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Chemical Compound Review

Rupintrivir     ethyl (E,4S)-4-[[(2R,5S)-2-[(4...

Synonyms: Ruprintrivir, CHEMBL20210, SureCN141565, AG-7088, AC1O5TFI, ...
 
 
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Disease relevance of Ruprintrivir

  • Phase II, randomized, double-blind, placebo-controlled studies of ruprintrivir nasal spray 2-percent suspension for prevention and treatment of experimentally induced rhinovirus colds in healthy volunteers [1].
 

High impact information on Ruprintrivir

  • Ruprintrivir (Agouron Pharmaceuticals, Inc., San Diego, Calif.) selectively inhibits HRV 3C protease and shows potent, broad-spectrum anti-HRV activity in vitro [1].
  • A single-dose study and a multiple-dose study of the safety and pharmacokinetics of ruprintrivir, a new selective irreversible inhibitor of human rhinovirus 3C protease, were conducted with healthy adult volunteers [2].
 

Biological context of Ruprintrivir

 

Analytical, diagnostic and therapeutic context of Ruprintrivir

  • We conducted three double-blind, placebo-controlled clinical trials in 202 healthy volunteers to assess the activity of ruprintrivir in experimental HRV infection [1].
  • These sequence analyses are consistent with the comparable in vitro antiviral potencies of rupintrivir against all HRV serotypes, HRV isolates, and HEV strains tested (50% effective concentration range, 3 to 183 nM; n = 125) [3].

References

  1. Phase II, randomized, double-blind, placebo-controlled studies of ruprintrivir nasal spray 2-percent suspension for prevention and treatment of experimentally induced rhinovirus colds in healthy volunteers. Hayden, F.G., Turner, R.B., Gwaltney, J.M., Chi-Burris, K., Gersten, M., Hsyu, P., Patick, A.K., Smith, G.J., Zalman, L.S. Antimicrob. Agents Chemother. (2003) [Pubmed]
  2. Pharmacokinetics and safety of an antirhinoviral agent, ruprintrivir, in healthy volunteers. Hsyu, P.H., Pithavala, Y.K., Gersten, M., Penning, C.A., Kerr, B.M. Antimicrob. Agents Chemother. (2002) [Pubmed]
  3. Conservation of amino acids in human rhinovirus 3C protease correlates with broad-spectrum antiviral activity of rupintrivir, a novel human rhinovirus 3C protease inhibitor. Binford, S.L., Maldonado, F., Brothers, M.A., Weady, P.T., Zalman, L.S., Meador, J.W., Matthews, D.A., Patick, A.K. Antimicrob. Agents Chemother. (2005) [Pubmed]
 
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