Identification

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Name
Mecasermin
Accession Number
DB01277
Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Hormones
Description

Mecasermin contains recombinant-DNA-engineered human insulin-like growth factor-1 (rhIGF-1)Label. 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 structure
Db01277
Protein chemical formula
C331H518N94O101S7
Protein average weight
7649.0 Da
Sequences
>Mecasermin
GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMY
CAPLKPAKSA
Download FASTA Format
Synonyms
  • Human somatomedin C
  • Mecasermin recombinant
  • Mecasermina
  • Mechano growth factor
External IDs
CEP 151 / CEP-151 / CG-GF2 / CG-IGF-1 / PV-802 / PV802
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
IncrelexInjection, solution40 mg/4mLSubcutaneousIpsen Biopharmaceuticals, Inc.2006-01-03Not applicableUs
IncrelexInjection, solution10 mg/mlSubcutaneousIpsen Pharma2007-08-03Not applicableEu
Additional Data Available
  • Application Number
    Application Number

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Cosmeceutical Mask PackMecasermin (0.044 mg/22g) + Basic Fibroblast Growth Factor (0.044 mg/22g) + Nepidermin (0.044 mg/22g) + Palmitoyl oligopeptide (0.044 mg/22g) + Prezatide copper (0.22 mg/22g) + Thioredoxin (0.044 mg/22g)PatchTopicalYBK Investment, INC2013-10-21Not applicableUs
Cosmeceutical Mask PackMecasermin (0.044 mg/22g) + Basic Fibroblast Growth Factor (0.044 mg/22g) + Nepidermin (0.044 mg/22g) + Palmitoyl oligopeptide (0.044 mg/22g) + Prezatide copper (0.22 mg/22g) + Thioredoxin (0.044 mg/22g)PatchTopicalYBK Investment, INC2013-10-212013-10-29Us
Dermaheal Cosmeceutical Mask Pack PlusMecasermin (0.044 mg/22g) + Basic Fibroblast Growth Factor (0.044 mg/22g) + Nepidermin (0.044 mg/22g) + Palmitoyl oligopeptide (0.044 mg/22g) + Prezatide copper (0.22 mg/22g) + Thioredoxin (0.044 mg/22g)PatchTopicalYBK Investment, INC2013-10-21Not applicableUs
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Cosmeceutical Mask PackMecasermin (0.044 mg/22g) + Basic Fibroblast Growth Factor (0.044 mg/22g) + Nepidermin (0.044 mg/22g) + Palmitoyl oligopeptide (0.044 mg/22g) + Prezatide copper (0.22 mg/22g) + Thioredoxin (0.044 mg/22g)PatchTopicalYBK Investment, INC2013-10-21Not applicableUs
Cosmeceutical Mask PackMecasermin (0.044 mg/22g) + Basic Fibroblast Growth Factor (0.044 mg/22g) + Nepidermin (0.044 mg/22g) + Palmitoyl oligopeptide (0.044 mg/22g) + Prezatide copper (0.22 mg/22g) + Thioredoxin (0.044 mg/22g)PatchTopicalYBK Investment, INC2013-10-212013-10-29Us
Dermaheal Cosmeceutical Mask Pack PlusMecasermin (0.044 mg/22g) + Basic Fibroblast Growth Factor (0.044 mg/22g) + Nepidermin (0.044 mg/22g) + Palmitoyl oligopeptide (0.044 mg/22g) + Prezatide copper (0.22 mg/22g) + Thioredoxin (0.044 mg/22g)PatchTopicalYBK Investment, INC2013-10-21Not applicableUs
Categories
UNII
7GR9I2683O
CAS number
68562-41-4

Pharmacology

Indication

For 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 1. 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.

Associated Conditions
Pharmacodynamics

Mecasermin is a biosynthetic (recombinant DNA origin) form of human insulin-like growth factor 1 (IGF-1) designed to replace natural IGF-1 in pediatric patients who are deficient, promoting normalized statural growth3. 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 2. 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 action

Mecasermin 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 growth3.

TargetActionsOrganism
AInsulin-like growth factor 1 receptor
agonist
Humans
UInsulin-like growth factor-binding protein 3Not AvailableHumans
UInsulin receptorNot AvailableHumans
UCation-independent mannose-6-phosphate receptorNot AvailableHumans
Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available
Blackbox Warnings

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Absorption

While 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 determined7.

Volume of distribution
  • 0.257 ± 0.073 L/kg [subjects with severe Primary IGFD] at a dose of 0.045mg/kg 7
Protein binding

In blood, IGF-1 is bound to six IGF binding proteins, with > 80% bound as a complex with IGFBP-3 and an acid-labile subunit 7.

Metabolism

Information on the metabolism of Mecasermin is not readily available, however it is likely to be metabolized by the liver and kidney like other injectable peptide drugs6.

Route of elimination

Information on the elimination of Mecasermin is not readily available, however it is likely to be metabolized by the liver and kidney like other injectable peptide drugs6.

Half life

Mean half life of 5.8 hours 7

Clearance

Clearance of Mecasermin is inversely proportional to IGF binding protein 3 (IGFBP-3) 7 * Clearance is estimated to be 0.04L/hr/kg at 0.5 micrograms/mL of IGFBP-3 * Clearance is estimated to be 0.01L/hr/kg at 3 micrograms/mL of IGFBP-3 (the median level of IGFBP-3 for patients with normal IGF-1 levels)

Toxicity

Overdosage of Mecasermin leads to hypoglycemia7. One case of acute overdose was treated with IV glucose. Long-term overdosage may result in signs and symptoms of acromegaly. The effects of Mecasermin in human pregnancy has not been studied, however effects on fetal development in animal studies were only seen at doses higher than the maximum recommended human dose based on body surface area. Studies on excretion of the drug in human milk, use in patients under 2 years, use in patients over 65 years, or use in patients with renal or hepatic impairment have not been performed.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
2,4-thiazolidinedioneThe risk or severity of hypoglycemia can be increased when Mecasermin is combined with 2,4-thiazolidinedione.
5-(2-methylpiperazine-1-sulfonyl)isoquinolineThe therapeutic efficacy of Mecasermin can be increased when used in combination with 5-(2-methylpiperazine-1-sulfonyl)isoquinoline.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypoglycemic activities of Mecasermin.
AcarboseThe risk or severity of hypoglycemia can be increased when Acarbose is combined with Mecasermin.
AcetazolamideThe therapeutic efficacy of Mecasermin can be increased when used in combination with Acetazolamide.
AcetohexamideThe risk or severity of hypoglycemia can be increased when Acetohexamide is combined with Mecasermin.
Acetyl sulfisoxazoleThe therapeutic efficacy of Mecasermin can be increased when used in combination with Acetyl sulfisoxazole.
Acetylsalicylic acidAcetylsalicylic acid may increase the hypoglycemic activities of Mecasermin.
AgmatineThe risk or severity of hypoglycemia can be increased when Agmatine is combined with Mecasermin.
AICA ribonucleotideThe risk or severity of hypoglycemia can be increased when Mecasermin is combined with AICA ribonucleotide.
Additional Data Available
  • Extended Description
    Extended Description

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Food Interactions
Not Available

References

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]
  6. Di L: Strategic approaches to optimizing peptide ADME properties. AAPS J. 2015 Jan;17(1):134-43. doi: 10.1208/s12248-014-9687-3. Epub 2014 Nov 4. [PubMed:25366889]
  7. Mecasermin Highlights of Prescribing Information Revised February 2010 [File]
  8. European Patent Specification [File]
External Links
KEGG Drug
D04870
PubChem Substance
46504889
ChEMBL
CHEMBL1201716
Therapeutic Targets Database
DAP000287
PharmGKB
PA164774876
Wikipedia
Mecasermin
ATC Codes
H01AC03 — Mecasermin
FDA label
Download (490 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentRett's Syndrome1
1TerminatedTreatmentCystic Fibrosis (CF)1
1TerminatedTreatmentHIV Lipodystrophy1
1, 2Active Not RecruitingTreatmentShort Stature1
1, 2CompletedNot AvailableAnorexia Nervosa (AN)1
1, 2CompletedTreatmentHeart Failure / Myocardial Infarction1
1, 2CompletedTreatmentSteinert's Disease1
1, 2TerminatedTreatmentGrowth Failure / Growth Hormone Resistence / X-linked Severe Combined Immunodeficiency (XSCID)1
1, 2Unknown StatusTreatmentDuchenne's Muscular Dystrophy (DMD)1
2CompletedPreventionRetinopathy of Prematurity / Retinopathy of Prematurity (ROP)1
2CompletedTreatmentDisseminated Sclerosis1
2CompletedTreatmentRett's Syndrome1
2RecruitingPreventionChronic Lung Disease of Prematurity / Intraventricular Hemorrhage / Retinopathy of Prematurity (ROP)1
2RecruitingTreatment22q13 Deletion Syndrome / Phelan-McDermid Syndrome1
2RecruitingTreatmentAutism Spectrum Conditions/Disorders1
2TerminatedTreatmentInsulin-Like Growth Factor-1 Deficiency1
2, 3CompletedTreatmentGrowth Hormone Insensitivity Syndrome (GHIS)1
2, 3CompletedTreatmentMinor burns1
2, 3TerminatedTreatmentCrohn's Disease (CD)1
3CompletedNot AvailableDiabetes Mellitus (DM)1
3CompletedTreatmentAmyotrophic Lateral Sclerosis (ALS)1
3CompletedTreatmentGrowth Disorders / Insulin-Like Growth Factor-1 Deficiency1
3RecruitingTreatmentAnorexia Nervosa (AN)1
3TerminatedTreatmentGrowth Disorders1
Not AvailableActive Not RecruitingTreatmentAnorexia Nervosa (AN) / Osteopenia / Osteoporosis1
Not AvailableCompletedBasic ScienceEhlers-Danlos Syndrome, Classic1
Not AvailableCompletedBasic ScienceType 1 Insulin-Dependent Diabetes Mellitus1
Not AvailableRecruitingNot AvailableIGF1 Deficiency1
Not AvailableTerminatedNot AvailablePrimary Insulin-like Growth Factor-1 Deficiency1
Not AvailableWithdrawnTreatmentChronic Liver Diseases (CLD) / Growth Failure1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Baxter International Inc.
  • Hospira Inc.
  • Tercica Inc.
Dosage forms
FormRouteStrength
PatchTopical
Injection, solutionSubcutaneous10 mg/ml
Injection, solutionSubcutaneous40 mg/4mL
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)
US5200509No1993-04-062010-04-06Us
US5681814No1997-10-282017-09-18Us
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

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Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilitySolubleMecasermin Highlights of Prescribing Information Revised February 2010

Taxonomy

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

Targets

Kind
Protein
Organism
Humans
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 involv...
Gene Name
IGF1R
Uniprot ID
P08069
Uniprot Name
Insulin-like growth factor 1 receptor
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
Humans
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 IGF...
Gene Name
IGFBP3
Uniprot ID
P17936
Uniprot Name
Insulin-like growth factor-binding protein 3
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
Humans
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 (...
Gene Name
INSR
Uniprot ID
P06213
Uniprot Name
Insulin receptor
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
Humans
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 r...
Gene Name
IGF2R
Uniprot ID
P11717
Uniprot Name
Cation-independent mannose-6-phosphate receptor
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]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Carrier
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 IGF...
Gene Name
IGFBP3
Uniprot ID
P17936
Uniprot Name
Insulin-like growth factor-binding protein 3
Molecular Weight
31673.87 Da
References
  1. Allard JB, Duan C: IGF-Binding Proteins: Why Do They Exist and Why Are There So Many? Front Endocrinol (Lausanne). 2018 Apr 9;9:117. doi: 10.3389/fendo.2018.00117. eCollection 2018. [PubMed:29686648]
  2. Mecasermin Highlights of Prescribing Information Revised February 2010 [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Carrier
General Function
Involved in protein-protein interactions that result in protein complexes, receptor-ligand binding or cell adhesion.
Specific Function
Insulin-like growth factor binding
Gene Name
IGFALS
Uniprot ID
P35858
Uniprot Name
Insulin-like growth factor-binding protein complex acid labile subunit
Molecular Weight
66034.13 Da
References
  1. Allard JB, Duan C: IGF-Binding Proteins: Why Do They Exist and Why Are There So Many? Front Endocrinol (Lausanne). 2018 Apr 9;9:117. doi: 10.3389/fendo.2018.00117. eCollection 2018. [PubMed:29686648]
  2. Mecasermin Highlights of Prescribing Information Revised February 2010 [File]
3. Insulin-like growth factor-binding protein 1
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Carrier
References
  1. Allard JB, Duan C: IGF-Binding Proteins: Why Do They Exist and Why Are There So Many? Front Endocrinol (Lausanne). 2018 Apr 9;9:117. doi: 10.3389/fendo.2018.00117. eCollection 2018. [PubMed:29686648]
  2. Mecasermin Highlights of Prescribing Information Revised February 2010 [File]
4. Insulin-like growth factor-binding protein 2
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Carrier
References
  1. Allard JB, Duan C: IGF-Binding Proteins: Why Do They Exist and Why Are There So Many? Front Endocrinol (Lausanne). 2018 Apr 9;9:117. doi: 10.3389/fendo.2018.00117. eCollection 2018. [PubMed:29686648]
  2. Mecasermin Highlights of Prescribing Information Revised February 2010 [File]
5. Insulin-like growth factor-binding protein 4
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Carrier
References
  1. Allard JB, Duan C: IGF-Binding Proteins: Why Do They Exist and Why Are There So Many? Front Endocrinol (Lausanne). 2018 Apr 9;9:117. doi: 10.3389/fendo.2018.00117. eCollection 2018. [PubMed:29686648]
  2. Mecasermin Highlights of Prescribing Information Revised February 2010 [File]
6. Insulin-like growth factor-binding protein 5
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Carrier
References
  1. Allard JB, Duan C: IGF-Binding Proteins: Why Do They Exist and Why Are There So Many? Front Endocrinol (Lausanne). 2018 Apr 9;9:117. doi: 10.3389/fendo.2018.00117. eCollection 2018. [PubMed:29686648]
  2. Mecasermin Highlights of Prescribing Information Revised February 2010 [File]
7. Insulin-like growth factor-binding protein 6
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Carrier
References
  1. Allard JB, Duan C: IGF-Binding Proteins: Why Do They Exist and Why Are There So Many? Front Endocrinol (Lausanne). 2018 Apr 9;9:117. doi: 10.3389/fendo.2018.00117. eCollection 2018. [PubMed:29686648]
  2. Mecasermin Highlights of Prescribing Information Revised February 2010 [File]

Drug created on May 16, 2007 14:46 / Updated on June 04, 2019 05:15