Octreotide (Sandostatin, Sandostatin LAR, Mycapssa, Bynfezia Pen)
Octreotide acetate (SMS 201-995); synonyms: L-Cysteinamide, D-phenylalanyl-L-cysteinyl-L-phenylalanyl-D-tryptophyl-L-lysyl-L-threonyl-N-[2-hydroxy-1-(hydroxymethyl)propyl]-, cyclic (2->7)-disulfide; [R-(R*,R*)] acetate salt
Octreotide is an FDA-approved synthetic somatostatin analogue that suppresses growth hormone, IGF-1, and gastrointestinal hormones, used primarily for acromegaly, carcinoid tumors, and VIPomas (StatPearls NBK544333; FDA NDA 019667).
Last updated: 2026-03-13
Safety Summary
Gastrointestinal side effects (diarrhea, nausea, abdominal discomfort) are the most common, occurring in 34-61% of acromegalic patients, though they tend to resolve with continued treatment and are less frequent with lower doses. Only 2.6% of patients discontinued due to GI symptoms (FDA label 2024). Gallbladder abnormalities are the most clinically significant long-term concern, with 63% developing biliary tract abnormalities (27% gallstones, 24% sludge, 12% duct dilatation) and 52% incidence with treatment >12 months (FDA label 2024). Cardiac effects include sinus bradycardia in 25% of acromegalic patients, with conduction abnormalities in 10% and arrhythmias in 9%; QT prolongation and other ECG changes have been observed (FDA label 2024). A new warning for steatorrhea and malabsorption of dietary fats was added to the label in July 2024, recommending evaluation for pancreatic exocrine insufficiency (FDA label 2024). Postmarketing reports include complete AV block (primarily with IV use at higher doses during surgical procedures), hypoxia, necrotizing enterocolitis, and death in pediatric patients under 2 years (FDA label 2024,;). Antibodies develop in up to 25% of SC-treated patients (77-81% nasal, 27% SC) but usually without clinical effect. No potential for abuse or dependence has been identified. Long-term safety monitoring should include thyroid function (TSH, free T4), glucose levels, gallbladder ultrasound, and vitamin B12 levels (FDA label 2024).
Known Side Effects
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Who Should NOT Use This
Only absolute contraindication per FDA label. Anaphylactoid reactions including anaphylactic shock have been reported.
Octreotide may decrease cyclosporine blood levels via altered nutrient absorption, potentially resulting in transplant rejection. Monitor cyclosporine levels.
Octreotide inhibits insulin and glucagon secretion, requiring glucose monitoring and potential dose adjustment of anti-diabetic medications.
Additive bradycardia effects. Dose adjustments of beta-blockers may be necessary.
Octreotide competitively binds somatostatin receptors and may interfere with Lu-177 dotatate efficacy. Must discontinue octreotide at least 24 hours prior to each Lu-177 dotatate dose.
Somatostatin analogues may decrease metabolic clearance of CYP3A4 substrates via GH suppression.
Limited human data insufficient to inform drug-associated risk. Animal studies showed no adverse developmental effects at 7-13x MRHD. Transient growth retardation in rat offspring at doses below MRHD.
Half-life increased and clearance reduced by ~50% in dialysis patients. Maintenance dose adjustment necessary.
Half-life increased to 3.7 hours and clearance decreased to 5.9 L/h. Dose adjustment may be needed.
Octreotide inhibits gallbladder contractility and decreases bile secretion. Discontinue if complications of cholelithiasis are suspected.
Talk to Your Doctor
Before considering Octreotide (Sandostatin, Sandostatin LAR, Mycapssa, Bynfezia Pen), discuss it with your healthcare provider. Ask about potential interactions with your current medications, whether it is appropriate for your health conditions, and what monitoring may be needed.
Sources: [1-9]
Evidence Assessment
Octreotide is FDA-approved (NDA 019667 approved 1988, Sandostatin LAR approved 1998, Mycapssa NDA 208232 approved 2020, Bynfezia Pen NDA 213224 approved 2024) for acromegaly, carcinoid tumors, and VIPomas. It has over 30 years of clinical use supported by multiple Phase III randomized controlled trials and extensive post-marketing surveillance. It is also on the WHO Essential Medicines List.
1Safety and Efficacy of Octreotide LAR in Treatment Naive Acromegalic PatientsNCT00128232
Novartis; PI: Stephan Petersenn - ClinicalTrials.gov (2005) - Phase III, single-arm, interventional - 100
Evaluated octreotide LAR in treatment-naive acromegaly patients. Assessed mean GH and IGF-1 at baseline, 12, 24, and 48 weeks, plus tumor volume changes.
Limitations: Non-randomized, single-arm design. No placebo comparator.
2Does Surgical Debulking of Pituitary Adenomas Improve Responsiveness to Octreotide LAR in Treatment of AcromegalyNCT01371643
David M Kleinberg; NYU Langone Health - ClinicalTrials.gov (2011) - Phase IV, randomized, open-label, multicenter - 41 (15 medical, 26 surgical)
Surgical debulking dramatically improved octreotide LAR response: 50% response rate in surgery-first arm vs 6.7% in medical-only arm (GH nadir <1 ng/mL + normal IGF-1). With all treatments combined: 76.9% vs 6.7% response.
Limitations: Small sample size, open-label design, multicenter variability.
3Safety and efficacy of oral octreotide in acromegaly: results of a multicenter phase III trialPMID 25664604
Melmed S et al. - J Clin Endocrinol Metab (2022) - Phase III, multicenter - 155
65% of patients maintained IGF-1 response with oral octreotide capsules (Mycapssa) as maintenance therapy after switching from injectable SSAs. Supported FDA approval of oral formulation.
Limitations: Maintenance study design (patients pre-selected as SSA responders).
4177Lu-Dotatate versus high-dose long-acting octreotide for treatment of patients with advanced GEP-NET (XT-XTR008-3-01)PMID 41111031
Not specified in raw data - Not specified (2025) - Phase III, randomized, open-label - Not specified in raw data
Compared 177Lu-DOTATATE vs high-dose octreotide LAR in advanced, well-differentiated Grade 1-2 GEP-NET. Results pending/recently published.
Limitations: Open-label design.
5SORENTO: Randomized Phase 3 Trial of Octreotide SC Depot (CAM2029) vs Octreotide LAR or Lanreotide ATG in GEP-NETNCT05050942
Singh S, Ferone D, Capdevila J, Chan JA, de Herder WW et al.; Camurus AB - Trials (2024) - Phase III, randomized, open-label, active-controlled, multicenter - 332 enrolled
Comparing CAM2029 (octreotide SC depot 20mg q2w) vs standard octreotide LAR 30mg or lanreotide ATG 120mg q4w. Primary endpoint: PFS by BIRC. Active, not yet recruiting completion.
Limitations: Open-label. Results not yet available.
6Pharmacokinetics of the long-acting somatostatin analogue octreotide (SMS 201-995) in acromegalyPMID 2364560
Nicholls J, Wynick D, Domin J, Sandler LM, Bloom SR - Clin Endocrinol (Oxf) (1990) - Pharmacokinetic study - Not specified in raw data
Characterized octreotide PK in acromegaly: Vd 21.6 +/- 8.5 L, clearance 18 L/h, t1/2 ~1.8h. Peak 2.8 ng/mL at 0.7h after 100 mcg SC.
Limitations: Small sample size typical of PK studies.
7Octreotide LAR as Maintenance Treatment After First-line Chemotherapy for Patients With NECNCT02409849
Shen Lin; Peking University - ClinicalTrials.gov (2015) - Phase II, randomized, open-label - 92 estimated
Evaluated octreotide LAR 30mg q28d as maintenance after first-line chemo in unresectable/metastatic GEP or esophageal NEC. Primary endpoint: PFS.
Limitations: Status unknown (last updated 2015). May not have completed enrollment.
8ACROINNOVA 1: Phase 3 Trial of CAM2029 (octreotide subcutaneous depot)NCT04125836
Ferone D, et al. - J Clin Endocrinol Metab (2023) - RCT - 72
72.2% of patients on once-monthly CAM2029 depot achieved IGF-1 <= ULN versus 37.5% on placebo (p=0.0018).
Limitations: Data extraction limitations.
9OPTIMAL Trial: Oral Octreotide CapsulesNCT03252353
Not listed - ClinicalTrials.gov (2020) - RCT - 56
58% maintained IGF-1 response on oral octreotide capsules vs 19% on placebo (p=0.008).
Limitations: Study primarily evaluated maintenance of effect in previously controlled patients.