Lanreotide is a medication used in the management of acromegaly and symptoms caused by neuroendocrine tumors, most notably carcinoid syndrome. It is a long-acting analog of somatostatin. It is available in several countries, including the United Kingdom, Australia and Canada, and was approved for sale in the United States by the Food and Drug Administration on August 30, 2007. Lanreotide was developed in the lab of Dr. David H. Coy, School of Medicine. Dr. Coy serves as Director of the Peptide Laboratory. Lanreotide (as lanreotide acetate) is manufactured by Ipsen, and marketed under the trade name Somatuline. 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 SSTR 2 and 5 is the primary mechanism believed responsible for GH inhibition. Like somatostatin, lanreotide is an inhibitor of various endocrine, neuroendocrine, exocrine and paracrine functions. Lanreotide inhibits the basal secretion of motilin, gastric inhibitory peptide and pancreatic polypeptide, but has no significant effect on the secretion of secretin. Lanreotide inhibits postprandial secretion of pancreatic polypeptide, gastrin and cholecystokinin (CCK). In healthy subjects, lanreotide produces a reduction and a delay in post-prandial insulin secretion, resulting in transient, mild glucose intolerance.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL1792 |
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Target ID: CHEMBL1804 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | SOMATULINE DEPOT Approved UseSomatuline Depot (lanreotide) Injection 60 mg, 90 mg and 120 mg is indicated for the long-term treatment of acromegalic patients who have had an inadequate response to surgery and/or radiotherapy, or for whom surgery and/or radiotherapy is not an option. The goal of treatment in acromegaly is to reduce growth hormone (GH) and insulin growth factor-1 (IGF-1) levels to normal. Somatuline Depot (lanreotide) Injection is a somatostatin analog indicated for: the long-term treatment of acromegalic patients who have had an inadequate response to or cannot be treated with surgery and/or radiotherapy (1) Launch Date2007 |
PubMed
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Effectiveness of long-acting octreotide in suppressing hormonogenesis and tumor growth in thyrotropin-secreting pituitary adenomas: report of two cases. | 2001 Aug |
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[Estimation of efficacy of the octreotide LAR administration in the patients with somatotropinoma]. | 2001 Aug |
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Serum levels of tumor necrosis factor-alpha, soluble intercellular adhesion molecule-1, soluble vascular cell adhesion molecule-1, and soluble interleukin-1 receptor antagonist in patients with thyroid eye disease undergoing treatment with somatostatin analogues. | 2001 Dec |
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[Lanreotide acetate may cure cystic dystrophy in heterotopic pancreas of the duodenal wall]. | 2001 Dec |
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Somatostatin analogs and radiopeptides in cancer therapy. | 2002 |
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Carcinoid tumors--somatostatine in the diagnosis and therapy. | 2002 |
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Experience with indium-111 and yttrium-90-labeled somatostatin analogs. | 2002 |
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Carcinoid of the pancreas. | 2002 |
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Treatment of malignant endocrine pancreatic tumors with a combination of alpha-interferon and somatostatin analogs. | 2002 |
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Effect of the somatostatin analogue lanreotide on meal-stimulated portal blood flow in patients with liver cirrhosis. | 2002 |
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[Somatuline(R) Autogel(R), a new formulation of lanreotide for the treatment of acromegalic patients]. | 2002 Apr |
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[Regulation of cell proliferation by somatostatin]. | 2002 Apr |
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Somatostatins and their role in thyroid cancer. | 2002 Apr |
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In- and Y-DOTA-lanreotide: results and implications of the MAURITIUS trial. | 2002 Apr |
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Radiolabeled peptides in diagnosis and tumor imaging: clinical overview. | 2002 Apr |
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Human somatostatin receptor specificity of backbone-cyclic analogues containing novel sulfur building units. | 2002 Apr 11 |
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Varying additive effects of bromocriptine with two somatostatin analogs in cultures of GH-secreting adenomas. | 2002 Aug |
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Management of thyroid eye disease. | 2002 Aug |
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Carcinoid tumors. | 2002 Aug |
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New approaches in targeting intracerebral tumours with 90Y-labelled radiopeptides. | 2002 Dec |
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Improvement of left ventricular hypertrophy and arrhythmias after lanreotide-induced GH and IGF-I decrease in acromegaly. A prospective multi-center study. | 2002 Dec |
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Evaluation of lanreotide effects on human exocrine pancreatic secretion after a single dose: preliminary study. | 2002 Feb |
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Drug design at peptide receptors: somatostatin receptor ligands. | 2002 Feb-Apr |
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Somatostatin analogs in acromegaly. | 2002 Jul |
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Ectopic growth hormone-releasing hormone secretion by thymic carcinoid tumour. | 2002 Jul |
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Lanreotide labeled with 99mTc: preparation, preclinical testing and comparison with (111)In-DTPA-octreotide. | 2002 Jul-Aug |
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Effects of two different somatostatin analogs on glucose tolerance in acromegaly. | 2002 Jun |
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Somatuline Autogel: an extended release lanreotide formulation. | 2002 Mar |
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Effect of a six-month treatment with lanreotide on cardiovascular risk factors and arterial intima-media thickness in patients with acromegaly. | 2002 Mar |
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Partial tachyphylaxis to somatostatin (SST) analogues in a patient with acromegaly: the role of SST receptor desensitisation and circulating antibodies to SST analogues. | 2002 Mar |
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Somatostatin analogs and prednisone in advanced refractory thymic tumors. | 2002 Mar 1 |
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The clinical role of somatostatin analogues as antineoplastic agents: much ado about nothing? | 2002 May |
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Somatostatin, but not somatostatin receptor subtypes 2 and 5 selective agonists, inhibits calcitonin secretion and gene expression in the human medullary thyroid carcinoma cell line, TT. | 2002 May |
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[Diurnal rhythm of endogenous somatostatin in patients with carcinoid]. | 2002 May |
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Elimination of vascular fibrointimal hyperplasia by somatostatin receptor 1,4-selective agonist. | 2002 May |
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[Novel pharmacologic therapies in acromegaly]. | 2002 May 12 |
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Carcinoid tumors and syndrome. | 2002 May-Jun |
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Labeling and quality control of 188Re-lanreotide. | 2002 Nov |
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Somatostatin receptor genes are expressed in lymphocytes from retroorbital tissues in Graves' disease. | 2002 Nov |
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Somatostatin analogs in the treatment of medullary thyroid carcinoma. | 2002 Oct |
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Serum leptin levels in acromegaly--a significant role for adipose tissue and fasting insulin/glucose ratio. | 2002 Oct |
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[Current treatment of carcinoid tumor]. | 2002 Oct |
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Use of octreotide and lanreotide in the treatment of symptomatic non-resectable carcinoid tumours. | 2002 Sep |
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Short-term suppression of GH and IGF-I levels improves gonadal function and sperm parameters in men with acromegaly. | 2002 Sep |
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Long-term safety and efficacy of depot long-acting somatostatin analogs for the treatment of acromegaly. | 2002 Sep |
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Glucagonoma syndrome: diagnosis and treatment. | 2003 Feb |
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Somatostatin receptors (sst2) are coupled to Go and modulate GTPase activity in the rabbit retina. | 2003 Feb |
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Sandostatin LAR (long-acting octreotide acetate) for malignant carcinoid syndrome: a 3-year experience. | 2003 Feb |
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The effect of the somatostatin analogue lanreotide on the prevention of urethral strictures in a rabbit model. | 2003 Mar |
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[The role of somatostatin analogues in the treatment of hypophyseal adenomas]. | 2003 Mar |
Patents
Sample Use Guides
Patients should begin treatment with Somatuline Depot (lanreotide) 90 mg given via the deep subcutaneous route, at 4 week intervals for 3 months. After 3 months dosage may be adjusted as follows:
• GH >1 to ≤ 2.5 ng/mL, IGF-1 normal and clinical symptoms controlled: maintain. Somatuline Depot dose at 90 mg every 4 weeks.
• GH > 2.5 ng/mL, IGF-1 elevated and/or clinical symptoms uncontrolled, increase Somatuline Depot dose to 120 mg every 4 weeks.
• GH ≤ 1 ng/mL, IGF-1 normal and clinical symptoms controlled: reduce Somatuline Depot dose to 60 mg every 4 weeks.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/?term=19528243
Treatment with lanreotide alone at doses of either 100 or 1000 nM for 48 h reduced clonogenic survival by 5–10%. Radiation alone produced a dose-dependent survival curve with a SF2 of 48–55%, and lanreotide had no effect on this curve. The addition of lanreotide resulted in a 23% increase in the proportion of apoptotic sub-G1 cells following irradiation.
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FDA ORPHAN DRUG |
347811
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ACTIVE MOIETY
SUBSTANCE RECORD