Peringatan Keamanan

Studies on carcinogenicity, genotoxicity, animal fertility, fetal development, excretion in breast milk, and use in patients over 65 years have not been performedFDA Label. Use in pregnant, breast feeding, or geriatric populations should be avoided as there is a lack of safety dataFDA Label.
Animal reproductive toxicity studies have shown increased incidence of abortion, post implantation loss, fewer viable fetuses, and an increase in fetal skeletal abnormalitiesF4054.
Insulin-like growth factor 1 (IGF-1) without insulin-like growth factor binding protein 3 (IGFBP-3) has been shown to not be mutagenic according to the Ames test and have no affect on fertility in rats given 7 times the maximum human recommended dose based on body surface areaFDA Label.
No studies have been performed in patients with impaired renal or hepatic function however these impairments are not expected to significantly affect the pharmacokinetics of Mecasermin rinfabateF4054.

Mecasermin rinfabate

DB14751

biotech approved

Deskripsi

Mecasermin rinfabate is approved for severe primary insulin-like growth factor (IGF) deficiency or in patients with GH gene deletion who have developed antibodies to growth hormone (GH)A176020. Mecasermin rinfabate is similar to DB01277 in that both drugs contain recombinant DNA origin insulin-like growth factor 1 (IGF-1). Mecasermin rinfabate however, is already bound to recombinant DNA origin insulin-like growth factor binding protein 3 (IGFBP-3)A12605. The binding of IGF-1 to IGFBP-3 is said to extend the half life and reduce the clearance of IGF-1 in patients with growth hormone resistant syndromes and low levels of IGFBP-3 though this may represent <500 patients worldwideA176065.

Mecasermin rinfabate manufactured by Insmed Incorporated under the brand name Iplex was approved by the FDA in 2005L5722. In 2007 Insmed withdrew their application for a marketing authorization with The European Medicines AgencyF4075.

Struktur Molekul 2D

Struktur tidak tersedia

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Half life ranges from 10 to 16 hours with a mean of 13 hours[F4054]. Mecasermin rinfabate is said to have a longer half life than [DB01277][A176065].
Volume Distribusi Approximately 1000mL/kg[F4054].
Klirens (Clearance) Clearance ranges from 50 to 56mL/hr/kg with a mean of 53mL/hr/kg[F4054]. Mecasermin rinfabate is said to have lower clearance than [DB01277][A176065]

Absorpsi

There is little published data on the pharmacokinetics of Mecasermin rinfabateA12605. Mecasermin rinfabate is injected subcutaneously and distributes rapidly throughout the body, especially in well vascularized tissueF4054.

Metabolisme

There is little published data on the pharmacokinetics of Mecasermin rinfabateA12605. Mecasermin rinfabate is expected to degrade into small peptides and amino acidsF4054. It is suspected that IGFBP-3 in Mecasermin rinfabate is broken down by serine proteases or metalloproteasesA12605.

Rute Eliminasi

An excretion study in monkeys showed elimination in the urine 72 hours after administrationF4054.

Interaksi Makanan

1 Data
  • 1. Take at the same time every day.

Interaksi Obat

0 Data
Tidak ada data.

Target Protein

Insulin-like growth factor 1 receptor IGF1R
Insulin receptor INSR
Cation-independent mannose-6-phosphate receptor IGF2R

Referensi & Sumber

Artikel (PubMed)
  • PMID: 17380212
    Kemp SF: Mecasermin rinfabate. Drugs Today (Barc). 2007 Mar;43(3):149-55. doi: 10.1358/dot.2007.43.3.1079876.
  • PMID: 19627167
    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.
  • PMID: 18363546
    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 .
  • PMID: 19198769
    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.
  • PMID: 16610982
    Kemp SF, Fowlkes JL, Thrailkill KM: Efficacy and safety of mecasermin rinfabate. Expert Opin Biol Ther. 2006 May;6(5):533-8. doi: 10.1517/14712598.6.5.533 .
  • PMID: 18165284
    Collett-Solberg PF, Misra M: The role of recombinant human insulin-like growth factor-I in treating children with short stature. J Clin Endocrinol Metab. 2008 Jan;93(1):10-8. doi: 10.1210/jc.2007-1534. Epub 2007 Dec 28.
  • PMID: 22654863
    Forbes BE, McCarthy P, Norton RS: Insulin-like growth factor binding proteins: a structural perspective. Front Endocrinol (Lausanne). 2012 Mar 2;3:38. doi: 10.3389/fendo.2012.00038. eCollection 2012.

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