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Chemical Compound Review

S1252_Selleck     2-amino-9-[(3R,4S)-4-hydroxy- 3...

Synonyms: AG-J-29189, SureCN4330844, AC1Q6IAA, CTK4E5461, AR-1D8720, ...
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Disease relevance of SQ 34676


High impact information on SQ 34676


Chemical compound and disease context of SQ 34676


Biological context of SQ 34676


Anatomical context of SQ 34676


Associations of SQ 34676 with other chemical compounds

  • METHODS: In a 24-week, double-blind, randomized, multicenter, phase II clinical trial, the safety and efficacy of entecavir (0.01 mg/day, 0.1 mg/day, or 0.5 mg/day orally) were compared with lamivudine (100 mg/day orally) [2].
  • However, while entecavir is associated with a low incidences of resistance, emtricitabine is associated with a relatively high incidence of resistance which limits its use as a monotherapy [17].
  • The potential for drug interactions with entecavir appears to be minimal, although medications that inhibit tubular secretion of drugs (eg, probenecid) may be expected to prolong serum concentrations of entecavir [12].

Gene context of SQ 34676


Analytical, diagnostic and therapeutic context of SQ 34676

  • In patients treated with entecavir 0.5 mg/day, 83.7% had an HBV-DNA level below the lower limit of detection of the Quantiplex branched DNA (bDNA) assay (Bayer-Versant Diagnostics, formerly Chiron Diagnostics, Emeryville, CA), compared with 57.5% treated with 100 mg/day lamivudine (P = 0.008) [2].
  • Entecavir (ETV) is a potent and selective inhibitor of hepatitis B virus (HBV) replication in vitro and in vivo that is currently in clinical trials for the treatment of chronic HBV infections [20].
  • Entecavir therapy combined with DNA vaccination for persistent duck hepatitis B virus infection [21].
  • Entecavir is eliminated primarily in the urine via glomerular filtration and tubular secretion (62%-73%) [12].
  • In view of the experimental and clinical data, the capacity of new antiviral strategies based on combination of new inhibitors, including adefavir and entecavir, with immune modulators needs to be further evaluated in animal models and clinical trials to prevent the emergence of resistant viral strains [22].


  1. Entecavir for treatment of lamivudine-refractory, HBeAg-positive chronic hepatitis B. Sherman, M., Yurdaydin, C., Sollano, J., Silva, M., Liaw, Y.F., Cianciara, J., Boron-Kaczmarska, A., Martin, P., Goodman, Z., Colonno, R., Cross, A., Denisky, G., Kreter, B., Hindes, R. Gastroenterology (2006) [Pubmed]
  2. Entecavir is superior to lamivudine in reducing hepatitis B virus DNA in patients with chronic hepatitis B infection. Lai, C.L., Rosmawati, M., Lao, J., Van Vlierberghe, H., Anderson, F.H., Thomas, N., Dehertogh, D. Gastroenterology (2002) [Pubmed]
  3. Safety and efficacy of oral entecavir given for 28 days in patients with chronic hepatitis B virus infection. de Man, R.A., Wolters, L.M., Nevens, F., Chua, D., Sherman, M., Lai, C.L., Gadano, A., Lee, Y., Mazzotta, F., Thomas, N., DeHertogh, D. Hepatology (2001) [Pubmed]
  4. Hepatitis B virus-related cirrhosis: natural history and treatment. Chu, C.M., Liaw, Y.F. Semin. Liver Dis. (2006) [Pubmed]
  5. Effect of antiviral treatment with entecavir on age- and dose-related outcomes of duck hepatitis B virus infection. Foster, W.K., Miller, D.S., Scougall, C.A., Kotlarski, I., Colonno, R.J., Jilbert, A.R. J. Virol. (2005) [Pubmed]
  6. A dose-ranging study of the efficacy and tolerability of entecavir in Lamivudine-refractory chronic hepatitis B patients. Chang, T.T., Gish, R.G., Hadziyannis, S.J., Cianciara, J., Rizzetto, M., Schiff, E.R., Pastore, G., Bacon, B.R., Poynard, T., Joshi, S., Klesczewski, K.S., Thiry, A., Rose, R.E., Colonno, R.J., Hindes, R.G. Gastroenterology (2005) [Pubmed]
  7. Inhibition of hepatitis B virus polymerase by entecavir. Langley, D.R., Walsh, A.W., Baldick, C.J., Eggers, B.J., Rose, R.E., Levine, S.M., Kapur, A.J., Colonno, R.J., Tenney, D.J. J. Virol. (2007) [Pubmed]
  8. Stepwise process for the development of entecavir resistance in a chronic hepatitis B virus infected patient. Villet, S., Ollivet, A., Pichoud, C., Barraud, L., Villeneuve, J.P., Trépo, C., Zoulim, F. J. Hepatol. (2007) [Pubmed]
  9. Treatment algorithm for chronic hepatitis B in HIV-infected patients. Benhamou, Y. J. Hepatol. (2006) [Pubmed]
  10. Entecavir versus lamivudine for HBeAg positive and negative chronic hepatitis B. Lampertico, P. J. Hepatol. (2006) [Pubmed]
  11. Antiviral drugs: current state of the art. De Clercq, E. J. Clin. Virol. (2001) [Pubmed]
  12. Entecavir for the treatment of chronic hepatitis B virus infection. Matthews, S.J. Clinical therapeutics. (2006) [Pubmed]
  13. Entecavir pharmacokinetics, safety, and tolerability after multiple ascending doses in healthy subjects. Yan, J.H., Bifano, M., Olsen, S., Smith, R.A., Zhang, D., Grasela, D.M., Lacreta, F. Journal of clinical pharmacology. (2006) [Pubmed]
  14. Treatment of chronic hepatitis B. Mohanty, S.R., Kupfer, S.S., Khiani, V. Nature clinical practice. Gastroenterology & hepatology. (2006) [Pubmed]
  15. Entecavir: a potent new antiviral drug for hepatitis B. Honkoop, P., De Man, R.A. Expert opinion on investigational drugs. (2003) [Pubmed]
  16. Potent efficacy of entecavir (BMS-200475) in a duck model of hepatitis B virus replication. Marion, P.L., Salazar, F.H., Winters, M.A., Colonno, R.J. Antimicrob. Agents Chemother. (2002) [Pubmed]
  17. Treatment of chronic hepatitis B. Marcellin, P., Asselah, T., Boyer, N. J. Viral Hepat. (2005) [Pubmed]
  18. A comparison of entecavir and lamivudine for HBeAg-positive chronic hepatitis B. Chang, T.T., Gish, R.G., de Man, R., Gadano, A., Sollano, J., Chao, Y.C., Lok, A.S., Han, K.H., Goodman, Z., Zhu, J., Cross, A., DeHertogh, D., Wilber, R., Colonno, R., Apelian, D. N. Engl. J. Med. (2006) [Pubmed]
  19. Treatment of chronic hepatitis B. Yuen, M.F., Lai, C.L. The Lancet infectious diseases. (2001) [Pubmed]
  20. Efficacies of entecavir against lamivudine-resistant hepatitis B virus replication and recombinant polymerases in vitro. Levine, S., Hernandez, D., Yamanaka, G., Zhang, S., Rose, R., Weinheimer, S., Colonno, R.J. Antimicrob. Agents Chemother. (2002) [Pubmed]
  21. Entecavir therapy combined with DNA vaccination for persistent duck hepatitis B virus infection. Foster, W.K., Miller, D.S., Marion, P.L., Colonno, R.J., Kotlarski, I., Jilbert, A.R. Antimicrob. Agents Chemother. (2003) [Pubmed]
  22. Detection of hepatitis B virus resistance to antivirals. Zoulim, F. J. Clin. Virol. (2001) [Pubmed]
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