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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2017/04/09 10:44:59」(JST)

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Lanreotide (INN) is a medication used in the management of acromegaly and symptoms caused by neuroendocrine tumors, most notably carcinoid syndrome. It is a long-acting analogue of somatostatin, like octreotide. Its sequence is H-D-2Nal-Cys(1)-Tyr-D-Trp-Lys-Val-Cys(1)-Thr-NH2.

Lanreotide (as lanreotide acetate) is manufactured by Ipsen, and marketed under the trade name Somatuline. 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 (FDA) on August 30, 2007.^[1]

Pharmacology

Lanreotide is a synthetic analogue of somatostatin, a naturally occurring inhibitory hormone which blocks the release of several other hormones, including growth hormone, thyroid-stimulating hormone (TSH), insulin and glucagon. Lanreotide binds to the same receptors as somatostatin, although with higher affinity to peripheral receptors, and has similar activity. However, while somatostatin is quickly broken down in the body (within minutes),^[2] lanreotide has a much longer half-life, and produces far more prolonged effects.

The efficacy of lanreotide has not been extensively studied, and results differ greatly between trials and formulations.^{[citation needed]}

Indications

Lanreotide is used in the treatment of acromegaly, due to both pituitary and non-pituitary growth hormone-secreting tumors, and the management of symptoms caused by neuroendocrine tumors, particularly carcinoid tumors and VIPomas. In the United States and Canada, lanreotide is only indicated for the treatment of acromegaly. In the United Kingdom, it is also indicated in the treatment of thyrotrophic adenoma,^[3] a rare tumor of the pituitary gland which secretes TSH.

Lanreotide also shows activity against non-endocrine tumors, and, along with other somatostatin analogues, is being studied as a possible general antitumor agent.^[4]^[5]

In Dec 2014 the US FDA approved lanreotide for the treatment of patients with unresectable, well or moderately differentiated, locally advanced or metastatic gastroenteropancreatic neuroendocrine tumors (GEP-NETs).^[6]

It is used for polycystic liver disease. It has also been shown that it reduces the volume by 264mls on average.

Side effects

The main side effects of lanreotide treatment are mild to moderate pain at the injection site and gastrointestinal disturbances, such as diarrhea, nausea and vomiting. Isolated cases of gallstone formation have been associated with use of lanreotide, particularly over long periods of time.^[3]

Formulations

Lanreotide is available in two formulations: a sustained release formulation (sold under the trade name 'Somatuline LA'), which is injected intramuscularly every ten or fourteen days,^[3] and an extended release formulation (UK trade name 'Somatuline Autogel', or 'Somatuline Depot' in the U.S.), which is administered subcutaneously once a month.^[7]

Self-assembling properties

Lanreotide has been shown to spontaneously self-assemble into monodisperse nanotubes of 24.4 nm diameter^[8] and has been thereafter used as a fruitful and versatile model system in several biophysical studies.

References

^ "FDA Approves New Drug to Treat Rare Disease, Acromegaly" (Press release). U.S. Food and Drug Administration. August 30, 2007. Retrieved 2007-09-06.
^ Rens-Domiano S, Reisine T (1992). "Biochemical and functional properties of somatostatin receptors". J Neurochem. 58 (6): 1987–96. doi:10.1111/j.1471-4159.1992.tb10938.x. PMID 1315373.
^ ^a ^b ^c "Somatuline LA". electronic Medicines Compendium. September 17, 2003. Retrieved 2007-03-02.
^ Kvols L, Woltering E (2006). "Role of somatostatin analogs in the clinical management of non-neuroendocrine solid tumors". Anticancer Drugs. 17 (6): 601–8. doi:10.1097/01.cad.0000210335.95828.ed. PMID 16917205.
^ Susini C, Buscail L (2006). "Rationale for the use of somatostatin analogs as antitumor agents". Ann Oncol. 17 (12): 1733–42. doi:10.1093/annonc/mdl105. PMID 16801334.
^ "FDA Approves Lanreotide Injection for GEP-NETs". 2014.
^ "Somatuline Autogel". electronic Medicines Compendium. April 12, 2007. Retrieved 2007-04-19.
^ Valéry C, Paternostre M, Robert B, Gulik-Krzywicki T, Narayanan T, Dedieu JC, Keller G, Torres ML, Cherif-Cheikh R, Calvo P, Artzner F (2003). "Biomimetic organization: Octapeptide self-assembly into nanotubes of viral capsid-like dimension". Proceedings of the National Academy of Sciences of the United States of America. 100 (18): 10258–62. doi:10.1073/pnas.1730609100. PMC 193548. PMID 12930900.

External links

www.AcromegalyCommunity.com: Emotional and communal support for those touched by Acromegaly- page discussing drug, side effects, and prescription programs
Home page for Somatuline in the U.S.
Somatuline Package insert prescribing information available in PDF format.
FDA press release

UpToDate Contents

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1. 転移性の胃腸系神経内分泌腫瘍（カルチノイド）：腫瘍増殖およびホルモン過剰分泌による症状を管理するための全身治療の選択肢 metastatic gastrointestinal neuroendocrine carcinoid tumors systemic therapy options to control tumor growth and symptoms of hormone hypersecretion
2. ソマトスタチンの生理学とその類縁体 physiology of somatostatin and its analogues
3. 先端巨大症の治療 treatment of acromegaly
4. 転移性膵神経内分泌腫瘍および低分化胃腸膵管神経内分泌腫瘍：腫瘍増殖をコントローするための全身療法およびホルモン分泌過剰の症状 metastatic pancreatic neuroendocrine tumors and poorly differentiated gastroenteropancreatic neuroendocrine carcinomas systemic therapy options to control tumor growth and symptoms of hormone hypersecretion
5. カルチノイド症候群の治療 treatment of the carcinoid syndrome

English Journal

Systematic review and meta-analysis of the role of somatostatin and its analogues in the treatment of enterocutaneous fistula.

Stevens P, Foulkes RE, Hartford-Beynon JS, Delicata RJ.SourceDepartment of General Surgery, Nevill Hall Hospital, Abergavenny, Wales, UK.
European journal of gastroenterology & hepatology.Eur J Gastroenterol Hepatol.2011 Oct;23(10):912-22.
OBJECTIVE: Somatostatin analogues may help pancreatic fistula although it remains unclear whether they help nonpancreatic fistula. This study involved meta-analysis of somatostatin analogues for treatment of enterocutaneous fistula.METHODS: Meta-analysis of studies was undertaken, to estimate the ef
PMID 21814141

Conversion of daily pegvisomant to weekly pegvisomant combined with long-acting somatostatin analogs, in controlled acromegaly patients.

Neggers SJ, de Herder WW, Feelders RA, van der Lely AJ.SourceDepartment of Medicine, Erasmus University Medical Center Rotterdam, PO box 2040, 3000 CA, Rotterdam, The Netherlands, s.neggers@erasmusmc.nl.
Pituitary.Pituitary.2011 Sep;14(3):253-8.
The efficacy of combined treatment in active acromegaly with both long-acting somatostatin analogs (SRIF) and pegvisomant (PEG-V) has been well established. The aim was to describe the PEG-V dose reductions after the conversion from daily PEG-V to combination treatment. To clarify the individual ben
PMID 21221818

Japanese Journal

Inhibition of early preneoplastic events in the rat liver by the somatostatin analog lanreotide

BORBATH Ivan,LECLERCQ Isabelle A.,ABARCA-QUINONES Jorge,DESAEGER Christine,LEBRUN Valerie,MOULIN Pierre,SEMPOUX Christine,HORSMANS Yves
Cancer science 98(12), 1831-1839, 2007-12-10
NAID 10019995976

Long-term Treatment of Acromegaly with Lanreotide : Evidence of Increased Serum Parathormone Concentration

CAPPELLI CARLO,GANDOSSI ELENA,AGOSTI BARBARA,CERUDELLI BRUNO,CUMETTI DAVIDE,CASTELLANO MAURIZIO,PIROLA ILENIA,MARTINO ELVIRA DE,AGABITI ROSEI ENRICO
Endocrine journal 51(6), 517-520, 2004-12-01
NAID 10014080305

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「ランレオチド」

Lanreotide
Clinical data
Trade names	Somatuline
AHFS/Drugs.com	Monograph
License data	US FDA: Lanreotide;
Pregnancy; category	AU: C; US: C (Risk not ruled out); ;
Routes of; administration	Intramuscular, subcutaneous
ATC code	H01CB03 (WHO);
Legal status
Legal status	UK: POM (Prescription only); US: ℞-only;
Pharmacokinetic data
Bioavailability	Approximately 80%
Protein binding	78%
Metabolism	In GI tract
Biological half-life	2 hours (immediate release); 5 days (sustained release)
Excretion	Mostly biliary
Identifiers
	IUPAC name 3-(2-naphthyl)-D-alanyl-L-cysteinyl-L-tyrosyl-D-tryptophyl-L-lysyl-L-valyl-L-cysteinyl-L-threoninamide (2->7)-disulfide;
CAS Number	108736-35-2 ;
PubChem CID	71349;
IUPHAR/BPS	2031;
ChemSpider	64450 ;
UNII	0G3DE8943Y;
ChEMBL	CHEMBL1201185 ;
ECHA InfoCard	100.215.992
Chemical and physical data
Formula	C54H69N11O10S2
Molar mass	1096.33 g/mol; 1156.380 g/mol (acetate)
3D model (Jmol)	Interactive image;
	SMILES C[C@H]([C@@H](C(=O)N)NC(=O)[C@@H]1CSSC[C@@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)C(C)C)CCCCN)Cc2c[nH]c3c2cccc3)Cc4ccc(cc4)O)NC(=O)[C@@H](Cc5ccc6ccccc6c5)N)O ;
	InChI InChI=1S/C54H69N11O10S2/c1-29(2)45-54(75)63-44(53(74)65-46(30(3)66)47(57)68)28-77-76-27-43(62-48(69)38(56)23-32-15-18-33-10-4-5-11-34(33)22-32)52(73)60-41(24-31-16-19-36(67)20-17-31)50(71)61-42(25-35-26-58-39-13-7-6-12-37(35)39)51(72)59-40(49(70)64-45)14-8-9-21-55/h4-7,10-13,15-20,22,26,29-30,38,40-46,58,66-67H,8-9,14,21,23-25,27-28,55-56H2,1-3H3,(H2,57,68)(H,59,72)(H,60,73)(H,61,71)(H,62,69)(H,63,75)(H,64,70)(H,65,74)/t30-,38-,40+,41+,42-,43+,44+,45+,46+/m1/s1 ; Key:PUDHBTGHUJUUFI-SCTWWAJVSA-N ;
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英: lanreotide
商: ソマチュリン

[1] "FDA Approves New Drug to Treat Rare Disease, Acromegaly" (Press release). U.S. Food and Drug Administration. August 30, 2007. Retrieved 2007-09-06.

[2] Rens-Domiano S, Reisine T (1992). "Biochemical and functional properties of somatostatin receptors". J Neurochem. 58 (6): 1987–96. doi:10.1111/j.1471-4159.1992.tb10938.x. PMID 1315373.

[eMC_LA-3] "Somatuline LA". electronic Medicines Compendium. September 17, 2003. Retrieved 2007-03-02.

[4] Kvols L, Woltering E (2006). "Role of somatostatin analogs in the clinical management of non-neuroendocrine solid tumors". Anticancer Drugs. 17 (6): 601–8. doi:10.1097/01.cad.0000210335.95828.ed. PMID 16917205.

[5] Susini C, Buscail L (2006). "Rationale for the use of somatostatin analogs as antitumor agents". Ann Oncol. 17 (12): 1733–42. doi:10.1093/annonc/mdl105. PMID 16801334.

[6] "FDA Approves Lanreotide Injection for GEP-NETs". 2014.

[7] "Somatuline Autogel". electronic Medicines Compendium. April 12, 2007. Retrieved 2007-04-19.

[8] Valéry C, Paternostre M, Robert B, Gulik-Krzywicki T, Narayanan T, Dedieu JC, Keller G, Torres ML, Cherif-Cheikh R, Calvo P, Artzner F (2003). "Biomimetic organization: Octapeptide self-assembly into nanotubes of viral capsid-like dimension". Proceedings of the National Academy of Sciences of the United States of America. 100 (18): 10258–62. doi:10.1073/pnas.1730609100. PMC 193548. PMID 12930900.

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lanreotide