Identification

Name
Pegvisomant
Accession Number
DB00082
Description

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
Db00082
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

Pharmacology

Pharmacology
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Indication

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

Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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.

TargetActionsOrganism
AGrowth hormone receptor
antagonist
Humans
Absorption
Not Available
Volume of distribution
  • 7 L
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
Medicalerrors
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Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
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.
DrugInteraction
AcarboseThe risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Acarbose.
AcebutololPegvisomant may increase the bradycardic activities of Acebutolol.
AcenocoumarolThe metabolism of Acenocoumarol can be increased when combined with Pegvisomant.
AcetohexamideThe risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Acetohexamide.
AcetylcholineThe risk or severity of adverse effects can be increased when Pegvisomant is combined with Acetylcholine.
AclidiniumPegvisomant may increase the neuromuscular blocking activities of Aclidinium.
AlbiglutideThe risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Albiglutide.
AlfentanilThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Alfentanil.
AlogliptinThe risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Alogliptin.
AmantadineThe therapeutic efficacy of Amantadine can be decreased when used in combination with Pegvisomant.
Interactions
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Food Interactions
No interactions found.

Products

Products
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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
SomavertInjection, powder, for solution10 mgSubcutaneousPfizer Europe Ma Eeig2016-09-08Not applicableEU flag
Somavert30 mg/1mLSubcutaneousPharmacia and Upjohn Company LLC2014-07-312019-02-28US flag
Somavert15 mg/1mLSubcutaneousPharmacia and Upjohn Company LLC2003-05-252018-07-31US flag
SomavertInjection, powder, for solution25 mgSubcutaneousPfizer Europe Ma Eeig2016-09-08Not applicableEU flag
SomavertKit; Powder, for solution25 mgSubcutaneousPfizer Canada Ulc2016-03-10Not applicableCanada flag
Somavert30 mg/1mLSubcutaneousPharmacia and Upjohn Company LLC2016-10-01Not applicableUS flag
SomavertInjection, powder, for solution20 mgSubcutaneousPfizer Europe Ma Eeig2016-09-08Not applicableEU flag
Somavert15 mg/1mLSubcutaneousPharmacia and Upjohn Company LLC2016-10-01Not applicableUS flag
Somavert25 mg/1mLSubcutaneousPharmacia and Upjohn Company LLC2014-07-312018-08-31US flag
SomavertKit; Powder, for solution10 mgSubcutaneousPfizer Canada Ulc2006-01-24Not applicableCanada flag

Categories

ATC Codes
H01AX01 — Pegvisomant
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available

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
Not Available
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
AHFS Codes
  • 68:30.08 — Somatotropin Antagonists
FDA label
Download (864 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedOtherBMI >30 kg/m21
4CompletedTreatmentAcromegaly6
4CompletedTreatmentAcromegaly / Quality of Life1
4Unknown StatusTreatmentAcromegaly1
4Unknown StatusTreatmentAcromegaly / Heart Failure / Left Ventricular Hypertrophy1
3Active Not RecruitingTreatmentAcromegaly1
3CompletedTreatmentAcromegaly2
3CompletedTreatmentMcCune Albright Syndrome / McCune-Albright Syndrome / Polyostotic Fibrous Dysplasia1
3RecruitingTreatmentPituitary Diseases1
2CompletedTreatmentDiabetes / Insulin Resistance / Metabolic Syndromes1

Pharmacoeconomics

Manufacturers
  • Pharmacia and upjohn co
Packagers
  • Hospira Inc.
  • Pfizer Inc.
  • Pharmacia Inc.
Dosage Forms
FormRouteStrength
Injection, powder, for solutionParenteral; Subcutaneous10 MG
Injection, powder, for solutionParenteral; Subcutaneous15 MG
Injection, powder, for solutionParenteral; Subcutaneous20 MG
Injection, powder, for solutionParenteral; Subcutaneous25 MG
Injection, powder, for solutionParenteral; Subcutaneous30 MG
Injection, powder, for solutionSubcutaneous10 mg
Injection, powder, for solutionSubcutaneous15 mg
Injection, powder, for solutionSubcutaneous20 mg
Injection, powder, for solutionSubcutaneous25 mg
Injection, powder, for solutionSubcutaneous30 mg
Kit; powder, for solutionSubcutaneous10 mg
Kit; powder, for solutionSubcutaneous15 mg
Kit; powder, for solutionSubcutaneous20 mg
Kit; powder, for solutionSubcutaneous25 mg
Kit; powder, for solutionSubcutaneous30 mg
Injection10 mg
Injection15 mg
Injection20 mg
Prices
Unit descriptionCostUnit
Somavert 20 mg vial208.38USD vial
Somavert 15 mg vial156.29USD vial
Somavert 10 mg vial104.18USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5350836No1994-09-272011-09-27US flag
CA2230492No2009-05-262016-09-20Canada flag
CA2102129No2003-04-012012-05-01Canada flag
US6057292No2000-05-022015-09-21US flag
US5849535No1998-12-152017-03-25US flag

Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)76 °C at pH 3.5Gomez-Orellana, I. et al., Protein Sci. 7:1352-1358 (1998)
hydrophobicity-0.411Not Available
isoelectric point5.27Not Available

Targets

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
  1. 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. [PubMed:19820031]
  2. 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. [PubMed:17322491]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  4. 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. [PubMed:20595800]

Enzymes

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
  1. 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. [PubMed:12597773]
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
  1. 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. [PubMed:1970314]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid 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 oxidizes a variety of structurally un...
Gene Name
CYP2C18
Uniprot ID
P33260
Uniprot Name
Cytochrome P450 2C18
Molecular Weight
55710.075 Da
References
  1. Lofgren S, Baldwin RM, Carleros M, Terelius Y, Fransson-Steen R, Mwinyi J, Waxman DJ, Ingelman-Sundberg M: Regulation of human CYP2C18 and CYP2C19 in transgenic mice: influence of castration, testosterone, and growth hormone. Drug Metab Dispos. 2009 Jul;37(7):1505-12. doi: 10.1124/dmd.109.026963. Epub 2009 Apr 1. [PubMed:19339376]
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
  1. 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. [PubMed:9661620]
  2. 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. [PubMed:16291874]
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
  1. Lamartiniere CA: Growth hormone modulates serum cholinesterase. Endocrinology. 1986 Mar;118(3):1252-4. [PubMed:3948777]
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
  1. 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. [PubMed:19366684]

Drug created on June 13, 2005 13:24 / Updated on February 24, 2021 19:34