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 |
|---|---|---|---|
Target ID: CHEMBL1792 |
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Target ID: CHEMBL1804 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| 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 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
38.3 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7826822/ |
30 mg single, intramuscular dose: 30 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
LANREOTIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
38 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16984213/ |
7 μg/kg single, intravenous dose: 7 μg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
LANREOTIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
4.246 ng/mL |
60 mg single, subcutaneous dose: 60 mg route of administration: Subcutaneous experiment type: SINGLE co-administered: |
LANREOTIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
8.391 ng/mL |
90 mg single, subcutaneous dose: 90 mg route of administration: Subcutaneous experiment type: SINGLE co-administered: |
LANREOTIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
6.785 ng/mL |
120 mg single, subcutaneous dose: 120 mg route of administration: Subcutaneous experiment type: SINGLE co-administered: |
LANREOTIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
3.053 ng/mL |
120 mg single, subcutaneous dose: 120 mg route of administration: Subcutaneous experiment type: SINGLE co-administered: |
LANREOTIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
3.543 ng/mL |
90 mg single, subcutaneous dose: 90 mg route of administration: Subcutaneous experiment type: SINGLE co-administered: |
LANREOTIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1.65 ng/mL |
60 mg single, subcutaneous dose: 60 mg route of administration: Subcutaneous experiment type: SINGLE co-administered: |
LANREOTIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
3.821 ng/mL |
60 mg 1 times / 4 weeks steady-state, subcutaneous dose: 60 mg route of administration: Subcutaneous experiment type: STEADY-STATE co-administered: |
LANREOTIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
5.694 ng/mL |
90 mg 1 times / 4 weeks steady-state, subcutaneous dose: 90 mg route of administration: Subcutaneous experiment type: STEADY-STATE co-administered: |
LANREOTIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
3.053 ng/mL |
120 mg 1 times / 4 weeks steady-state, subcutaneous dose: 120 mg route of administration: Subcutaneous experiment type: STEADY-STATE co-administered: |
LANREOTIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
65.98 ng × day/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7826822/ |
30 mg single, intramuscular dose: 30 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
LANREOTIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
22.1 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16984213/ |
7 μg/kg single, intravenous dose: 7 μg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
LANREOTIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1904.98 ng × h/mL |
60 mg single, subcutaneous dose: 60 mg route of administration: Subcutaneous experiment type: SINGLE co-administered: |
LANREOTIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
2984.35 ng × h/mL |
90 mg single, subcutaneous dose: 90 mg route of administration: Subcutaneous experiment type: SINGLE co-administered: |
LANREOTIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
3552.26 ng × h/mL |
120 mg single, subcutaneous dose: 120 mg route of administration: Subcutaneous experiment type: SINGLE co-administered: |
LANREOTIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
48.49 ng × day/mL |
120 mg single, subcutaneous dose: 120 mg route of administration: Subcutaneous experiment type: SINGLE co-administered: |
LANREOTIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
37.29 ng × day/mL |
90 mg single, subcutaneous dose: 90 mg route of administration: Subcutaneous experiment type: SINGLE co-administered: |
LANREOTIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
22.27 ng × day/mL |
60 mg single, subcutaneous dose: 60 mg route of administration: Subcutaneous experiment type: SINGLE co-administered: |
LANREOTIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
68.79 ng × day/mL |
60 mg 1 times / 4 weeks steady-state, subcutaneous dose: 60 mg route of administration: Subcutaneous experiment type: STEADY-STATE co-administered: |
LANREOTIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
85.11 ng × day/mL |
90 mg 1 times / 4 weeks steady-state, subcutaneous dose: 90 mg route of administration: Subcutaneous experiment type: STEADY-STATE co-administered: |
LANREOTIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
4.523 ng × day/mL |
120 mg 1 times / 4 weeks steady-state, subcutaneous dose: 120 mg route of administration: Subcutaneous experiment type: STEADY-STATE co-administered: |
LANREOTIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
4.52 day EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7826822/ |
30 mg single, intramuscular dose: 30 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
LANREOTIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
1.03 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16984213/ |
7 μg/kg single, intravenous dose: 7 μg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
LANREOTIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
664 h |
60 mg single, subcutaneous dose: 60 mg route of administration: Subcutaneous experiment type: SINGLE co-administered: |
LANREOTIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
860 h |
90 mg single, subcutaneous dose: 90 mg route of administration: Subcutaneous experiment type: SINGLE co-administered: |
LANREOTIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
816 h |
120 mg single, subcutaneous dose: 120 mg route of administration: Subcutaneous experiment type: SINGLE co-administered: |
LANREOTIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
19% |
unknown, unknown |
LANREOTIDE plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
PubMed
| Title | Date | PubMed |
|---|---|---|
| The effect of the somatostatin analogue lanreotide on the prevention of urethral strictures in a rabbit model. | 2003-03 |
|
| [The role of somatostatin analogues in the treatment of hypophyseal adenomas]. | 2003-03 |
|
| Glucagonoma syndrome: diagnosis and treatment. | 2003-02 |
|
| Somatostatin receptors (sst2) are coupled to Go and modulate GTPase activity in the rabbit retina. | 2003-02 |
|
| Sandostatin LAR (long-acting octreotide acetate) for malignant carcinoid syndrome: a 3-year experience. | 2003-02 |
|
| New approaches in targeting intracerebral tumours with 90Y-labelled radiopeptides. | 2002-12 |
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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. | 2002-12 |
|
| [Effect of lanreotide on prolactin level in patients with pituitary mixed tumors]. | 2002-12 |
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| Labeling and quality control of 188Re-lanreotide. | 2002-11 |
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| Radiolabeled peptides in the diagnosis and therapy of oncological diseases. | 2002-11 |
|
| Somatostatin receptor genes are expressed in lymphocytes from retroorbital tissues in Graves' disease. | 2002-11 |
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| Somatostatin analogs in the treatment of medullary thyroid carcinoma. | 2002-10 |
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| Serum leptin levels in acromegaly--a significant role for adipose tissue and fasting insulin/glucose ratio. | 2002-10 |
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| [Current treatment of carcinoid tumor]. | 2002-10 |
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| Are somatostatin analogues (octreotide and lanreotide) effective in promoting healing of enterocutaneous fistulas? | 2002-09 |
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| Use of octreotide and lanreotide in the treatment of symptomatic non-resectable carcinoid tumours. | 2002-09 |
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| Short-term suppression of GH and IGF-I levels improves gonadal function and sperm parameters in men with acromegaly. | 2002-09 |
|
| Long-term safety and efficacy of depot long-acting somatostatin analogs for the treatment of acromegaly. | 2002-09 |
|
| Lanreotide labeled with 99mTc: preparation, preclinical testing and comparison with (111)In-DTPA-octreotide. | 2002-08-15 |
|
| Varying additive effects of bromocriptine with two somatostatin analogs in cultures of GH-secreting adenomas. | 2002-08 |
|
| Management of thyroid eye disease. | 2002-08 |
|
| Carcinoid tumors. | 2002-08 |
|
| Somatostatin analogs in acromegaly. | 2002-07 |
|
| Ectopic growth hormone-releasing hormone secretion by thymic carcinoid tumour. | 2002-07 |
|
| Carcinoid tumors and syndrome. | 2002-06-11 |
|
| Somatostatin analogues in the treatment of endocrine tumors of the gastrointestinal tract. | 2002-06 |
|
| Effects of two different somatostatin analogs on glucose tolerance in acromegaly. | 2002-06 |
|
| [Novel pharmacologic therapies in acromegaly]. | 2002-05-12 |
|
| The clinical role of somatostatin analogues as antineoplastic agents: much ado about nothing? | 2002-05 |
|
| 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. | 2002-05 |
|
| [Diurnal rhythm of endogenous somatostatin in patients with carcinoid]. | 2002-05 |
|
| Human somatostatin receptor specificity of backbone-cyclic analogues containing novel sulfur building units. | 2002-04-11 |
|
| Drug design at peptide receptors: somatostatin receptor ligands. | 2002-04-05 |
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| [Somatuline(R) Autogel(R), a new formulation of lanreotide for the treatment of acromegalic patients]. | 2002-04 |
|
| [Regulation of cell proliferation by somatostatin]. | 2002-04 |
|
| Somatostatins and their role in thyroid cancer. | 2002-04 |
|
| In- and Y-DOTA-lanreotide: results and implications of the MAURITIUS trial. | 2002-04 |
|
| Radiolabeled peptides in diagnosis and tumor imaging: clinical overview. | 2002-04 |
|
| Somatuline Autogel: an extended release lanreotide formulation. | 2002-03 |
|
| Evaluation of lanreotide effects on human exocrine pancreatic secretion after a single dose: preliminary study. | 2002-02 |
|
| Somatostatin analogs and radiopeptides in cancer therapy. | 2002 |
|
| Carcinoid tumors--somatostatine in the diagnosis and therapy. | 2002 |
|
| Experience with indium-111 and yttrium-90-labeled somatostatin analogs. | 2002 |
|
| Carcinoid of the pancreas. | 2002 |
|
| Treatment of malignant endocrine pancreatic tumors with a combination of alpha-interferon and somatostatin analogs. | 2002 |
|
| Effect of the somatostatin analogue lanreotide on meal-stimulated portal blood flow in patients with liver cirrhosis. | 2002 |
|
| 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. | 2001-12 |
|
| Decreased insulin requirements after LAR-octreotide but not after lanreotide in an acromegalic patient. | 2001-09 |
|
| Pituitary macroadenoma secreting thyrotropin and growth hormone: remission of bihormonal hypersecretion in response to lanreotide therapy. | 2001-09 |
|
| Effectiveness of long-acting octreotide in suppressing hormonogenesis and tumor growth in thyrotropin-secreting pituitary adenomas: report of two cases. | 2001-08 |
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.
| Substance Class |
Protein
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| Sequence Type | COMPLETE |
| Record UNII |
0G3DE8943Y
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Validated (UNII)
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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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H01CB03
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NDF-RT |
N0000175904
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C060347
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LANREOTIDE
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m6682
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Lanreotide
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ACTIVE MOIETY |
Structural Modifications
| Modification Type | Location Site | Location Type | Residue Modified | Extent | Fragment Name | Fragment Approval |
|---|---|---|---|---|---|---|
| AMINO ACID SUBSTITUTION | [1_1] | 3-(2-NAPHTHYL)-D-ALANINE | 571V312YMY | |||
| AMINO ACID SUBSTITUTION | [1_8] | THREONINAMIDE | G5H9PK5HEK | |||
| AMINO ACID SUBSTITUTION | [1_4] | TRYPTOPHAN, D- | 7NS97N9H1G |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| MOL_WEIGHT:NUMBER(CALCULATED) | CHEMICAL |
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| Molecular Formula | CHEMICAL |
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| Biological Half-life | PHARMACOKINETIC |
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