Edoxudine

DB13421

small molecule approved investigational withdrawn

Deskripsi

Edoxudine is a deoxythymidine analog with activity against herpes simplex virus. It is a potent and selective inhibitor of herpes simplex virus type 1 and 2. The obtained product is an antiviral ointment.L2407 The activity of edoxudine against herpes simplex virus was first recognized in 1967. It was later recognized to be effective in vivo in a preclinical model of keratitis caused by herpes virus.A32643 It was developed by McNeil Pharmaceutical and approved by Health Canada on December 31, 1992. This medication was later discontinued from the market in 1998.L1113

Struktur Molekul 2D

Berat 256.258
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) In preclinical trials on mice, after intravenous administration, edoxudine presented a very short distribution half-life of 1.4 min. In the same trials, the elimination half-life was reported to be of 24.1 min.[A27185]
Volume Distribusi This pharmacokinetic property is not available.
Klirens (Clearance) The plasma clearance of edoxudine is reported to be 85 ml/min.[A32659]

Absorpsi

Edoxudine cream is able to penetrate the skin in a very rapid manner. This easy penetration allows edoxudine to have a greater activity when compared with other topical antivirals that have better antiviral activity in vitro.A32643 In preclinical trials in mice, after intravenous administration of edoxudine, the mean residence time was 25 min. Edoxudine presented a bioavailability of 49% with a Cmax and tmax of 2.4 mcg/g and 31.1 min respectively. The AUC in plasma of edoxudine is significantly higher when administered orally when compared with intravenous administration.A27185

Metabolisme

In preclinical trials it has been reported that edoxudine presents a biotransformation marked by a cleavage of the glycoside bond. The degradation of edoxudine, after oral administration, seems to be processed by the activity of phosphorylases presented in the gastrointestinal tract and by pre-systemic metabolism.A27185

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

0 Data
Tidak ada data.

Target Protein

Thymidine kinase, cytosolic TK1
DNA polymerase DNApol

Referensi & Sumber

Artikel (PubMed)
  • PMID: 4037770
    Spruance SL, Freeman DJ, Sheth NV: Comparison of topically applied 5-ethyl-2'-deoxyuridine and acyclovir in the treatment of cutaneous herpes simplex virus infection in guinea pigs. Antimicrob Agents Chemother. 1985 Jul;28(1):103-6.
  • PMID: 2822705
    De Clercq E, Bernaerts R: Specific phosphorylation of 5-ethyl-2'-deoxyuridine by herpes simplex virus-infected cells and incorporation into viral DNA. J Biol Chem. 1987 Nov 5;262(31):14905-11.
  • PMID: 15621867
    Remeijer L, Osterhaus A, Verjans G: Human herpes simplex virus keratitis: the pathogenesis revisited. Ocul Immunol Inflamm. 2004 Dec;12(4):255-85. doi: 10.1080/092739490500363.
  • PMID: 7710272
    Cheraghali AM, Knaus EE, Wiebe LI: Bioavailability and pharmacokinetic parameters for 5-ethyl-2'-deoxyuridine. Antiviral Res. 1994 Dec;25(3-4):259-67.
  • PMID: 8185676
    Cheraghali AM, Kumar R, Wang L, Knaus EE, Wiebe LI: Synthesis, biotransformation, pharmacokinetics, and antiviral properties of 5-ethyl-5-halo-6-methoxy-5,6-dihydro-2'-deoxyuridine diastereomers. Biochem Pharmacol. 1994 Apr 29;47(9):1615-25.

Contoh Produk & Brand

Produk: 1 • International brands: 0
Produk
  • Virostat Cream 3%
    Cream • 3 % • Topical • Canada • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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