You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
Identification
NameMecasermin
Accession NumberDB01277
TypeBiotech
GroupsApproved, Investigational
DescriptionMecasermin contains recombinant-DNA-engineered human insulin-like growth factor-1 (rhIGF-1). IGF-1 consists of 70 amino acids in a single chain with three intramolecular disulfide bridges and a molecular weight of 7649 daltons. The amino acid sequence of the product is identical to that of endogenous human IGF-1. The rhIGF-1 protein is synthesized in bacteria (E. coli) that have been modified by the addition of the gene for human IGF-1.
Protein structureDb01277
Related Articles
Protein chemical formulaC331H518N94O101S7
Protein average weight7649.0 Da
Sequences
>Mecasermin
GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMY
CAPLKPAKSA
Download FASTA Format
Synonyms
IGF-1
IGF1
Insulin-like growth factor 1
Mecasermin recombinant
Mecasermin rinfabate
Mecasermin rinfabate recombinant
Mechano growth factor
Somatomedin-C
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Increlexinjection, solution40 mg/4mLsubcutaneousIpsen Biopharmaceuticals, Inc.2006-01-03Not applicableUs
IncrelexSolution for injection.10 mg/ mlSubcutaneous useIpsen Pharma2007-08-03Not applicableEu
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
IplexNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII7GR9I2683O
CAS number68562-41-4
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
IndicationFor the long-term treatment of growth failure in pediatric patients with Primary IGFD or with GH gene deletion who have developed neutralizing antibodies to GH. It is not indicated to treat Secondary IGFD resulting from GH deficiency, malnutrition, hypothyroidism or other causes; it is not a substitute for GH therapy.
PharmacodynamicsMecasermin is a biosynthetic (recombinant DNA origin) form of human insulin growth factor 1 (IGF-1) designed to replace natural IGF-1 in pediatric patients who are deficient, promoting normalized statural growth. Growth hormones (GH) bind to growth hormone receptors (GHR) in the liver and other tissues, which stimulates the synthesis of IGF-1. In target tissues, IGF-1 activates the IGF-1 receptor, resulting in intracellular signals that stimulate growth. Although many actions of the GH are mediated through IGF-1, the precise roles of GH and IGF-1 have not been fully elucidated. Patients with severe primary IGF-1 deficiency (Primary IGFD) fail to produce adequate levels of IGF-1, due to disruption of the GH pathway used to promote IGF-1 release (possible GH pathway disruptions include mutations in the GHR, post-GHR signaling pathway, and IGF-1 gene defects).
Mechanism of actionMecasermin supplies recombinant-DNA-origin IGF-1, which binds to the Type I IGF-1 receptor. This receptor exerts intra-cellular signaling activity in a number of processes involved in statural growth, including mitogenesis in multiple tissue types, chondrocyte growth and division along cartilage growth plates, and increases in organ growth.
Related Articles
AbsorptionWhile the bioavailability of rhIGF-1 after subcutaneous administration in healthy subjects has been reported to be close to 100%, the absolute bioavailability of mecasermin given subcutaneously to subjects with primary insulin-like growth factor-1 deficiency (Primary IGFD) has not been determined.
Volume of distribution
  • 0.257 ± 0.073 L/kg [subjects with severe Primary IGFD]
Protein bindingIn blood, IGF-1 is bound to six IGF binding proteins, with > 80% bound as a complex with IGFBP-3 and an acid-labile subunit.
Metabolism

Both the liver and the kidney have been shown to metabolize IGF-1.

Route of eliminationBoth the liver and the kidney have been shown to metabolize IGF-1.
Half life2 hours
ClearanceNot Available
ToxicityThere is no clinical experience with overdosage of mecasermin. Based on known pharmacological effects, acute overdosage would be predicted to lead to hypoglycemia. Long-term overdosage may result in signs and symptoms of acromegaly.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Injection, solutionsubcutaneous40 mg/4mL
Solution for injection.Subcutaneous use10 mg/ ml
Prices
Unit descriptionCostUnit
Increlex 40 mg/4 ml vial232.8USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5200509 No1993-04-062010-04-06Us
US5681814 No1997-09-182017-09-18Us
Properties
StateLiquid
Experimental PropertiesNot Available
References
Synthesis ReferenceNot Available
General References
  1. Keating GM: Mecasermin. BioDrugs. 2008;22(3):177-88. [PubMed:18481900 ]
  2. Rosenbloom AL: Mecasermin (recombinant human insulin-like growth factor I). Adv Ther. 2009 Jan;26(1):40-54. doi: 10.1007/s12325-008-0136-5. Epub 2009 Jan 28. [PubMed:19198769 ]
  3. Kemp SF: Insulin-like growth factor-I deficiency in children with growth hormone insensitivity: current and future treatment options. BioDrugs. 2009;23(3):155-63. doi: 10.2165/00063030-200923030-00002. [PubMed:19627167 ]
  4. Rosenbloom AL: Is there a role for recombinant insulin-like growth factor-I in the treatment of idiopathic short stature? Lancet. 2006 Aug 12;368(9535):612-6. [PubMed:16905026 ]
  5. Lewis ME, Neff NT, Contreras PC, Stong DB, Oppenheim RW, Grebow PE, Vaught JL: Insulin-like growth factor-I: potential for treatment of motor neuronal disorders. Exp Neurol. 1993 Nov;124(1):73-88. [PubMed:8282084 ]
External Links
ATC CodesH01AC05H01AC03
AHFS CodesNot Available
PDB Entries
FDA labelDownload (490 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE may increase the hypoglycemic activities of Mecasermin.
AcarboseAcarbose may increase the hypoglycemic activities of Mecasermin.
AcetohexamideAcetohexamide may increase the hypoglycemic activities of Mecasermin.
Acetylsalicylic acidAcetylsalicylic acid may increase the hypoglycemic activities of Mecasermin.
AicarAicar may increase the hypoglycemic activities of Mecasermin.
AlogliptinAlogliptin may increase the hypoglycemic activities of Mecasermin.
Aminosalicylic AcidAminosalicylic Acid may increase the hypoglycemic activities of Mecasermin.
AmoxapineAmoxapine may increase the hypoglycemic activities of Mecasermin.
BenmoxinBenmoxin may increase the hypoglycemic activities of Mecasermin.
BuforminBuformin may increase the hypoglycemic activities of Mecasermin.
CanagliflozinCanagliflozin may increase the hypoglycemic activities of Mecasermin.
CaroxazoneCaroxazone may increase the hypoglycemic activities of Mecasermin.
CastanospermineCastanospermine may increase the hypoglycemic activities of Mecasermin.
ChlorpropamideChlorpropamide may increase the hypoglycemic activities of Mecasermin.
CiglitazoneCiglitazone may increase the hypoglycemic activities of Mecasermin.
CitalopramCitalopram may increase the hypoglycemic activities of Mecasermin.
ClomipramineClomipramine may increase the hypoglycemic activities of Mecasermin.
DapoxetineDapoxetine may increase the hypoglycemic activities of Mecasermin.
DiflunisalDiflunisal may increase the hypoglycemic activities of Mecasermin.
DihydrotestosteroneDihydrotestosterone may increase the hypoglycemic activities of Mecasermin.
DisopyramideDisopyramide may increase the hypoglycemic activities of Mecasermin.
DulaglutideDulaglutide may increase the hypoglycemic activities of Mecasermin.
EmpagliflozinEmpagliflozin may increase the hypoglycemic activities of Mecasermin.
EscitalopramEscitalopram may increase the hypoglycemic activities of Mecasermin.
EtoperidoneEtoperidone may increase the hypoglycemic activities of Mecasermin.
ExenatideExenatide may increase the hypoglycemic activities of Mecasermin.
FenfluramineFenfluramine may increase the hypoglycemic activities of Mecasermin.
FluoxetineFluoxetine may increase the hypoglycemic activities of Mecasermin.
FluoxymesteroneFluoxymesterone may increase the hypoglycemic activities of Mecasermin.
FluvoxamineFluvoxamine may increase the hypoglycemic activities of Mecasermin.
FurazolidoneFurazolidone may increase the hypoglycemic activities of Mecasermin.
GlibornurideGlibornuride may increase the hypoglycemic activities of Mecasermin.
GliclazideGliclazide may increase the hypoglycemic activities of Mecasermin.
GlimepirideGlimepiride may increase the hypoglycemic activities of Mecasermin.
GlipizideGlipizide may increase the hypoglycemic activities of Mecasermin.
GliquidoneGliquidone may increase the hypoglycemic activities of Mecasermin.
GlyburideGlyburide may increase the hypoglycemic activities of Mecasermin.
HydracarbazineHydracarbazine may increase the hypoglycemic activities of Mecasermin.
IndalpineIndalpine may increase the hypoglycemic activities of Mecasermin.
Insulin AspartInsulin Aspart may increase the hypoglycemic activities of Mecasermin.
Insulin DetemirInsulin Detemir may increase the hypoglycemic activities of Mecasermin.
Insulin GlargineInsulin Glargine may increase the hypoglycemic activities of Mecasermin.
Insulin GlulisineInsulin Glulisine may increase the hypoglycemic activities of Mecasermin.
Insulin HumanInsulin Human may increase the hypoglycemic activities of Mecasermin.
Insulin LisproInsulin Lispro may increase the hypoglycemic activities of Mecasermin.
Insulin PorkInsulin Pork may increase the hypoglycemic activities of Mecasermin.
IproclozideIproclozide may increase the hypoglycemic activities of Mecasermin.
IproniazidIproniazid may increase the hypoglycemic activities of Mecasermin.
IsocarboxazidIsocarboxazid may increase the hypoglycemic activities of Mecasermin.
LanreotideMecasermin may increase the hypoglycemic activities of Lanreotide.
LevomilnacipranLevomilnacipran may increase the hypoglycemic activities of Mecasermin.
LinagliptinLinagliptin may increase the hypoglycemic activities of Mecasermin.
LiraglutideLiraglutide may increase the hypoglycemic activities of Mecasermin.
Lu AA21004Lu AA21004 may increase the hypoglycemic activities of Mecasermin.
MebanazineMebanazine may increase the hypoglycemic activities of Mecasermin.
MesalazineMesalazine may increase the hypoglycemic activities of Mecasermin.
MetforminMetformin may increase the hypoglycemic activities of Mecasermin.
Methylene blueMethylene blue may increase the hypoglycemic activities of Mecasermin.
MethyltestosteroneMethyltestosterone may increase the hypoglycemic activities of Mecasermin.
MifepristoneMifepristone may increase the hypoglycemic activities of Mecasermin.
MiglitolMiglitol may increase the hypoglycemic activities of Mecasermin.
MiglustatMiglustat may increase the hypoglycemic activities of Mecasermin.
MilnacipranMilnacipran may increase the hypoglycemic activities of Mecasermin.
MinaprineMinaprine may increase the hypoglycemic activities of Mecasermin.
MitiglinideMitiglinide may increase the hypoglycemic activities of Mecasermin.
MoclobemideMoclobemide may increase the hypoglycemic activities of Mecasermin.
NateglinideNateglinide may increase the hypoglycemic activities of Mecasermin.
NialamideNialamide may increase the hypoglycemic activities of Mecasermin.
OctamoxinOctamoxin may increase the hypoglycemic activities of Mecasermin.
OctreotideOctreotide may increase the hypoglycemic activities of Mecasermin.
OlanzapineOlanzapine may increase the hypoglycemic activities of Mecasermin.
OxandroloneOxandrolone may increase the hypoglycemic activities of Mecasermin.
OxymetholoneOxymetholone may increase the hypoglycemic activities of Mecasermin.
PargylinePargyline may increase the hypoglycemic activities of Mecasermin.
ParoxetineParoxetine may increase the hypoglycemic activities of Mecasermin.
PasireotideMecasermin may increase the hypoglycemic activities of Pasireotide.
PegvisomantPegvisomant may increase the hypoglycemic activities of Mecasermin.
PentamidinePentamidine may increase the hypoglycemic activities of Mecasermin.
PhenelzinePhenelzine may increase the hypoglycemic activities of Mecasermin.
PhenforminPhenformin may increase the hypoglycemic activities of Mecasermin.
PheniprazinePheniprazine may increase the hypoglycemic activities of Mecasermin.
PhenoxypropazinePhenoxypropazine may increase the hypoglycemic activities of Mecasermin.
PioglitazonePioglitazone may increase the hypoglycemic activities of Mecasermin.
PirlindolePirlindole may increase the hypoglycemic activities of Mecasermin.
PivhydrazinePivhydrazine may increase the hypoglycemic activities of Mecasermin.
PramlintidePramlintide may increase the hypoglycemic activities of Mecasermin.
QuinineQuinine may increase the hypoglycemic activities of Mecasermin.
RasagilineRasagiline may increase the hypoglycemic activities of Mecasermin.
RepaglinideRepaglinide may increase the hypoglycemic activities of Mecasermin.
RosiglitazoneRosiglitazone may increase the hypoglycemic activities of Mecasermin.
SafrazineSafrazine may increase the hypoglycemic activities of Mecasermin.
Salicylic acidSalicylic acid may increase the hypoglycemic activities of Mecasermin.
SaxagliptinSaxagliptin may increase the hypoglycemic activities of Mecasermin.
SelegilineSelegiline may increase the hypoglycemic activities of Mecasermin.
SertralineSertraline may increase the hypoglycemic activities of Mecasermin.
SitagliptinSitagliptin may increase the hypoglycemic activities of Mecasermin.
StanozololStanozolol may increase the hypoglycemic activities of Mecasermin.
SulfadiazineSulfadiazine may increase the hypoglycemic activities of Mecasermin.
SulfamethoxazoleSulfamethoxazole may increase the hypoglycemic activities of Mecasermin.
SulfisoxazoleSulfisoxazole may increase the hypoglycemic activities of Mecasermin.
SulodexideSulodexide may increase the hypoglycemic activities of Mecasermin.
SunitinibSunitinib may increase the hypoglycemic activities of Mecasermin.
TestosteroneTestosterone may increase the hypoglycemic activities of Mecasermin.
TolazamideTolazamide may increase the hypoglycemic activities of Mecasermin.
TolbutamideTolbutamide may increase the hypoglycemic activities of Mecasermin.
ToloxatoneToloxatone may increase the hypoglycemic activities of Mecasermin.
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypoglycemic activities of Mecasermin.
TranylcypromineTranylcypromine may increase the hypoglycemic activities of Mecasermin.
TrazodoneTrazodone may increase the hypoglycemic activities of Mecasermin.
TroglitazoneTroglitazone may increase the hypoglycemic activities of Mecasermin.
VilazodoneVilazodone may increase the hypoglycemic activities of Mecasermin.
VildagliptinVildagliptin may increase the hypoglycemic activities of Mecasermin.
VogliboseVoglibose may increase the hypoglycemic activities of Mecasermin.
VortioxetineVortioxetine may increase the hypoglycemic activities of Mecasermin.
ZimelidineZimelidine may increase the hypoglycemic activities of Mecasermin.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Protein tyrosine kinase activity
Specific Function:
Receptor tyrosine kinase which mediates actions of insulin-like growth factor 1 (IGF1). Binds IGF1 with high affinity and IGF2 and insulin (INS) with a lower affinity. The activated IGF1R is involved in cell growth and survival control. IGF1R is crucial for tumor transformation and survival of malignant cell. Ligand binding activates the receptor kinase, leading to receptor autophosphorylation,...
Gene Name:
IGF1R
Uniprot ID:
P08069
Molecular Weight:
154791.73 Da
References
  1. Rosenbloom AL: Mecasermin (recombinant human insulin-like growth factor I). Adv Ther. 2009 Jan;26(1):40-54. doi: 10.1007/s12325-008-0136-5. Epub 2009 Jan 28. [PubMed:19198769 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Protein tyrosine phosphatase activator activity
Specific Function:
IGF-binding proteins prolong the half-life of the IGFs and have been shown to either inhibit or stimulate the growth promoting effects of the IGFs on cell culture. They alter the interaction of IGFs with their cell surface receptors. Also exhibits IGF-independent antiproliferative and apoptotic effects mediated by its receptor TMEM219/IGFBP-3R.
Gene Name:
IGFBP3
Uniprot ID:
P17936
Molecular Weight:
31673.87 Da
References
  1. Kemp SF: Insulin-like growth factor-I deficiency in children with growth hormone insensitivity: current and future treatment options. BioDrugs. 2009;23(3):155-63. doi: 10.2165/00063030-200923030-00002. [PubMed:19627167 ]
  2. Williams RM, McDonald A, O'Savage M, Dunger DB: Mecasermin rinfabate: rhIGF-I/rhIGFBP-3 complex: iPLEX. Expert Opin Drug Metab Toxicol. 2008 Mar;4(3):311-24. doi: 10.1517/17425255.4.3.311 . [PubMed:18363546 ]
  3. Authors unspecified: Mecasermin rinfabate: insulin-like growth factor-I/insulin-like growth factor binding protein-3, mecaserimin rinfibate, rhIGF-I/rhIGFBP-3. Drugs R D. 2005;6(2):120-7. [PubMed:15777106 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Receptor signaling protein tyrosine kinase activity
Specific Function:
Receptor tyrosine kinase which mediates the pleiotropic actions of insulin. Binding of insulin leads to phosphorylation of several intracellular substrates, including, insulin receptor substrates (IRS1, 2, 3, 4), SHC, GAB1, CBL and other signaling intermediates. Each of these phosphorylated proteins serve as docking proteins for other signaling proteins that contain Src-homology-2 domains (SH2 ...
Gene Name:
INSR
Uniprot ID:
P06213
Molecular Weight:
156331.465 Da
References
  1. Rosenbloom AL: Mecasermin (recombinant human insulin-like growth factor I). Adv Ther. 2009 Jan;26(1):40-54. doi: 10.1007/s12325-008-0136-5. Epub 2009 Jan 28. [PubMed:19198769 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Transporter activity
Specific Function:
Transport of phosphorylated lysosomal enzymes from the Golgi complex and the cell surface to lysosomes. Lysosomal enzymes bearing phosphomannosyl residues bind specifically to mannose-6-phosphate receptors in the Golgi apparatus and the resulting receptor-ligand complex is transported to an acidic prelyosomal compartment where the low pH mediates the dissociation of the complex. This receptor a...
Gene Name:
IGF2R
Uniprot ID:
P11717
Molecular Weight:
274372.42 Da
References
  1. Rosenbloom AL: Mecasermin (recombinant human insulin-like growth factor I). Adv Ther. 2009 Jan;26(1):40-54. doi: 10.1007/s12325-008-0136-5. Epub 2009 Jan 28. [PubMed:19198769 ]
Comments
comments powered by Disqus
Drug created on May 16, 2007 14:46 / Updated on September 24, 2016 02:16