Pegvisomant

Identification

Summary

Pegvisomant is a growth hormone receptor antagonist used to treat acromegaly.

Brand Names

Somavert

Generic Name

Pegvisomant

DrugBank Accession Number

DB00082

Background

Pegvisomant is a highly selective growth hormone (GH) receptor antagonist. It is used to treat acromegaly. Unlike dopamine or somatostatin analogs (which inhibit growth hormone secretion), this drug actually blocks the hepatic (GH-mediated) production of insulin like growth factor (IGF-1), which is the main mediator of growth hormone activity.

Type

Biotech

Groups

Approved

Biologic Classification

Protein Based Therapies
Hormones

Protein Structure

Protein Chemical Formula: C₉₉₀H₁₅₃₂N₂₆₂O₃₀₀S₇
Protein Average Weight: 22129.0 Da

Sequences

>DB00082 sequence
FPTIPLSRLFDNAMLRAHRLHQLAFDTYQEFEEAYIPKEQKYSFLQNPQTSLCFSESIPT
PSNREETQQKSNLELLRISLLLIQSWLEPVQFLRSVFANSLVYGASDSNVYDLLKDLEEG
IQTLMGRLEDGSPRTGQIFKQTYSKFDTNSHNDDALLKNYGLLYCFRKDMDKVETFLRIV
QCRSVEGSCGF

Download FASTA Format

Synonyms

Pegvisomant

External IDs

B-2036-PEG
B2036-PEG

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Pharmacology

Indication

Pegvisomant is a growth hormone receptor antagonist used for the treatment of acromegaly.

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Associated Conditions

Indication Type	Indication	Combined Product Details	Approval Level	Age Group	Patient Characteristics	Dose Form
Management of	Acromegaly		••••••••••••		•••••••••• •• •• •••••••••• •• ••••• •••••••••	•••••••••

Contraindications & Blackbox Warnings

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Pharmacodynamics

Somavert is used for the treatment of acromegaly, which arises from excessive IGF-1 levels. Somavert selectively binds to growth hormone (GH) receptors on cell surfaces, where it blocks the binding of endogenous GH, and thus interferes with GH signal transduction. Inhibition of GH action results in decreased serum concentrations of insulin-like growth factor-I (IGF-I), and IGF binding protein-3 (IGFBP-3). This reduces the symptoms of acromegaly.

Mechanism of action

Somavert selectively binds to growth hormone (GH) receptors on cell surfaces, where it blocks the binding of endogenous GH. This leads to the normalization of serum IGF-1 levels.

Target	Actions	Organism
AGrowth hormone receptor	antagonist	Humans

Absorption

Not Available

Volume of distribution

Protein binding

Not Available

Metabolism

Not Available

Route of elimination

Not Available

Half-life

~6 days

Clearance

36 - 28 mL/h [SC doses ranging from 10 to 20 mg/day]

Adverse Effects

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Toxicity

Not Available

Pathways

Not Available

Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">

Not Available

Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">

This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

Drug	Interaction
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Acarbose	The risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Acarbose.
Acebutolol	Pegvisomant may increase the bradycardic activities of Acebutolol.
Acenocoumarol	The metabolism of Acenocoumarol can be increased when combined with Pegvisomant.
Acetohexamide	The risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Acetohexamide.
Acetylcholine	The risk or severity of adverse effects can be increased when Pegvisomant is combined with Acetylcholine.

Food Interactions

No interactions found.

Products

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Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Somavert	Injection, powder, lyophilized, for solution; Kit	30 mg/1mL	Subcutaneous	Pharmacia & Upjohn Company LLC	2016-10-01	Not applicable
Somavert	Injection, powder, for solution	25 mg	Subcutaneous	Pfizer Europe Ma Eeig	2016-09-08	Not applicable
Somavert	Injection, powder, lyophilized, for solution; Kit	15 mg/1mL	Subcutaneous	Pharmacia & Upjohn Company LLC	2016-10-01	Not applicable
Somavert	Injection, powder, for solution	20 mg	Subcutaneous	Pfizer Europe Ma Eeig	2016-09-08	Not applicable
Somavert	Injection, powder, lyophilized, for solution; Kit	25 mg/1mL	Subcutaneous	Pharmacia and Upjohn Company LLC	2014-07-31	2018-08-31

Chemical Identifiers

UNII: N824AOU5XV
CAS number: 218620-50-9

References

Synthesis Reference

Mandayam J. Narasimhan, John A. Anderson, "Process for the large scale production of human growth hormone by serial secondary suspension culture." U.S. Patent US4124448, issued January, 1963.

US4124448

General References

FDA Approved Drug Products: Somavert (pegvisomant) for subcutaneous injection [Link]

External Links

UniProt: P58756
Genbank: AF374232
PubChem Substance: 46505507
RxNav: 278739
ChEMBL: CHEMBL1201515
Therapeutic Targets Database: DAP000286
PharmGKB: PA164749630
RxList: RxList Drug Page
Drugs.com: Drugs.com Drug Page
Wikipedia: Pegvisomant

FDA label

Download (864 KB)

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">

Phase	Status	Purpose	Conditions	Count
4	Completed	Other	Obesity	1
4	Completed	Treatment	Acromegaly	6
4	Completed	Treatment	Acromegaly / Quality of Life (QOL)	1
4	Unknown Status	Treatment	Acromegaly	1
4	Unknown Status	Treatment	Acromegaly / Heart Failure / Left Ventricular Hypertrophy	1

Pharmacoeconomics

Manufacturers

Pharmacia and upjohn co

Packagers

Hospira Inc.
Pfizer Inc.
Pharmacia Inc.

Dosage Forms

Form	Route	Strength
Injection, powder, for solution	Parenteral; Subcutaneous	10 MG
Injection, powder, for solution	Parenteral; Subcutaneous	15 MG
Injection, powder, for solution	Parenteral; Subcutaneous	20 MG
Injection, powder, for solution	Parenteral; Subcutaneous	25 MG
Injection, powder, for solution	Parenteral; Subcutaneous	30 MG
Injection, powder, for solution	Subcutaneous	10 mg
Injection, powder, for solution	Subcutaneous	15 mg
Injection, powder, for solution	Subcutaneous	20 mg
Injection, powder, for solution	Subcutaneous	25 mg
Injection, powder, for solution	Subcutaneous	30 mg
Injection, powder, lyophilized, for solution; kit	Subcutaneous	10 mg/1mL
Injection, powder, lyophilized, for solution; kit	Subcutaneous	15 mg/1mL
Injection, powder, lyophilized, for solution; kit	Subcutaneous	20 mg/1mL
Injection, powder, lyophilized, for solution; kit	Subcutaneous	25 mg/1mL
Injection, powder, lyophilized, for solution; kit	Subcutaneous	30 mg/1mL
Kit; powder, for solution	Subcutaneous	10 mg / vial
Kit; powder, for solution	Subcutaneous	15 mg / vial
Kit; powder, for solution	Subcutaneous	20 mg / vial
Kit; powder, for solution	Subcutaneous	25 mg / vial
Kit; powder, for solution	Subcutaneous	30 mg / vial
Injection, powder, lyophilized, for solution	Subcutaneous	10 mg
Injection, solution		10 mg
Injection, solution		15 mg
Injection, solution		20 mg
Injection, powder, lyophilized, for solution	Subcutaneous	15 mg

Prices

Unit description	Cost	Unit
Somavert 20 mg vial	208.38USD	vial
Somavert 15 mg vial	156.29USD	vial
Somavert 10 mg vial	104.18USD	vial

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)
US5350836	No	1994-09-27	2011-09-27
CA2230492	No	2009-05-26	2016-09-20
CA2102129	No	2003-04-01	2012-05-01
US6057292	No	2000-05-02	2015-09-21
US5849535	No	1998-12-15	2017-03-25

Properties

State

Liquid

Experimental Properties

Property	Value	Source
melting point (°C)	76 °C at pH 3.5	Gomez-Orellana, I. et al., Protein Sci. 7:1352-1358 (1998)
hydrophobicity	-0.411	Not Available
isoelectric point	5.27	Not Available

Targets

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Details1. Growth hormone receptor

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Antagonist

General Function: Protein kinase binding
Specific Function: Receptor for pituitary gland growth hormone involved in regulating postnatal body growth. On ligand binding, couples to the JAK2/STAT5 pathway (By similarity).The soluble form (GHBP) acts as a rese...
Gene Name: GHR
Uniprot ID: P10912
Uniprot Name: Growth hormone receptor
Molecular Weight: 71498.885 Da

References

Moller L, Norrelund H, Jessen N, Flyvbjerg A, Pedersen SB, Gaylinn BD, Liu J, Thorner MO, Moller N, Lunde Jorgensen JO: Impact of growth hormone receptor blockade on substrate metabolism during fasting in healthy subjects. J Clin Endocrinol Metab. 2009 Nov;94(11):4524-32. doi: 10.1210/jc.2009-0381. Epub 2009 Oct 9. [Article]
Paisley AN, Hayden K, Ellis A, Anderson J, Wieringa G, Trainer PJ: Pegvisomant interference in GH assays results in underestimation of GH levels. Eur J Endocrinol. 2007 Mar;156(3):315-9. [Article]
Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
De Martino MC, Auriemma RS, Brevetti G, Vitale G, Schiano V, Galdiero M, Grasso L, Lombardi G, Colao A, Pivonello R: The treatment with growth hormone receptor antagonist in acromegaly: effect on vascular structure and function in patients resistant to somatostatin analogues. J Endocrinol Invest. 2010 Oct;33(9):663-70. doi: 10.3275/7143. Epub 2010 Jul 1. [Article]

Enzymes

Details1. Sterol 26-hydroxylase, mitochondrial

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inducer

General Function: Vitamin d3 25-hydroxylase activity
Specific Function: Catalyzes the first step in the oxidation of the side chain of sterol intermediates; the 27-hydroxylation of 5-beta-cholestane-3-alpha,7-alpha,12-alpha-triol. Has also a vitamin D3-25-hydroxylase a...
Gene Name: CYP27A1
Uniprot ID: Q02318
Uniprot Name: Sterol 26-hydroxylase, mitochondrial
Molecular Weight: 60234.28 Da

References

Araya Z, Tang W, Wikvall K: Hormonal regulation of the human sterol 27-hydroxylase gene CYP27A1. Biochem J. 2003 Jun 1;372(Pt 2):529-34. [Article]

Details2. Glutamine synthetase

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inhibitor

General Function: Manganese ion binding
Specific Function: This enzyme has 2 functions: it catalyzes the production of glutamine and 4-aminobutanoate (gamma-aminobutyric acid, GABA), the latter in a pyridoxal phosphate-independent manner (By similarity). E...
Gene Name: GLUL
Uniprot ID: P15104
Uniprot Name: Glutamine synthetase
Molecular Weight: 42064.15 Da

References

Nolan EM, Masters JN, Dunn A: Growth hormone regulation of hepatic glutamine synthetase mRNA levels in rats. Mol Cell Endocrinol. 1990 Mar 5;69(2-3):101-10. [Article]

Details3. Cytochrome P450 3A4

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inducer

General Function: Vitamin d3 25-hydroxylase activity
Specific Function: Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name: CYP3A4
Uniprot ID: P08684
Uniprot Name: Cytochrome P450 3A4
Molecular Weight: 57342.67 Da

References

Liddle C, Goodwin BJ, George J, Tapner M, Farrell GC: Separate and interactive regulation of cytochrome P450 3A4 by triiodothyronine, dexamethasone, and growth hormone in cultured hepatocytes. J Clin Endocrinol Metab. 1998 Jul;83(7):2411-6. [Article]
Cheung C, Yu AM, Chen CS, Krausz KW, Byrd LG, Feigenbaum L, Edwards RJ, Waxman DJ, Gonzalez FJ: Growth hormone determines sexual dimorphism of hepatic cytochrome P450 3A4 expression in transgenic mice. J Pharmacol Exp Ther. 2006 Mar;316(3):1328-34. Epub 2005 Nov 16. [Article]

Details4. Cholinesterase

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inhibitor

General Function: Identical protein binding
Specific Function: Esterase with broad substrate specificity. Contributes to the inactivation of the neurotransmitter acetylcholine. Can degrade neurotoxic organophosphate esters.
Gene Name: BCHE
Uniprot ID: P06276
Uniprot Name: Cholinesterase
Molecular Weight: 68417.575 Da

References

Lamartiniere CA: Growth hormone modulates serum cholinesterase. Endocrinology. 1986 Mar;118(3):1252-4. [Article]

Details5. Cytochrome P450 4A11

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inhibitor

General Function: Leukotriene-b4 20-monooxygenase activity
Specific Function: Catalyzes the omega- and (omega-1)-hydroxylation of various fatty acids such as laurate, myristate and palmitate. Has little activity toward prostaglandins A1 and E1. Oxidizes arachidonic acid to 2...
Gene Name: CYP4A11
Uniprot ID: Q02928
Uniprot Name: Cytochrome P450 4A11
Molecular Weight: 59347.31 Da

References

Savas U, Machemer DE, Hsu MH, Gaynor P, Lasker JM, Tukey RH, Johnson EF: Opposing roles of peroxisome proliferator-activated receptor alpha and growth hormone in the regulation of CYP4A11 expression in a transgenic mouse model. J Biol Chem. 2009 Jun 12;284(24):16541-52. doi: 10.1074/jbc.M902074200. Epub 2009 Apr 14. [Article]

Drug created at June 13, 2005 13:24 / Updated at January 02, 2024 23:41

Pegvisomant

Identification

Pharmacology

Interactions

Products

Categories

Chemical Identifiers

References

Clinical Trials

Pharmacoeconomics

Properties

Targets

References

Enzymes

References

References

References

References

References