Radalbuvir - CAS 1314795-11-3
Catalog number: 1314795-11-3
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
Radalbuvir is a Hepatitis C virus NS 5 protein inhibitor for the treatment of hepatitis C virus (HCV) infection developed by Gilead Sciences. In 2014, Gilead completed a phase II trial for Hepatitis C in USA.
GS-9669; GS 9669; GS9669; Radalbuvir;5-(3,3-dimethyl-1-butyn-1-yl)-3-((cis-4-hydroxy-4-((((3S)-tetrahydro-3-furanyl)oxy)methyl)cyclohexyl)(((1R)-4-methyl-3-cyclohexen-1-yl)carbonyl)amino)- 2-Thiophenecarboxylic acid
Soluble in DMSO
-20°C Freezer
Hepatitis C
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
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Current Developer:
Gilead Sciences; National Institute of Allergy and Infectious Diseases
1.Clinical and in vitro resistance to GS-9669, a thumb site II nonnucleoside inhibitor of the hepatitis C virus NS5B polymerase.
Dvory-Sobol H;Voitenleitner C;Mabery E;Skurnac T;Lawitz EJ;McHutchison J;Svarovskaia ES;Delaney W;Miller MD;Mo H Antimicrob Agents Chemother. 2014 Nov;58(11):6599-606. doi: 10.1128/AAC.02815-14. Epub 2014 Aug 25.
Treatment with GS-9669, a novel nonnucleoside inhibitor (site II) of hepatitis C virus (HCV) nonstructural 5B (NS5B) polymerase, resulted in significant antiviral activity in HCV genotype (GT) 1 patients dosed at 50 and 500 mg once daily (QD) and at 50, 100, and 500 mg twice daily (BID) for 3 days. This report characterizes the virologic resistance to GS-9669 in vitro and in GT1 HCV-infected patients from a phase I clinical study. An in vitro resistance selection study with GS-9669 revealed substitutions at several NS5B residues that conferred resistance. The M423 variants were selected at low drug concentrations (5× the 50% effective concentration [EC50]), and the L419, R422, and I482 variants were selected at higher drug concentrations (20× the EC50). During the phase I clinical study, substitutions at NS5B residues 419, 422, and 486 were the predominant changes associated with GS-9669 monotherapy. Substitutions at position 423 were observed only in GT1a patients in the low-dose groups (50 and 100 mg BID). Interestingly, four HCV patients had substitutions at position 423 at baseline. Consistent with the low resistance level at this position, three patients with M423I or M423V at baseline achieved >2-log10 reductions of HCV RNA when treated with 100 mg BID or with 500 mg QD or BID of GS-9669.
2.Discovery of GS-9669, a thumb site II non-nucleoside inhibitor of NS5B for the treatment of genotype 1 chronic hepatitis C infection.
Lazerwith SE;Lew W;Zhang J;Morganelli P;Liu Q;Canales E;Clarke MO;Doerffler E;Byun D;Mertzman M;Ye H;Chong L;Xu L;Appleby T;Chen X;Fenaux M;Hashash A;Leavitt SA;Mabery E;Matles M;Mwangi JW;Tian Y;Lee YJ;Zhang J;Zhu C;Murray BP;Watkins WJ J Med Chem. 2014 Mar 13;57(5):1893-901. doi: 10.1021/jm401420j. Epub 2013 Nov 6.
Investigation of thiophene-2-carboxylic acid HCV NS5B site II inhibitors, guided by measurement of cell culture medium binding, revealed the structure-activity relationships for intrinsic cellular potency. The pharmacokinetic profile was enhanced through incorporation of heterocyclic ethers on the N-alkyl substituent. Hydroxyl groups were incorporated to modulate protein binding. Intrinsic potency was further improved through enantiospecific introduction of an olefin in the N-acyl motif, resulting in the discovery of the phase 2 clinical candidate GS-9669. The unexpected activity of this compound against the clinically relevant NS5B M423T mutant, relative to the wild type, was shown to arise from both the N-alkyl substituent and the N-acyl group.
3.Four-Week Direct-Acting Antiviral Regimens in Noncirrhotic Patients With Hepatitis C Virus Genotype 1 Infection: An Open-Label, Nonrandomized Trial.
Kohli A;Kattakuzhy S;Sidharthan S;Nelson A;McLaughlin M;Seamon C;Wilson E;Meissner EG;Sims Z;Silk R;Gross C;Akoth E;Tang L;Price A;Jolley TA;Emmanuel B;Proschan M;Teferi G;Chavez J;Abbott S;Osinusi A;Mo H;Polis MA;Masur H;Kottilil S Ann Intern Med. 2015 Dec 15;163(12):899-907. doi: 10.7326/M15-0642. Epub 2015 Nov 24.
BACKGROUND: ;Treatment of chronic hepatitis C virus (HCV) infection with direct-acting antivirals (DAAs) for 6 weeks achieves sustained virologic response (SVR) rates of 95% in some patients. If effective, shorter therapeutic courses could improve adherence and treatment costs.;OBJECTIVE: ;To determine factors predictive of SVR to 4 weeks of DAA treatment in patients with stage F0 to F2 liver fibrosis.;DESIGN: ;Open-label, nonrandomized, phase 2a trial. (Clinical Trials.gov: ;NCT01805882;).;SETTING: ;Single-center.;PATIENTS: ;50 treatment-naive and predominantly African American patients with HCV genotype 1 infection and early-stage liver fibrosis were sequentially enrolled into 2 treatment groups.;INTERVENTION: ;25 participants received a 3-drug regimen consisting of ledipasvir and sofosbuvir plus GS-9451 for 4 weeks, and 25 received a 4-drug regimen consisting of ledipasvir, sofosbuvir, GS-9451, and GS-9669 for 4 weeks.;MEASUREMENTS: ;The primary efficacy end point was SVR12 (HCV RNA level below the lower limit of quantification at posttreatment week 12).;RESULTS: ;Forty percent (10 of 25) (95% CI, 21% to 61%) of patients in the 3-drug group and 20% (5 of 25) (CI, 7% to 41%) of those in the 4-drug group achieved SVR12.
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CAS 1314795-11-3 Radalbuvir

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