Lanreotide

Mechanism (as reported)

A review of the peptide’s biological targeting describes its action as being mediated by affinity to somatostatin receptors, especially SSTR2 and SSTR5. [PMID 30582380] In preclinical work, lanreotide (as a targeting peptide) was described as having high affinity to somatostatin receptors such as SSTR2. [PMID 32919636]

Key findings (each cites a source)

• A randomized, double-blind, placebo-controlled multinational phase III study reported that lanreotide extended-release aqueous-gel formulation (Autogel/Depot) was associated with significantly prolonged progression-free survival versus placebo in metastatic enteropancreatic neuroendocrine tumors of grade 1 or 2 (Ki-67 <10%). [PMID 25014687]
• In the CLARINET open-label extension study, long-term data were reported for patients who entered the extension from the randomized CLARINET study, with median PFS reported in a lanreotide-treated cohort (LAN-LAN group) and safety/treatment-related adverse event incidence described as lower in the extension than in the core study. [PMID 33052555]
• Preclinical research reported that electrostatically bound gold nanoparticle–lanreotide peptide complexes showed higher cellular uptake in SSTR2-expressed cancer cells than in control cells lacking SSTR2 expression, and the increased uptake was associated with increased oxidative stress signals and preferential cytotoxicity in the tested cancer cell models. [PMID 32919636]
• A study of a lanreotide-derived SSTR2-targeting peptide modification for peptide-drug conjugate development reported that LanTC (a modified peptide derived from lanreotide) enabled high stability and high agonist affinity to SSTR2, and reported antitumor activity of the constructed LanTC-DM1 peptide-drug conjugate in small cell lung cancer models described as overexpressing SSTR2. [PMID 40533489]
• A cyclodextrin complexation study reported NMR spectroscopy findings consistent with aromatic side-chain inclusion interactions between lanreotide acetate and two beta-cyclodextrin derivatives, and docking analysis suggesting favorable 1:1 inclusion complex formation over higher-order complexes due to steric considerations. [PMID 39491674]
• A review described lanreotide as an eight-amino-acid peptide analog of native somatostatin, stating that its binding affinity for somatostatin receptors SSTR2 and SSTR5 is a primary mechanism considered in acromegaly, and summarized published clinical reports describing antisecretory responses and antitumoral effects in acromegaly. [PMID 19533047]
• A review stated that lanreotide autogel is a synthetic somatostatin analogue and described its action as being mediated by affinity to somatostatin receptors, especially SSTR2 and SSTR5, and discussed progression-free survival benefit compared to placebo in locally advanced or metastatic gastroenteropancreatic neuroendocrine tumors. [PMID 30582380]