Octreotide, sold under the brand name Sandostatin among others, is an octa

peptide Peptides are short chains of amino acids linked by peptide bonds. A polypeptide is a longer, continuous, unbranched peptide chain. Polypeptides that have a molecular mass of 10,000 Da or more are called proteins. Chains of fewer than twenty am ...

that mimics natural

somatostatin Somatostatin, also known as growth hormone-inhibiting hormone (GHIH) or by #Nomenclature, several other names, is a peptide hormone that regulates the endocrine system and affects neurotransmission and cell proliferation via interaction with G ...

pharmacologically, though it is a more potent inhibitor of

growth hormone Growth hormone (GH) or somatotropin, also known as human growth hormone (hGH or HGH) in its human form, is a peptide hormone that stimulates growth, cell reproduction, and cell regeneration in humans and other animals. It is thus important in ...

glucagon Glucagon is a peptide hormone, produced by alpha cells of the pancreas. It raises the concentration of glucose and fatty acids in the bloodstream and is considered to be the main catabolic hormone of the body. It is also used as a Glucagon (medic ...

, and

insulin Insulin (, from Latin ''insula'', 'island') is a peptide hormone produced by beta cells of the pancreatic islets encoded in humans by the insulin (''INS)'' gene. It is the main Anabolism, anabolic hormone of the body. It regulates the metabol ...

than the natural hormone. It was first synthesized in 1979 and binds predominantly to the somatostatin receptors SSTR2 and SSTR5. It was approved for use in the United States in 1988. Octreotide was approved for medical use in the European Union in 2022. , octreotide is the first oral somatostatin analog (SSA) approved by the FDA. It is on the

World Health Organization's List of Essential Medicines The WHO Model List of Essential Medicines (aka Essential Medicines List or EML), published by the World Health Organization (WHO), contains the medications considered to be most effective and safe to meet the most important needs in a health s ...

Medical uses

Tumors

Octreotide is used for the treatment of

producing tumors (

acromegaly Acromegaly is a disorder that results in excess growth of certain parts of the human body. It is caused by excess growth hormone (GH) after the growth plates have closed. The initial symptom is typically enlargement of the hands and feet. There ...

and

gigantism Gigantism (, ''gígas'', "wiktionary:giant, giant", plural γίγαντες, ''gígantes''), also known as giantism, is a condition characterized by excessive growth and height significantly above average height, average. In humans, this conditi ...

), when surgery is contraindicated, pituitary tumors that secrete thyroid-stimulating hormone (thyrotropinoma),

diarrhea Diarrhea (American English), also spelled diarrhoea or diarrhœa (British English), is the condition of having at least three loose, liquid, or watery bowel movements in a day. It often lasts for a few days and can result in dehydration d ...

and flushing episodes associated with

carcinoid syndrome Carcinoid syndrome is a paraneoplastic syndrome comprising the signs and symptoms that occur secondary to neuroendocrine tumors (formerly known as carcinoid tumors). The syndrome is caused by neuroendocrine tumors most often found in the gut ...

, and diarrhea in people with

vasoactive intestinal peptide Vasoactive intestinal peptide, also known as vasoactive intestinal polypeptide or VIP, is a peptide hormone that is vasoactive in the intestine. VIP is a peptide of 28 amino acid residue (chemistry), residues that belongs to a Secretin family, glu ...

-secreting tumors ( VIPomas). Octreotide is also used in mild cases of glucagonoma when surgery is not an option.

Bleeding esophageal varices

Octreotide is often given as an infusion for management of acute

hemorrhage Bleeding, hemorrhage, haemorrhage or blood loss, is blood escaping from the circulatory system from damaged blood vessels. Bleeding can occur internally, or externally either through a natural opening such as the mouth, nose, ear, urethra, ...

from

esophageal varices Esophageal varices are extremely Vasodilation, dilated sub-mucosal veins in the lower third of the esophagus. They are most often a consequence of portal hypertension, commonly due to cirrhosis. People with esophageal varices have a strong tendenc ...

in liver

cirrhosis Cirrhosis, also known as liver cirrhosis or hepatic cirrhosis, chronic liver failure or chronic hepatic failure and end-stage liver disease, is a chronic condition of the liver in which the normal functioning tissue, or parenchyma, is replaced ...

on the basis that it reduces portal venous pressure, though current evidence suggests that this effect is transient and does not improve survival.

Radiolabeling

Octreotide is used in nuclear medicine imaging by labeling with indium-111 (Octreoscan) to noninvasively image neuroendocrine and other tumours expressing somatostatin receptors. It has been radiolabeled with

carbon-11 Carbon (6C) has 14 known isotopes, from to as well as , of which only and are stable nuclide, stable. The longest-lived radionuclide, radioisotope is , with a half-life of years. This is also the only carbon radioisotope found in nature, as ...

as well as

gallium-68 Natural gallium (31Ga) consists of a mixture of two stable Isotope, isotopes: gallium-69 and gallium-71. Twenty-nine radioisotopes are known, all synthetic, with atomic masses ranging from 60 to 89; along with three nuclear isomer, nuclear isomer ...

(using edotreotide), enabling imaging with

positron emission tomography Positron emission tomography (PET) is a functional imaging technique that uses radioactive substances known as radiotracers to visualize and measure changes in metabolic processes, and in other physiological activities including blood flow, r ...

(PET).

Acromegaly

In June 2020, octreotide (Mycapssa) was approved for medical use in the United States with an indication for the long-term maintenance treatment in acromegaly patients who have responded to and tolerated treatment with octreotide or lanreotide. Mycapssa is the first oral somatostatin analog (SSA) approved by the FDA.

Hypoglycemia

Octreotide is also used in the treatment of refractory hypoglycemia or congenital hyperinsulinism in neonates and sulphonylurea-induced hypoglycemia in adults.

Contraindications

Octreotide has not been adequately studied for the treatment of children as well as pregnant and lactating women. The medication is given to these groups only if a risk-benefit analysis is positive.

Adverse effects

The most common adverse effects are headache,

hypothyroidism Hypothyroidism is an endocrine disease in which the thyroid gland does not produce enough thyroid hormones. It can cause a number of symptoms, such as cold intolerance, poor ability to tolerate cold, fatigue, extreme fatigue, muscle aches, co ...

, cardiac conduction changes,

gastrointestinal The gastrointestinal tract (GI tract, digestive tract, alimentary canal) is the tract or passageway of the digestive system that leads from the mouth to the anus. The tract is the largest of the body's systems, after the cardiovascular system. ...

reactions (including cramps, nausea/vomiting and diarrhoea or constipation),

gallstone A gallstone is a stone formed within the gallbladder from precipitated bile components. The term cholelithiasis may refer to the presence of gallstones or to any disease caused by gallstones, and choledocholithiasis refers to the presence of ...

s, reduction of

release,

hyperglycemia Hyperglycemia is a condition where unusually high amount of glucose is present in blood. It is defined as blood glucose level exceeding 6.9 mmol/L (125 mg/dL) after fasting for 8 hours or 10 mmol/L (180 mg/dL) 2 hours after eating. Blood gluc ...

or sometimes

hypoglycemia Hypoglycemia (American English), also spelled hypoglycaemia or hypoglycæmia (British English), sometimes called low blood sugar, is a fall in blood sugar to levels below normal, typically below 70 mg/dL (3.9 mmol/L). Whipple's tria ...

, and (usually transient) injection site reactions. Slow heart rate, skin reactions such as

pruritus An itch (also known as pruritus) is a sensation that causes a strong desire or reflex to scratch. Itches have resisted many attempts to be classified as any one type of sensory experience. Itches have many similarities to pain, and while both ...

, hyperbilirubinemia,

dizziness Dizziness is an imprecise term that can refer to a sense of disorientation in space, vertigo, or lightheadedness. It can also refer to Balance disorder, disequilibrium or a non-specific feeling, such as giddiness or foolishness. Dizziness is a ...

and dyspnoea are also fairly common (more than 1%). Rare side effects include acute anaphylactic reactions,

pancreatitis Pancreatitis is a condition characterized by inflammation of the pancreas. The pancreas is a large organ behind the stomach that produces digestive enzymes and a number of hormone A hormone (from the Ancient Greek, Greek participle , "se ...

and

hepatitis Hepatitis is inflammation of the liver parenchyma, liver tissue. Some people or animals with hepatitis have no symptoms, whereas others develop yellow discoloration of the skin and whites of the eyes (jaundice), Anorexia (symptom), poor appetite ...

. Some studies reported

alopecia Hair loss, also known as alopecia or baldness, refers to a loss of hair from part of the head or body. Typically at least the head is involved. The severity of hair loss can vary from a small area to the entire body. Inflammation or scarring ...

in those who were treated by octreotide. Rats which were treated by octreotide experienced

erectile dysfunction Erectile dysfunction (ED), also referred to as impotence, is a form of sexual dysfunction in males characterized by the persistent or recurring inability to achieve or maintain a Human penis, penile erection with sufficient rigidity and durat ...

in a 1998 study. A prolonged

QT interval The QT interval is a measurement made on an Electrocardiography, electrocardiogram used to assess some of the electrical properties of the heart. It is calculated as the time from the start of the QRS complex, Q wave to the end of the T wave, an ...

has been observed, but it is uncertain whether this is a reaction to the medication or the result of an existing illness.

Interactions

Octreotide can reduce the intestinal reabsorption of

ciclosporin Ciclosporin, also spelled cyclosporine and cyclosporin, is a calcineurin inhibitor, used as an immunosuppressant medication. It is taken Oral administration, orally or intravenously for rheumatoid arthritis, psoriasis, Crohn's disease, nephr ...

, possibly making it necessary to increase the dose. People with

diabetes mellitus Diabetes mellitus, commonly known as diabetes, is a group of common endocrine diseases characterized by sustained hyperglycemia, high blood sugar levels. Diabetes is due to either the pancreas not producing enough of the hormone insulin, or th ...

might need less

or oral antidiabetics when treated with octreotide, as it inhibits glucagon secretion more strongly and for a longer time span than insulin secretion. The

bioavailability In pharmacology, bioavailability is a subcategory of absorption and is the fraction (%) of an administered drug that reaches the systemic circulation. By definition, when a medication is administered intravenously, its bioavailability is 100%. H ...

of bromocriptine is increased; besides being an antiparkinsonian, bromocriptine is also used for the treatment of acromegaly.

Pharmacology

Since octreotide resembles somatostatin in physiological activities, it can: * inhibit secretion of many hormones, such as

gastrin Gastrin is a peptide hormone that stimulates secretion of gastric acid (HCl) by the parietal cells of the stomach and aids in gastric motility. It is released by G cells in the pyloric antrum of the stomach, duodenum, and the pancreas. ...

cholecystokinin Cholecystokinin (CCK or CCK-PZ; from Greek ''chole'', "bile"; ''cysto'', "sac"; ''kinin'', "move"; hence, ''move the bile-sac (gallbladder)'') is a peptide hormone of the gastrointestinal system responsible for stimulating the digestion of fat a ...

secretin Secretin is a hormone that regulates water homeostasis throughout the body and influences the environment of the duodenum by regulating secretions in the stomach, pancreas, and liver. It is a peptide hormone produced in the S cells of the duodenum ...

, pancreatic polypeptide, TSH, and

, * reduce secretion of fluids by the intestine and

pancreas The pancreas (plural pancreases, or pancreata) is an Organ (anatomy), organ of the Digestion, digestive system and endocrine system of vertebrates. In humans, it is located in the abdominal cavity, abdomen behind the stomach and functions as a ...

, * reduce gastrointestinal motility and inhibit contraction of the

gallbladder In vertebrates, the gallbladder, also known as the cholecyst, is a small hollow Organ (anatomy), organ where bile is stored and concentrated before it is released into the small intestine. In humans, the pear-shaped gallbladder lies beneath t ...

, * inhibit the action of certain hormones from the

anterior pituitary The anterior pituitary (also called the adenohypophysis or pars anterior) is a major Organ (anatomy), organ of the endocrine system. The anterior pituitary is the glandular, Anatomical terms of location#Usage in human anatomy, anterior lobe that t ...

, * cause

vasoconstriction Vasoconstriction is the narrowing of the blood vessels resulting from contraction of the muscular wall of the vessels, in particular the large arteries and small arterioles. The process is the opposite of vasodilation, the widening of blood vesse ...

in the blood vessels, and * reduce portal vessel pressures in bleeding varices. It has also been shown to produce

analgesic An analgesic drug, also called simply an analgesic, antalgic, pain reliever, or painkiller, is any member of the group of drugs used for pain management. Analgesics are conceptually distinct from anesthetics, which temporarily reduce, and in s ...

effects, most probably acting as a

partial agonist In pharmacology, partial agonists are drugs that bind to and activate a given Receptor (biochemistry), receptor, but have only partial Intrinsic activity, efficacy at the receptor relative to a full agonist. They may also be considered Ligand (bio ...

at the mu opioid receptor.

Pharmacokinetics

Octreotide is absorbed quickly and completely after subcutaneous application. Maximal plasma concentration is reached after 30 minutes. The

elimination half-life Biological half-life (elimination half-life, pharmacological half-life) is the time taken for concentration of a biological substance (such as a medication) to decrease from its maximum concentration ( Cmax) to half of Cmax in the blood plasma. ...

is 100 minutes (1.7 hours) on average when applied subcutaneously; after

intravenous injection Intravenous therapy (abbreviated as IV therapy) is a medical technique that administers fluids, medications and nutrients directly into a person's vein. The intravenous route of administration is commonly used for rehydration or to provide nutr ...

, the substance is eliminated in two phases with half-lives of 10 and 90 minutes, respectively.

History

Octreotide acetate was approved for use in the United States in 1988. In January 2020, approval of octreotide acetate in the United States was granted to Sun Pharmaceutical under the brand name Bynfezia Pen for the treatment of: * the reduction of

and

insulin-like growth factor 1 Insulin-like growth factor 1 (IGF-1), also called somatomedin C, is a hormone similar in tertiary structure, molecular structure to insulin which plays an important role in childhood growth, and has Anabolism, anabolic effects in adults. In the ...

(somatomedin C) in adults with

who have had inadequate response to or cannot be treated with surgical resection, pituitary irradiation, and bromocriptine mesylate at maximally tolerated doses * severe diarrhea/flushing episodes associated with metastatic carcinoid tumors in adults * profuse watery diarrhea associated with vasoactive intestinal peptide tumors (VIPomas) in adults

Society and culture

Legal status

In September 2022, the

Committee for Medicinal Products for Human Use The Committee for Medicinal Products for Human Use (CHMP), formerly known as the Committee for Proprietary Medicinal Products (CPMP), is the European Medicines Agency's committee responsible for elaborating the agency's opinions on all issues regar ...

(CHMP) of the

European Medicines Agency The European Medicines Agency (EMA) is an agency of the European Union (EU) in charge of the evaluation and supervision of pharmaceutical products. Prior to 2004, it was known as the European Agency for the Evaluation of Medicinal Products ...

adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Mycapssa, intended for the treatment of adults with acromegaly. The applicant for this medicinal product is Amryt Pharmaceuticals DAC. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged. Mycapssa was approved for medical use in the European Union in December 2022. In April 2025, the CHMP adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Oczyesa, intended for the maintenance treatment of adults with acromegaly. The applicant for this medicinal product is Camurus AB. Oczyesa is a hybrid medicine of Sandostatin, which has been authorized in the EU since November 1988. Oczyesa contains the same active substance as Sandostatin but as a different salt and is available at a higher strength and in a different pharmaceutical form. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.

Research

Octreotide has also been used

off-label Off-label use is the use of pharmaceutical drugs for an unapproved indication (medicine), indication or in an unapproved age group, dose (biochemistry), dosage, or route of administration. Both prescription drugs and over-the-counter drugs (OTCs) ca ...

for the treatment of severe, refractory diarrhea from other causes. It is used in toxicology for the treatment of prolonged recurrent hypoglycemia after

sulfonylurea Sulfonylureas or sulphonylureas are a class of organic compounds used in medicine and agriculture. The functional group consists of a sulfonyl group (-S(=O)2) with its sulphur atom bonded to a nitrogen atom of a ureylene group (N,N-dehydrourea ...

and possibly meglitinide overdose. It has also been used with varying degrees of success in infants with nesidioblastosis to help decrease insulin hypersecretion. Several clinical trials have demonstrated the effect of octreotide as acute treatment (abortive agent) in

cluster headache Cluster headache is a neurological disorder characterized by recurrent severe headaches on one side of the head, typically around the eye, eye(s). There is often accompanying eye watering, nasal congestion, or swelling around the eye on the aff ...

, where it has been shown that administration of subcutaneous octreotide is effective when compared with placebo. Octreotide has also been investigated in people with pain from chronic pancreatitis. It has been used in the treatment of malignant bowel obstruction. Octreotide may be used in conjunction with

midodrine Midodrine, sold under the brand names ProAmatine and Orvaten among others, is an antihypotensive medication used to treat orthostatic hypotension (low blood pressure when standing) and urinary incontinence. It is taken oral administration, by m ...

to partially reverse peripheral vasodilation in the

hepatorenal syndrome Hepatorenal syndrome (HRS) is a life-threatening medical condition that consists of acute kidney failure, rapid deterioration in kidney function in individuals with cirrhosis or fulminant liver failure. HRS is usually fatal unless a liver transp ...

. By increasing systemic vascular resistance, these medications reduce shunting and improve renal perfusion, prolonging survival until definitive treatment with liver transplant. Similarly, octreotide can be used to treat refractory chronic hypotension. While successful treatment has been demonstrated in case reports, larger studies have failed to demonstrate efficacy in treating

chylothorax A chylothorax is an abnormal accumulation of chyle, a type of lipid-rich lymph, in the pleural space surrounding the lung. The lymphatic vessels of the digestive system normally return lipids absorbed from the small bowel via the thoracic duct, ...

. A small study has shown that octreotide may be effective in the treatment of idiopathic intracranial hypertension.

Obesity

Octreotide has been used experimentally to treat

obesity Obesity is a medical condition, considered by multiple organizations to be a disease, in which excess Adipose tissue, body fat has accumulated to such an extent that it can potentially have negative effects on health. People are classifi ...

, particularly obesity caused by lesions in the hunger and satiety centers of the

hypothalamus The hypothalamus (: hypothalami; ) is a small part of the vertebrate brain that contains a number of nucleus (neuroanatomy), nuclei with a variety of functions. One of the most important functions is to link the nervous system to the endocrin ...

, a region of the brain central to the regulation of food intake and energy expenditure. The circuit begins with an area of the hypothalamus, the

arcuate nucleus The arcuate nucleus of the hypothalamus (ARH), or ARC, is also known as the infundibular nucleus to distinguish it from the arcuate nucleus of the medulla oblongata in the brainstem. The arcuate nucleus is an aggregation of neurons in the medio ...

, that has outputs to the

lateral hypothalamus The lateral hypothalamus (LH), also called the lateral hypothalamic area (LHA), contains the primary orexinergic nucleus within the hypothalamus that widely projects throughout the nervous system; this system of neurons mediates an array of cogni ...

(LH) and ventromedial hypothalamus (VMH), the brain's feeding and satiety centers, respectively. The ventromedial hypothalamus is sometimes injured by ongoing treatment for

acute lymphoblastic leukemia Acute lymphoblastic leukemia (ALL) is a cancer of the Lymphocyte, lymphoid line of blood cells characterized by the development of large numbers of lymphoblast, immature lymphocytes. Symptoms may include feeling tired, pale skin color, fever, ...

or surgery or radiation to treat

posterior cranial fossa The posterior cranial fossa is the part of the cranial cavity located between the foramen magnum, and tentorium cerebelli. It is formed by the sphenoid bones, temporal bones, and occipital bone. It lodges the cerebellum, and parts of the brai ...

tumors. With the ventromedial hypothalamus disabled and no longer responding to peripheral energy balance signals, "Efferent sympathetic activity drops, resulting in malaise and reduced energy expenditure, and

vagal The vagus nerve, also known as the tenth cranial nerve (CN X), plays a crucial role in the autonomic nervous system, which is responsible for regulating involuntary functions within the human body. This nerve carries both sensory and motor fibe ...

activity increases, resulting in increased

secretion and

adipogenesis Adipogenesis is the formation of adipocytes (fat cells) from stem cells. It involves 2 phases, determination, and terminal differentiation. Determination is mesenchymal stem cells committing to the adipocyte precursor cells, also known as lipoblast ...

." "VMH dysfunction promotes excessive caloric intake and decreased caloric expenditure, leading to continuous and unrelenting weight gain. Attempts at caloric restriction or pharmacotherapy with adrenergic or serotonergic agents have previously met with little or only brief success in treating this syndrome." In this context, octreotide suppresses the excessive release of insulin and may increase its action, thereby inhibiting excessive adipose storage. In a small

clinical trial Clinical trials are prospective biomedical or behavioral research studies on human subject research, human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel v ...

in eighteen pediatric subjects with intractable weight gain following therapy for acute lymphoblastic leukemia or brain tumors and other evidence of hypothalamic dysfunction, octreotide reduced

body mass index Body mass index (BMI) is a value derived from the mass (Mass versus weight, weight) and height of a person. The BMI is defined as the human body weight, body mass divided by the square (algebra), square of the human height, body height, and is ...

(BMI) and insulin response during glucose tolerance test, while increasing parent-reported physical activity and

quality of life Quality of life (QOL) is defined by the World Health Organization as "an individual's perception of their position in life in the context of the culture and value systems in which they live and in relation to their goals, expectations, standards ...

(QoL) relative to

placebo A placebo ( ) can be roughly defined as a sham medical treatment. Common placebos include inert tablets (like sugar pills), inert injections (like saline), sham surgery, and other procedures. Placebos are used in randomized clinical trials ...

. In a separate placebo-controlled trial of obese adults without known hypothalamic lesions, obese subjects who received long-acting octreotide lost weight and reduced their BMI compared to subjects receiving placebo; post hoc analysis suggested greater effects in participants receiving the higher dose of the medication, and among " Caucasian subjects having insulin secretion greater than the median of the cohort." "There were no statistically significant changes in QoL scores, body fat, leptin concentration, Beck Depression Inventory, or macronutrient intake", although subjects taking octreotide had higher blood glucose after a glucose tolerance test than those receiving placebo.

References

{{Authority control Cyclic peptides Drugs developed by Novartis Opioids Somatostatin inhibitors Bynfezia Pen Substances discovered in the 1970s Orphan drugs World Health Organization essential medicines Systemic hormonal preparations Octapeptides