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Page 1
In Vitro Antiviral Profile of Ruzasvir, a Potent and Pangenotype Inhibitor of Hepatitis C Virus NS5A.
Asante-Appiah E, Liu R, Curry S, McMonagle P, Agrawal S, Carr D, Rokosz L, Lahser F, Bystol K, Chase R, Black S, Ferrari E, Ingravallo P, Tong L, Yu W, Kozlowski J. Asante-Appiah E, et al. Antimicrob Agents Chemother. 2018 Oct 24;62(11):e01280-18. doi: 10.1128/AAC.01280-18. Print 2018 Nov. Antimicrob Agents Chemother. 2018. PMID: 30150466 Free PMC article.
With the exception of GT4, the reintroduction of selected RASs conferred a 100-fold potency reduction in the antiviral activity of ruzasvir. Common RASs from other classes of direct-acting antiviral agents (DAAs) did not confer cross-resistance to …
With the exception of GT4, the reintroduction of selected RASs conferred a 100-fold potency reduction in the antiviral activity of …
Efficacy and safety of a two-drug direct-acting antiviral agent regimen ruzasvir 180 mg and uprifosbuvir 450 mg for 12 weeks in adults with chronic hepatitis C virus genotype 1, 2, 3, 4, 5 or 6.
Lawitz E, Gane E, Feld JJ, Buti M, Foster GR, Rabinovitz M, Burnevich E, Katchman H, Tomasiewicz K, Lahser F, Jackson B, Shaughnessy M, Klopfer S, Yeh WW, Robertson MN, Hanna GJ, Barr E, Platt HL; C-BREEZE-2 Study Investigators. Lawitz E, et al. J Viral Hepat. 2019 Sep;26(9):1127-1138. doi: 10.1111/jvh.13132. Epub 2019 Jul 11. J Viral Hepat. 2019. PMID: 31108015 Clinical Trial.
Ruzasvir (MK-8408, an NS5A inhibitor) and uprifosbuvir (MK-3682, a nonstructural protein 5B nucleotide inhibitor) are highly potent direct-acting antiviral agents for the treatment of hepatitis C virus (HCV) infection. A phase III clinical trial evaluating th …
Ruzasvir (MK-8408, an NS5A inhibitor) and uprifosbuvir (MK-3682, a nonstructural protein 5B nucleotide inhibitor) are highly potent d …
Bemnifosbuvir and ruzasvir in combination exhibit potent synergistic antiviral activity in vitro while maintaining a favorable nonclinical safety profile in vivo.
Good SS, Luo S, Lin K, Vo A, Agrawal NGB, Sommadossi JP. Good SS, et al. Antiviral Res. 2025 May;237:106137. doi: 10.1016/j.antiviral.2025.106137. Epub 2025 Mar 5. Antiviral Res. 2025. PMID: 40054502 Free article.
Bemnifosbuvir (BEM), the orally available hemisulfate salt of the double prodrug of a guanosine nucleotide analog, is a potent, selective, and pan-genotypic inhibitor of HCV nonstructural protein 5B, an RNA-dependent RNA polymerase necessary for viral replication. Similarly, r …
Bemnifosbuvir (BEM), the orally available hemisulfate salt of the double prodrug of a guanosine nucleotide analog, is a potent, selective, a …
Safety and efficacy of an 8-week regimen of grazoprevir plus ruzasvir plus uprifosbuvir compared with grazoprevir plus elbasvir plus uprifosbuvir in participants without cirrhosis infected with hepatitis C virus genotypes 1, 2, or 3 (C-CREST-1 and C-CREST-2, part A): two randomised, phase 2, open-label trials.
Gane EJ, Pianko S, Roberts SK, Thompson AJ, Zeuzem S, Zuckerman E, Ben-Ari Z, Foster GR, Agarwal K, Laursen AL, Gerstoft J, Gao W, Huang HC, Fitzgerald B, Fernsler D, Li JJ, Grandhi A, Liu H, Su FH, Wan S, Zeng Z, Chen HL, Dutko FJ, Nguyen BT, Wahl J, Robertson MN, Barr E, Yeh WW, Plank RM, Butterton JR, Esteban R. Gane EJ, et al. Lancet Gastroenterol Hepatol. 2017 Nov;2(11):805-813. doi: 10.1016/S2468-1253(17)30159-0. Epub 2017 Aug 10. Lancet Gastroenterol Hepatol. 2017. PMID: 28802816 Clinical Trial.
In particular, among those with genotype 2 infection, the grazoprevir plus ruzasvir plus uprifosbuvir 450 mg regimen had a higher SVR12 (15 [94%] of 16) than the grazoprevir plus ruzasvir plus uprifosbuvir 300 mg regimen (ten [71%] of 14), grazoprevir plus elbasvir …
In particular, among those with genotype 2 infection, the grazoprevir plus ruzasvir plus uprifosbuvir 450 mg regimen had a higher SVR …
Grazoprevir, ruzasvir, and uprifosbuvir for hepatitis C virus after NS5A treatment failure.
Wyles D, Wedemeyer H, Ben-Ari Z, Gane EJ, Hansen JB, Jacobson IM, Laursen AL, Luetkemeyer A, Nahass R, Pianko S, Zeuzem S, Jumes P, Huang HC, Butterton J, Robertson M, Wahl J, Barr E, Joeng HK, Martin E, Serfaty L; C-CREST Part C and C-SURGE Investigators. Wyles D, et al. Hepatology. 2017 Dec;66(6):1794-1804. doi: 10.1002/hep.29358. Epub 2017 Oct 30. Hepatology. 2017. PMID: 28688129 Clinical Trial.
The present studies evaluated the safety and efficacy of grazoprevir, ruzasvir, and uprifosbuvir, with or without ribavirin, in participants who had failed an NS5A inhibitor-containing regimen. ...One participant with GT2 infection discontinued study medication after a sin …
The present studies evaluated the safety and efficacy of grazoprevir, ruzasvir, and uprifosbuvir, with or without ribavirin, in parti …
Discovery of Ruzasvir (MK-8408): A Potent, Pan-Genotype HCV NS5A Inhibitor with Optimized Activity against Common Resistance-Associated Polymorphisms.
Tong L, Yu W, Chen L, Selyutin O, Dwyer MP, Nair AG, Mazzola R, Kim JH, Sha D, Yin J, Ruck RT, Davies IW, Hu B, Zhong B, Hao J, Ji T, Zan S, Liu R, Agrawal S, Xia E, Curry S, McMonagle P, Bystol K, Lahser F, Carr D, Rokosz L, Ingravallo P, Chen S, Feng KI, Cartwright M, Asante-Appiah E, Kozlowski JA. Tong L, et al. J Med Chem. 2017 Jan 12;60(1):290-306. doi: 10.1021/acs.jmedchem.6b01310. Epub 2016 Nov 15. J Med Chem. 2017. PMID: 27808515 Free article.
We describe the research that led to the discovery of compound 40 (ruzasvir, MK-8408), a pan-genotypic HCV nonstructural protein 5A (NS5A) inhibitor with a "flat" GT1 mutant profile. ...
We describe the research that led to the discovery of compound 40 (ruzasvir, MK-8408), a pan-genotypic HCV nonstructural protein 5A ( …
Clinical Evaluation of Potential Interaction Between Bemnifosbuvir and Ruzasvir With an Assessment of Food Effect: Results of a Phase 1 Study in Healthy Participants.
Zhou XJ, Morelli G, Montrond M, Lynch S, Pietropaolo K, Belanger B, Horga A, Hammond J. Zhou XJ, et al. Clin Pharmacol Drug Dev. 2025 Jun;14(6):461-471. doi: 10.1002/cpdd.1540. Epub 2025 Apr 24. Clin Pharmacol Drug Dev. 2025. PMID: 40272375 Free PMC article. Clinical Trial.
Under fasted conditions, the peak, trough, and total exposure to bemnifosbuvir and its metabolites were increased upon coadministration with ruzasvir (by a maximum of 33% vs bemnifosbuvir alone), whereas the corresponding values for ruzasvir were decreased upon coad …
Under fasted conditions, the peak, trough, and total exposure to bemnifosbuvir and its metabolites were increased upon coadministration with …
Efficacy of NS5A Inhibitors Against Hepatitis C Virus Genotypes 1-7 and Escape Variants.
Gottwein JM, Pham LV, Mikkelsen LS, Ghanem L, Ramirez S, Scheel TKH, Carlsen THR, Bukh J. Gottwein JM, et al. Gastroenterology. 2018 Apr;154(5):1435-1448. doi: 10.1053/j.gastro.2017.12.015. Epub 2017 Dec 22. Gastroenterology. 2018. PMID: 29274866
METHODS: We measured the efficacy of different concentrations of daclatasvir, ledipasvir, ombitasvir, elbasvir, ruzasvir, velpatasvir, and pibrentasvir in cultured cells infected with HCV recombinants expressing genotype 1-7 NS5A proteins with or without RAS. ...Among thes …
METHODS: We measured the efficacy of different concentrations of daclatasvir, ledipasvir, ombitasvir, elbasvir, ruzasvir, velpatasvir …
Safety and efficacy of a fixed-dose combination regimen of grazoprevir, ruzasvir, and uprifosbuvir with or without ribavirin in participants with and without cirrhosis with chronic hepatitis C virus genotype 1, 2, or 3 infection (C-CREST-1 and C-CREST-2, part B): two randomised, phase 2, open-label trials.
Lawitz E, Buti M, Vierling JM, Almasio PL, Bruno S, Ruane PJ, Hassanein TI, Muellhaupt B, Pearlman B, Jancoriene L, Gao W, Huang HC, Shepherd A, Tannenbaum B, Fernsler D, Li JJ, Grandhi A, Liu H, Su FH, Wan S, Dutko FJ, Nguyen BT, Wahl J, Robertson MN, Barr E, Yeh WW, Plank RM, Butterton JR, Yoshida EM. Lawitz E, et al. Lancet Gastroenterol Hepatol. 2017 Nov;2(11):814-823. doi: 10.1016/S2468-1253(17)30163-2. Epub 2017 Aug 10. Lancet Gastroenterol Hepatol. 2017. PMID: 28802814 Clinical Trial.
Part A of the C-CREST-1 and C-CREST-2 trials led to the selection of a three-drug regimen of grazoprevir (MK-5172; an HCV NS3/4A protease inhibitor; 100 mg/day) plus ruzasvir (MK-8408; an NS5A inhibitor; 60 mg/day) plus uprifosbuvir (MK-3682; an HCV NS5B polymerase inhibit …
Part A of the C-CREST-1 and C-CREST-2 trials led to the selection of a three-drug regimen of grazoprevir (MK-5172; an HCV NS3/4A protease in …
Glecaprevir/pibrentasvir+sofosbuvir: an optimal retreatment strategy in the setting of HCV NS5A resistance.
Alimohammadi A, Conway B, Yamamoto L. Alimohammadi A, et al. BMJ Case Rep. 2020 Feb 11;13(2):e233098. doi: 10.1136/bcr-2019-233098. BMJ Case Rep. 2020. PMID: 32051160 Free PMC article.
We report a 56-year-old Caucasian man with fatigue, depression and confusion in the setting of untreated HCV genotype 3a infection. He received ruzasvir and uprifosbuvir for 12 weeks within a clinical trial. The patient relapsed 4 weeks after the end of treatment and at th …
We report a 56-year-old Caucasian man with fatigue, depression and confusion in the setting of untreated HCV genotype 3a infection. He recei …
15 results