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Identification
NamePegvisomant
Accession NumberDB00082  (BIOD00044, BTD00044)
TypeBiotech
GroupsApproved
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.

Protein structureDb00082
Protein chemical formulaC990H1532N262O300S7
Protein average weight22129.0 Da
Sequences
>DB00082 sequence
FPTIPLSRLFDNAMLRAHRLHQLAFDTYQEFEEAYIPKEQKYSFLQNPQTSLCFSESIPT
PSNREETQQKSNLELLRISLLLIQSWLEPVQFLRSVFANSLVYGASDSNVYDLLKDLEEG
IQTLMGRLEDGSPRTGQIFKQTYSKFDTNSHNDDALLKNYGLLYCFRKDMDKVETFLRIV
QCRSVEGSCGF
Download FASTA Format
Synonyms
GH
GH-N
Growth hormone
Growth hormone 1
Pituitary growth hormone
Somatotropin precursor
External Identifiers Not Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
SomavertkitPharmacia and Upjohn Company2003-05-25Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Somavertkit; powder for solution20 mgsubcutaneousPfizer Canada Inc2006-01-24Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Somavertkit; powder for solution15 mgsubcutaneousPfizer Canada Inc2006-01-24Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Somavertkit; powder for solution10 mgsubcutaneousPfizer Canada Inc2006-01-24Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
SomavertkitPharmacia and Upjohn Company2014-07-31Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
SomavertkitPharmacia and Upjohn Company2014-07-31Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
SomavertkitPharmacia and Upjohn Company2003-05-25Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Somavertkit; powder for solution30 mgsubcutaneousPfizer Canada IncNot applicableNot applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
SomavertkitPharmacia and Upjohn Company2003-05-25Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Somavertkit; powder for solution25 mgsubcutaneousPfizer Canada IncNot applicableNot applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Generic Prescription ProductsNot Available
Over the Counter ProductsNot Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIN824AOU5XV
CAS number218620-50-9
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available
Pharmacology
IndicationPegvisomant is a growth hormone receptor antagonist used for the treatment of acromegaly.
PharmacodynamicsSomavert 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 actionSomavert 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.
AbsorptionNot Available
Volume of distribution
  • 7 L
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half life~6 days
Clearance
  • 36 – 28 mL/h [SC doses ranging from 10 to 20 mg/day]
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Pharmacoeconomics
Manufacturers
  • Pharmacia and upjohn co
Packagers
Dosage forms
FormRouteStrength
Kit
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
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
CountryPatent NumberApprovedExpires (estimated)
Canada21021292003-04-012012-05-01
Canada22304922009-05-262016-09-20
United States53508361994-09-272011-09-27
United States58495351997-03-252017-03-25
Properties
StateLiquid
Experimental Properties
PropertyValueSource
melting point76 °C at pH 3.5Gomez-Orellana, I. et al., Protein Sci. 7:1352-1358 (1998)
hydrophobicity-0.411Not Available
isoelectric point5.27Not Available
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 ReferencesNot Available
External Links
ATC CodesH01AX01
AHFS Codes
  • 68:30.08
PDB Entries
FDA labelDownload (864 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AcarbosePegvisomant may increase the hypoglycemic activities of Acarbose.
AlbiglutidePegvisomant may increase the hypoglycemic activities of Albiglutide.
AlfentanilThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Alfentanil.
AlogliptinPegvisomant may increase the hypoglycemic activities of Alogliptin.
BromocriptinePegvisomant may increase the hypoglycemic activities of Bromocriptine.
BuprenorphineThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Buprenorphine.
ButorphanolThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Butorphanol.
ChlorpropamidePegvisomant may increase the hypoglycemic activities of Chlorpropamide.
DapagliflozinPegvisomant may increase the hypoglycemic activities of Dapagliflozin.
DisopyramidePegvisomant may increase the hypoglycemic activities of Disopyramide.
DulaglutidePegvisomant may increase the hypoglycemic activities of Dulaglutide.
EmpagliflozinPegvisomant may increase the hypoglycemic activities of Empagliflozin.
ExenatidePegvisomant may increase the hypoglycemic activities of Exenatide.
FentanylThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Fentanyl.
GliclazidePegvisomant may increase the hypoglycemic activities of Gliclazide.
GlimepiridePegvisomant may increase the hypoglycemic activities of Glimepiride.
GlipizidePegvisomant may increase the hypoglycemic activities of Glipizide.
GlyburidePegvisomant may increase the hypoglycemic activities of Glyburide.
HydrocodoneThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Hydrocodone.
HydromorphoneThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Hydromorphone.
inhaled insulinPegvisomant may increase the hypoglycemic activities of inhaled insulin.
Insulin AspartPegvisomant may increase the hypoglycemic activities of Insulin Aspart.
Insulin degludecPegvisomant may increase the hypoglycemic activities of Insulin degludec.
Insulin DetemirPegvisomant may increase the hypoglycemic activities of Insulin Detemir.
Insulin GlarginePegvisomant may increase the hypoglycemic activities of Insulin Glargine.
Insulin GlulisinePegvisomant may increase the hypoglycemic activities of Insulin Glulisine.
Insulin LisproPegvisomant may increase the hypoglycemic activities of Insulin Lispro.
Insulin RegularPegvisomant may increase the hypoglycemic activities of Insulin Regular.
LanreotideThe risk or severity of adverse effects can be increased when Lanreotide is combined with Pegvisomant.
LevorphanolThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Levorphanol.
LiraglutidePegvisomant may increase the hypoglycemic activities of Liraglutide.
MecaserminPegvisomant may increase the hypoglycemic activities of Mecasermin.
MetforminPegvisomant may increase the hypoglycemic activities of Metformin.
MethadoneThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Methadone.
MifepristonePegvisomant may increase the hypoglycemic activities of Mifepristone.
MiglitolPegvisomant may increase the hypoglycemic activities of Miglitol.
MorphineThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Morphine.
NalbuphineThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Nalbuphine.
NateglinidePegvisomant may increase the hypoglycemic activities of Nateglinide.
OctreotideThe risk or severity of adverse effects can be increased when Octreotide is combined with Pegvisomant.
OxycodoneThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Oxycodone.
OxymorphoneThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Oxymorphone.
PasireotideThe risk or severity of adverse effects can be increased when Pasireotide is combined with Pegvisomant.
PegloticaseThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Pegloticase.
PentamidinePegvisomant may increase the hypoglycemic activities of Pentamidine.
PentazocineThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Pentazocine.
PethidineThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Pethidine.
PioglitazonePegvisomant may increase the hypoglycemic activities of Pioglitazone.
PramlintidePegvisomant may increase the hypoglycemic activities of Pramlintide.
QuininePegvisomant may increase the hypoglycemic activities of Quinine.
RemifentanilThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Remifentanil.
RepaglinidePegvisomant may increase the hypoglycemic activities of Repaglinide.
RosiglitazonePegvisomant may increase the hypoglycemic activities of Rosiglitazone.
SaxagliptinPegvisomant may increase the hypoglycemic activities of Saxagliptin.
SitagliptinPegvisomant may increase the hypoglycemic activities of Sitagliptin.
SufentanilThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Sufentanil.
SulfadiazinePegvisomant may increase the hypoglycemic activities of Sulfadiazine.
SunitinibPegvisomant may increase the hypoglycemic activities of Sunitinib.
TapentadolThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Tapentadol.
TolazamidePegvisomant may increase the hypoglycemic activities of Tolazamide.
TolbutamidePegvisomant may increase the hypoglycemic activities of Tolbutamide.
TramadolThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Tramadol.
Food InteractionsNot Available

Targets

1. Growth hormone receptor

Kind: Protein

Organism: Human

Pharmacological action: yes

Actions: antagonist

Components

Name UniProt ID Details
Growth hormone receptor P10912 Details

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. Epub 2009 Oct 9. Pubmed
  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
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  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 Jul 1. Pubmed

Enzymes

1. Sterol 26-hydroxylase, mitochondrial

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Sterol 26-hydroxylase, mitochondrial Q02318 Details

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

2. Glutamine synthetase

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Glutamine synthetase P15104 Details

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

3. Cytochrome P450 2C18

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2C18 P33260 Details

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. Epub 2009 Apr 1. Pubmed

4. Cytochrome P450 3A4

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

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
  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

5. Cholinesterase

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cholinesterase P06276 Details

References:

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

6. Cytochrome P450 2C19

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2C19 P33261 Details

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. Epub 2009 Apr 1. Pubmed

7. Cytochrome P450 4A11

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 4A11 Q02928 Details

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. Epub 2009 Apr 14. Pubmed]

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Drug created on June 13, 2005 07:24 / Updated on September 13, 2013 10:49