What is the mechanism of action of Lanreotide (Somatostatin analogue)?

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From the Guidelines

Lanreotide is a synthetic analog of somatostatin that inhibits the secretion of various hormones, including growth hormone, insulin, glucagon, and gastrointestinal hormones, and is primarily used to treat conditions involving excessive hormone production, such as acromegaly and neuroendocrine tumors (NETs), including those that cause carcinoid syndrome. Lanreotide works by binding to somatostatin receptors on cell surfaces, which inhibits the secretion of various hormones. For acromegaly, it helps normalize growth hormone and insulin-like growth factor-1 levels when surgery is not an option or has been unsuccessful. For NETs, it helps control tumor growth and reduces the symptoms caused by excess hormone secretion. The most recent and highest quality study, 1, shows that lanreotide is effective in controlling tumor growth in patients with locally advanced or metastatic nonfunctioning pancreatic or intestinal NETs, with a median progression-free survival of over 27 months. Lanreotide is typically administered as a deep subcutaneous injection (Lanreotide Autogel/Somatuline Depot) every 4 weeks, with dosages ranging from 60 to 120 mg depending on the condition being treated and patient response. Common side effects include gastrointestinal disturbances (diarrhea, abdominal pain, nausea), injection site reactions, and potential gallstone formation with long-term use. The use of lanreotide has been recommended by several guidelines, including the European Society for Medical Oncology (ESMO) and the National Comprehensive Cancer Network (NCCN), for the treatment of NETs, including those that cause carcinoid syndrome. Some key points to consider when using lanreotide include:

  • Lanreotide can be used to control tumor growth in patients with locally advanced or metastatic NETs, including those with carcinoid syndrome.
  • The medication should be administered via deep subcutaneous injection every 4 weeks.
  • Dosages range from 60 to 120 mg, depending on the condition being treated and patient response.
  • Common side effects include gastrointestinal disturbances, injection site reactions, and potential gallstone formation with long-term use.
  • Lanreotide has been shown to improve progression-free survival in patients with NETs, with a median progression-free survival of over 27 months in one study 1.

From the FDA Drug Label

Lanreotide, the active component of SOMATULINE DEPOT is an octapeptide analog of natural somatostatin. The mechanism of action of lanreotide is believed to be similar to that of natural somatostatin. Lanreotide has a high affinity for human somatostatin receptors (SSTR) 2 and 5 and a reduced binding affinity for human SSTR1, 3, and 4. Activity at human SSTR2 and 5 is the primary mechanism believed responsible for GH inhibition. The primary pharmacodynamic effect of lanreotide is a reduction of GH and/or IGF-1 levels enabling normalization of levels in acromegalic patients.

Lanreotide inhibits various endocrine, neuroendocrine, exocrine, and paracrine functions. Its main effects include:

  • Reduction of GH and/or IGF-1 levels
  • Inhibition of basal secretion of motilin, gastric inhibitory peptide, and pancreatic polypeptide
  • Inhibition of postprandial secretion of pancreatic polypeptide, gastrin, and cholecystokinin (CCK)
  • Reduction and delay in postprandial insulin secretion
  • Inhibition of meal-stimulated pancreatic secretions
  • Reduction in duodenal bicarbonate and amylase concentrations
  • Transient reduction in gastric acidity
  • Inhibition of gallbladder contractility and bile secretion 2

From the Research

What is Lanreotide

  • Lanreotide is a synthetic somatostatin analogue used to control symptoms of patients with functional gastro-entero-pancreatic neuroendocrine tumors (GEP-NETs) 3.
  • It is also used for tumor growth control in advanced low/intermediate grade NET 4.

Mechanism of Action

  • Lanreotide works by binding to somatostatin receptors, especially sst2 and sst5 receptors, to suppress excess hormone secretion 5, 6.
  • It has a longer half-life, offering the convenience of 4-week dosing 6.

Effects on the Body

  • Lanreotide can decrease gastric acid secretion, abolish bile salts and lipase responses to a meal, and increase the duodeno-caecal transit time 7.
  • It can also decrease the duodenal absorption of carbohydrates and triglycerides 7.

Clinical Uses

  • Lanreotide is used to manage carcinoid symptoms and has a robust anti-tumor effect in NET 6.
  • It is also being studied for its potential use in preventing or treating pancreatic and bowel fistulas, as well as short bowel syndrome 7.

Safety and Efficacy

  • Lanreotide is generally well-tolerated with low rates of treatment discontinuation due to toxicity 6.
  • It offers a progression-free survival benefit in locally advanced or metastatic neuroendocrine tumor (NET) compared to placebo 6.

Professional Medical Disclaimer

This information is intended for healthcare professionals. Any medical decision-making should rely on clinical judgment and independently verified information. The content provided herein does not replace professional discretion and should be considered supplementary to established clinical guidelines. Healthcare providers should verify all information against primary literature and current practice standards before application in patient care. Dr.Oracle assumes no liability for clinical decisions based on this content.

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