Peringatan Keamanan

There has been one case of accidental overdose of fomivirsen with administration once bilaterally with 990 ?g per eye; vision was restored with anterior chamber paracentesis performed bilaterally L1428.
According to the findings in Salmonella/Microsome (Ames) and mouse lymphoma tests, fomivirsen was not shown to be mutagenic. In the in vivo mouse micronucleus assay, fomivirsen was not clastogenic. Animal reproductive studies or studies evaluating the carcinogenic potential of fomivirsen has not been conducted FDA Label.

Fomivirsen

DB06759

biotech approved investigational withdrawn

Deskripsi

Fomivirsen is a antisense 21 mer phosphorothioate oligonucleotide. It is an antiviral agent that was used in the treatment of cytomegalovirus retinitis (CMV) in immunocompromised patients, including those with AIDS. As a complementary nucleotide to the messenger RNA of the major immediate-early region proteins of human cytomegalovirus, it disrupts the replication of the virus through an antisense mechanism L1428. It was discovered by scientists at the National Institutes of Health (NIH) and was first developed by Isis Pharmaceuticals and subsequently licensed to Novartis A31990. The drug was withdrawn by the FDA because while there was a high unmet need for drugs to treat CMV when the drug was initially discovered and developed due to the CMV arising in people with AIDS, the development of HAART dramatically reduced the number of cases of CMV. Fomivirsen is marketed under the trade name Vitravene for intravitreal injection and was the first antisense drug to be approved by the Food and Drug Administration (FDA).

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) Intravitreal drug clearance studies have revealed first-order kinetics [A31989]. Following intravitreal administration, fomivirsen is slowly cleared from vitreous with a half-life of approximately 55 hours in humans [A31988]. The half life from retina in monkeys following administration of 115 mcg fomivirsen is estimated to be 78 hours [A31988].
Volume Distribusi Preclinical studies show that fomivirsen distributes to retina [A31988].
Klirens (Clearance) Clearance from retina was shown to be similarly slow following loading from the vitreous [A31988].

Absorpsi

Following intravitreal injection in rabbits and monkeys, peak concentrations in the vitreous was detectable immediately after injection with the concentrations increasing in a dose-proportional manner L1428. Due to low doses of intravitreal administration with slow disposition from the eye, there is limited absorption of the drug into the systemic circulation A31988. Fomivirsen is detectable in retina of rabbits within hours following administration and concentrations increase over 3 to 5 days. The concentrations of the drug were highest in the retina and iris FDA Label.

Metabolisme

Fomivirsen undergoes metabolism mediated by endo- and exonuclease, where the resides from the terminal ends of the oligonucleotide are sequentially removed FDA Label, L1428. Resulting shortened oligonucleotides and mononucleotide metabolites can be detected in the retina and vitreous of animals FDA Label. Mononucleotides may also be further catabolized to endogenous nucleotides and excreted as low molecular weight metabolites FDA Label.

Rute Eliminasi

In rabbits, 16% of total radiolabelled fomivirsen was detected in urine and 3% was detected in feces FDA Label.

Interaksi Obat

0 Data
Tidak ada data.

Target Protein

30 kDa immediate-early protein 2 UL122
45 kDa immediate-early protein 2 UL122

Referensi & Sumber

Artikel (PubMed)
  • PMID: 11978144
    Geary RS, Henry SP, Grillone LR: Fomivirsen: clinical pharmacology and potential drug interactions. Clin Pharmacokinet. 2002;41(4):255-60. doi: 10.2165/00003088-200241040-00002.
  • PMID: 10611727
    de Smet MD, Meenken CJ, van den Horn GJ: Fomivirsen - a phosphorothioate oligonucleotide for the treatment of CMV retinitis. Ocul Immunol Inflamm. 1999 Dec;7(3-4):189-98.
  • PMID: 11497353
    Orr RM: Technology evaluation: fomivirsen, Isis Pharmaceuticals Inc/CIBA vision. Curr Opin Mol Ther. 2001 Jun;3(3):288-94.
  • PMID: 12610136
    Isomura H, Stinski MF: The human cytomegalovirus major immediate-early enhancer determines the efficiency of immediate-early gene transcription and viral replication in permissive cells at low multiplicity of infection. J Virol. 2003 Mar;77(6):3602-14.
  • PMID: 11160686
    Marchini A, Liu H, Zhu H: Human cytomegalovirus with IE-2 (UL122) deleted fails to express early lytic genes. J Virol. 2001 Feb;75(4):1870-8. doi: 10.1128/JVI.75.4.1870-1878.2001.

Contoh Produk & Brand

Produk: 0 • International brands: 0
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Sekuens Gen/Protein (FASTA)

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