Identification
NamePegvisomant
Accession NumberDB00082  (BTD00044, BIOD00044)
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
Related Articles
Protein chemical formulaC990H1532N262O300S7
Protein average weight22129.0 Da
Sequences
>DB00082 sequence
FPTIPLSRLFDNAMLRAHRLHQLAFDTYQEFEEAYIPKEQKYSFLQNPQTSLCFSESIPT
PSNREETQQKSNLELLRISLLLIQSWLEPVQFLRSVFANSLVYGASDSNVYDLLKDLEEG
IQTLMGRLEDGSPRTGQIFKQTYSKFDTNSHNDDALLKNYGLLYCFRKDMDKVETFLRIV
QCRSVEGSCGF
Download FASTA Format
SynonymsNot Available
External IDs B-2036-PEG / B2036-PEG
Product Ingredients Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
SomavertKitPharmacia & Upjohn Inc2003-05-25Not applicableUs
SomavertInjection, powder, for solution25 mgSubcutaneousPfizer2002-11-13Not applicableEu
SomavertKitPharmacia & Upjohn Inc2016-10-01Not applicableUs
SomavertKit; Powder, for solution15 mgSubcutaneousPfizer2006-01-24Not applicableCanada
SomavertKit; Powder, for solution30 mgSubcutaneousPfizer2016-03-10Not applicableCanada
SomavertKitPharmacia & Upjohn Inc2014-07-31Not applicableUs
SomavertInjection, powder, for solution30 mgSubcutaneousPfizer2002-11-13Not applicableEu
SomavertKitPharmacia & Upjohn Inc2016-10-01Not applicableUs
SomavertInjection, powder, for solution20 mgSubcutaneousPfizer2002-11-13Not applicableEu
SomavertKit; Powder, for solution20 mgSubcutaneousPfizer2006-01-24Not applicableCanada
SomavertKitPharmacia & Upjohn Inc2003-05-25Not applicableUs
SomavertInjection, powder, for solution25 mgSubcutaneousPfizer2002-11-13Not applicableEu
SomavertKitPharmacia & Upjohn Inc2016-10-01Not applicableUs
SomavertInjection, powder, for solution10 mgSubcutaneousPfizer2002-11-13Not applicableEu
SomavertKitPharmacia & Upjohn Inc2014-07-31Not applicableUs
SomavertInjection, powder, for solution20 mgSubcutaneousPfizer2002-11-13Not applicableEu
SomavertKitPharmacia & Upjohn Inc2016-10-01Not applicableUs
SomavertKit; Powder, for solution25 mgSubcutaneousPfizer2016-03-10Not applicableCanada
SomavertKitPharmacia & Upjohn Inc2003-05-25Not applicableUs
SomavertInjection, powder, for solution30 mgSubcutaneousPfizer2002-11-13Not applicableEu
SomavertKit; Powder, for solution10 mgSubcutaneousPfizer2006-01-24Not applicableCanada
SomavertInjection, powder, for solution15 mgSubcutaneousPfizer2002-11-13Not applicableEu
SomavertKitPharmacia & Upjohn Inc2016-10-01Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Categories
UNIIN824AOU5XV
CAS number218620-50-9
Pharmacology
Indication

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

Structured Indications
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.

TargetKindPharmacological actionActionsOrganismUniProt ID
Growth hormone receptorProteinyes
antagonist
HumanP10912 details
Related Articles
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
Pharmacogenomic Effects/ADRs Not Available
Interactions
Drug Interactions
DrugInteractionDrug group
AcarbosePegvisomant may increase the hypoglycemic activities of Acarbose.Approved, Investigational
AlbiglutidePegvisomant may increase the hypoglycemic activities of Albiglutide.Approved
AlfentanilThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Alfentanil.Approved, Illicit
AlogliptinPegvisomant may increase the hypoglycemic activities of Alogliptin.Approved
AlphacetylmethadolThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Alphacetylmethadol.Experimental, Illicit
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Pegvisomant.Approved, Investigational
BezitramideThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Bezitramide.Experimental, Illicit, Withdrawn
BromocriptinePegvisomant may increase the hypoglycemic activities of Bromocriptine.Approved, Investigational
BuprenorphineThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
ButorphanolThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Butorphanol.Approved, Illicit, Vet Approved
CanagliflozinPegvisomant may increase the hypoglycemic activities of Canagliflozin.Approved
CarfentanilThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Carfentanil.Illicit, Vet Approved
ChlorpropamidePegvisomant may increase the hypoglycemic activities of Chlorpropamide.Approved
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Pegvisomant.Approved
CodeineThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Codeine.Approved, Illicit
DapagliflozinPegvisomant may increase the hypoglycemic activities of Dapagliflozin.Approved
DextromoramideThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Dextromoramide.Experimental, Illicit
DextropropoxypheneThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Dextropropoxyphene.Approved, Illicit, Withdrawn
DezocineThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Dezocine.Approved
DihydrocodeineThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Dihydrocodeine.Approved, Illicit
DihydroetorphineThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Dihydroetorphine.Experimental, Illicit
DihydromorphineThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Dihydromorphine.Experimental, Illicit
DiphenoxylateThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Diphenoxylate.Approved, Illicit
DisopyramidePegvisomant may increase the hypoglycemic activities of Disopyramide.Approved
DulaglutidePegvisomant may increase the hypoglycemic activities of Dulaglutide.Approved
EmpagliflozinPegvisomant may increase the hypoglycemic activities of Empagliflozin.Approved
EthylmorphineThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Ethylmorphine.Approved, Illicit
EtorphineThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Etorphine.Illicit, Vet Approved
ExenatidePegvisomant may increase the hypoglycemic activities of Exenatide.Approved, Investigational
FentanylThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Fentanyl.Approved, Illicit, Investigational, Vet Approved
GliclazidePegvisomant may increase the hypoglycemic activities of Gliclazide.Approved
GlimepiridePegvisomant may increase the hypoglycemic activities of Glimepiride.Approved
GlipizidePegvisomant may increase the hypoglycemic activities of Glipizide.Approved
GlyburidePegvisomant may increase the hypoglycemic activities of Glyburide.Approved
HeroinThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Heroin.Approved, Illicit
HydrocodoneThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Hydrocodone.Approved, Illicit
HydromorphoneThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Hydromorphone.Approved, Illicit
Insulin AspartPegvisomant may increase the hypoglycemic activities of Insulin Aspart.Approved
Insulin DetemirPegvisomant may increase the hypoglycemic activities of Insulin Detemir.Approved
Insulin GlarginePegvisomant may increase the hypoglycemic activities of Insulin Glargine.Approved
Insulin GlulisinePegvisomant may increase the hypoglycemic activities of Insulin Glulisine.Approved
Insulin HumanPegvisomant may increase the hypoglycemic activities of Insulin Human.Approved, Investigational
Insulin LisproPegvisomant may increase the hypoglycemic activities of Insulin Lispro.Approved
KetobemidoneThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Ketobemidone.Approved
LanreotideThe risk or severity of adverse effects can be increased when Lanreotide is combined with Pegvisomant.Approved
Levomethadyl AcetateThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Levomethadyl Acetate.Approved
LevorphanolThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Levorphanol.Approved
LiraglutidePegvisomant may increase the hypoglycemic activities of Liraglutide.Approved
LofentanilThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Lofentanil.Illicit
MecaserminPegvisomant may increase the hypoglycemic activities of Mecasermin.Approved, Investigational
MetforminPegvisomant may increase the hypoglycemic activities of Metformin.Approved
MethadoneThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Methadone.Approved
Methadyl AcetateThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Methadyl Acetate.Approved, Illicit
MifepristonePegvisomant may increase the hypoglycemic activities of Mifepristone.Approved, Investigational
MiglitolPegvisomant may increase the hypoglycemic activities of Miglitol.Approved
MorphineThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Morphine.Approved, Investigational
NalbuphineThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Nalbuphine.Approved
NateglinidePegvisomant may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
NormethadoneThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Normethadone.Approved, Illicit
OctreotideThe risk or severity of adverse effects can be increased when Octreotide is combined with Pegvisomant.Approved, Investigational
OpiumThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Opium.Approved, Illicit
OxycodoneThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Oxycodone.Approved, Illicit, Investigational
OxymorphoneThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Oxymorphone.Approved, Investigational, Vet Approved
PasireotideThe risk or severity of adverse effects can be increased when Pasireotide is combined with Pegvisomant.Approved
PegloticaseThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Pegloticase.Approved
PentamidinePegvisomant may increase the hypoglycemic activities of Pentamidine.Approved
PentazocineThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Pentazocine.Approved, Vet Approved
PethidineThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Pethidine.Approved
PioglitazonePegvisomant may increase the hypoglycemic activities of Pioglitazone.Approved, Investigational
PiritramideThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Piritramide.Investigational
PramlintidePegvisomant may increase the hypoglycemic activities of Pramlintide.Approved, Investigational
QuininePegvisomant may increase the hypoglycemic activities of Quinine.Approved
RemifentanilThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Remifentanil.Approved
RepaglinidePegvisomant may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
RosiglitazonePegvisomant may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Pegvisomant.Approved
SitagliptinPegvisomant may increase the hypoglycemic activities of Sitagliptin.Approved, Investigational
SufentanilThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Sufentanil.Approved, Investigational
SulfadiazinePegvisomant may increase the hypoglycemic activities of Sulfadiazine.Approved, Vet Approved
SulfamethoxazolePegvisomant may increase the hypoglycemic activities of Sulfamethoxazole.Approved
SulfisoxazolePegvisomant may increase the hypoglycemic activities of Sulfisoxazole.Approved, Vet Approved
SunitinibPegvisomant may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
TapentadolThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Tapentadol.Approved
TolazamidePegvisomant may increase the hypoglycemic activities of Tolazamide.Approved
TolbutamidePegvisomant may increase the hypoglycemic activities of Tolbutamide.Approved
TramadolThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Tramadol.Approved, Investigational
Food InteractionsNot 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 — Pegvisomant
AHFS Codes
  • 68:30.08
PDB Entries
FDA labelDownload (864 KB)
MSDSNot Available
Clinical Trials
Clinical Trials
PhaseStatusPurposeConditionsCount
0Active Not RecruitingTreatmentAging / Immune System and Related Disorders1
0CompletedTreatmentGrowth Hormone Deficiency (GHD)1
0Unknown StatusTreatmentTraumatic Brain Injury (TBI)1
1Active Not RecruitingDiagnosticTraumatic Brain Injury (TBI)1
1CompletedBasic ScienceBioavailability1
1CompletedTreatmentInfertilities1
1RecruitingBasic ScienceDiabetes, Diabetes Mellitus Type 11
1TerminatedTreatmentCystic Fibrosis (CF)1
1TerminatedTreatmentInfection, Human Immunodeficiency Virus I1
1TerminatedTreatmentNeoplasms, Breast / Neoplasms, Colorectal / Neoplasms, Lung / Prostatic Neoplasms / Sarcomas1
1, 2CompletedTreatmentX Linked Hypophosphatemic Rickets1
2CompletedTreatmentAmyotrophic Lateral Sclerosis (ALS)1
2CompletedTreatmentConstitutional Delay of Growth and Development / Pituitary Dwarfism / Short Stature1
2CompletedTreatmentConstitutional Growth Delay / Growth Disorders / Nutrition Disorders1
2CompletedTreatmentCrohn's Disease (CD)1
2CompletedTreatmentCystic Fibrosis (CF)1
2CompletedTreatmentDiabetes / Insulin Resistance / Metabolic Syndromes1
2CompletedTreatmentEnd Stage Renal Disease (ESRD) / Renal Osteodystrophy1
2CompletedTreatmentGonadal Dysgenesis / Turner's Syndrome1
2CompletedTreatmentGrowth Hormone Deficiency (GHD)1
2CompletedTreatmentInfertilities / Poor Ovarian Reserve1
2CompletedTreatmentTurner's Syndrome1
2Not Yet RecruitingBasic ScienceTendinopathy1
2RecruitingTreatmentGrowth Hormone Treatment / Human Immunodeficiency Virus (HIV)1
2RecruitingTreatmentInfertilities1
2SuspendedTreatmentChronic Heart Failure (CHF)1
2TerminatedTreatmentHormone Deficiency1
2TerminatedTreatmentInsulin-Like Growth Factor-1 Deficiency1
2WithdrawnTreatmentCrohn's Disease (CD)1
2, 3CompletedNot AvailableHypopituitarism1
2, 3CompletedTreatmentMinor burns1
2, 3RecruitingTreatmentAlbright Hereditary Osteodystrophy / Pseudohypoparathyroidism Type 1A1
2, 3RecruitingTreatmentGrowth Hormone Treatment / Minor burns1
2, 3RecruitingTreatmentLiver Cirrhosis1
2, 3RecruitingTreatmentMinor burns1
2, 3Unknown StatusDiagnosticShort Stature1
3CompletedNot AvailableDiabetes1
3CompletedDiagnosticChromosome 18 / Growth Hormone Deficiency (GHD) / Loss of Chromosome 18q1
3CompletedTreatmentAcromegaly2
3CompletedTreatmentAdult Growth Hormone Deficiency (AGHD) / Pituitary Disorders1
3CompletedTreatmentChronic Heart Failure (CHF)1
3CompletedTreatmentGrowth Hormone Treatment1
3CompletedTreatmentIdiopathic Short Stature (ISS)1
3CompletedTreatmentMcCune Albright Syndrome / Polyostotic Fibrous Dysplasia1
3CompletedTreatmentTurner's Syndrome1
3Not Yet RecruitingTreatmentAcromegaly1
3RecruitingNot AvailableAtherosclerotic Cardiovascular Diseases1
3Unknown StatusTreatmentGrowth Hormone Deficiency (GHD)1
3Unknown StatusTreatmentSpinal Cord Injuries (SCI)1
3Unknown StatusTreatmentBone destruction1
4Active Not RecruitingTreatmentAcromegaly1
4CompletedNot AvailableSmall For Gestational Age (SGA)1
4CompletedDiagnosticGrowth Hormone Deficiency (GHD) / Kidney Failure,Chronic1
4CompletedOtherBMI >30 kg/m21
4CompletedPreventionHealthy Volunteers1
4CompletedTreatmentAcromegaly6
4CompletedTreatmentAcromegaly / Quality of Life1
4CompletedTreatmentFemale Infertility Due to Diminished Ovarian Reserve3
4CompletedTreatmentGrowth Hormone Deficiency (GHD) / Panhypopituitarism / Short Stature1
4CompletedTreatmentGrowth Hormone Deficiency (GHD) / Prader-Willi Syndrome1
4CompletedTreatmentHypothyroidism1
4CompletedTreatmentTurner's Syndrome1
4Not Yet RecruitingTreatmentLow Ovarian Reserve1
4RecruitingTreatmentIdiopathic Short Stature (ISS)1
4RecruitingTreatmentSubfertility1
4TerminatedTreatmentShort Bowel Syndrome (SBS)1
4Unknown StatusDiagnosticAtaxia Telangiectasia (AT) / Growth Failure1
4Unknown StatusDiagnosticChronic Myelogenous Leukemia (CML) / Short Stature1
4Unknown StatusTreatmentAcromegaly / Heart Failure, Unspecified / Left Ventricular Hypertrophy1
4Unknown StatusTreatmentMetabolic Syndromes1
Not AvailableActive Not RecruitingDiagnosticGrowth Hormone Deficiency (GHD)1
Not AvailableActive Not RecruitingOtherBMI >30 kg/m2 / Osteopenia1
Not AvailableCompletedNot AvailableAcromegaly1
Not AvailableCompletedNot AvailableCardiovascular Disease (CVD)1
Not AvailableCompletedNot AvailableGrowth Hormone Deficiency (GHD)2
Not AvailableCompletedBasic ScienceAcromegaly / Metabolic Diseases1
Not AvailableCompletedBasic ScienceDiabetes, Diabetes Mellitus Type 1 / Ketoacidosis1
Not AvailableCompletedBasic ScienceFatty Liver / Metabolism1
Not AvailableCompletedBasic ScienceGrowth Hormone Deficiency (GHD)1
Not AvailableCompletedBasic ScienceHealthy Volunteers2
Not AvailableCompletedBasic ScienceInsulin Resistance1
Not AvailableCompletedBasic ScienceIntracellular Signaling Peptides and Proteins1
Not AvailableCompletedDiagnosticBMI >30 kg/m21
Not AvailableCompletedTreatmentAcromegaly1
Not AvailableCompletedTreatmentAcromegaly / Impaired Glucose Tolerance (IGT) / Insulin Resistance1
Not AvailableCompletedTreatmentElderly / Growth Hormone1
Not AvailableCompletedTreatmentBone destruction / Growth Hormone Deficiency (GHD)1
Not AvailableCompletedTreatmentGrowth Hormone Secretion Abnormality / Obese1
Not AvailableCompletedTreatmentHIV Lipodystrophy1
Not AvailableCompletedTreatmentKidney Failure,Chronic1
Not AvailableCompletedTreatmentSGA and Growth1
Not AvailableCompletedTreatmentTurner's Syndrome1
Not AvailableCompletedTreatmentWerner's Syndrome1
Not AvailableNot Yet RecruitingTreatmentSmall for Gestational Age1
Not AvailableRecruitingNot AvailableAcromegaly / Osteoporosis Risk1
Not AvailableRecruitingBasic ScienceGrowth Hormone Treatment / Metabolic Diseases1
Not AvailableRecruitingTreatmentAcromegaly1
Not AvailableRecruitingTreatmentNonalcoholic Fatty Liver Disease (NAFLD)1
Not AvailableTerminatedNot AvailableGrowth Hormone Deficiency (GHD)1
Not AvailableUnknown StatusNot AvailableGrowth Hormone Deficiency (GHD)1
Not AvailableUnknown StatusNot AvailableHypopituitary Adults1
Not AvailableUnknown StatusBasic ScienceInteraction Between the GH/IGF-I System and the Immune-system1
Not AvailableUnknown StatusBasic ScienceTurner's Syndrome1
Not AvailableUnknown StatusDiagnosticAdult Growth Hormone Deficiency (AGHD)1
Not AvailableUnknown StatusTreatmentCerebral Palsy With Muscle Wasting / Crohn's Disease (CD) / Human Immunodeficiency Virus (HIV) Infections / Hurler Syndrome (MPS-1) With Short Stature and Muscle Wasting / Juvenile Rheumatoid Arthritis With Muscle Wasting and Short Stature1
Not AvailableUnknown StatusTreatmentCystic Fibrosis (CF)1
Not AvailableWithdrawnTreatmentOsteoporosis Pseudoglioma Syndrome1
Pharmacoeconomics
Manufacturers
  • Pharmacia and upjohn co
Packagers
Dosage forms
FormRouteStrength
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
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
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5350836 No1994-09-272011-09-27Us
CA2230492 No2009-05-262016-09-20Canada
CA2102129 No2003-04-012012-05-01Canada
US6057292 No1995-09-212015-09-21Us
US5849535 No1997-03-252017-03-25Us
Properties
StateLiquid
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
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

Targets

Kind
Protein
Organism
Human
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 reservoir of growth hormone in plasma and may be a modulator/inhibitor of GH signaling.Isoform 2 up-regulates the production of GHBP and acts as a negative inhibitor of GH signaling.
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
Human
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 activity.
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
Human
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). Essential for proliferation of fetal skin fibroblasts.
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
Human
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 unrelated compounds, including steroids, fatty acids, and xenobiotics.
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
Human
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
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
Human
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
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Uniprot Name:
Cytochrome P450 2C19
Molecular Weight:
55930.545 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
Human
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 20-hydroxyeicosatetraenoic acid (20-HETE).
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 07:24 / Updated on August 08, 2017 04:48