Peringatan Keamanan

The FDA label includes a black box warning of mipomersem induced hepatoxicity. Other less serious adverse effects include nausea, headache, fatigue, local injection site reactions, and flu-like symptoms.

Mipomersen

DB05528

biotech approved investigational

Deskripsi

Mipomersen sodium, which was known as the investigational drug, isis-301012, is the salt form of a synthetic phosphorothioate oligonucleotide. Mipomersen sodium prevents the formation of apo B-100, resulting in a decrease in the levels of apolipoprotein B (apo B), low density lipoprotein (LDL), and total cholesterol. Mipomersen is indicated in patients with homozygous familial hypercholesterolemia as an adjunct to diet and other lipid-lowering medications. It is marketed under the brand name Kynamro in the United States, and the FDA label includes a black box warning of hepatoxicity. Specifically, elevations in the liver enzymes, i.e. transaminases, and in liver fat (hepatic steatosis) have been reported. Due to this serious risk of liver toxicity, mipomersen sodium is only available to patients under the restricted program called Kynamro Risk Evaluation and Mitigation Strategy program.

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) Mipomersem has a very long half life of 1-2 months.
Volume Distribusi The volume of distribution for mipomersen was not quantified.
Klirens (Clearance) Clearance of mipomersem was not quantified.

Absorpsi

The maximum mipomersen concentration is reached in about 3-4 hours after subcutaneous injection. Additionally the bioavailability of mipomersn is dose-dependant and ranges from 54%-78%.

Metabolisme

Mipomersem is metabolized by endonucleases. Once degraded into shorter oligonucleotides, it is metabolized further by exonucleases.

Rute Eliminasi

24 hours after mipomersem administration, less than 4% of mipomersem and/or it's metabolites were excreted in the urine.

Interaksi Makanan

1 Data
  • 1. Avoid excessive or chronic alcohol consumption. Alcohol may increase the risk of liver injury.

Interaksi Obat

26 Data
Doxycycline Doxycycline may increase the hepatotoxic activities of Mipomersen.
Lymecycline Lymecycline may increase the hepatotoxic activities of Mipomersen.
Clomocycline Clomocycline may increase the hepatotoxic activities of Mipomersen.
Tigecycline Tigecycline may increase the hepatotoxic activities of Mipomersen.
Oxytetracycline Oxytetracycline may increase the hepatotoxic activities of Mipomersen.
Demeclocycline Demeclocycline may increase the hepatotoxic activities of Mipomersen.
Tetracycline Tetracycline may increase the hepatotoxic activities of Mipomersen.
Metacycline Metacycline may increase the hepatotoxic activities of Mipomersen.
Minocycline Minocycline may increase the hepatotoxic activities of Mipomersen.
Rolitetracycline Rolitetracycline may increase the hepatotoxic activities of Mipomersen.
Sarecycline Sarecycline may increase the hepatotoxic activities of Mipomersen.
Eravacycline Eravacycline may increase the hepatotoxic activities of Mipomersen.
Omadacycline Omadacycline may increase the hepatotoxic activities of Mipomersen.
Penimepicycline Penimepicycline may increase the hepatotoxic activities of Mipomersen.
Acetaminophen Acetaminophen may increase the hepatotoxic activities of Mipomersen.
Propacetamol Propacetamol may increase the hepatotoxic activities of Mipomersen.
Methotrexate Mipomersen may increase the hepatotoxic activities of Methotrexate.
Tamoxifen Tamoxifen may increase the hepatotoxic activities of Mipomersen.
Isotretinoin Isotretinoin may increase the hepatotoxic activities of Mipomersen.
Amiodarone Amiodarone may increase the hepatotoxic activities of Mipomersen.
Lomitapide Lomitapide may increase the hepatotoxic activities of Mipomersen.
Ethanol Ethanol may increase the hepatotoxic activities of Mipomersen.
Pexidartinib Mipomersen may increase the hepatotoxic activities of Pexidartinib.
Valoctocogene roxaparvovec The therapeutic efficacy of Valoctocogene roxaparvovec can be decreased when used in combination with Mipomersen.
Leflunomide The risk or severity of liver damage can be increased when Mipomersen is combined with Leflunomide.
Teriflunomide The risk or severity of liver damage can be increased when Mipomersen is combined with Teriflunomide.

Target Protein

Apolipoprotein B-100 APOB
mRNA of ApoB-100

Referensi & Sumber

Artikel (PubMed)
  • PMID: 17030687
    Kastelein JJ, Wedel MK, Baker BF, Su J, Bradley JD, Yu RZ, Chuang E, Graham MJ, Crooke RM: Potent reduction of apolipoprotein B and low-density lipoprotein cholesterol by short-term administration of an antisense inhibitor of apolipoprotein B. Circulation. 2006 Oct 17;114(16):1729-35. Epub 2006 Oct 9.
  • PMID: 23564617
    Hair P, Cameron F, McKeage K: Mipomersen sodium: first global approval. Drugs. 2013 Apr;73(5):487-93. doi: 10.1007/s40265-013-0042-2.

Contoh Produk & Brand

Produk: 3 • International brands: 1
Produk
  • Kynamro
    Injection, solution • 200 mg/1mL • Subcutaneous • US • Approved
  • Kynamro
    Injection, solution • 200 mg/1mL • Subcutaneous • US • Approved
  • Kynamro
    Injection, solution • 200 mg/1mL • Subcutaneous • US • Approved
International Brands
  • Kynamro

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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