Octreotide is a synthetic eight-amino-acid analog of somatostatin, the body’s own “off switch” for growth hormone (GH) and several gut hormones. Novartis’s subcutaneous injection, Sandostatin, was first approved by the FDA in 1988. A monthly intramuscular depot (Sandostatin LAR Depot) followed in 1998, and an oral capsule (Mycapssa) in 2020 (Drugs@FDA).
Its main endocrine use is acromegaly, the disease caused by a GH-secreting pituitary tumor. Octreotide lowers GH and, as a result, insulin-like growth factor 1 (IGF-1). That makes it the pharmacological opposite of GH, IGF-1 and GH secretagogues. It also treats the diarrhea and flushing of hormone-secreting gut tumors (carcinoid tumors and VIPomas).
This page summarizes what the FDA labels and the clinical trials report. It is for education only and is not medical advice.
| Property | Detail |
|---|---|
| Drug class | Somatostatin analog (somatostatin receptor ligand) |
| Brands / FDA approval | Sandostatin injection (NDA 019667, 1988); Sandostatin LAR Depot (NDA 021008, 1998); Mycapssa oral capsules (NDA 208232, 2020); Bynfezia Pen; generic injections |
| Routes | Subcutaneous or IV (Sandostatin); gluteal IM every 4 weeks (LAR); oral (Mycapssa) |
| Strengths | 50, 100 and 500 mcg/mL ampuls; LAR 10, 20 and 30 mg kits; 20 mg delayed-release capsules |
| Half-life (labels) | 1.7–1.9 h after injection (natural somatostatin: 1–3 minutes); 2.7 h for oral in healthy people and 3.2–4.5 h at steady state in acromegaly |
| Key mechanism | Mimics somatostatin; a more potent inhibitor of GH, glucagon and insulin than the natural hormone |
| Main endocrine effect | Lowers GH and IGF-1 in acromegaly |
| Boxed warning | None on any of the three labels |
| US status | Prescription-only |
| WADA status | Not named on the WADA 2026 Prohibited List |
What it is
Octreotide (research code SMS 201-995) is a cyclic octapeptide: eight amino acids closed into a ring by a disulfide bond. It was built by stepwise modification of the fragment of somatostatin thought to carry its biological activity, and the result proved highly resistant to breakdown by enzymes (Bauer et al., Life Sci 1982). The free peptide has the formula C49H66N10O10S2 and a molecular weight of 1019.3 g/mol; the drug is supplied as the acetate salt (Sandostatin label).
In the original 1982 report, octreotide was three times more potent than native somatostatin at inhibiting GH secretion in vitro. In rats and rhesus monkeys it was at least 20 times more active, acted much longer and inhibited GH more selectively than insulin (Bauer et al., Life Sci 1982). Those were animal results; in people, the label describes octreotide as a more potent inhibitor of GH, glucagon and insulin than somatostatin.
Somatostatin acts on five receptor subtypes (SSTR1–5). In a study of 32 synthetic analogs tested on all five cloned human receptors under identical conditions, cyclic octapeptide analogs (the class octreotide belongs to) bound subtypes 2, 3 and 5 potently and subtypes 1 and 4 poorly (Patel and Srikant, Endocrinology 1994).
According to the labels, octreotide does the following:
- inhibits GH, glucagon and insulin secretion;
- suppresses thyroid-stimulating hormone (TSH);
- suppresses the luteinizing hormone (LH) response to gonadotropin-releasing hormone (GnRH);
- reduces blood flow to the gut organs;
- inhibits serotonin, gastrin, vasoactive intestinal peptide (VIP), secretin, motilin and pancreatic polypeptide;
- inhibits gallbladder contraction and bile secretion.
The three FDA-approved brand forms deliver the same peptide in different ways:
| Product | Form | How it works | Dosing interval |
|---|---|---|---|
| Sandostatin | Aqueous solution, 1 mL ampuls | Absorbed rapidly and completely after subcutaneous injection | Usually three times daily |
| Sandostatin LAR Depot | Microspheres of a biodegradable lactic/glycolic acid copolymer, mixed into a suspension | Octreotide is released as the polymer breaks down in the muscle | Every 4 weeks, gluteal IM only |
| Mycapssa | Enteric-coated capsule with absorption-enhancing excipients (including sodium caprylate) | Briefly opens the gaps between gut-lining cells so the peptide can be absorbed | Twice daily on an empty stomach |
A multi-dose pen (Bynfezia Pen, 2.5 mg/mL) and several generic octreotide acetate injections are also FDA-approved (Drugs@FDA, NDA 213224).
Pharmacokinetics
Injection (Sandostatin)
From the Sandostatin and Sandostatin LAR labels:
| Parameter | Healthy volunteers | Acromegaly |
|---|---|---|
| Peak after 100 mcg subcutaneous | 5.2 ng/mL at 0.4 h | 2.8 ng/mL at 0.7 h |
| Volume of distribution | 13.6 L | 21.6 L |
| Total body clearance | 7–10 L/h | 18 L/h |
| Plasma protein binding | About 65% (mainly lipoprotein) | 41.2% |
| Elimination half-life | 1.7–1.9 h | Similar to healthy people |
| Excreted unchanged in urine | About 32% | — |
The label puts the duration of action at up to 12 hours, which is why the immediate-release form is given several times a day. Half-life rises by 46% in older adults and to 3.7 h in liver cirrhosis. In dialysis patients, clearance falls to about half of normal.
Monthly depot (Sandostatin LAR)
After a single LAR injection in healthy volunteers, octreotide levels show a small peak within the first hour, dip over 3–5 days, then rise to a plateau at about 2–3 weeks. The plateau lasts about 2–3 more weeks, and levels fade by weeks 12–13 as the polymer finishes degrading (Sandostatin LAR label).
In acromegaly with dosing every 4 weeks, the label reports:
| Measure | 20 mg every 4 weeks | 30 mg every 4 weeks |
|---|---|---|
| Steady-state trough | 1.2 ng/mL | 2.1 ng/mL |
| Steady-state peak | 1.6 ng/mL | 2.6 ng/mL |
Steady state is reached after the third injection. Peak-to-trough swing is 44–68% with the depot, compared with 163–209% on three-times-daily injections. Relative bioavailability versus the subcutaneous solution is 60–63%.
Oral capsules (Mycapssa)
Peptides are normally destroyed or poorly absorbed in the gut. Mycapssa’s excipients increase paracellular permeability (passage between gut-lining cells): in a dedicated study, permeability rose 2 hours after a dose and returned to baseline by 5.5 hours (Mycapssa label).
| Parameter | Value (Mycapssa label) |
|---|---|
| Exposure vs injection | 20 mg orally gave similar total exposure (AUC) to 0.1 mg subcutaneously, with a 33% lower peak |
| Time to peak | Median 1.67–2.5 h (vs 0.5 h after injection) |
| Effect of food | Taken with food, peak and total absorption fell by about 90% |
| Half-life | 2.7 h in healthy people; 3.2–4.5 h at steady state in acromegaly |
| Accumulation | About 10% with repeated dosing |
| End-stage kidney disease | AUC 87% higher and half-life 85% longer than matched controls |
This is why the label requires the capsules to be taken at least 1 hour before or 2 hours after a meal.
Approved medical use
Indications
| Product | Acromegaly | Carcinoid tumors | VIPomas |
|---|---|---|---|
| Sandostatin injection | To lower GH and IGF-1 when surgery, pituitary irradiation and bromocriptine at maximally tolerated doses have failed or cannot be used | Severe diarrhea and flushing from metastatic carcinoid tumors | Profuse watery diarrhea |
| Sandostatin LAR Depot | Long-term maintenance after inadequate response to surgery and/or radiotherapy, or when these are not an option; only in patients who responded to and tolerated the injection | Long-term treatment of the same symptoms | Long-term treatment of the same symptoms |
| Mycapssa | Long-term maintenance in patients who responded to and tolerated octreotide or lanreotide | Not indicated | Not indicated |
For the tumor indications, the labels state that octreotide was not shown to improve tumor size, growth rate or metastases; it controls the hormone-driven symptoms.
Labeled acromegaly dosing
| Product | Start | Titration and maximum |
|---|---|---|
| Sandostatin injection | 50 mcg subcutaneously three times daily | Most common dose 100 mcg three times daily; some patients need up to 500 mcg three times daily. Doses above 300 mcg/day seldom add biochemical benefit. |
| Sandostatin LAR Depot | After at least 2 weeks of the injection: 20 mg IM every 4 weeks for 3 months | 10, 20 or 30 mg every 4 weeks based on GH, IGF-1 and symptoms; may increase to 40 mg; doses above 40 mg are not recommended |
| Mycapssa | 20 mg twice daily (40 mg/day) | Increase in 20 mg steps; maximum 80 mg/day. ESRD: start at 20 mg once daily. |
The labels set the treatment targets around GH and IGF-1. For the injection, the goal is GH under 5 ng/mL or IGF-1 within the normal range, checked every 2 weeks during titration. For the LAR depot, a GH of 2.5 ng/mL or less with a normal IGF-1 is the cut-off for staying at 20 mg. Patients who have had pituitary radiation should have the drug withdrawn yearly (about 4 weeks for the injection, about 8 weeks for LAR) to see whether the disease is still active.
What the research shows
GH and IGF-1 control in acromegaly: injection and LAR
In a 14-day double-blind, placebo-controlled trial in 18 patients with acromegaly, subcutaneous octreotide significantly lowered GH and IGF-1 throughout treatment. The mean age-adjusted IGF-1 standard deviation score fell from 6.47 to 3.60 by day 14. Octreotide also suppressed insulin by 40–48% compared with placebo (Fredstorp et al., Clin Endocrinol 1994).
The LAR depot was approved on trials that switched patients already controlled on the injection to the monthly form. The label reports these results, as the average of monthly values over the trial (Sandostatin LAR label):
| Outcome | Trials 1–2: injection | Trials 1–2: LAR (n = 88, 27–28 injections) | Trial 3: injection | Trial 3: LAR (n = 122, 12 injections) |
|---|---|---|---|---|
| GH under 5 ng/mL | 78% | 83% | 95% | 97% |
| GH under 2.5 ng/mL | 50% | 47% | 69% | 66% |
| IGF-1 normalized | 41% | 51% | 67% | 67% |
| GH under 2.5 ng/mL and normal IGF-1 | 34% | 42% | 53% | 57% |
Control on LAR was at least as good as on the injection it replaced. Among 25 partial responders to the injection, only 1 (4%) reached GH under 2.5 ng/mL on LAR. In two open-label 48-week studies in 143 previously untreated patients, median tumor volume shrank by 20.6% and 24.5% at 24 weeks, and by 36.2% at 48 weeks in the larger study.
Oral octreotide (Mycapssa)
Three phase 3 programs tested the capsules in patients already controlled on injectable somatostatin analogs:
| Trial | Design | Main result |
|---|---|---|
| Phase 3 open-label (Melmed et al., JCEM 2015) | 155 patients switched from injections; dose titrated 40–80 mg/day; 7-month core plus 6-month extension | 65% kept IGF-1 under 1.3 × the upper limit of normal (ULN) and GH under 2.5 ng/mL at end of core; 62% at up to 13 months |
| OPTIMAL (Samson et al., JCEM 2020) | Double-blind, 56 patients, oral capsules vs placebo for 36 weeks | IGF-1 at or below ULN maintained in 58.2% vs 19.4% (P = .008); GH under 2.5 ng/mL in 77.7% vs 30.4% |
| MPOWERED (Fleseriu et al., Lancet Diabetes Endocrinol 2022) | Open-label; 92 responders randomized 3:2 to capsules or their prior injection | Response maintained in 91% on capsules vs 100% on injections; met the non-inferiority margin of −20 points (95% CI −19.9 to 0.5) |
In OPTIMAL, the median time to losing IGF-1 control on placebo was 16 weeks; on capsules it was not reached during the trial. A quarter of capsule-treated patients still needed rescue with an injectable analog over the 9 months, as the label notes. In the MPOWERED open-label extension, 89.7%, 87.8% and 93.5% of patients who entered each extension year as responders were still responders at its end (years 1–3) (Fleseriu et al., JCEM 2023).
All of these trials enrolled patients who were already controlled on injections. A 2025 network meta-analysis of 27 studies (4,131 patients, 11 treatments) found octreotide LAR superior to oral octreotide capsules for IGF-1 normalization (OR 5.41, 95% CI 1.89–15.52). Pegvisomant ranked best overall for IGF-1 normalization, followed by pasireotide LAR (Kaparounaki et al., Eur J Endocrinol 2025). The authors noted that differences in study methods may have affected the comparisons.
A newer subcutaneous depot (CAM2029)
CAM2029 is a once-monthly subcutaneous octreotide depot designed for self-injection. In the 24-week double-blind ACROINNOVA 1 trial, 72 controlled patients were randomized 2:1 to CAM2029 or placebo. IGF-1 stayed at or below ULN in 72.2% vs 37.5% (risk difference 34.6 points, 95% CI 11.3–57.9) (Ferone et al., JCEM 2025).
The European Commission authorized it as Oczyesa on June 30, 2025, for maintenance treatment of adult acromegaly (EMA). It is not FDA-approved. The FDA issued a complete response letter on June 10, 2026, tied to a manufacturing inspection, and accepted a resubmission with a target action date of December 18, 2026 (Camurus press release, July 2026).
Relevance to GH, IGF-1 and secretagogues
Octreotide works upstream of GH: it reduces how much GH the pituitary releases, and IGF-1 falls as a consequence. Three points from the evidence help put this in context:
- It does not block GH that is given from outside. Researchers use octreotide to switch off the body’s own GH so they can study infused GH. In 26 healthy men on octreotide, GH infusions still produced significant changes in IGF-1, free fatty acids and insulin (Hansen et al., JCEM 2002).
- It can blunt secretagogue-driven release, at least in cell culture. In cultured cells from 12 human GH-secreting adenomas, a GH-releasing peptide stimulated GH in all of them. Octreotide lowered basal GH in 5 of 9 cultures tested, and in those it also suppressed the peptide-induced release (Renner et al., JCEM 1994). This was tumor tissue in vitro, not healthy people.
- It lowers insulin and glucagon too. The effect on GH comes with effects on glucose regulation, the thyroid and the gallbladder (below).
No controlled human study has tested octreotide in people using GH, IGF-1 or GH secretagogues outside medicine, and there is no evidence it has any role there. Related pages: growth hormone, IGF-1, tesamorelin and sermorelin.
Side effects and risks
None of the three labels carries a boxed warning. The warnings are shared across forms and follow from what somatostatin does.
Gallbladder
Octreotide slows gallbladder emptying and bile secretion, so stones and sludge are its signature long-term risk (Sandostatin label; Sandostatin LAR label):
| Finding | Rate |
|---|---|
| Biliary tract abnormalities in injection trials (mainly acromegaly or psoriasis) | 63% (27% gallstones, 24% sludge, 12% duct dilatation) |
| Stones or sludge after 12 months or more of injections | 52% |
| Gallstones after 1 month or less | Under 2% |
| New biliary abnormalities in acromegaly, mostly on LAR for 12 months or more | 52% (new gallstones 22%) |
| Acute symptoms requiring gallbladder removal | 1% |
The risk was tied to duration of exposure, not age, sex or dose. Cholecystitis, cholangitis, pancreatitis and one death from ascending cholangitis have been reported. The labels say to stop the drug if complications are suspected.
Blood sugar
Because octreotide suppresses insulin, glucagon and GH together, blood sugar can go either way:
| Population | Hyperglycemia | Hypoglycemia |
|---|---|---|
| Acromegaly, Sandostatin injection | 16% | 3% |
| Acromegaly, injection or LAR | About 15% | About 2% |
| Mycapssa trials | Increased blood glucose 7%; new diabetes 1% | 4% |
The labels call for glucose monitoring when starting or changing the dose and adjusting diabetes drugs as needed.
Heart rhythm
In acromegaly patients on the injection, the label reports:
- sinus bradycardia (heart rate under 50 bpm) in 25%;
- conduction abnormalities in 10%;
- arrhythmias in 9%.
Complete heart block has been reported with IV use during surgery, mostly at higher-than-recommended doses or by continuous infusion. Drugs that slow the heart, such as beta-blockers, may need dose changes.
Gut, thyroid and nutrients
- GI effects: Diarrhea, loose stools, nausea and abdominal discomfort were each seen in 34–61% of acromegaly patients on the injection; 2.6% stopped for these symptoms. On LAR, diarrhea occurred in 36.4% and was concentrated in the first month. With Mycapssa in the placebo-controlled trial, diarrhea occurred in 29% vs 21%, nausea in 21% vs 11% and vomiting in 14% vs 0%.
- Fat malabsorption: Somatostatin analogs reversibly inhibit pancreatic enzyme and bile acid secretion. This can cause steatorrhea (fatty stools), bloating and weight loss.
- Thyroid: Octreotide suppresses TSH. In acromegaly on the injection, 12% developed biochemical hypothyroidism, 8% goiter, and 4% needed thyroid hormone.
- Vitamin B12: Low B12 levels have been observed, and the labels recommend monitoring.
- Injection-site pain: Reported by 2%, 9% and 11% of acromegaly patients on LAR 10, 20 and 30 mg.
Interactions
| Drug | Effect (labels) |
|---|---|
| Cyclosporine | Lower cyclosporine levels; transplant rejection risk. Mycapssa reduced cyclosporine AUC to 0.38 of baseline. |
| Insulin and oral diabetes drugs | Dose adjustment may be needed |
| Beta-blockers, calcium channel blockers | Additive slowing of heart rate |
| Bromocriptine | Increased bromocriptine exposure |
| Lutetium Lu 177 dotatate | Stop Sandostatin injection at least 24 hours before each dose |
| CYP3A4 drugs with a narrow margin (e.g. quinidine) | Clearance may fall; use with caution |
| PPIs, H2 blockers, antacids (Mycapssa only) | Esomeprazole cut Mycapssa AUC to 0.59; higher doses may be needed |
| Combined oral contraceptives (Mycapssa only) | Levonorgestrel exposure fell (AUC 0.76); the label advises a back-up or non-hormonal method |
| Lisinopril, digoxin (Mycapssa only) | Lisinopril AUC rose 1.40-fold; digoxin peak fell to 0.63 |
Who should not use it, and special groups
- Contraindications: hypersensitivity to octreotide or the product’s ingredients (Sandostatin, Mycapssa). The LAR label lists none.
- Fertility and pregnancy: Lowering GH and normalizing IGF-1 may improve fertility in women with acromegaly, so the labels warn about unintended pregnancy. Human pregnancy data are limited.
- Children: Safety and efficacy are not established. Serious events, including necrotizing enterocolitis and death, have been reported in children, mostly under 2 years old with serious underlying illness.
- Kidney and liver disease: Lower starting doses are labeled for kidney failure on dialysis (LAR 10 mg), end-stage kidney disease (Mycapssa 20 mg/day) and cirrhosis (LAR 10 mg).
Monitoring
The labels list these checks for acromegaly treatment:
| What | When |
|---|---|
| GH and/or IGF-1 | Every 2 weeks during titration (injection, Mycapssa), then monthly or as indicated (Mycapssa) |
| Blood glucose | At the start and after dose changes |
| Thyroid function (TSH, total and/or free T4) | Baseline and periodically |
| Gallbladder | Periodically; evaluate symptoms promptly |
| Vitamin B12 | During therapy |
| Disease activity off drug | Yearly withdrawal in patients who had pituitary radiation (injection, LAR); periodic withdrawal (Mycapssa) |
Key takeaways
- A long-acting somatostatin. Octreotide copies somatostatin’s hormone-blocking effects but lasts hours instead of minutes. It comes as a multiple-daily injection, a monthly depot and twice-daily capsules.
- It lowers GH and IGF-1. In acromegaly, the monthly depot normalized IGF-1 in 51–67% of previously controlled patients across the label’s trials, and oral capsules maintained control in 58% vs 19% on placebo.
- The oral form needs an empty stomach. Food cuts Mycapssa absorption by about 90%, and acid-suppressing drugs also reduce it.
- Gallstones are the main long-term risk. About half of patients develop stones or sludge after a year or more, though few need surgery. Blood sugar, heart rate, thyroid function and B12 also need watching.
- No role outside medicine. Octreotide suppresses the body’s own GH but does not stop injected GH from raising IGF-1, and it has not been studied in people using GH or secretagogues.
Sources
- Novartis Pharmaceuticals. Sandostatin (octreotide acetate) injection, prescribing information. DailyMed; Drugs@FDA, NDA 019667.
- Novartis Pharmaceuticals. Sandostatin LAR Depot (octreotide acetate) for injectable suspension, prescribing information. DailyMed; Drugs@FDA, NDA 021008.
- Chiesi USA. Mycapssa (octreotide) delayed-release capsules, prescribing information. DailyMed; Drugs@FDA, NDA 208232.
- Sun Pharmaceutical Industries. Bynfezia Pen (octreotide acetate) injection. Drugs@FDA, NDA 213224.
- Bauer W, Briner U, Doepfner W, et al. SMS 201-995: a very potent and selective octapeptide analogue of somatostatin with prolonged action. Life Sci. 1982;31(11):1133–1140. PubMed.
- Patel YC, Srikant CB. Subtype selectivity of peptide analogs for all five cloned human somatostatin receptors (hsstr 1-5). Endocrinology. 1994;135(6):2814–2817. PubMed.
- Fredstorp L, Werner S, Bang P, Hall K. Inverse correlation between insulin-like growth factor binding protein-1 and insulin in patients with acromegaly during treatment with the somatostatin analogue octreotide. Clin Endocrinol (Oxf). 1994;41(4):495–501. PubMed.
- Melmed S, Popovic V, Bidlingmaier M, et al. Safety and efficacy of oral octreotide in acromegaly: results of a multicenter phase III trial. J Clin Endocrinol Metab. 2015;100(4):1699–1708. PubMed.
- Samson SL, Nachtigall LB, Fleseriu M, et al. Maintenance of acromegaly control in patients switching from injectable somatostatin receptor ligands to oral octreotide. J Clin Endocrinol Metab. 2020;105(10):e3785–e3797. PubMed.
- Fleseriu M, Dreval A, Bondar I, et al. Maintenance of response to oral octreotide compared with injectable somatostatin receptor ligands in patients with acromegaly: a phase 3, multicentre, randomised controlled trial. Lancet Diabetes Endocrinol. 2022;10(2):102–111. PubMed.
- Fleseriu M, Molitch M, Dreval A, et al. MPOWERED trial open-label extension: long-term efficacy and safety data for oral octreotide capsules in acromegaly. J Clin Endocrinol Metab. 2023;108(12):3214–3222. PubMed.
- Kaparounaki C, Ilie MD, De Alcubierre D, et al. Medical treatment in acromegaly: a network meta-analysis. Eur J Endocrinol. 2025;193(5):S83–S94. PubMed.
- Ferone D, Freda P, Katznelson L, et al. Octreotide subcutaneous depot for acromegaly: a randomized, double-blind, placebo-controlled phase 3 trial, ACROINNOVA 1. J Clin Endocrinol Metab. 2025;110(6):1729–1739. PubMed.
- European Medicines Agency. Oczyesa (octreotide): EPAR. EMA.
- Camurus AB. Camurus NDA resubmission for CAM2029 in acromegaly accepted for review by the US FDA. Press release, July 17, 2026. Camurus.
- Hansen TK, Jørgensen JO, Christiansen JS. Body composition and circulating levels of insulin, insulin-like growth factor-binding protein-1 and growth hormone (GH)-binding protein affect the pharmacokinetics of GH in adults independently of age. J Clin Endocrinol Metab. 2002;87(5):2185–2193. PubMed.
- Renner U, Brockmeier S, Strasburger CJ, et al. Growth hormone (GH)-releasing peptide stimulation of GH release from human somatotroph adenoma cells: interaction with GH-releasing hormone, thyrotropin-releasing hormone, and octreotide. J Clin Endocrinol Metab. 1994;78(5):1090–1096. PubMed.
- World Anti-Doping Agency. The 2026 Prohibited List. WADA 2026 Prohibited List.