Pegvisomant
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
- Protein Chemical Formula
- C990H1532N262O300S7
- Protein Average Weight
- 22129.0 Da
- Sequences
>DB00082 sequence FPTIPLSRLFDNAMLRAHRLHQLAFDTYQEFEEAYIPKEQKYSFLQNPQTSLCFSESIPT PSNREETQQKSNLELLRISLLLIQSWLEPVQFLRSVFANSLVYGASDSNVYDLLKDLEEG IQTLMGRLEDGSPRTGQIFKQTYSKFDTNSHNDDALLKNYGLLYCFRKDMDKVETFLRIV QCRSVEGSCGF
Download FASTA Format- Synonyms
- Not Available
- External IDs
- B-2036-PEG
- B2036-PEG
Pharmacology
- Indication
Pegvisomant is a growth hormone receptor antagonist used for the treatment of acromegaly.
- Associated Conditions
- Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More- 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 antagonistHumans - 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
Learn about our commercial Adverse Effects data.
Learn More- 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.
Drug Interaction Unlock Additional DataAcarbose 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. Aclidinium Pegvisomant may increase the neuromuscular blocking activities of Aclidinium. Albiglutide The risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Albiglutide. Alfentanil The therapeutic efficacy of Pegvisomant can be decreased when used in combination with Alfentanil. Alogliptin The risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Alogliptin. Amantadine The therapeutic efficacy of Amantadine can be decreased when used in combination with Pegvisomant. Additional Data Available- Extended DescriptionExtended DescriptionAvailable for Purchase
Extended description of the mechanism of action and particular properties of each drug interaction.
Learn more - SeveritySeverityAvailable for Purchase
A severity rating for each drug interaction, from minor to major.
Learn more - Evidence LevelEvidence LevelAvailable for Purchase
A rating for the strength of the evidence supporting each drug interaction.
Learn more - ActionActionAvailable for Purchase
An effect category for each drug interaction. Know how this interaction affects the subject drug.
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- Food Interactions
- Not Available
Products
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Unlock Additional DataSomavert 15 mg/1mL Subcutaneous Pharmacia and Upjohn Company LLC 2003-05-25 2018-07-31 US 
Somavert Kit; Powder, for solution 25 mg Subcutaneous Pfizer Canada Ulc 2016-03-10 Not applicable Canada 
Somavert Injection, powder, for solution 30 mg Subcutaneous Pfizer 2002-11-13 Not applicable EU 
Somavert 30 mg/1mL Subcutaneous Pharmacia and Upjohn Company LLC 2016-10-01 Not applicable US Somavert 15 mg/1mL Subcutaneous Pharmacia and Upjohn Company LLC 2016-10-01 Not applicable US Somavert 25 mg/1mL Subcutaneous Pharmacia and Upjohn Company LLC 2014-07-31 2018-08-31 US Somavert Kit; Powder, for solution 10 mg Subcutaneous Pfizer Canada Ulc 2006-01-24 Not applicable Canada Somavert Injection, powder, for solution 15 mg Subcutaneous Pfizer 2002-11-13 Not applicable EU Somavert Kit; Powder, for solution 20 mg Subcutaneous Pfizer Canada Ulc 2006-01-24 Not applicable Canada Somavert 10 mg/1mL Subcutaneous Pharmacia and Upjohn Company LLC 2003-05-25 Not applicable US Additional Data Available- Application NumberApplication NumberAvailable for Purchase
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct CodeAvailable for Purchase
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
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Categories
- ATC Codes
- H01AX01 — Pegvisomant
- Drug Categories
- Acromegaly
- Amino Acids, Peptides, and Proteins
- Anterior Pituitary Lobe Hormones and Analogues
- Cholinesterase Inhibitors
- Cytochrome P-450 CYP2C18 Inhibitors
- Cytochrome P-450 CYP2C18 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A Inducers
- Cytochrome P-450 CYP3A4 Inducers
- Cytochrome P-450 CYP3A4 Inducers (strength unknown)
- Cytochrome P-450 Enzyme Inducers
- Cytochrome P-450 Enzyme Inhibitors
- Growth Hormone Receptor Antagonist
- Growth Hormone Receptor Antagonists
- Hormones
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Hypoglycemia-Associated Agents
- Pegylated agents
- Peptide Hormones
- Peptides
- Pituitary and Hypothalamic Hormones and Analogues
- Pituitary Hormones
- Pituitary Hormones, Anterior
- Receptors, Somatotropin, antagonists & inhibitors
- Somatotropin Antagonists
- Systemic Hormonal Preparations, Excl. Sex Hormones and Insulins
- 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
- External Links
- UniProt
- P58756
- Genbank
- AF374232
- PubChem Substance
- 46505507
- 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
Phase Status Purpose Conditions Count 4 Completed Other BMI >30 kg/m2 1 4 Completed Treatment Acromegaly 6 4 Completed Treatment Acromegaly / Quality of Life 1 4 Unknown Status Treatment Acromegaly 1 4 Unknown Status Treatment Acromegaly / Heart Failure / Left Ventricular Hypertrophy 1 3 Active Not Recruiting Treatment Acromegaly 1 3 Completed Treatment Acromegaly 2 3 Completed Treatment McCune Albright Syndrome / McCune-Albright Syndrome / Polyostotic Fibrous Dysplasia 1 3 Recruiting Treatment Pituitary Diseases 1 2 Completed Treatment Diabetes / Insulin Resistance / Metabolic Syndromes 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 Kit; powder, for solution Subcutaneous 10 mg Kit; powder, for solution Subcutaneous 15 mg Kit; powder, for solution Subcutaneous 20 mg Kit; powder, for solution Subcutaneous 25 mg Kit; powder, for solution Subcutaneous 30 mg Injection 10 mg Injection 15 mg Injection 20 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) Region Unlock Additional DataUS5350836 No 1994-09-27 2011-09-27 US CA2230492 No 2009-05-26 2016-09-20 Canada CA2102129 No 2003-04-01 2012-05-01 Canada US6057292 No 2000-05-02 2015-09-21 US US5849535 No 1998-12-15 2017-03-25 US Additional Data Available- Filed OnFiled OnAvailable for Purchase
The date on which a patent was filed with the relevant government.
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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
- 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. [PubMed:19820031]
- 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]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
- 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
- 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
- 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
- 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
- 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]
- 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
- 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
- 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 07:24 / Updated on January 25, 2021 22:38