Identification

Name
Mecasermin
Accession Number
DB01277
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.

Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Hormones
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

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
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.

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
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.

Affected organisms
  • Humans and other mammals
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.
DrugInteraction
AcarboseThe risk or severity of hypoglycemia can be increased when Acarbose is combined with Mecasermin.
AcebutololThe therapeutic efficacy of Mecasermin can be increased when used in combination with Acebutolol.
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 acidThe risk or severity of hypoglycemia can be increased when Acetylsalicylic acid is combined with Mecasermin.
AlbiglutideThe risk or severity of hypoglycemia can be increased when Mecasermin is combined with Albiglutide.
AlclometasoneThe risk or severity of hyperglycemia can be increased when Alclometasone is combined with Mecasermin.
AlogliptinThe risk or severity of hypoglycemia can be increased when Mecasermin is combined with Alogliptin.
AmcinonideThe risk or severity of hyperglycemia can be increased when Amcinonide is combined with Mecasermin.
Additional Data Available
  • Extended Description
    Extended Description
    Available for Purchase

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity
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    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level
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    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
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    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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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
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
IncrelexInjection, solution40 mg/4mLSubcutaneousIpsen Biopharmaceuticals, Inc.2006-01-03Not applicableUS flag
IncrelexInjection, solution10 mg/mlSubcutaneousIpsen Pharma2007-08-03Not applicableEU flag
Additional Data Available
  • Application Number
    Application Number
    Available for Purchase

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code
    Available for Purchase

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

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Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
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 flag
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 flag
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 flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
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 flag
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 flag
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 flag

Categories

ATC Codes
H01AC03 — Mecasermin
Drug Categories
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

Chemical Identifiers

UNII
7GR9I2683O
CAS number
68562-41-4

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. FDA Approved Drug Products: Increlex Mecasermin Subcutaneous Injection [Link]
  8. Mecasermin Highlights of Prescribing Information Revised February 2010 [File]
  9. European Patent Specification [File]
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
PhaseStatusPurposeConditionsCount
3Active Not RecruitingTreatmentAnorexia Nervosa (AN)1
3CompletedNot AvailableDiabetes1
3CompletedTreatmentGrowth Disorders / Insulin-Like Growth Factor-1 Deficiency1
3TerminatedTreatmentGrowth Disorders1
2CompletedTreatmentDisseminated Sclerosis1
2CompletedTreatmentRett's Syndrome1
2RecruitingTreatment22q13 Deletion Syndrome / Phelan-McDermid Syndrome1
2RecruitingTreatmentAutism Spectrum Conditions/Disorders1
2TerminatedTreatmentInsulin-Like Growth Factor-1 Deficiency1
2, 3CompletedTreatmentGrowth Disorders / Insulin-Like Growth Factor-1 Deficiency1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Baxter International Inc.
  • Hospira Inc.
  • Tercica Inc.
Dosage Forms
FormRouteStrength
PatchTopical
Injection, solutionCutaneous; Parenteral10 MG/ML
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)Region
US5200509No1993-04-062010-04-06US flag
US5681814No1997-10-282017-09-18US flag
Additional Data Available
  • Filed On
    Filed On
    Available for Purchase

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

    Learn more

Properties

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

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]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Carrier
General 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. Promotes cell migration.
Specific Function
Insulin-like growth factor binding
Gene Name
IGFBP1
Uniprot ID
P08833
Uniprot Name
Insulin-like growth factor-binding protein 1
Molecular Weight
27903.38 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
Inhibits IGF-mediated growth and developmental rates. 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.
Specific Function
Insulin-like growth factor i binding
Gene Name
IGFBP2
Uniprot ID
P18065
Uniprot Name
Insulin-like growth factor-binding protein 2
Molecular Weight
34813.85 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
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.
Specific Function
Insulin-like growth factor i binding
Gene Name
IGFBP4
Uniprot ID
P22692
Uniprot Name
Insulin-like growth factor-binding protein 4
Molecular Weight
27933.695 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
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.
Specific Function
Fibronectin binding
Gene Name
IGFBP5
Uniprot ID
P24593
Uniprot Name
Insulin-like growth factor-binding protein 5
Molecular Weight
30569.985 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
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.
Specific Function
Fibronectin binding
Gene Name
IGFBP6
Uniprot ID
P24592
Uniprot Name
Insulin-like growth factor-binding protein 6
Molecular Weight
25322.225 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]

Drug created on May 16, 2007 14:46 / Updated on June 12, 2020 10:51

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