Octreotide
approvedAlso known as: Sandostatin, SMS 201-995
**Mechanism of Action** Octreotide is a synthetic octapeptide analog of endogenous somatostatin with enhanced metabolic stability and a longer half-life (approximately 2 hours vs. 2–3 minutes for somatostatin). It binds with high affinity to somatostatin receptors (primarily SSTR2 and SSTR5), inhibiting adenylyl cyclase activity and reducing intracellular cyclic AMP levels. This suppresses the secretion of growth hormone (GH), insulin-like growth factor 1 (IGF-1), glucagon, insulin, gastrin, vasoactive intestinal peptide (VIP), and other gastrointestinal hormones. Additionally, octreotide reduces splanchnic blood flow and inhibits exocrine pancreatic secretion. **Key Research Findings** Clinical trials have demonstrated octreotide’s efficacy in normalizing GH and IGF-1 levels in approximately 60–70% of acromegaly patients, with tumor shrinkage observed in 30–50% of cases. In neuroendocrine tumors (e.g., carcinoid syndrome, VIPomas), octreotide significantly reduces hormone-related symptoms (e.g., flushing, diarrhea) and prolongs time to tumor progression. Long-acting release (LAR) formulations provide sustained therapeutic effects with monthly intramuscular injections. Adverse effects include gallstones (due to reduced gallbladder motility), bradycardia, and glucose metabolism disturbances. **Clinical Relevance** Octreotide is a first-line pharmacotherapy for acromegaly and symptomatic control of neuroendocrine tumors. It is also used off-label for variceal bleeding, refractory diarrhea, and hypoglycemia due to insulinoma. Its approval by regulatory agencies (FDA, EMA) is supported by robust evidence from over 9,000 PubMed-indexed studies. Octreotide’s role in targeted radionuclide therapy (e.g., ⁶⁸Ga-DOTATATE PET imaging) further underscores its utility in oncology. For research purposes only — not medical advice.
Key data
C49H66N10O10S2Research & studies
Octreotide was prescribed to 89% of PLE dogs with suspected or confirmed IL refractory to standard therapies.; Median serum albumin at prescription was 1.7 g/dL (range 1.0-3.1 g/dL).; Adverse effects occurred in 17% of dogs; only 1 dog required drug discontinuation.; Clinical improvement was observed in 50% of dogs (6/12) with available follow-up.
Octreotide reduces drainage in selected chylothorax patients not responding to conservative treatment.; Prompt postoperative octreotide therapy may decrease expense and morbidity from prolonged hospitalization.; Individual patient response to octreotide varies, requiring careful risk-benefit assessment.; Clinical data on octreotide use in pediatric patients are limited.
Frequently asked questions
What is Octreotide?
**Mechanism of Action** Octreotide is a synthetic octapeptide analog of endogenous somatostatin with enhanced metabolic stability and a longer half-life (approximately 2 hours vs. 2–3 minutes for somatostatin). It binds with high affinity to somatostatin receptors (primarily SSTR2 and SSTR5), inhibiting adenylyl cyclas
How does Octreotide work?
Long-acting somatostatin analog that inhibits GH, glucagon, and gut hormone secretion; used for acromegaly and neuroendocrine tumors.
What is the research status of Octreotide?
Octreotide is currently classified as approved, with 9,252 research references on record. This is for research purposes only and is not medical advice.
What is the half-life of Octreotide?
The reported half-life of Octreotide is ~1.5 hours.
What is the molecular weight of Octreotide?
Octreotide has a molecular weight of approximately 1019.2 g/mol (formula C49H66N10O10S2).
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