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IDX184 in combination with pegylated interferon-alpha2a and ribavirin for 2 weeks in treatment-naive patients with chronic hepatitis C.
Lalezari J, Box T, O'Riordan W, Mehra P, Nguyen T, Poordad F, Dejesus E, Kwo P, Godofsky E, Lawrence S, Dubuc-Patrick G, Chen J, McCarville J, Pietropaolo K, Zhou XJ, Sullivan-Bólyai J, Mayers D. Lalezari J, et al. Antivir Ther. 2013;18(6):755-64. doi: 10.3851/IMP2552. Epub 2013 Feb 25. Antivir Ther. 2013. PMID: 23439365 Clinical Trial.
BACKGROUND: IDX184 is a liver-targeted nucleotide prodrug that selectively inhibits HCV NS5B polymerase. ...Patients with genotypes-1a or -1b responded similarly. No viral breakthrough or resistance associated with IDX184 was observed. Anti-HCV activity of IDX184 …
BACKGROUND: IDX184 is a liver-targeted nucleotide prodrug that selectively inhibits HCV NS5B polymerase. ...Patients with genotypes-1 …
Pharmacokinetics of IDX184, a liver-targeted oral prodrug of 2'-methylguanosine-5'-monophosphate, in the monkey and formulation optimization for human exposure.
Pan-Zhou XR, Mayes BA, Rashidzadeh H, Gasparac R, Smith S, Bhadresa S, Gupta K, Cohen ML, Bu C, Good SS, Moussa A, Rush R. Pan-Zhou XR, et al. Eur J Drug Metab Pharmacokinet. 2016 Oct;41(5):567-74. doi: 10.1007/s13318-015-0267-4. Epub 2015 Apr 22. Eur J Drug Metab Pharmacokinet. 2016. PMID: 25898809 Clinical Trial.
IDX184 is a phosphoramidate prodrug of 2'-methylguanosine-5'-monophosphate, developed to treat patients infected with hepatitis C virus. A mass balance study of radiolabeled IDX184 and pharmacokinetic studies of IDX184 in portal vein-cannulated monkeys reveal …
IDX184 is a phosphoramidate prodrug of 2'-methylguanosine-5'-monophosphate, developed to treat patients infected with hepatitis C vir …
Safety and pharmacokinetics of IDX184, a liver-targeted nucleotide polymerase inhibitor of hepatitis C virus, in healthy subjects.
Zhou XJ, Pietropaolo K, Chen J, Khan S, Sullivan-Bólyai J, Mayers D. Zhou XJ, et al. Antimicrob Agents Chemother. 2011 Jan;55(1):76-81. doi: 10.1128/AAC.01101-10. Epub 2010 Nov 8. Antimicrob Agents Chemother. 2011. PMID: 21060109 Free PMC article. Clinical Trial.
Mean cumulative urine excretion was 0.2% and 12 to 20% of administered doses for the unchanged IDX184 and 2'-MeG, respectively. IDX184 was safe and well tolerated; no serious adverse events (SAEs), dose-dependent adverse events (AEs), or dose-limiting toxicities wer …
Mean cumulative urine excretion was 0.2% and 12 to 20% of administered doses for the unchanged IDX184 and 2'-MeG, respectively. ID …
Short-term monotherapy with IDX184, a liver-targeted nucleotide polymerase inhibitor, in patients with chronic hepatitis C virus infection.
Lalezari J, Asmuth D, Casiró A, Vargas H, Lawrence S, Dubuc-Patrick G, Chen J, McCarville J, Pietropaolo K, Zhou XJ, Sullivan-Bólyai J, Mayers D. Lalezari J, et al. Antimicrob Agents Chemother. 2012 Dec;56(12):6372-8. doi: 10.1128/AAC.01521-12. Epub 2012 Oct 15. Antimicrob Agents Chemother. 2012. PMID: 23070151 Free PMC article. Clinical Trial.
IDX184 is a liver-targeted prodrug of 2'-methylguanosine (2'-MeG) monophosphate. ...During the posttreatment period, plasma viremia and serum aminotransferase levels returned to near pretreatment levels. No resistance mutations associated with IDX184 were detected. …
IDX184 is a liver-targeted prodrug of 2'-methylguanosine (2'-MeG) monophosphate. ...During the posttreatment period, plasma viremia a …
Design, synthesis and antiviral evaluation of 2'-C-methyl branched guanosine pronucleotides: the discovery of IDX184, a potent liver-targeted HCV polymerase inhibitor.
Sizun G, Pierra C, Peyronnet J, Badaroux E, Rabeson C, Benzaria-Prad S, Surleraux D, Loi AG, Musiu C, Liuzzi M, Seifer M, Standring D, Sommadossi JP, Gosselin G. Sizun G, et al. Future Med Chem. 2015;7(13):1675-700. doi: 10.4155/fmc.15.96. Epub 2015 Oct 1. Future Med Chem. 2015. PMID: 26424162
CONCLUSION: The most promising compound, namely the O-[S-(hydroxyl)pivaloyl-2-thioethyl]{abbreviated as O-[(HO)tBuSATE)]} N-benzylamine phosphoramidate diester derivative (IDX184), was selected for further in vivo studies, and was the first clinical pronucleotide evaluated …
CONCLUSION: The most promising compound, namely the O-[S-(hydroxyl)pivaloyl-2-thioethyl]{abbreviated as O-[(HO)tBuSATE)]} N-benzylamine phos …
Insight into the biological impact of COVID-19 and its vaccines on human health.
Ashwlayan VD, Antlash C, Imran M, Asdaq SMB, Alshammari MK, Alomani M, Alzahrani E, Sharma D, Tomar R, Arora MK. Ashwlayan VD, et al. Saudi J Biol Sci. 2022 May;29(5):3326-3337. doi: 10.1016/j.sjbs.2022.02.010. Epub 2022 Feb 12. Saudi J Biol Sci. 2022. PMID: 35185356 Free PMC article. Review.
Dynamics and binding affinity of nucleoside and non-nucleoside inhibitors with RdRp of SARS-CoV-2: a molecular screening, docking, and molecular dynamics simulation study.
Chinnamadhu A, Ramakrishnan J, Suresh S, Ramadurai P, Poomani K. Chinnamadhu A, et al. J Biomol Struct Dyn. 2023 Dec;41(20):10396-10410. doi: 10.1080/07391102.2022.2154844. Epub 2022 Dec 12. J Biomol Struct Dyn. 2023. PMID: 36510678
The results of molecular docking and MD simulation studies reveal that IDX184 is a stable molecule and forms strong interactions with the key amino acids and shows high binding affinity towards RdRp. Hence, IDX184 may also be considered as a potential inhibitor of R …
The results of molecular docking and MD simulation studies reveal that IDX184 is a stable molecule and forms strong interactions with …
24 results