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 Date1.18843205E12 |
PubMed
Title | Date | PubMed |
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Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies. | 1999 Nov |
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Established clinical use of octreotide and lanreotide in oncology. | 2001 |
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Different response to the long-acting somatostatin analogues lanreotide and octreotide in a patient with a malignant carcinoid. | 2001 |
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Pituitary gangliocytoma-adenoma presenting with acromegaly: response to treatment. | 2001 Apr 9 |
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[Lanreotide acetate may cure cystic dystrophy in heterotopic pancreas of the duodenal wall]. | 2001 Dec |
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[Somatostatin analogues for the treatment of gastro-entero-pancreatic neuroendocrine tumours]. | 2001 Dec |
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A combination therapy of dexamethasone and somatostatin analog reintroduces objective clinical responses to LHRH analog in androgen ablation-refractory prostate cancer patients. | 2001 Dec |
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Somatostatin octapeptides (lanreotide, octreotide, vapreotide, and their analogs) share the growth hormone-releasing peptide receptor in the human pituitary gland. | 2001 Feb |
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Cortistatin, but not somatostatin, binds to growth hormone secretagogue (GHS) receptors of human pituitary gland. | 2001 Jan |
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New trends in peptide receptor radioligands. | 2001 Jun |
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Administration of somatostatin analogue reduces uterine and myoma volume in women with uterine leiomyomata. | 2001 Mar |
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Antitumour activity of somatostatin analogues in progressive metastatic neuroendocrine tumours. | 2001 May |
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Effects of the somatostatin analog lanreotide on the circulating levels of chromogranin-A, prostate-specific antigen, and insulin-like growth factor-1 in advanced prostate cancer patients. | 2001 May 15 |
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[Therapy of pituitary diseases. What can be achieved with medication and hormones?]. | 2001 Nov 1 |
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Effectiveness of slow-release lanreotide in previously operated and untreated patients with GH-secreting pituitary macroadenoma. | 2001 Oct |
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Decreased insulin requirements after LAR-octreotide but not after lanreotide in an acromegalic patient. | 2001 Sep |
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Pituitary macroadenoma secreting thyrotropin and growth hormone: remission of bihormonal hypersecretion in response to lanreotide therapy. | 2001 Sep |
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Carcinoid tumors--somatostatine in the diagnosis and therapy. | 2002 |
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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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Somatostatin analogs in acromegaly. | 2002 Jul |
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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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Somatostatin analogs and prednisone in advanced refractory thymic tumors. | 2002 Mar 1 |
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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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Serum leptin levels in acromegaly--a significant role for adipose tissue and fasting insulin/glucose ratio. | 2002 Oct |
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Use of octreotide and lanreotide in the treatment of symptomatic non-resectable carcinoid tumours. | 2002 Sep |
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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LIVERTOX |
NBK548368
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FDA ORPHAN DRUG |
136300
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WHO-VATC |
QH01CB03
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NCI_THESAURUS |
C62799
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NDF-RT |
N0000000194
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WHO-ATC |
H01CB03
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NDF-RT |
N0000175904
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C060347
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LANREOTIDE
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Lanreotide
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ACTIVE MOIETY