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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2012/06/11 11:50:06」(JST)

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Pegvisomant (trade name Somavert) is a growth hormone receptor antagonist used in the treatment of acromegaly.^[1] It is used if the tumor of the pituitary gland causing the acromegaly cannot be controlled with surgery or radiation, and the use of somatostatin analogues is unsuccessful. It is delivered as a powder that is mixed with water and injected under the skin.^[2]

Structure

Pegvisomant is a protein containing 191 amino acid residues to which several polyethylene glycol polymers have been covalently bound in order to slow clearance from the blood. The protein is a modified version of human growth hormone designed to bind to and block the growth hormone receptor. It is manufactured using genetically modified E. coli bacteria. The polyethylene glycol polymers are subsequently added chemically.^[2]

Mechanism of action

Pegvisomant blocks the action of growth hormone at the growth hormone receptor to reduce the production of IGF-1. IGF-1 is responsible for most of the symptoms of acromegaly thus normalising its levels is effective to control the symptoms.

Side effects

Side effects of Pegvisomant include reactions at the injection site, swelling of the limbs, chest pain, hypoglycemia, nausea and hepatitis.^[3]

Blocking of the growth hormone's receptor reduces feedback control of the growth hormone regulation leading to approximately doubled GH levels.^[4]

References

^ Schreiber, I; Buchfelder M, Droste M et al. (January 2007). "Treatment of acromegaly with the GH receptor antagonist pegvisomant in clinical practice: safety and efficacy evaluation from the German Pegvisomant Observational Study". European Journal of Endocrinology 156 (1): 75–82. DOI:10.1530/eje.1.02312. PMID 17218728. http://www.eje-online.org/cgi/content/full/156/1/75?maxtoshow=&HITS=10&hits=10&RESULTFORMAT=&author1=Schreiber&andorexactfulltext=and&searchid=1&FIRSTINDEX=0&sortspec=relevance&volume=156&resourcetype=HWCIT.
^ ^a ^b "Scientific Discussion of Somavert". European Medicines Agency. 2004. http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Scientific_Discussion/human/000409/WC500054625.pdf.
^ Feenstra, J; Van Aken, MO; De Herder, WW; Feelders, RA; Van Der Lely, AJ (2006). "Drug-induced hepatitis in an acromegalic patient during combined treatment with pegvisomant and octreotide long-acting repeatable attributed to the use of pegvisomant". European Journal of Endocrinology 154 (6): 805–806. DOI:10.1530/eje.1.02160. PMID 16728538. edit
^ Moore, D.; Adi, Y.; Connock, M.; Bayliss, S. (2009). "Clinical effectiveness and cost-effectiveness of pegvisomant for the treatment of acromegaly: a systematic review and economic evaluation". BMC endocrine disorders 9: 20. DOI:10.1186/1472-6823-9-20. PMC 2768727. PMID 19814797. //www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2768727. edit

UpToDate Contents

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1. 先端巨大症の治療 treatment of acromegaly
2. 下垂体巨人症 pituitary gigantism
3. 患者情報：先端肥大症（詳細） acromegaly beyond the basics

English Journal

Pegvisomant and cabergoline combination therapy in acromegaly.

Bernabeu I, Alvarez-Escolá C, Paniagua AE, Lucas T, Pavón I, Cabezas-Agrícola JM, Casanueva FF, Marazuela M.SourceEndocrinology Department, Complejo Hospitalario Universitario de Santiago de Compostela (SERGAS), Travesía de la Choupana s/n, 15706, Santiago de Compostela, Spain, ignacio.bernabeu.moron@sergas.es.
Pituitary.Pituitary.2013 Mar;16(1):101-8. doi: 10.1007/s11102-012-0382-z.
Combination with cabergoline may offer additional benefits to acromegalic patients on pegvisomant monotherapy. We evaluated the safety and efficacy profile of this combination and investigated the determinants of response. An observational, retrospective, cross-sectional study. Fourteen acromegalic
PMID 22396133

Control of disease activity and tumor size after introduction of pegvisomant in a lanreotide-resistant acromegalic patient.

Fendri S, Karaca P, Tiev E, Buchfelder M, Lalau JD.SourceService d'endocrinologie-nutrition, hôpital Sud, université Picardie-Jules-Verne, centre hospitalier universitaire, 80054 Amiens, France.
Annales d'endocrinologie.Ann Endocrinol (Paris).2013 Feb;74(1):49-52. doi: 10.1016/j.ando.2012.10.002. Epub 2013 Jan 18.
We report on a 30-year-old female acromegalic patient treated with the growth hormone (GH) receptor antagonist pegvisomant at a low dose after the failure of long-acting lanreotide, neurosurgery and radiotherapy treatment to restore IGF-1 levels. The combination treatment was well tolerated and prod
PMID 23337021

Optic neuropathy in McCune-Albright syndrome: effects of early diagnosis and treatment of growth hormone excess.

Boyce AM, Glover M, Kelly MH, Brillante BA, Butman JA, Fitzgibbon EJ, Brewer CC, Zalewski CK, Cutler Peck CM, Kim HJ, Collins MT.SourceSkeletal Clinical Studies Unit, Craniofacial and Skeletal Diseases Branch, National Institute of Dental and Craniofacial Research, National Institutes of Health (NIH), Bethesda, Maryland 20892, USA. aboyce@childrensnational.org
The Journal of clinical endocrinology and metabolism.J Clin Endocrinol Metab.2013 Jan;98(1):E126-34. doi: 10.1210/jc.2012-2111. Epub 2012 Oct 23.
CONTEXT: GH excess is a serious complication of McCune-Albright syndrome (MAS) and has been associated with craniofacial morbidity.OBJECTIVE: The aim of the study was to determine whether early diagnosis and treatment of MAS-associated GH excess prevents optic neuropathy and hearing impairment, the
PMID 23093488

Japanese Journal

Poorly-controlled Acromegaly Accompanied by Subclinical Adrenal Cushing's Syndrome after Surgery for Multiple Endocrine Tumors

, , , , , , ,
Internal Medicine 54(6), 617-620, 2015
… Her GH and insulin-like growth factor-1 levels were insufficiently controlled, and pegvisomant was administered in addition to octreotide acetate. …
NAID 130004903084

下垂体腺腫の最前線

松野彰
Neuro-Oncologyの進歩 21(1), 29-39, 2014
… Long-acting octreotide, lanreotide and pegvisomant are now available for growth hormone producing adenoma. …
NAID 130004648362

下垂体腺腫に対する薬物療法 : 現状と課題

富永篤,木下康之,碓井智,栗栖薫
脳神経外科ジャーナル = Japanese journal of neurosurgery 22(2), 101-108, 2013-02-20
… 先端巨大症ではsomatostatin analogやpegvisomantなど有効率が高い薬剤があるが, 根治できないことが課題である. …
NAID 10031138807

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「ペグビソマント」

Pegvisomant
Clinical data
Trade names	Somavert
AHFS/Drugs.com	monograph
Pregnancy cat.	?
Legal status	?
Identifiers
CAS number	218620-50-9
ATC code	H01AX01
DrugBank	DB00082
UNII	N824AOU5XV
KEGG	D05394
ChEMBL	CHEMBL1201515
Chemical data
Formula	C990H1532N262O300S7
Mol. mass	22129.0 g/mol (unpegylated)
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　　[★]

英: pegvisomant
商: ソマバート
関: 成長ホルモン。その他のホルモン剤

[Schreiber-0] Schreiber, I; Buchfelder M, Droste M et al. (January 2007). "Treatment of acromegaly with the GH receptor antagonist pegvisomant in clinical practice: safety and efficacy evaluation from the German Pegvisomant Observational Study". European Journal of Endocrinology 156 (1): 75–82. DOI:10.1530/eje.1.02312. PMID 17218728. http://www.eje-online.org/cgi/content/full/156/1/75?maxtoshow=&HITS=10&hits=10&RESULTFORMAT=&author1=Schreiber&andorexactfulltext=and&searchid=1&FIRSTINDEX=0&sortspec=relevance&volume=156&resourcetype=HWCIT.

[ema-1] "Scientific Discussion of Somavert". European Medicines Agency. 2004. http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Scientific_Discussion/human/000409/WC500054625.pdf.

[2] Feenstra, J; Van Aken, MO; De Herder, WW; Feelders, RA; Van Der Lely, AJ (2006). "Drug-induced hepatitis in an acromegalic patient during combined treatment with pegvisomant and octreotide long-acting repeatable attributed to the use of pegvisomant". European Journal of Endocrinology 154 (6): 805–806. DOI:10.1530/eje.1.02160. PMID 16728538. edit

[3] Moore, D.; Adi, Y.; Connock, M.; Bayliss, S. (2009). "Clinical effectiveness and cost-effectiveness of pegvisomant for the treatment of acromegaly: a systematic review and economic evaluation". BMC endocrine disorders 9: 20. DOI:10.1186/1472-6823-9-20. PMC 2768727. PMID 19814797. //www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2768727. edit

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pegvisomant