LANREOTIDE ACETATE

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022074lbl.pdf

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
Somatostatin receptor 5 5 Target ID: CHEMBL1792 Sources: http://www.bccancer.bc.ca/drug-database-site/Drug%20Index/Lanreotide_monograph_14Jul2011.pdf	Agonist 2678
Somatostatin receptor 2 6 Target ID: CHEMBL1804 Sources: http://www.bccancer.bc.ca/drug-database-site/Drug%20Index/Lanreotide_monograph_14Jul2011.pdf	Agonist 2678

Conditions

Condition	Modality	Targets	Highest Phase	Product
Acromegaly 21 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022074lbl.pdf	Primary		Approved 8429	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

PubMed

Title	Date	PubMed
Effectiveness of long-acting octreotide in suppressing hormonogenesis and tumor growth in thyrotropin-secreting pituitary adenomas: report of two cases.	2001 Aug	12138986
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	12186498
Decreased insulin requirements after LAR-octreotide but not after lanreotide in an acromegalic patient.	2001 Sep	12501980
Pituitary macroadenoma secreting thyrotropin and growth hormone: remission of bihormonal hypersecretion in response to lanreotide therapy.	2001 Sep	12501978
Somatostatin analogs and radiopeptides in cancer therapy.	2002	12385036
Carcinoid tumors--somatostatine in the diagnosis and therapy.	2002	12190042
Experience with indium-111 and yttrium-90-labeled somatostatin analogs.	2002	12171531
Carcinoid of the pancreas.	2002	12123097
Treatment of malignant endocrine pancreatic tumors with a combination of alpha-interferon and somatostatin analogs.	2002	12025889
Effect of the somatostatin analogue lanreotide on meal-stimulated portal blood flow in patients with liver cirrhosis.	2002	11961344
[Somatuline(R) Autogel(R), a new formulation of lanreotide for the treatment of acromegalic patients].	2002 Apr	12037499
[Regulation of cell proliferation by somatostatin].	2002 Apr	12037498
Somatostatins and their role in thyroid cancer.	2002 Apr	11994118
In- and Y-DOTA-lanreotide: results and implications of the MAURITIUS trial.	2002 Apr	11965610
Radiolabeled peptides in diagnosis and tumor imaging: clinical overview.	2002 Apr	11965602
Human somatostatin receptor specificity of backbone-cyclic analogues containing novel sulfur building units.	2002 Apr 11	11931620
Varying additive effects of bromocriptine with two somatostatin analogs in cultures of GH-secreting adenomas.	2002 Aug	12198598
Management of thyroid eye disease.	2002 Aug	12192546
Carcinoid tumors.	2002 Aug	12074768
New approaches in targeting intracerebral tumours with 90Y-labelled radiopeptides.	2002 Dec	12599329
Improvement of left ventricular hypertrophy and arrhythmias after lanreotide-induced GH and IGF-I decrease in acromegaly. A prospective multi-center study.	2002 Dec	12553557
[Effect of lanreotide on prolactin level in patients with pituitary mixed tumors].	2002 Dec	12527855
Evaluation of lanreotide effects on human exocrine pancreatic secretion after a single dose: preliminary study.	2002 Feb	11926556
Drug design at peptide receptors: somatostatin receptor ligands.	2002 Feb-Apr	11931345
Somatostatin analogs in acromegaly.	2002 Jul	12107192
Ectopic growth hormone-releasing hormone secretion by thymic carcinoid tumour.	2002 Jul	12100081
Lanreotide labeled with 99mTc: preparation, preclinical testing and comparison with (111)In-DTPA-octreotide.	2002 Jul-Aug	12174893
Somatostatin analogues in the treatment of endocrine tumors of the gastrointestinal tract.	2002 Jun	12472080
Effects of two different somatostatin analogs on glucose tolerance in acromegaly.	2002 Jun	12109620
Somatuline Autogel: an extended release lanreotide formulation.	2002 Mar	11933820
The clinical role of somatostatin analogues as antineoplastic agents: much ado about nothing?	2002 May	12075733
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	12063634
[Diurnal rhythm of endogenous somatostatin in patients with carcinoid].	2002 May	12053490
[Novel pharmacologic therapies in acromegaly].	2002 May 12	12063860
Carcinoid tumors and syndrome.	2002 May-Jun	12055378
Labeling and quality control of 188Re-lanreotide.	2002 Nov	12619968
Radiolabeled peptides in the diagnosis and therapy of oncological diseases.	2002 Nov	12433051
Somatostatin receptor genes are expressed in lymphocytes from retroorbital tissues in Graves' disease.	2002 Nov	12414882
Somatostatin analogs in the treatment of medullary thyroid carcinoma.	2002 Oct	12398235
Serum leptin levels in acromegaly--a significant role for adipose tissue and fasting insulin/glucose ratio.	2002 Oct	12388920
[Current treatment of carcinoid tumor].	2002 Oct	12361534
Are somatostatin analogues (octreotide and lanreotide) effective in promoting healing of enterocutaneous fistulas?	2002 Sep	12510468
Use of octreotide and lanreotide in the treatment of symptomatic non-resectable carcinoid tumours.	2002 Sep	12269913
Short-term suppression of GH and IGF-I levels improves gonadal function and sperm parameters in men with acromegaly.	2002 Sep	12213870
Long-term safety and efficacy of depot long-acting somatostatin analogs for the treatment of acromegaly.	2002 Sep	12213862
Glucagonoma syndrome: diagnosis and treatment.	2003 Feb	12582409
Somatostatin receptors (sst2) are coupled to Go and modulate GTPase activity in the rabbit retina.	2003 Feb	12562507
Sandostatin LAR (long-acting octreotide acetate) for malignant carcinoid syndrome: a 3-year experience.	2003 Feb	12562458
The effect of the somatostatin analogue lanreotide on the prevention of urethral strictures in a rabbit model.	2003 Mar	12624660
[The role of somatostatin analogues in the treatment of hypophyseal adenomas].	2003 Mar	12621362

Patents

Sample Use Guides

In Vivo Use Guide

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

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 `Sat Dec 16 00:14:48 GMT 2023` Edited by `admin` on `Sat Dec 16 00:14:48 GMT 2023`
Protein Sub Type
Sequence Type	COMPLETE
Record UNII	IEU56G3J9C
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

LANREOTIDE ACETATE

Official 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, ACETATE (SALT)

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, ACETATE (SALT)

Common Name

English

SOMATULINE

Brand Name

English

LANREOTIDE ACETATE [USAN]

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, ACETATE (1:2)

Systematic Name

English

LANREOTIDE ACETATE [ORANGE BOOK]

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, ACETATE (SALT)

Common Name

English

SOMATULINE LP

Brand Name

English

Lanreotide acetate [WHO-DD]

Common Name

English

LANREOTIDE ACETATE [JAN]

Common Name

English

SOMATULINE DEPOT

Brand Name

English

LANREOTIDE ACETATE [MART.]

Common Name

English

LANREOTIDE ACETATE [MI]

Common Name

English

SOMATULINE AUTOGEL

Brand 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, ACETATE (SALT)

Common Name

English

BIM-23014C

Code

English

Classification Tree Code System Code

NCI_THESAURUS

C62799