Peringatan Keamanan

Overdosage of Mecasermin leads to hypoglycemiaF4009. 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.

Mecasermin

DB01277

biotech approved investigational

Deskripsi

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.

Struktur Molekul 2D

Struktur tidak tersedia

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Mean half life of 5.8 hours [F4009]
Volume Distribusi * 0.257 ± 0.073 L/kg [subjects with severe Primary IGFD] at a dose of 0.045mg/kg [F4009]
Klirens (Clearance) Clearance of Mecasermin is inversely proportional to IGF binding protein 3 (IGFBP-3) [F4009] * 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)

Absorpsi

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 determinedF4009.

Metabolisme

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 drugsA176017.

Rute Eliminasi

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 drugsA176017.

Interaksi Makanan

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

Interaksi Obat

603 Data
Pegvisomant The risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Mecasermin.
Lipoic acid The risk or severity of hypoglycemia can be increased when Lipoic acid is combined with Mecasermin.
Moxifloxacin The therapeutic efficacy of Mecasermin can be increased when used in combination with Moxifloxacin.
Grepafloxacin The therapeutic efficacy of Mecasermin can be increased when used in combination with Grepafloxacin.
Enoxacin The therapeutic efficacy of Mecasermin can be increased when used in combination with Enoxacin.
Pefloxacin The therapeutic efficacy of Mecasermin can be increased when used in combination with Pefloxacin.
Ciprofloxacin The therapeutic efficacy of Mecasermin can be increased when used in combination with Ciprofloxacin.
Trovafloxacin The therapeutic efficacy of Mecasermin can be increased when used in combination with Trovafloxacin.
Nalidixic acid The therapeutic efficacy of Mecasermin can be increased when used in combination with Nalidixic acid.
Rosoxacin The therapeutic efficacy of Mecasermin can be increased when used in combination with Rosoxacin.
Cinoxacin The therapeutic efficacy of Mecasermin can be increased when used in combination with Cinoxacin.
Lomefloxacin The therapeutic efficacy of Mecasermin can be increased when used in combination with Lomefloxacin.
Gatifloxacin The therapeutic efficacy of Mecasermin can be increased when used in combination with Gatifloxacin.
Norfloxacin The therapeutic efficacy of Mecasermin can be increased when used in combination with Norfloxacin.
Levofloxacin The therapeutic efficacy of Mecasermin can be increased when used in combination with Levofloxacin.
Gemifloxacin The therapeutic efficacy of Mecasermin can be increased when used in combination with Gemifloxacin.
Ofloxacin The therapeutic efficacy of Mecasermin can be increased when used in combination with Ofloxacin.
Sparfloxacin The therapeutic efficacy of Mecasermin can be increased when used in combination with Sparfloxacin.
Temafloxacin The therapeutic efficacy of Mecasermin can be increased when used in combination with Temafloxacin.
Fleroxacin The therapeutic efficacy of Mecasermin can be increased when used in combination with Fleroxacin.
Technetium Tc-99m ciprofloxacin The therapeutic efficacy of Mecasermin can be increased when used in combination with Technetium Tc-99m ciprofloxacin.
Garenoxacin The therapeutic efficacy of Mecasermin can be increased when used in combination with Garenoxacin.
Nemonoxacin The therapeutic efficacy of Mecasermin can be increased when used in combination with Nemonoxacin.
Flumequine The therapeutic efficacy of Mecasermin can be increased when used in combination with Flumequine.
Enrofloxacin The therapeutic efficacy of Mecasermin can be increased when used in combination with Enrofloxacin.
Orbifloxacin The therapeutic efficacy of Mecasermin can be increased when used in combination with Orbifloxacin.
Sarafloxacin The therapeutic efficacy of Mecasermin can be increased when used in combination with Sarafloxacin.
Difloxacin The therapeutic efficacy of Mecasermin can be increased when used in combination with Difloxacin.
Pazufloxacin The therapeutic efficacy of Mecasermin can be increased when used in combination with Pazufloxacin.
Prulifloxacin The therapeutic efficacy of Mecasermin can be increased when used in combination with Prulifloxacin.
Delafloxacin The therapeutic efficacy of Mecasermin can be increased when used in combination with Delafloxacin.
Sitafloxacin The therapeutic efficacy of Mecasermin can be increased when used in combination with Sitafloxacin.
Oxolinic acid The therapeutic efficacy of Mecasermin can be increased when used in combination with Oxolinic acid.
Rufloxacin The therapeutic efficacy of Mecasermin can be increased when used in combination with Rufloxacin.
Pipemidic acid The therapeutic efficacy of Mecasermin can be increased when used in combination with Pipemidic acid.
Methyclothiazide The therapeutic efficacy of Mecasermin can be decreased when used in combination with Methyclothiazide.
Chlorthalidone The therapeutic efficacy of Mecasermin can be decreased when used in combination with Chlorthalidone.
Bendroflumethiazide The therapeutic efficacy of Mecasermin can be decreased when used in combination with Bendroflumethiazide.
Metolazone The therapeutic efficacy of Mecasermin can be decreased when used in combination with Metolazone.
Benzthiazide The therapeutic efficacy of Mecasermin can be decreased when used in combination with Benzthiazide.
Hydroflumethiazide The therapeutic efficacy of Mecasermin can be decreased when used in combination with Hydroflumethiazide.
Indapamide The therapeutic efficacy of Mecasermin can be decreased when used in combination with Indapamide.
Chlorothiazide The therapeutic efficacy of Mecasermin can be decreased when used in combination with Chlorothiazide.
Hydrochlorothiazide The therapeutic efficacy of Mecasermin can be decreased when used in combination with Hydrochlorothiazide.
Trichlormethiazide The therapeutic efficacy of Mecasermin can be decreased when used in combination with Trichlormethiazide.
Polythiazide The therapeutic efficacy of Mecasermin can be decreased when used in combination with Polythiazide.
Quinethazone The therapeutic efficacy of Mecasermin can be decreased when used in combination with Quinethazone.
Cyclopenthiazide The therapeutic efficacy of Mecasermin can be decreased when used in combination with Cyclopenthiazide.
Epitizide The therapeutic efficacy of Mecasermin can be decreased when used in combination with Epitizide.
Amitriptyline Amitriptyline may decrease the hypoglycemic activities of Mecasermin.
Protriptyline Protriptyline may decrease the hypoglycemic activities of Mecasermin.
Imipramine Imipramine may decrease the hypoglycemic activities of Mecasermin.
Nortriptyline Nortriptyline may decrease the hypoglycemic activities of Mecasermin.
Amoxapine Amoxapine may decrease the hypoglycemic activities of Mecasermin.
Trimipramine Trimipramine may decrease the hypoglycemic activities of Mecasermin.
Doxepin Doxepin may decrease the hypoglycemic activities of Mecasermin.
Desipramine Desipramine may decrease the hypoglycemic activities of Mecasermin.
Clomipramine Clomipramine may decrease the hypoglycemic activities of Mecasermin.
Amineptine Amineptine may decrease the hypoglycemic activities of Mecasermin.
Dimetacrine Dimetacrine may decrease the hypoglycemic activities of Mecasermin.
Butriptyline Butriptyline may decrease the hypoglycemic activities of Mecasermin.
Dosulepin Dosulepin may decrease the hypoglycemic activities of Mecasermin.
Tianeptine Tianeptine may decrease the hypoglycemic activities of Mecasermin.
Oxaprotiline Oxaprotiline may decrease the hypoglycemic activities of Mecasermin.
Opipramol Opipramol may decrease the hypoglycemic activities of Mecasermin.
Amitriptylinoxide Amitriptylinoxide may decrease the hypoglycemic activities of Mecasermin.
Dibenzepin Dibenzepin may decrease the hypoglycemic activities of Mecasermin.
Quinupramine Quinupramine may decrease the hypoglycemic activities of Mecasermin.
Melitracen Melitracen may decrease the hypoglycemic activities of Mecasermin.
Lofepramine Lofepramine may decrease the hypoglycemic activities of Mecasermin.
Iprindole Iprindole may decrease the hypoglycemic activities of Mecasermin.
Imipramine oxide Imipramine oxide may decrease the hypoglycemic activities of Mecasermin.
Dapagliflozin Dapagliflozin may increase the hypoglycemic activities of Mecasermin.
Canagliflozin Canagliflozin may increase the hypoglycemic activities of Mecasermin.
Leuprolide The therapeutic efficacy of Mecasermin can be decreased when used in combination with Leuprolide.
Goserelin The therapeutic efficacy of Mecasermin can be decreased when used in combination with Goserelin.
Nelfinavir The therapeutic efficacy of Mecasermin can be decreased when used in combination with Nelfinavir.
Indinavir The therapeutic efficacy of Mecasermin can be decreased when used in combination with Indinavir.
Ziprasidone The therapeutic efficacy of Mecasermin can be decreased when used in combination with Ziprasidone.
Etonogestrel The therapeutic efficacy of Mecasermin can be decreased when used in combination with Etonogestrel.
Desogestrel The therapeutic efficacy of Mecasermin can be decreased when used in combination with Desogestrel.
Olanzapine The therapeutic efficacy of Mecasermin can be decreased when used in combination with Olanzapine.
Megestrol acetate The therapeutic efficacy of Mecasermin can be decreased when used in combination with Megestrol acetate.
Clozapine The therapeutic efficacy of Mecasermin can be decreased when used in combination with Clozapine.
Levonorgestrel The therapeutic efficacy of Mecasermin can be decreased when used in combination with Levonorgestrel.
Progesterone The therapeutic efficacy of Mecasermin can be decreased when used in combination with Progesterone.
Chlorpromazine The therapeutic efficacy of Mecasermin can be decreased when used in combination with Chlorpromazine.
Haloperidol The therapeutic efficacy of Mecasermin can be decreased when used in combination with Haloperidol.
Ritonavir The therapeutic efficacy of Mecasermin can be decreased when used in combination with Ritonavir.
Piperazine The therapeutic efficacy of Mecasermin can be decreased when used in combination with Piperazine.
Medroxyprogesterone acetate The therapeutic efficacy of Mecasermin can be decreased when used in combination with Medroxyprogesterone acetate.
Niacin The therapeutic efficacy of Mecasermin can be decreased when used in combination with Niacin.
Epinephrine The therapeutic efficacy of Mecasermin can be decreased when used in combination with Epinephrine.
Norethisterone The therapeutic efficacy of Mecasermin can be decreased when used in combination with Norethisterone.
Risperidone The therapeutic efficacy of Mecasermin can be decreased when used in combination with Risperidone.
Pentamidine The therapeutic efficacy of Mecasermin can be decreased when used in combination with Pentamidine.
Ethynodiol diacetate The therapeutic efficacy of Mecasermin can be decreased when used in combination with Ethynodiol diacetate.
Pseudoephedrine The therapeutic efficacy of Mecasermin can be decreased when used in combination with Pseudoephedrine.
Tacrolimus The therapeutic efficacy of Mecasermin can be decreased when used in combination with Tacrolimus.
Sirolimus The therapeutic efficacy of Mecasermin can be decreased when used in combination with Sirolimus.

Target Protein

Insulin-like growth factor 1 receptor IGF1R
Insulin-like growth factor-binding protein 3 IGFBP3
Insulin receptor INSR
Cation-independent mannose-6-phosphate receptor IGF2R

Referensi & Sumber

Artikel (PubMed)
  • PMID: 18481900
    Keating GM: Mecasermin. BioDrugs. 2008;22(3):177-88.
  • 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: 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: 16905026
    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.
  • PMID: 8282084
    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.
  • PMID: 25366889
    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.

Contoh Produk & Brand

Produk: 6 • International brands: 0
Produk
  • Cosmeceutical Mask Pack
    Patch • - • Topical • US • OTC
  • Cosmeceutical Mask Pack
    Patch • - • Topical • US • OTC
  • Dermaheal Cosmeceutical Mask Pack Plus
    Patch • - • Topical • US • OTC
  • Increlex
    Injection, solution • 40 mg/4mL • Subcutaneous • US • Approved
  • Increlex
    Solution • 40 mg / 4 mL • Subcutaneous • Canada • Approved
  • Increlex
    Injection, solution • 10 mg/ml • Subcutaneous • EU • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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