Octreotide

Octreotide (brand names Sandostatin and Mycapssa) is a prescription medicine that turns growth hormone down. It is a lab-made version of somatostatin, the body's own "stop" signal for growth hormone. Its main use is acromegaly — a condition where a small benign tumor in the pituitary gland makes far too much growth hormone, causing bones and organs to keep growing in adulthood. It is FDA-approved, and comes both as a long-acting injection and, more recently, as a capsule.

Octreotide has been studied mainly in acromegaly, where the goal is bringing growth hormone and IGF-1 back into normal range. A Phase 3 trial compared the newer capsule form against the established injections in people already responding to the injections, and found the capsules held that response in most patients — 50 of 55, against 37 of 37 who stayed on injections. Older work using the injection as a first treatment in newly diagnosed patients found it shrank tumors and lowered hormone levels, though only about half reached a normal IGF-1. The honest part: the capsule trial only enrolled people already known to respond to this drug class, so it does not tell you how a new patient would do, and the first-line study was small with several dropouts.

FDA-approved prescription drug, available as an immediate-release injection dosed three times daily (Sandostatin), a long-acting depot injection (Sandostatin LAR Depot), and oral capsules (Mycapssa). Used in acromegaly — a disease of too much growth hormone — and in certain neuroendocrine tumor and carcinoid settings. Approved indications differ BY FORMULATION — the injections cover acromegaly plus symptom control in carcinoid tumors and VIPomas, while the oral capsule (Mycapssa) is approved for acromegaly only. Verified against current FDA labeling, 2026-09-08.[⁴] ⭐ Note the direction: octreotide SUPPRESSES growth hormone. It is the pharmacological opposite of the growth-hormone secretagogues and releasing factors that make up a large part of this library. WADA status: octreotide is not named on the 2026 WADA Prohibited List, and no somatostatin drug class appears on that list (verified directly against the 2026 list text, 2026-08-04). Because it holds regulatory approval, S0 does not capture it. Note the sharp contrast with S2.2.4, which prohibits growth hormone releasing factors and secretagogues by name — including sermorelin, tesamorelin, CJC-1295, ipamorelin, MK-677, hexarelin and the GHRPs, all of which are in this library. Octreotide is on the opposite side of that axis and is not listed. Athletes should still verify with their anti-doping organization. Not DEA-scheduled (prescription, non-controlled).

Octreotide is a prescription drug used under specialist endocrine care. In the Phase 3 trial the most common treatment-related side effects in both the capsule and injection groups were gastrointestinal. It is not named on the WADA Prohibited List and, being an approved medicine, is not captured by the S0 non-approved-substances category — though athletes should verify with their anti-doping organization. Worth understanding in context: this drug lowers growth hormone, the opposite direction to the growth-hormone secretagogues elsewhere in this library, several of which are explicitly prohibited in sport. VialWise is a research and educational reference, not medical advice — consult a licensed professional.

⚠️ This is an approved prescription medicine, not a research peptide. Octreotide is dispensed by a pharmacy and used under specialist endocrine care. The reconstitution and self-dosing workflows used elsewhere in this library do not apply. Information here is informational, not medical advice.

⚠️ Read the Phase 3 trial's entry criteria before reading its result. The MPOWERED trial only randomized patients who were already responding to injectable somatostatin receptor ligands and who then also responded during a 26-week oral run-in.[¹] It is a maintenance and formulation-switching study. It does not tell you how likely a newly diagnosed patient is to respond to octreotide at all.

Octreotide is a synthetic cyclic octapeptide analogue of somatostatin, the body's endogenous inhibitor of growth hormone release. It is marketed as Sandostatin and Sandostatin LAR (injectable) and Mycapssa (oral capsules).

Mechanism. Somatostatin binds receptors on pituitary cells and suppresses growth hormone secretion, but its natural half-life is far too short to be a drug. Octreotide is engineered for a much longer duration while retaining that suppressive activity.[²] In acromegaly, reducing GH secretion lowers hepatic IGF-1 production, which is the marker clinicians track.[¹]

The oral formulation problem, and why it is interesting. Peptides are normally destroyed in the gut, which is why nearly everything in this library is injected. Oral octreotide capsules pair the peptide with a transient permeability enhancer technology that lets it cross the intestinal wall intact — the first oral somatostatin receptor ligand approved in the United States.[²] Alongside `orforglipron` and `linaclotide` in this library, it is one of the few worked examples of getting peptide-class pharmacology into a swallowed dose.

Evidence quality.

- MPOWERED was a Phase 3, global, open-label, randomized controlled trial across 29 sites in 10 countries.[¹] Design matters here: eligible adults were already on injectable SRLs for at least 6 months at a stable dose and already biochemically responding. All 146 enrolled patients first took oral octreotide for a 26-week run-in; only those still responding at week 24 were randomized 3:2 to oral octreotide (n=55) or back to injectable SRL (n=37).[¹] At the end of the randomized phase, 50 of 55 (91%) on oral and 37 of 37 (100%) on injectable maintained biochemical response — meeting the prespecified non-inferiority margin of −20 percentage points (95% CI −19.9 to 0.5).[¹] ⚠️ That confidence interval only just clears the margin, and 30 of the 146 enrolled patients discontinued during the run-in.[¹] Treatment-related adverse events occurred in 35% (oral) and 41% (injectable), most commonly gastrointestinal.[¹] Funded by Chiasma.[¹] - A clinical review covering 4 pivotal trials and 238 patients treated with oral octreotide capsules described effective GH and IGF-1 suppression, maintenance of disease control, and a safety profile comparable to injectable SRLs, and noted that most trial patients preferred oral to injectable administration.[²] - Injectable octreotide LAR as first-line therapy was studied prospectively in 19 treatment-naive acromegalic patients over 12 months.[³] Tumor volume fell 25 ± 23% (p = 0.046) regardless of initial tumor extension; basal GH fell 76 ± 18% and fasting IGF-1 fell 52 ± 31%; 6 of 13 completers (46%) normalized IGF-1, and 8 patients (42%) achieved >25% tumor shrinkage.[³] ⚠️ 19 patients, 6 of whom withdrew — this is a small observational study, not a controlled trial, and roughly half of completers did *not* reach a normal IGF-1.

Regulatory status (US). The approved indications are formulation-specific — the oral capsule is not approved for the tumor indications. Verified against current FDA labeling on DailyMed, 2026-09-08.[⁴]

Limitations of Use, from the Sandostatin Injection label: *"Improvement in clinical signs and symptoms, or reduction in tumor size or rate of growth, were not shown in clinical trials performed with Sandostatin Injection; these trials were not optimally designed to detect such effects."* The carcinoid and VIPoma indications are for symptom control, not tumor treatment — worth stating plainly, because the shorthand "approved for neuroendocrine tumors" invites the opposite reading.

Not DEA-scheduled.

Regulatory status (sport — WADA). Octreotide is not named on the 2026 WADA Prohibited List, and no somatostatin class appears anywhere on it (checked directly against the list text, 2026-08-04). Because it holds regulatory approval, S0 does not capture it.

⭐ The instructive contrast: S2.2.4 of the same list prohibits *growth hormone releasing factors* and *growth hormone secretagogues* explicitly and by name — the verbatim list includes GHRH analogues (CJC-1293, CJC-1295, sermorelin, tesamorelin), secretagogues (anamorelin, capromorelin, ibutamoren/MK-677, ipamorelin, lenomorelin/ghrelin, macimorelin, tabimorelin), and the GHRPs (alexamorelin, examorelin/hexarelin, GHRP-1 through GHRP-6). Nearly all of those are entries in this library. Octreotide moves the same axis in the opposite direction and is not listed. Athletes should verify current status with their National Anti-Doping Organization.

Commonly reported

• Treatment-related adverse events in 35% (oral) and 41% (injectable) of patients, most commonly gastrointestinal.[¹]
• 30 of 146 patients discontinued during the 26-week oral run-in phase, though the trial report does not attribute all of those to adverse events.[¹]
• The safety profile of oral capsules was described as comparable to injectable SRLs, with the benefit of avoiding injection-related side effects.[²]

This is a prescription medicine used under specialist endocrine care for a serious chronic condition. Use outside that context is outside everything the evidence base covers.

Not a growth-hormone enhancer — the opposite. Anyone approaching this entry from the GH-peptide side of the library should be clear that octreotide lowers GH and IGF-1.[¹][³]

Concurrent GH secretagogues or releasing factors — pharmacologically opposed, unstudied in combination.

Pregnancy and lactation — not addressed by the sources here. Refer to current labeling.

Pediatric use — the trials cited enrolled adults (MPOWERED: 18–75 years).[¹]

Full contraindication list is set by labeling. The three sources here cover efficacy and headline tolerability, not the complete safety profile.

Regulatory note (sport): not named on the 2026 WADA Prohibited List and not captured by S0 (approved medicine) — in contrast to the GH secretagogues in S2.2.4, which are named and prohibited. Verify with your anti-doping organization.

Not DEA-scheduled.

Peptide

A short chain of amino acids, the building blocks of proteins. Many compounds in this library are peptides.

Somatostatin

A natural hormone that acts as the body's brake on growth hormone release. Octreotide is a longer-lasting synthetic version of it.

Acromegaly

A condition caused by too much growth hormone in adulthood, usually from a benign pituitary tumor. It causes gradual enlargement of the hands, feet and facial features, along with joint and metabolic problems.

IGF-1

Insulin-like growth factor 1 — a hormone the liver makes in response to growth hormone. Because it is steadier in the blood than growth hormone itself, it is the standard blood marker for whether acromegaly is controlled.

Biochemical response

In acromegaly, having growth hormone and IGF-1 brought into a target range by treatment. It is a lab measurement, not a measure of how a person feels.

1. Fleseriu M, Dreval A, Bondar I, Vagapova G, Macut D, Pokramovich YG, Molitch ME, Leonova N, Raverot G, Grineva E, Poteshkin YE, Gilgun-Sherki Y, Ludlam WH, Patou G, Haviv A, Gordon MB, Biermasz NR, Melmed S, Strasburger CJ. (2022). Maintenance of response to oral octreotide compared with injectable somatostatin receptor ligands in patients with acromegaly: a phase 3, multicentre, randomised controlled trial. The Lancet Diabetes & Endocrinology, 10(2):102–111.(PMID 34953531 · NCT02685709)
2. Yuen KCJ, Samson SL. (2022). Oral Octreotide: A Review of Recent Clinical Trials and Practical Recommendations for Its Use in the Treatment of Patients With Acromegaly. Endocrine Practice, 28(6):637–645.(PMID 35452815)
3. Luque-Ramírez M, Portoles GR, Varela C, Albero R, Halperin I, Moreiro J, Soto A, Casamitjana R. (2010). The efficacy of octreotide LAR as firstline therapy for patients with newly diagnosed acromegaly is independent of tumor extension: predictive factors of tumor and biochemical response. Hormone and Metabolic Research, 42(1):38–44.(PMID 19798622)
4. U.S. Food and Drug Administration, current prescribing information via DailyMed (NLM), retrieved 2026-09-08. Three separate labels, because the approved indications are not the same across formulations and a single-label check would have missed that: Sandostatin (octreotide acetate) Injection, Novartis, SPL version 23, published 2026-07-24, setid `4e2c9856-1836-49f0-9472-4dbeeb408f39`; Sandostatin LAR Depot, Novartis, SPL version 29, published 2025-12-23, setid `d0b7fe9e-7000-4b79-ba3b-291ce92c14f9`; Mycapssa (octreotide) delayed-release capsules, Chiesi USA, SPL version 6, published 2025-07-28, setid `58d80bc6-bdfb-4908-93e7-aace447c8d1a`. Cited for the indications and usage and Limitations of Use sections quoted above. dailymed.nlm.nih.gov

• AOD-9604 — same mechanism class
• HGH (Human Growth Hormone) / Somatropin — same mechanism class
• IGF-1 LR3 — same mechanism class
• MGF — same mechanism class
• CJC-1295 / Ipamorelin Blend — shared research area
• CJC-1295 — shared research area