Mecasermin

Identification

Summary

Mecasermin is a recombinant insulin-like growth factor-1 used for the long-term treatment of growth failure in pediatric patients with primary IGF-1 deficiency or with growth hormone gene deletion due to the development of neutralizing antibodies to GH.

Brand Names

Increlex

Generic Name

Mecasermin

DrugBank Accession Number

DB01277

Background

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.

Type

Biotech

Groups

Approved, Investigational

Biologic Classification

Protein Based Therapies
Hormones

Protein Structure

Protein Chemical Formula

C₃₃₁H₅₁₈N₉₄O₁₀₁S₇

Protein Average Weight

7649.0 Da

Sequences

>Mecasermin
GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMY
CAPLKPAKSA

Download FASTA Format

Synonyms

• Human somatomedin C
• Mecasermin
• Mecasermin recombinant
• Mecasermina
• Mechano growth factor

External IDs

• CEP 151
• CEP-151
• CG-GF2
• CG-IGF-1
• PV-802
• PV802

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.

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Associated Conditions

• Primary Insulin-like Growth Factor-1 Deficiency

Contraindications & Blackbox Warnings

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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.

Target	Actions	Organism
AInsulin-like growth factor 1 receptor	agonist	Humans
UInsulin-like growth factor-binding protein 3	Not Available	Humans
UInsulin receptor	Not Available	Humans
UCation-independent mannose-6-phosphate receptor	Not Available	Humans

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 determined⁸.

Volume of distribution

• 0.257 ± 0.073 L/kg [subjects with severe Primary IGFD] at a dose of 0.045mg/kg ⁸

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 ⁸.

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 ⁸

Clearance

Clearance of Mecasermin is inversely proportional to IGF binding protein 3 (IGFBP-3) ⁸ * 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)

Adverse Effects

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Toxicity

Overdosage of Mecasermin leads to hypoglycemia⁸. 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.

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.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drug	Interaction
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Acarbose	The risk or severity of hypoglycemia can be increased when Acarbose is combined with Mecasermin.
Acebutolol	The therapeutic efficacy of Mecasermin can be increased when used in combination with Acebutolol.
Acetazolamide	The therapeutic efficacy of Mecasermin can be increased when used in combination with Acetazolamide.
Acetohexamide	The risk or severity of hypoglycemia can be increased when Mecasermin is combined with Acetohexamide.
Acetyl sulfisoxazole	The therapeutic efficacy of Mecasermin can be increased when used in combination with Acetyl sulfisoxazole.
Acetylsalicylic acid	The risk or severity of hypoglycemia can be increased when Acetylsalicylic acid is combined with Mecasermin.
Albiglutide	The risk or severity of hypoglycemia can be increased when Mecasermin is combined with Albiglutide.
Alclometasone	The risk or severity of hyperglycemia can be increased when Alclometasone is combined with Mecasermin.
Alogliptin	The risk or severity of hypoglycemia can be increased when Mecasermin is combined with Alogliptin.
Amcinonide	The risk or severity of hyperglycemia can be increased when Amcinonide is combined with Mecasermin.

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Food Interactions

• Take with food. Mecasermin should be administered shortly before or after a meal due to its hypoglycemic effects.

Products

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Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Increlex	Injection, solution	40 mg/4mL	Subcutaneous	Ipsen Biopharmaceuticals, Inc.	2006-01-03	Not applicable
Increlex	Injection, solution	10 mg/ml	Subcutaneous	Ipsen Pharma	2016-09-08	Not applicable
Increlex	Solution	40 mg / 4 mL	Subcutaneous	Ipsen Biopharmaceuticals Canada Inc	2021-03-01	Not applicable

Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End	Region	Image
Cosmeceutical Mask Pack	Mecasermin (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)	Patch	Topical	YBK Investment, INC	2013-10-21	2013-10-29
Cosmeceutical Mask Pack	Mecasermin (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)	Patch	Topical	YBK Investment, INC	2013-10-21	Not applicable
Dermaheal Cosmeceutical Mask Pack Plus	Mecasermin (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)	Patch	Topical	YBK Investment, INC	2013-10-21	Not applicable

Unapproved/Other Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End	Region	Image
Cosmeceutical Mask Pack	Mecasermin (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)	Patch	Topical	YBK Investment, INC	2013-10-21	2013-10-29
Cosmeceutical Mask Pack	Mecasermin (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)	Patch	Topical	YBK Investment, INC	2013-10-21	Not applicable
Dermaheal Cosmeceutical Mask Pack Plus	Mecasermin (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)	Patch	Topical	YBK Investment, INC	2013-10-21	Not applicable

Categories

ATC Codes

H01AC03 — Mecasermin

• H01AC — Somatropin and somatropin agonists
• H01A — ANTERIOR PITUITARY LOBE HORMONES AND ANALOGUES
• H01 — PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES
• H — SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS

Drug Categories

• Amino Acids, Peptides, and Proteins
• Anterior Pituitary Lobe Hormones and Analogues
• Biological Factors
• Blood Glucose Lowering Agents
• Blood Proteins
• Growth Substances
• Human Insulin-like Growth Factor Analogs
• Hypoglycemia-Associated Agents
• Intercellular Signaling Peptides and Proteins
• Peptides
• Pituitary and Hypothalamic Hormones and Analogues
• Proteins
• Recombinant Human Insulin-like Growth Factor-1
• Somatomedins
• Somatotropin Agonists
• Somatropin and Somatropin Agonists
• 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

Affected organisms

• Humans and other mammals

Chemical Identifiers

UNII

7GR9I2683O

CAS number

68562-41-4

References

General References

1. Keating GM: Mecasermin. BioDrugs. 2008;22(3):177-88. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]
7. FDA Approved Drug Products: Increlex Mecasermin Subcutaneous Injection [Link]
8. Mecasermin Highlights of Prescribing Information Revised February 2010 [File]
9. European Patent Specification [File]

External Links

KEGG Drug

D04870

PubChem Substance

46504889

RxNav

274403

ChEMBL

CHEMBL1201716

Therapeutic Targets Database

DAP000287

PharmGKB

PA164774876

RxList

RxList Drug Page

Drugs.com

Drugs.com Drug Page

Wikipedia

Mecasermin

FDA label

Download (490 KB)

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
3	Completed	Not Available	Diabetes	1
3	Completed	Treatment	Anorexia Nervosa (AN)	1
3	Completed	Treatment	Growth Disorders / Insulin-Like Growth Factor-1 Deficiency	1
3	Terminated	Treatment	Growth Disorders	1
2	Completed	Treatment	22Q13.3 Deletion Syndrome / Phelan McDermid Syndrome	1
2	Completed	Treatment	Multiple Sclerosis	1
2	Completed	Treatment	Rett Syndrome	1
2	Recruiting	Treatment	Autism Disorder	1
2	Terminated	Treatment	Insulin-Like Growth Factor-1 Deficiency	1
2, 3	Completed	Treatment	Growth Disorders / Insulin-Like Growth Factor-1 Deficiency	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

• Baxter International Inc.
• Hospira Inc.
• Tercica Inc.

Dosage Forms

Form	Route	Strength
Patch	Topical
Injection, solution	Parenteral; Subcutaneous	10 MG/ML
Injection, solution	Subcutaneous	10 mg/ml
Injection, solution	Subcutaneous	40 mg/4mL
Solution	Subcutaneous	40 mg / 4 mL

Prices

Unit description	Cost	Unit
Increlex 40 mg/4 ml vial	232.8USD	ml

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)	Region
US5200509	No	1993-04-06	2010-04-06
US5681814	No	1997-10-28	2017-09-18

Properties

State

Solid

Experimental Properties

Property	Value	Source
water solubility	Soluble	Mecasermin Highlights of Prescribing Information Revised February 2010

Targets

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Details1. Insulin-like growth factor 1 receptor

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. [Article]

Details2. Insulin-like growth factor-binding protein 3

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. [Article]
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 . [Article]
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. [Article]

Details3. Insulin receptor

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. [Article]

Details4. Cation-independent mannose-6-phosphate receptor

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. [Article]

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Drug created at May 16, 2007 20:46 / Updated at June 03, 2022 07:24