Octreotide
Synthetic octapeptide somatostatin analog with a longer half-life than endogenous somatostatin. FDA- and EMA-approved since the 1980s for acromegaly and neuroendocrine tumours.
Mechanism of action
Octreotide is a cyclic octapeptide that selectively binds somatostatin-receptor subtypes SSTR2 and SSTR5. Via G-protein-coupled signalling, adenylyl cyclase is inhibited, reducing the secretion of multiple hormones (growth hormone, IGF-1, glucagon, insulin, VIP, serotonin). Structural stabilisation via a disulfide bridge and D-amino acids extends the half-life relative to natural somatostatin (minutes to several hours).
Evidence at a glance
What the studies show
Where studies disagree
Does octreotide's symptom benefit outweigh its long-term downsides?
Pharmacokinetics
Theoretical concentration curve at a half-life of 1.7 h. Pure pharmacokinetic model — not a dosing recommendation.
Open in PK tool →Routes of administration in the literature
Amounts reported in sources
Safer use & risks
Known adverse events from studies
Interactions & combinations
Regulatory voices
Sandostatin LAR Depot is indicated for the symptomatic improvement (flushing, diarrhoea) in patients with metastatic carcinoid syndrome and for the treatment of profuse watery diarrhoea associated with VIPoma.
The CLARINET trial demonstrated a statistically significant prolongation of progression-free survival — a finding that has since shaped the clinical use of somatostatin analogs in first-line NET treatment.
Legal status by country
Reconstitution calculator
Peptides ship as a dry powder. Once dissolved in a liquid (reconstitution), this calculator answers a single question: how much substance is in one millilitre of solution afterwards?
- 1Enter the vial's substance amount (printed on the label).
- 2Enter how much solvent you add.
- 3Result = concentration in mg per mL.
Cofactors
These cofactors relate to the peptide class, not to a specific use. No recommendation, no dosing.
Study register
Placebo-controlled, double-blind, prospective, randomized study on the effect of octreotide LAR in the control of tumor growth in patients with metastatic neuroendocrine midgut tumors (PROMID)
SMS 201-995: a very potent and selective octapeptide analogue of somatostatin with prolonged action
Lanreotide in metastatic enteropancreatic neuroendocrine tumors (CLARINET)
Somatostatin Analogs in Acromegaly and NET — EMA / FDA Label Reviews
Sources & method
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