Lanreotide
Also known as: Somatuline, Somatuline Depot, Somatuline Autogel, BIM-23014, lanreotide acetate, lanreotide autogel, lanreotide ATG
Synthetic somatostatin analog; cyclic octapeptide; hormonal antineoplastic and antisecretory agent
What it is
Lanreotide (Somatuline) is a monthly injection used by people with rare hormonal tumors called neuroendocrine tumors or acromegaly — a condition caused by a pituitary tumor producing too much growth hormone. It works by mimicking a natural hormone that slows hormone overproduction and tumor growth. FDA-approved for both conditions.
The scientific side
lanreotide is a synthetic octapeptide analog of native somatostatin-14 that exerts its effects through high-affinity binding to somatostatin receptor subtypes 2 and 5 (SSTR2 and SSTR5). These G-protein-coupled receptors are broadly expressed on pituitary somatotroph cells and on gastroenteropancreatic neuroendocrine tumor cells, making them critical pharmacological targets. At SSTR2 and SSTR5 on pituitary somatotrophs, lanreotide potently suppresses growth hormone (GH) secretion and, downstream, reduces hepatic production of insulin-like growth factor 1 (IGF-1) — the principal mediator of acromegaly symptoms including soft tissue swelling, arthropathy, and cardiovascular enlargement. Antisecretory efficacy — defined as normalization of GH and/or IGF-1 — is reported in 35–70% of treated acromegaly patients, with wide variability reflecting differences in tumor SSTR subtype expression and prior treatment status (PMID 19533047). In GEP-NETs, which predominantly overexpress SSTR2 (PMID 14713257), lanreotide produces both antisecretory effects — controlling hormone-excess symptoms such as flushing and diarrhea in carcinoid syndrome — and a direct antiproliferative effect. The antiproliferative mechanism involves receptor-mediated inhibition of cell-cycle progression, induction of apoptosis, and suppression of angiogenic signaling. The pivotal CLARINET Phase III trial (n=204, PMID 25014687) demonstrated that 120 mg lanreotide autogel every 28 days produced a statistically and clinically significant prolongation of progression-free survival versus placebo (median PFS not reached vs. 18 months; hazard ratio 0.47, 95% CI 0.30–0.73, p<0.001) in patients with non-functioning, well-to-moderately-differentiated GEP-NETs. The long-acting extended-release aqueous-gel formulation (Autogel/Depot) achieves sustained therapeutic plasma concentrations via a slow-release depot mechanism following a single deep subcutaneous injection, enabling monthly dosing over the shorter injection intervals required for first-generation somatostatin analogs (PMID 18191325, 30582380). Lanreotide's receptor binding profile is distinct from octreotide: both share high SSTR2 affinity, but differences in SSTR5 binding and pharmacokinetic profiles result in clinically meaningful distinctions in individual patient response.
Class: Synthetic somatostatin analog; cyclic octapeptide; hormonal antineoplastic and antisecretory agent
Administration & storage
- Administration
- Deep subcutaneous injection into the superior outer quadrant of the buttock — the approved and standard route for Somatuline DepotAlternating sides (left/right) on successive injections for site rotationSelf-injection by the patient at home is an approved option following healthcare provider training; systematic review (Europe PMC PPR523821) confirmed comparable safety and tolerability for home vs. healthcare-setting injection
- Storage
- Refrigerate at 2–8°C (36–46°F) until use. Remove from refrigerator 30 minutes before injection. Do not freeze. Protect from light. The pre-filled syringe is intended for single use only.
- Cautions
- Cholelithiasis and biliary sludge: somatostatin analogs inhibit gallbladder motility and bile secretion; lanreotide increases the risk of gallstone formation with chronic use. Periodic ultrasound monitoring is recommended.,Hyperglycemia and hypoglycemia: lanreotide alters the balance of insulin, glucagon, and GH secretion. Blood glucose monitoring is recommended, particularly at initiation; pre-existing diabetes may require insulin dose adjustment.,Bradycardia: somatostatin analogs can reduce heart rate; monitor patients with baseline sinus bradycardia or those on beta-blockers or calcium channel blockers.,Hypothyroidism: thyroid function should be monitored during lanreotide therapy in acromegaly patients, as GH reduction may unmask or contribute to central hypothyroidism.,Injection site reactions: pain, nodule formation, and induration at the deep subcutaneous injection site are reported; site rotation and correct deep injection technique minimize this risk.,Diarrhea, abdominal pain, nausea: gastrointestinal adverse effects are the most common adverse events, particularly in the first weeks of therapy, and are generally mild-to-moderate in severity (PMID 30582380).,Alopecia: reported with SSA therapy, mechanism unclear, generally reversible.,Drug interactions: lanreotide may reduce cyclosporine bioavailability via slowed intestinal absorption; monitor cyclosporine levels at initiation and after dose changes.
Legal & regulatory status
FDA-approved (NDA) as Somatuline Depot (lanreotide injection) 120 mg for: (1) acromegaly in patients for whom surgery and/or radiotherapy are not an option or have failed to achieve adequate disease control; (2)…
Lanreotide is not listed on the current WADA Prohibited List as a performance-enhancing substance. It is a prescription-only therapeutic agent used under medical supervision for acromegaly and neuroendocrine tumors. Its…
Somatuline Autogel is approved by Health Canada for treatment of acromegaly and for symptomatic relief of patients with carcinoid syndrome; approved under the brand name Somatuline Autogel. Health Canada approval is…
What it's studied for
- Acromegaly — biochemical control of GH and IGF-1 hypersecretion Phase III RCT / regulatory approval
- Gastroenteropancreatic neuroendocrine tumors (GEP-NETs) — antiproliferative / progression-free survival Phase III RCT (pivotal)
- Carcinoid syndrome — symptomatic control of flushing and diarrhea Clinical evidence / observational and comparative studies
- Neuroendocrine tumor — quality of life and patient-reported outcomes Systematic review
- Lanreotide receptor pharmacology — somatostatin receptor subtype targeting in GEP-NETs Basic/translational science
Safety signals
- Cholelithiasis and biliary complications
- Gastrointestinal adverse effects (diarrhea, abdominal pain, nausea, steatorrhea)
- Glycemic dysregulation (hyperglycemia and hypoglycemia)
- Bradycardia and cardiac conduction effects
- Injection site reactions
- Hypothyroidism
Contraindications
About these dose ranges
Dose ranges below reflect commonly reported community protocols. Where published research cites a specific dose, the PMID is linked. Doses without citations are not clinical recommendations — they reflect what practitioners and researchers commonly report using.
Community-reported dosing
| Route | Dose | Frequency / Duration | Population / context | Source tier |
|---|---|---|---|---|
| Unspecified | 90–120 mg extended-release aqueous gel | — | Adults with acromegaly | Research |
| Unspecified | 120 mg extended-release aqueous gel | — | Adults with GEP-NETs | Research |
| deep subcutaneous injection (superior outer quadrant of buttock) | 90 mg titrated to 120 mg | every 28 days; may extend to every 42–56 days if well controlled | adults with acromegaly inadequately controlled by surgery and/or radiotherapy | |
| deep subcutaneous injection (superior outer quadrant of buttock) | 120 mg | every 28 days; dose intensification to every 14 days considered in progressive disease | adults with unresectable, well- or moderately-differentiated, locally advanced or metastatic GEP-NETs |