Tegobuvir

• CAT Number: I000067
• CAS Number: 1000787-75-6
• Molecular Formula: C25H14F7N5
• Molecular Weight: 517.4
• Purity: ≥95%
• Synonyms: 5-[[6-[2,4-bis(trifluoromethyl)phenyl]pyridazin-3-yl]methyl]-2-(2-fluorophenyl)imidazo[4,5-c]pyridine
• Target: HCV Protease
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• InChI: InChI=1S/C25H14F7N5/c26-19-4-2-1-3-17(19)23-33-21-9-10-37(13-22(21)34-23)12-15-6-8-20(36-35-15)16-7-5-14(24(27,28)29)11-18(16)25(30,31)32/h1-11,13H,12H2
• InChIKey: XBEQSQDCBSKCHJ-UHFFFAOYSA-N
• SMILES: C1=CC=C(C(=C1)C2=NC3=CN(C=CC3=N2)CC4=NN=C(C=C4)C5=C(C=C(C=C5)C(F)(F)F)C(F)(F)F)F

Tegobuvir (CAT: I000067) is an investigational antiviral drug that belongs to the class of non-nucleoside inhibitors of the hepatitis C virus (HCV) NS5B polymerase. It is being studied for the treatment of chronic HCV infection. Tegobuvir works by inhibiting the replication of the HCV RNA genome, thereby suppressing viral replication. It has demonstrated potent antiviral activity against various genotypes of HCV in preclinical and clinical studies. Tegobuvir is often used in combination with other direct-acting antiviral agents as part of an interferon-free regimen for the treatment of HCV infection. Clinical trials have shown promising results, and further research is ongoing to evaluate its efficacy and safety.

Overview of Clinical Research

Tegobuvir is a hepatitis C virus NS 5 protein inhibitor.

Reference

1:In vitro combinations containing Tegobuvir are highly efficient in curing cells from HCV replicon and in delaying/preventing the development of drug resistance. Vliegen I, Paeshuyse J, Zhong W, Neyts J.Antiviral Res. 2015 Aug;120:112-21. doi: 10.1016/j.antiviral.2015.05.011. Epub 2015 May 30. PMID: 26036224
2:All-oral combination of ledipasvir, vedroprevir, tegobuvir, and ribavirin in treatment-naïve patients with genotype 1 HCV infection. Wyles DL, Rodriguez-Torres M, Lawitz E, Shiffman ML, Pol S, Herring RW, Massetto B, Kanwar B, Trenkle JD, Pang PS, Zhu Y, Mo H, Brainard DM, Subramanian GM, McHutchison JG, Habersetzer F, Sulkowski MS.Hepatology. 2014 Jul;60(1):56-64. doi: 10.1002/hep.27053. Epub 2014 May 28. PMID: 24501005
3:The HCV non-nucleoside inhibitor Tegobuvir utilizes a novel mechanism of action to inhibit NS5B polymerase function. Hebner CM, Han B, Brendza KM, Nash M, Sulfab M, Tian Y, Hung M, Fung W, Vivian RW, Trenkle J, Taylor J, Bjornson K, Bondy S, Liu X, Link J, Neyts J, Sakowicz R, Zhong W, Tang H, Schmitz U.PLoS One. 2012;7(6):e39163. doi: 10.1371/journal.pone.0039163. Epub 2012 Jun 13. PMID: 22720059 Free PMC Article
4:Tegobuvir (GS-9190) potency against HCV chimeric replicons derived from consensus NS5B sequences from genotypes 2b, 3a, 4a, 5a, and 6a. Wong KA, Xu S, Martin R, Miller MD, Mo H.Virology. 2012 Jul 20;429(1):57-62. doi: 10.1016/j.virol.2012.03.025. Epub 2012 Apr 28. PMID: 22543048 Free Article
5:The protease inhibitor, GS-9256, and non-nucleoside polymerase inhibitor tegobuvir alone, with ribavirin, or pegylated interferon plus ribavirin in hepatitis C. Zeuzem S, Buggisch P, Agarwal K, Marcellin P, Sereni D, Klinker H, Moreno C, Zarski JP, Horsmans Y, Mo H, Arterburn S, Knox S, Oldach D, McHutchison JG, Manns MP, Foster GR.Hepatology. 2012 Mar;55(3):749-58. doi: 10.1002/hep.24744. PMID: 22006408
6:Mechanistic characterization of GS-9190 (Tegobuvir), a novel nonnucleoside inhibitor of hepatitis C virus NS5B polymerase. Shih IH, Vliegen I, Peng B, Yang H, Hebner C, Paeshuyse J, Pürstinger G, Fenaux M, Tian Y, Mabery E, Qi X, Bahador G, Paulson M, Lehman LS, Bondy S, Tse W, Reiser H, Lee WA, Schmitz U, Neyts J, Zhong W.Antimicrob Agents Chemother. 2011 Sep;55(9):4196-203. doi: 10.1128/AAC.00307-11. Epub 2011 Jul 11. PMID: 21746939 Free PMC Article