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 the secretion of growth hormone (GH), glucagon, insulin, and gastrointestinal hormones (e.g., gastrin, vasoactive intestinal peptide, serotonin). This receptor activation also suppresses exocrine pancreatic secretion, reduces splanchnic blood flow, and modulates cell proliferation via inhibition of cyclic AMP and calcium-dependent signaling pathways. **Key Research Findings** Clinical trials have established octreotide as first-line pharmacotherapy for acromegaly, achieving normalization of GH and insulin-like growth factor-1 (IGF-1) levels in 50–70% of patients. In neuroendocrine tumors (NETs), octreotide reduces hormone-related symptoms (e.g., flushing, diarrhea) and prolongs progression-free survival, as demonstrated in the PROMID trial (median time to progression: 14.3 months vs. 6 months for placebo). Long-term use is associated with gallbladder sludge/stones (up to 50% of patients), bradycardia, and glucose metabolism alterations. Radiolabeled octreotide analogs (e.g., ⁶⁸Ga-DOTATATE) are also used for PET imaging of SSTR-expressing tumors. **Clinical Relevance** Octreotide is FDA-approved for acromegaly, carcinoid syndrome, and vasoactive intestinal peptide tumors (VIPomas). It is also used off-label for refractory diarrhea, gastrointestinal bleeding, and polycystic liver disease. Depot formulations (e.g., octreotide LAR) enable monthly intramuscular administration, improving adherence. Despite its efficacy, tachyphylaxis and adverse effects necessitate periodic monitoring of gallbladder ultrasound, thyroid function, and glucose levels. For research purposes only — not medical advice.
Key data
C49H66N10O10S2Research & studies
Octreotide disposition was best described by a two-compartment model with first-order elimination.; CAM2029 release was characterized by two simultaneous first-order absorption processes, while octreotide IR had a single pathway.; Simulated steady-state average concentration for 20 mg CAM2029 Q4W was similar to 0.25 mg octreotide IR every 8 h, with reduced daily fluctuation.; Octreotide bioavailability for CAM2029 was approximately 5-6 fold higher than octreotide LAR.
92% (12/13) of dogs with available histopathology had intestinal lymphangiectasia.; Octreotide was prescribed at a median dose of 20 μg/kg SQ daily.; Adverse effects occurred in 17% of dogs, leading to drug discontinuation in one case.; Clinical signs improved in 50% (6/12) of dogs with follow-up data.
Octreotide is a somatostatin analog with targeting and therapeutic abilities.; Octreotide-based radioactive conjugates are used clinically to detect small neuroendocrine tumour sites.; Various Octreotide-derived delivery strategies have been explored for tumour targeted therapeutics or diagnostics.; The review covers preclinical nanosystems including drug delivery, diagnostic, therapeutic, and multifunctional types.
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 the secretion o
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 9,301 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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