Description

Simple

A medication used to promote growth in children with growth hormone deficiency.

Clinical

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.

Overview

Mecasermin contains recombinant-DNA-engineered human insulin-like growth factor-1 (rhIGF-1)[FDA 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.

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 t... Read more

Pharmacodynamic

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 growth[ Read more

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 gro... Read more

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 determined[ Read more

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].

Volume of distribution

0.257 ± 0.073 L/kg [subjects with severe Primary IGFD] at a dose of 0.045mg/kg [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-3Clearanc... Read more

Half life

Mean half life of 5.8 hours [8]

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 drugs[ Read more

Toxicity

Overdosage of Mecasermin leads to hypoglycemia[8]. One case of acute overdose was treated with IV glucose. Long-term overdosage may result in signs and symptoms of acro... Read more

Adverse Effects

Contraindications

  • Route:
    • Subcutaneous
  • Dose Form:
    • Injection, solution
  • Regions: US
  • Patient Conditions:
      • Name: Hypersensitive
      • Drugbank Id: DBCOND0104833
  • Route:
    • Subcutaneous
  • Dose Form:
    • Injection, solution
  • Regions: US
  • Patient Conditions:
      • Name: Neoplasia
      • Drugbank Id: DBCOND0035000
  • Route:
    • Subcutaneous
  • Dose Form:
    • Injection, solution
  • Regions: US
  • With Therapies:
      • Name: Intravenous
      • Drugbank Id: DBCOND0066723

Food Interactions

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

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
2,4-thiazolidinedione
The risk or severity of hypoglycemia can be increased when Mecasermin is combined with 2,4-thiazolidinedione.
5-(2-methylpiperazine-1-sulfonyl)isoquinoline
The 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-tetrahydroisoquinoline
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypoglycemic activities of Mecasermin.
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 Acetohexamide is combined with Mecasermin.
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.
Agmatine
The risk or severity of hypoglycemia can be increased when Agmatine is combined with Mecasermin.
AICA ribonucleotide
The risk or severity of hypoglycemia can be increased when Mecasermin is combined with AICA ribonucleotide.
Alaproclate
The risk or severity of hypoglycemia can be increased when Mecasermin is combined with Alaproclate.
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.
Aldosterone
The risk or severity of hyperglycemia can be increased when Aldosterone is combined with Mecasermin.
Allicin
The risk or severity of hypoglycemia can be increased when Mecasermin is combined with Allicin.
Alogliptin
The risk or severity of hypoglycemia can be increased when Mecasermin is combined with Alogliptin.
Aloxiprin
Aloxiprin may increase the hypoglycemic activities of Mecasermin.
Alprenolol
The therapeutic efficacy of Mecasermin can be increased when used in combination with Alprenolol.
Amcinonide
The risk or severity of hyperglycemia can be increased when Amcinonide is combined with Mecasermin.
9 References
  1. 1 . Keating GM: Mecasermin. BioDrugs. 2008;22(3):177-88.PubMed: 18481900
  2. 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. 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. 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. 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. 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. 7 . FDA Approved Drug Products: Increlex Mecasermin Subcutaneous Injection Link
  8. 8 . Mecasermin Highlights of Prescribing Information Revised February 2010 File
  9. 9 . European Patent Specification File