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.
74 patients met inclusion criteria, of whom 27 (36.5%) received octreotide.; Kaplan-Meier analysis showed no significant effect of octreotide on chest tube duration (P = 0.890), hospital length of stay (P = 0.740), or overall survival (P = 0.570).; Multivariable Cox regression corroborated no effect on chest tube duration (HR = 0.62, 95% CI: 0.32-1.20, P = 0.155), hospital length of stay (HR = 0.64, CI: 0.34-1.21, P = 0.168), or overall survival (HR = 1.08, CI: 0.53-2.19, P = 0.833).; Octreotide use in adult patients with chyle leak following esophagectomy lacks evidence of association with meaningful clinical outcomes, and Level 1 evidence is needed prior to further consideration in this population.
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.
Mycapssa is the first FDA-approved oral octreotide capsule for acromegaly, offering a twice-daily alternative to injections.; Oral octreotide capsules maintain consistent biochemical normalization of IGF-1 and GH levels across multiple trials.; Safety profiles of oral octreotide capsules are similar to injected somatostatin receptor ligands.; Limited data exist on efficacy and tolerability in female or pediatric-specific populations.
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.
Octreotide altered ~300 salivary proteins with p < .05 and ~50 with FDR-corrected p < .05.; Four isoforms of human cystatins showed significantly lower abundance after octreotide treatment.; Downregulation of cystatins may decrease inhibition of cysteine proteases like Cathepsin S, potentially enhancing wound healing.
Octreotide has been administered in doses ranging from 0.5 g/kg/h to >20 g/kg/h in neonates with chylothorax.; Both low- and high-dose octreotide were effective in resolving chylothorax with little to no side effects.; Reported side effects, when they occurred, were less significant in nature and scope.; The authors recommend titrating octreotide safely to a maximum of 20 g/kg/h without significant side effects.
Three of seven patients completed asparaginase treatment without pancreatitis recurrence; four experienced recurrence despite prophylactic octreotide.; A PubMed literature search identified four additional patients successfully re-administered asparaginase with octreotide.; Prophylactic octreotide may be warranted for patients who would benefit from asparaginase re-administration.; Careful observation is needed to monitor for breakthrough recurrence of pancreatitis.
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 9,383 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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