approved for patients with an inadequate response to, or who cannot be treated with, surgery, radiation and bromocriptine (Sandostatin, Bynfezia labels). Mycapssa is approved for long-term maintenance in patients who have responded to and tolerated octreotide or lanreotide.
• Metastatic carcinoid tumours: symptomatic treatment of severe diarrhoea and flushing (labels).
• VIPoma: treatment of watery diarrhoea (labels).

Sandostatin LAR Depot has the same three indications for patients who have responded to and tolerated subcutaneous Sandostatin.

Oral octreotide in acromegaly

• In a phase 3 open-label trial after switching from injectable somatostatin analogues, 65% of evaluable patients (n=151) maintained response at the end of the core period (Melmed 2015).
• In the placebo-controlled CHIASMA OPTIMAL trial, IGF-1 normalisation was maintained in 58.2% with oral octreotide versus 19.4% with placebo (Samson 2020).
• In MPOWERED, oral octreotide was non-inferior to injectable somatostatin receptor ligands (maintained response 91% vs 100%; the −20% non-inferiority margin was met) (Fleseriu 2022), with an open-label extension reported in 2023 (Fleseriu 2023).

The EU central authorisation of Mycapssa (December 2022) was withdrawn at the holder's request on 26 February 2025; this page does not speculate about the reason.

Neuroendocrine tumours

In the randomised PROMID trial in metastatic midgut neuroendocrine tumours, octreotide LAR prolonged median time to progression to 14.3 months versus 6 months with placebo (hazard ratio 0.34) (Rinke 2009). The overall-survival analysis was not confirmatory because there were few deaths; long-term survival was reported separately (Rinke 2017). Tumour control is not an indication in the US label; whether national European product information (including the Swedish SmPC) lists it has not been verified here. In NETTER-1, high-dose octreotide LAR was the active comparator for 177Lu-dotatate (Strosberg 2017) — that trial is about the radioligand, not a claim for octreotide.

Warnings and precautions

Current FDA labels carry no boxed warning. The labels list:

• Gallstones and biliary sludge.
• High or low blood glucose (hyperglycaemia and hypoglycaemia).
• Thyroid function: hypothyroidism.
• Heart: bradycardia, arrhythmias and conduction abnormalities.
• Steatorrhoea and fat malabsorption.
• Altered vitamin B12 levels.

For Mycapssa, proton-pump inhibitors, H2 blockers and antacids can reduce absorption, and the label lists interactions with medicines such as ciclosporin, digoxin and antidiabetic drugs; details are only in the label.

Off-label use and misuse

• Variceal bleeding: a Cochrane review of somatostatin and octreotide in acute variceal bleeding found an effect roughly equivalent to one unit of blood saved per patient, called the treatment "of doubtful value", and found a wide confidence interval for mortality (Gøtzsche 2000). This is an older review and later guidance may differ; no protocol is given here.
• "Fat-burning" or "anti-GH" use: vendor and forum claims that octreotide is a weight-loss peptide are not supported by any randomised trial.

Grey-market octreotide has not been analytically studied; approved products are the reference point.

Dosing

No dose is given here. Doses, intervals and formulations depend on the product and indication and are defined only by the official prescribing information — see the Sandostatin FDA label on DailyMed (opens in a new tab) and the other labels in the references.

Claims vs evidence

Related pages

Tesamorelin, Sermorelin, CJC-1295 (growth-hormone axis, opposite direction).