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Treatment of chronic hepatitis C patients with the NS3/4A protease inhibitor danoprevir (ITMN-191/RG7227) leads to robust reductions in viral RNA: a phase 1b multiple ascending dose study.
Forestier N, Larrey D, Guyader D, Marcellin P, Rouzier R, Patat A, Smith P, Bradford W, Porter S, Blatt L, Seiwert SD, Zeuzem S. Forestier N, et al. Among authors: seiwert sd. J Hepatol. 2011 Jun;54(6):1130-6. doi: 10.1016/j.jhep.2010.11.001. Epub 2011 Feb 24. J Hepatol. 2011. PMID: 21145848 Clinical Trial.
Virologic escape during danoprevir (ITMN-191/RG7227) monotherapy is hepatitis C virus subtype dependent and associated with R155K substitution.
Lim SR, Qin X, Susser S, Nicholas JB, Lange C, Herrmann E, Hong J, Arfsten A, Hooi L, Bradford W, Nájera I, Smith P, Zeuzem S, Kossen K, Sarrazin C, Seiwert SD. Lim SR, et al. Among authors: seiwert sd. Antimicrob Agents Chemother. 2012 Jan;56(1):271-9. doi: 10.1128/AAC.05636-11. Epub 2011 Nov 7. Antimicrob Agents Chemother. 2012. PMID: 22064535 Free PMC article. Clinical Trial.
Preclinical characteristics of the hepatitis C virus NS3/4A protease inhibitor ITMN-191 (R7227).
Seiwert SD, Andrews SW, Jiang Y, Serebryany V, Tan H, Kossen K, Rajagopalan PT, Misialek S, Stevens SK, Stoycheva A, Hong J, Lim SR, Qin X, Rieger R, Condroski KR, Zhang H, Do MG, Lemieux C, Hingorani GP, Hartley DP, Josey JA, Pan L, Beigelman L, Blatt LM. Seiwert SD, et al. Antimicrob Agents Chemother. 2008 Dec;52(12):4432-41. doi: 10.1128/AAC.00699-08. Epub 2008 Sep 29. Antimicrob Agents Chemother. 2008. PMID: 18824605 Free PMC article.
Preclinical Characterization and Human Microdose Pharmacokinetics of ITMN-8187, a Nonmacrocyclic Inhibitor of the Hepatitis C Virus NS3 Protease.
Rajagopalan R, Pan L, Schaefer C, Nicholas J, Lim S, Misialek S, Stevens S, Hooi L, Aleskovski N, Ruhrmund D, Kossen K, Huang L, Yap S, Beigelman L, Serebryany V, Liu J, Sastry S, Seiwert S, Buckman B. Rajagopalan R, et al. Among authors: seiwert s. Antimicrob Agents Chemother. 2016 Dec 27;61(1):e01569-16. doi: 10.1128/AAC.01569-16. Print 2017 Jan. Antimicrob Agents Chemother. 2016. PMID: 27795376 Free PMC article.
Discovery of danoprevir (ITMN-191/R7227), a highly selective and potent inhibitor of hepatitis C virus (HCV) NS3/4A protease.
Jiang Y, Andrews SW, Condroski KR, Buckman B, Serebryany V, Wenglowsky S, Kennedy AL, Madduru MR, Wang B, Lyon M, Doherty GA, Woodard BT, Lemieux C, Geck Do M, Zhang H, Ballard J, Vigers G, Brandhuber BJ, Stengel P, Josey JA, Beigelman L, Blatt L, Seiwert SD. Jiang Y, et al. Among authors: seiwert sd. J Med Chem. 2014 Mar 13;57(5):1753-69. doi: 10.1021/jm400164c. Epub 2013 May 28. J Med Chem. 2014. PMID: 23672640
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