Octreotide
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Synthetic cyclic octapeptide somatostatin analog; FDA-approved SSTR2/SSTR5 agonist for acromegaly, carcinoid syndrome, and VIPomas.
Quick Facts
| Property | Value |
|---|---|
| Also Known As | Sandostatin, Sandostatin LAR, SMS 201-995, octreotide acetate |
| Category | Somatostatin analog |
| Sequence | D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr(ol) (cyclic via disulfide) |
| Molecular Weight | ~1019.24 Da |
| Molecular Formula | C49H66N10O10S2 |
| PubChem CID | 448601 |
| Administration | SubQ (immediate-release), IM (LAR depot monthly) |
| Typical Dose Range | SubQ: 50-500 mcg 2-3x daily; LAR: 10-30 mg IM q28d |
| Half-Life | ~100 min (SubQ); ~28 days (LAR depot) |
| Storage | Refrigerate (2-8C); SubQ solution stable at RT for 14 days; LAR must be reconstituted immediately before injection |
| FDA Status | Approved (1988) — Sandostatin for acromegaly, carcinoid syndrome, VIPomas; Sandostatin LAR Depot (1998) |
| WADA Status | Not listed |
Mechanism of Action
Octreotide is a synthetic octapeptide analog of native somatostatin (SST-14) that retains the pharmacophore (Phe-Trp-Lys-Thr) responsible for receptor binding while being resistant to enzymatic degradation. Native somatostatin has a half-life of only ~3 minutes, making it impractical for clinical use. Octreotide extends this to ~100 minutes via subcutaneous injection and ~28 days as a long-acting release (LAR) microsphere depot formulation.
Octreotide binds with high affinity to somatostatin receptor subtypes SSTR2 (Ki ~0.4 nM) and SSTR5 (Ki ~7 nM), with moderate affinity for SSTR3 and minimal binding to SSTR1 and SSTR4. Through SSTR2 activation, octreotide inhibits growth hormone (GH) and insulin-like growth factor-1 (IGF-1) secretion from the anterior pituitary, making it effective in acromegaly. SSTR2 is also highly expressed on neuroendocrine tumor cells, enabling both antisecretory and antiproliferative effects in carcinoid tumors and VIPomas (PMID 29872467).
Downstream signaling includes inhibition of adenylyl cyclase (reducing cAMP), activation of phosphotyrosine phosphatases (SHP-1, SHP-2), modulation of MAPK pathways, and induction of cell cycle arrest. Octreotide also reduces splanchnic blood flow, inhibits gastric acid secretion, and suppresses release of glucagon, insulin, secretin, motilin, VIP, and pancreatic polypeptide.
Key Research Areas
- Acromegaly — First-line or adjunctive medical therapy for GH-secreting pituitary adenomas; normalizes GH/IGF-1 in 50-70% of patients and induces tumor shrinkage in >50% (PMID 22574156)
- Neuroendocrine tumors (NETs) — Antiproliferative activity demonstrated in the landmark PROMID trial, with median time to progression doubled vs placebo (PMID 19704057)
- Carcinoid syndrome — Controls diarrhea and flushing in 60-70% of patients by suppressing serotonin and other bioactive peptide secretion
- VIPomas — Controls watery diarrhea syndrome (Verner-Morrison) by directly inhibiting VIP secretion
- GI bleeding — Used off-label for variceal bleeding (reduces splanchnic blood flow) and refractory GI bleeding
- Diagnostic imaging — Octreotide serves as the peptide backbone for OctreoScan (111In-DTPA-octreotide) somatostatin receptor scintigraphy
Evidence Level Summary
| Evidence Type | Count | Notes |
|---|---|---|
| Human RCTs | 1 | PROMID trial (neuroendocrine tumors) |
| Meta-analysis | 1 | Tumor mass effects in acromegaly |
| Human observational | — | Extensive post-marketing experience since 1988 |
| Narrative reviews | 1 | Comprehensive NET treatment review |
| Systematic reviews | — | Multiple exist in literature (not yet in vault) |
Clinical Applications
- Cancer Adjunct Therapy — FDA-approved for carcinoid tumors, VIPomas; antiproliferative in NETs
- Sarcopenia — GH axis suppression (indirect relationship)
Protocols Using This Peptide
- No Ageless Peps protocols (FDA-approved prescription drug, not a research peptide)
Ageless Peps Products
- Not sold — Octreotide is an FDA-approved prescription medication (Sandostatin/Sandostatin LAR) manufactured by Novartis. It is not a research peptide and is not available through Ageless Peps.
Dosing Reference
FDA-Approved Dosing
| Indication | Route | Dose | Frequency | Duration | Source |
|---|---|---|---|---|---|
| Acromegaly (initial) | SubQ | 50 mcg TID | 3x daily | Titrate to response | FDA label |
| Acromegaly (maintenance) | IM | 20-30 mg LAR | q28 days | Ongoing | FDA label |
| Carcinoid syndrome | SubQ | 100-600 mcg/day | 2-4 divided doses | Ongoing | FDA label |
| Carcinoid (maintenance) | IM | 20-30 mg LAR | q28 days | Ongoing | FDA label |
| VIPomas | SubQ | 200-300 mcg/day | 2-4 divided doses | Ongoing | FDA label |
Cycling
Not applicable — octreotide is prescribed as continuous therapy. Dose adjustments are made based on biochemical response (GH, IGF-1, chromogranin A levels) and symptom control. Tachyphylaxis can occur; dose escalation or switch to pasireotide may be considered.
Contraindications & Safety
- Contraindications: Hypersensitivity to octreotide or any excipient
- Common side effects: Gallstones/biliary sludge (15-30%), diarrhea, abdominal pain, nausea, flatulence, injection site pain (LAR), headache
- Drug interactions: May alter absorption of orally administered drugs; reduces cyclosporine levels; may require adjustment of insulin/oral hypoglycemics, beta-blockers, calcium channel blockers
- Pregnancy/nursing: Category B (no adequate human studies); use only if clearly needed
- Special populations: Dose adjustment may be needed in renal impairment (dialysis patients); hepatic cirrhosis may alter pharmacokinetics; monitor thyroid function with long-term use (TSH suppression)
Synergistic Combinations
- Lanreotide — Alternative somatostatin analog; head-to-head comparisons show equivalent efficacy
- Pasireotide — Second-line after octreotide failure (broader SSTR profile)
- Lutetium-177-DOTATATE — PRRT builds on octreotide's receptor targeting; often used sequentially after octreotide progression
Related Research
| PMID | Title | Year | Study Type |
|---|---|---|---|
| 22574156 | Meta-analysis on the effects of octreotide on tumor mass in acromegaly | 2012 | Meta-analysis |
| 19704057 | PROMID: Octreotide LAR antiproliferative effect in midgut NETs | 2009 | RCT |
| 29872467 | Octreotide – A Review of its Use in Treating Neuroendocrine Tumours | 2018 | Narrative Review |
References
- PMID 22574156 — Giustina et al. Meta-analysis on octreotide tumor mass effects in acromegaly (2012)
- PMID 19704057 — Rinke et al. PROMID trial: octreotide LAR antiproliferative in midgut NETs (2009)
- PMID 29872467 — Broder et al. Octreotide review in treating NETs (2018)
Related
- Peptide Index
- Condition Index
- Protocol Index
- Cancer Adjunct Therapy
- Lanreotide
- Pasireotide
- Lutetium-177-DOTATATE
FDA Disclaimer: Octreotide (Sandostatin) is an FDA-approved prescription medication. The information in this note is for educational and reference purposes only and does not constitute medical advice. Prescribing and administration must be performed by qualified healthcare providers.
#peptide #gh-axis #fda-approved #not-sold #subq