U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS
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.

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
SOMATULINE DEPOT

Approved Use

Somatuline 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 Date

2007
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
38.3 ng/mL
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
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

AUC

ValueDoseCo-administeredAnalytePopulation
65.98 ng × day/mL
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
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

T1/2

ValueDoseCo-administeredAnalytePopulation
4.52 day
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
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

Funbound

ValueDoseCo-administeredAnalytePopulation
19%
unknown, unknown
LANREOTIDE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
PubMed

PubMed

TitleDatePubMed
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
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
Labeling and quality control of 188Re-lanreotide.
2002-11
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
Somatostatin analogs in the treatment of medullary thyroid carcinoma.
2002-10
Serum leptin levels in acromegaly--a significant role for adipose tissue and fasting insulin/glucose ratio.
2002-10
[Current treatment of carcinoid tumor].
2002-10
Are somatostatin analogues (octreotide and lanreotide) effective in promoting healing of enterocutaneous fistulas?
2002-09
Use of octreotide and lanreotide in the treatment of symptomatic non-resectable carcinoid tumours.
2002-09
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
[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

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
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
Created
by admin
on Mon Mar 31 20:33:59 GMT 2025
Edited
by admin
on Mon Mar 31 20:33:59 GMT 2025
Protein Sub Type
Sequence Type COMPLETE
Record UNII
0G3DE8943Y
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
LANREOTIDE
INN   MART.   MI   VANDF   WHO-DD  
INN  
Official Name English
ANGIOPEPTIN
Preferred Name English
LANREOTIDE [MI]
Common Name English
lanreotide [INN]
Common Name English
L-THREONINAMIDE, 3-(2-NAPHTHALENYL)-D-ALANYL-L-CYSTEINYL-L-TYROSYL-D-TRYPTOPHYL-L-LYSYL-L-VALYL-L-CYSTEINYL-, CYCLIC (2->7)-DISULPHIDE
Common Name English
LANREOTIDE [VANDF]
Common Name English
3-(2-NAPHTHYL)-D-ALANYL-L-CYSTEINYL-L-TYROSYL-D-TRYPTOPHYL-L-LYSYL-L-VALYL-L-CYSTEINYL-L-THREONINAMIDE, CYCLIC (2->7)-DISULPHIDE
Common Name English
3-(2-NAPHTHYL)-D-ALANYL-L-CYSTEINYL-L-TYROSYL-D-TRYPTOPHYL-L-LYSYL-L-VALYL-L-CYSTEINYL-L-THREONINAMIDE, CYCLIC (2->7)-DISULFIDE
Common Name English
Lanreotide [WHO-DD]
Common Name English
L-THREONINAMIDE, 3-(2-NAPHTHALENYL)-D-ALANYL-L-CYSTEINYL-L-TYROSYL-D-TRYPTOPHYL-L-LYSYL-L-VALYL-L-CYSTEINYL-, CYCLIC (2->7)-DISULFIDE
Common Name English
LANREOTIDE [MART.]
Common Name English
Classification Tree Code System Code
LIVERTOX NBK548368
Created by admin on Mon Mar 31 20:33:59 GMT 2025 , Edited by admin on Mon Mar 31 20:33:59 GMT 2025
FDA ORPHAN DRUG 136300
Created by admin on Mon Mar 31 20:33:59 GMT 2025 , Edited by admin on Mon Mar 31 20:33:59 GMT 2025
WHO-VATC QH01CB03
Created by admin on Mon Mar 31 20:33:59 GMT 2025 , Edited by admin on Mon Mar 31 20:33:59 GMT 2025
NCI_THESAURUS C62799
Created by admin on Mon Mar 31 20:33:59 GMT 2025 , Edited by admin on Mon Mar 31 20:33:59 GMT 2025
NDF-RT N0000000194
Created by admin on Mon Mar 31 20:33:59 GMT 2025 , Edited by admin on Mon Mar 31 20:33:59 GMT 2025
WHO-ATC H01CB03
Created by admin on Mon Mar 31 20:33:59 GMT 2025 , Edited by admin on Mon Mar 31 20:33:59 GMT 2025
NDF-RT N0000175904
Created by admin on Mon Mar 31 20:33:59 GMT 2025 , Edited by admin on Mon Mar 31 20:33:59 GMT 2025
Code System Code Type Description
MESH
C060347
Created by admin on Mon Mar 31 20:33:59 GMT 2025 , Edited by admin on Mon Mar 31 20:33:59 GMT 2025
PRIMARY
WIKIPEDIA
LANREOTIDE
Created by admin on Mon Mar 31 20:33:59 GMT 2025 , Edited by admin on Mon Mar 31 20:33:59 GMT 2025
PRIMARY
RXCUI
68092
Created by admin on Mon Mar 31 20:33:59 GMT 2025 , Edited by admin on Mon Mar 31 20:33:59 GMT 2025
PRIMARY RxNorm
SMS_ID
100000082556
Created by admin on Mon Mar 31 20:33:59 GMT 2025 , Edited by admin on Mon Mar 31 20:33:59 GMT 2025
PRIMARY
PUBCHEM
6918011
Created by admin on Mon Mar 31 20:33:59 GMT 2025 , Edited by admin on Mon Mar 31 20:33:59 GMT 2025
PRIMARY
INN
6649
Created by admin on Mon Mar 31 20:33:59 GMT 2025 , Edited by admin on Mon Mar 31 20:33:59 GMT 2025
PRIMARY
MERCK INDEX
m6682
Created by admin on Mon Mar 31 20:33:59 GMT 2025 , Edited by admin on Mon Mar 31 20:33:59 GMT 2025
PRIMARY Merck Index
ChEMBL
CHEMBL1201185
Created by admin on Mon Mar 31 20:33:59 GMT 2025 , Edited by admin on Mon Mar 31 20:33:59 GMT 2025
PRIMARY
EPA CompTox
DTXSID60897514
Created by admin on Mon Mar 31 20:33:59 GMT 2025 , Edited by admin on Mon Mar 31 20:33:59 GMT 2025
PRIMARY
EVMPD
SUB08402MIG
Created by admin on Mon Mar 31 20:33:59 GMT 2025 , Edited by admin on Mon Mar 31 20:33:59 GMT 2025
PRIMARY
DRUG BANK
DB06791
Created by admin on Mon Mar 31 20:33:59 GMT 2025 , Edited by admin on Mon Mar 31 20:33:59 GMT 2025
PRIMARY
DAILYMED
0G3DE8943Y
Created by admin on Mon Mar 31 20:33:59 GMT 2025 , Edited by admin on Mon Mar 31 20:33:59 GMT 2025
PRIMARY
NCI_THESAURUS
C1523
Created by admin on Mon Mar 31 20:33:59 GMT 2025 , Edited by admin on Mon Mar 31 20:33:59 GMT 2025
PRIMARY
FDA UNII
0G3DE8943Y
Created by admin on Mon Mar 31 20:33:59 GMT 2025 , Edited by admin on Mon Mar 31 20:33:59 GMT 2025
PRIMARY
DRUG CENTRAL
1546
Created by admin on Mon Mar 31 20:33:59 GMT 2025 , Edited by admin on Mon Mar 31 20:33:59 GMT 2025
PRIMARY
IUPHAR
2031
Created by admin on Mon Mar 31 20:33:59 GMT 2025 , Edited by admin on Mon Mar 31 20:33:59 GMT 2025
PRIMARY
CAS
108736-35-2
Created by admin on Mon Mar 31 20:33:59 GMT 2025 , Edited by admin on Mon Mar 31 20:33:59 GMT 2025
PRIMARY
LACTMED
Lanreotide
Created by admin on Mon Mar 31 20:33:59 GMT 2025 , Edited by admin on Mon Mar 31 20:33:59 GMT 2025
PRIMARY
Related Record Type Details
PARENT -> DERIVATIVE
Related Record Type Details
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
Molecular Formula CHEMICAL
Biological Half-life PHARMACOKINETIC