Besifovir

• CAT Number: I004161
• CAS Number: 441785-25-7
• Molecular Formula: C10H14N5O4P
• Molecular Weight: 299.227
• Purity: ≥95%
• Synonyms: LB80380; LB-80380; LB 80380; PMCDG; Besifovir;((1-((2-amino-9H-purin-9-yl)methyl)cyclopropoxy)methyl)phosphonic acid
• Solubility: Soluble in DMSO, not in water
• Storage: 0 - 4 °C for short term or -20 °C for long term
• IUPAC Name: [1-[(2-aminopurin-9-yl)methyl]cyclopropyl]oxymethylphosphonic acid
• InChI: InChI=1S/C10H14N5O4P/c11-9-12-3-7-8(14-9)15(5-13-7)4-10(1-2-10)19-6-20(16,17)18/h3,5H,1-2,4,6H2,(H2,11,12,14)(H2,16,17,18)
• InChIKey: KDNSSKPZBDNJDF-UHFFFAOYSA-N
• SMILES: C1CC1(CN2C=NC3=CN=C(N=C32)N)OCP(=O)(O)O

Besifovir, also known as LB80380, is an orally available phosphonate nucleotide for the potential treatment of hepatitis B virus infection. Besifovir inhibits viral replication by incorporation into the viral DNA. Antiviral activity against wild-type virus and virus with drug-resistant mutations was demonstrated in Phase II trials, with significant reduction of viral load in patients treated with LB80380. Besifovir had the same antiviral property as compared to entecavir over 96 weeks of treatment for chronic hepatitis B patients. Besifovir was well tolerated and also had a good clinical safety profile.

Reference

1:Two-year treatment outcome of chronic hepatitis B infection treated with besifovir vs. entecavir: results from a multicentre study. Yuen MF, Ahn SH, Lee KS, Um SH, Cho M, Yoon SK, Lee JW, Park NH, Kweon YO, Sohn JH, Lee J, Kim JA, Lai CL, Han KH.J Hepatol. 2015 Mar;62(3):526-32. doi: 10.1016/j.jhep.2014.10.026. Epub 2014 Oct 25. PMID: 25450709 2:Oral antiviral therapy for hepatitis B: the case of besifovir, a new kid on the block with a long way to go. Lampertico P.Gut. 2014 Jun;63(6):869-70. doi: 10.1136/gutjnl-2013-305859. Epub 2013 Oct 25. No abstract available. PMID: 24162592 3:Phase IIb multicentred randomised trial of besifovir (LB80380) versus entecavir in Asian patients with chronic hepatitis B. Lai CL, Ahn SH, Lee KS, Um SH, Cho M, Yoon SK, Lee JW, Park NH, Kweon YO, Sohn JH, Lee J, Kim JA, Han KH, Yuen MF.Gut. 2014 Jun;63(6):996-1004. doi: 10.1136/gutjnl-2013-305138. Epub 2013 Aug 26. PMID: 23979965