Lanreotide
approvedAlso known as: Somatuline, BIM 23014
**Mechanism of Action** Lanreotide is a synthetic somatostatin analog with high affinity for somatostatin receptor subtypes 2 (SSTR2) and 5 (SSTR5). By activating these G-protein-coupled receptors, it inhibits adenylate cyclase activity, reducing cyclic AMP levels and suppressing the secretion of growth hormone (GH), insulin-like growth factor 1 (IGF-1), and various neuroendocrine hormones (e.g., serotonin, gastrin, vasoactive intestinal peptide). Its depot formulation provides sustained release, enabling prolonged receptor occupancy and downstream inhibition of tumor growth and hormone hypersecretion. **Key Research Findings** Clinical trials (e.g., the ELECT and CLARINET studies) demonstrated that lanreotide significantly reduces GH and IGF-1 levels in acromegaly, achieving biochemical control in ~50–60% of patients. In gastroenteropancreatic neuroendocrine tumors (GEP-NETs), the CLARINET trial (N=204) showed a 53% reduction in the risk of disease progression versus placebo (median progression-free survival not reached vs. 18 months). Additional studies confirm its efficacy in controlling carcinoid syndrome symptoms and improving quality of life, with a safety profile dominated by transient gastrointestinal effects and gallstone formation. **Clinical Relevance** Lanreotide is a first-line therapy for acromegaly and a standard treatment for unresectable, well-differentiated GEP-NETs. Its long-acting formulation (administered every 4 weeks) improves patient adherence compared to daily injections. It is also used off-label for other neuroendocrine tumors and polycystic liver disease. Ongoing research explores its role in combination therapies and earlier disease stages. For research purposes only — not medical advice.
Key data
C54H69N11O10S2Research & studies
Octreotide showed a strong association with necrotizing enterocolitis in neonates.; Pasireotide was significantly linked to acute pancreatitis and glucose metabolism disorders.; Elevated risks of liver and biliary tract infections were identified for somatostatin analogs.; Gastrointestinal and hepatobiliary adverse events were prominent across all three drugs.
High-resolution cryo-EM structures of SSTR1 with lanreotide and pasireotide were solved.; Each ligand induces unique conformational changes in the SSTR1 orthosteric pocket.; Comparative analysis highlights subtle differences in SSTR1 activation by the two analogs.; Insights support development of next-generation SSTR1-targeted therapies with enhanced selectivity and reduced side effects.
Pasireotide reduced tumor volume in all six patients with large, T2-hyperintense, sparsely granulated tumors.; GH and IGF-1 levels improved, and visual field defects normalized in all patients.; Hyperglycemia occurred, requiring antidiabetic treatment in two patients.; Pasireotide is effective as first-line therapy for selected acromegaly patients likely resistant to first-generation SRLs.
NET incidence increased from 6.98 to 8.3 per 100,000 between 2012 and 2018.; Most NET patients are diagnosed with metastatic disease, precluding curative surgery.; Pre-2017 treatments included somatostatin analogues, targeted therapy, and chemotherapy.; The 2017 WHO classification created a new category for well-differentiated grade 3 NETs (Ki67 > 20% and ≤55%), leaving treatment options undefined.
Frequently asked questions
What is Lanreotide?
**Mechanism of Action** Lanreotide is a synthetic somatostatin analog with high affinity for somatostatin receptor subtypes 2 (SSTR2) and 5 (SSTR5). By activating these G-protein-coupled receptors, it inhibits adenylate cyclase activity, reducing cyclic AMP levels and suppressing the secretion of growth hormone (GH), i
How does Lanreotide work?
Depot somatostatin analog inhibiting GH/IGF-1 and neuroendocrine secretion; approved for acromegaly and GEP-NETs.
What is the research status of Lanreotide?
Lanreotide is currently classified as approved, with 1,227 research references on record. This is for research purposes only and is not medical advice.
What is the molecular weight of Lanreotide?
Lanreotide has a molecular weight of approximately 1096.3 g/mol (formula C54H69N11O10S2).
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