Lanreotide
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Synthetic cyclic octapeptide somatostatin analog; FDA-approved SSTR2-selective agonist for acromegaly and gastroenteropancreatic neuroendocrine tumors.
Quick Facts
| Property | Value |
|---|---|
| Also Known As | Somatuline Depot, Somatuline Autogel, lanreotide acetate, BIM-23014, Ipstyl |
| Category | Somatostatin analog |
| Sequence | D-2Nal-Cys-Tyr-D-Trp-Lys-Val-Cys-Thr-NH2 (cyclic via disulfide) |
| Molecular Weight | ~1096.34 Da |
| Molecular Formula | C54H69N11O10S2 |
| PubChem CID | 71349 |
| Administration | Deep SubQ (Autogel depot; self-injectable) |
| Typical Dose Range | 60-120 mg deep SubQ q28 days |
| Half-Life | ~23-30 days (Autogel depot formulation) |
| Storage | Refrigerate (2-8C); pre-filled syringe, ready-to-use |
| FDA Status | Approved (2007) — Somatuline Depot for acromegaly; (2014) for GEP-NETs |
| WADA Status | Not listed |
Mechanism of Action
Lanreotide is a synthetic octapeptide analog of native somatostatin with high selectivity for somatostatin receptor subtype 2 (SSTR2; Ki ~0.5 nM) and moderate affinity for SSTR5 (Ki ~5.2 nM). Its receptor binding profile is similar to octreotide, though structural differences (D-2-naphthylalanine substitution, valine at position 6, C-terminal amidation) confer distinct pharmacokinetic properties.
The Autogel formulation is an aqueous solution that forms a gel depot upon deep subcutaneous injection, providing sustained release over 28 days. This depot technology enables patient self-injection — a key differentiator from octreotide LAR, which requires intramuscular injection by a healthcare provider.
Through SSTR2 activation, lanreotide suppresses GH and IGF-1 secretion (acromegaly indication) and exerts antiproliferative effects on SSTR-positive neuroendocrine tumor cells. The landmark CLARINET trial (PMID 25014687) demonstrated significant prolongation of progression-free survival in GEP-NETs (HR 0.47, p < 0.001), establishing lanreotide as a first-line antitumor therapy beyond symptom control.
Downstream signaling mirrors that of other somatostatin analogs: inhibition of adenylyl cyclase, activation of phosphotyrosine phosphatases, cell cycle arrest via p27/p21 upregulation, and inhibition of angiogenesis through VEGF suppression.
Key Research Areas
- Gastroenteropancreatic NETs — CLARINET trial demonstrated antiproliferative activity with HR 0.47 for progression; extended follow-up (CLARINET OLE) showed median PFS of 32.8 months (PMID 33052555)
- Acromegaly — RCT evidence supporting biochemical control (GH + IGF-1 normalization) in 43% of treatment-naive patients at 52 weeks (PMID 19639415)
- Carcinoid syndrome symptom control — Effective in controlling diarrhea and flushing associated with functional NETs
- Thymic and bronchial NETs — Emerging data supporting activity in non-GEP neuroendocrine tumors
Evidence Level Summary
| Evidence Type | Count | Notes |
|---|---|---|
| Human RCTs | 2 | CLARINET (NETs) + Melmed acromegaly RCT |
| RCT extension | 1 | CLARINET OLE final results |
| Human observational | — | Extensive post-marketing data since 2007 |
| Systematic reviews | — | Multiple exist in literature (not yet in vault) |
Clinical Applications
- Cancer Adjunct Therapy — FDA-approved for GEP-NETs; antiproliferative therapy
Protocols Using This Peptide
- No Ageless Peps protocols (FDA-approved prescription drug, not a research peptide)
Ageless Peps Products
- Not sold — Lanreotide is an FDA-approved prescription medication (Somatuline Depot) manufactured by Ipsen. It is not a research peptide and is not available through Ageless Peps.
Dosing Reference
FDA-Approved Dosing
| Indication | Route | Dose | Frequency | Duration | Source |
|---|---|---|---|---|---|
| Acromegaly (initial) | Deep SubQ | 90 mg | q28 days | Titrate based on GH/IGF-1 | FDA label |
| Acromegaly (range) | Deep SubQ | 60-120 mg | q28 days | Ongoing | FDA label |
| GEP-NETs | Deep SubQ | 120 mg | q28 days | Until progression | FDA label |
Cycling
Not applicable — lanreotide is prescribed as continuous therapy. Dose adjustments for acromegaly are based on GH and IGF-1 levels. For NETs, the standard dose is 120 mg with no dose modification.
Contraindications & Safety
- Contraindications: Hypersensitivity to lanreotide, somatostatin, or related peptides
- Common side effects: Diarrhea (37-65%), abdominal pain (19%), cholelithiasis (14-27%), injection site reactions (9-22%), nausea, flatulence
- Drug interactions: May reduce cyclosporine levels; may alter insulin and oral hypoglycemic requirements; co-administration with bradycardia-inducing drugs requires monitoring
- Pregnancy/nursing: Category C; use only if benefit outweighs risk
- Special populations: No dose adjustment needed for renal or hepatic impairment per labeling; monitor glucose in diabetic patients
Synergistic Combinations
- Octreotide — Interchangeable first-generation somatostatin analog; head-to-head data show equivalent efficacy
- Pasireotide — Second-line option after lanreotide failure (broader SSTR binding)
- Lutetium-177-DOTATATE — PRRT can be used sequentially after lanreotide progression in SSTR-positive NETs
Related Research
| PMID | Title | Year | Study Type |
|---|---|---|---|
| 25014687 | CLARINET: Lanreotide for enteropancreatic NETs (landmark Phase III) | 2014 | RCT |
| 33052555 | CLARINET OLE: Final results of open-label extension | 2021 | RCT (extension) |
| 19639415 | Lanreotide Autogel RCT in acromegaly (52-week) | 2010 | RCT |
References
- PMID 25014687 — Caplin et al. CLARINET: Lanreotide antiproliferative in GEP-NETs (2014)
- PMID 33052555 — Caplin et al. CLARINET OLE final results (2021)
- PMID 19639415 — Melmed et al. Lanreotide Autogel RCT in acromegaly (2010)
Related
- Peptide Index
- Condition Index
- Protocol Index
- Cancer Adjunct Therapy
- Octreotide
- Pasireotide
- Lutetium-177-DOTATATE
FDA Disclaimer: Lanreotide (Somatuline Depot) is an FDA-approved prescription medication. The information in this note is for educational and reference purposes only and does not constitute medical advice. Prescribing and administration must be performed by qualified healthcare providers.
#peptide #gh-axis #fda-approved #not-sold #subq