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Chemical Compound Review

lamavudine     4-amino-1-[(2S,5R)-2- (hydroxymethyl)-1,3...

Synonyms: ent-Lamivudine, SureCN33979, AG-C-01570, AC1L2JOS, CTK7D9902, ...
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Disease relevance of lamivudine


Psychiatry related information on lamivudine


High impact information on lamivudine


Chemical compound and disease context of lamivudine


Biological context of lamivudine


Anatomical context of lamivudine

  • Interestingly, lamivudine also enhanced the responses to mitogens and recall antigens, showing that its effect was not limited to HBV-specific T cells [24].
  • In hepatocyte cultures infected with pretreatment serum, HBV DNA concentrations were reduced to less than 6% of those in control cultures by addition of lamivudine in concentrations as low as 0.03 mumol/L [25].
  • After 1 year of therapy, viral RNA levels in LN of individuals remained detectable but were log10 = 4 lower than in subjects on the triple drug regimen with interruption of therapy or in those treated with ZDV/3TC alone, who had viral loads in their lymph nodes indistinguishable from those expected for untreated patients [26].
  • Using these cell lines, we assessed the susceptibility of all four strains of lamivudine-resistant HBV to eleven nucleoside analogues in various stages of clinical development [27].
  • Pre-emptive use of lamivudine in bone marrow transplantation with chronic hepatitis B virus infection [28].

Associations of lamivudine with other chemical compounds


Gene context of lamivudine

  • Finally, an increased expression of the MRP5 homologue, ATP-binding cassette C11 (ABCC11) was observed in the CEM 3TC cells [34].
  • However, despite a small overexpression of multidrug resistance protein (MRP) 4, additional studies with cells specifically engineered to overexpress MRP4 demonstrated there was no impact on either 3TC accumulation or efflux [34].
  • Lamivudine treatment reduced TRAIL-mediated apoptosis and TRAIL-R1/DR4 expression in Hep G2.2.15 cells [35].
  • BCH 189 inhibited the proliferation of B and T lymphocytes from normal and HIV+ subjects less than AZT; even if lymphocytes from HIV+ (CDC III) subjects produced higher levels of IL-6 and TNF-alpha, neither BCH 189 nor AZT molecule interfered with cytokine release [36].
  • In addition, A-ODNs specific for Hsp60 also inhibit replication of a mutant HBV strain that is resistant to the nucleoside analogue 3TC, which is the main drug used for HBV treatment, and we suggest that A-ODNs directed against Hsp60 are possible reagents as anti-HBV drugs [37].

Analytical, diagnostic and therapeutic context of lamivudine


  1. Lamivudine in the treatment of acute hepatitis B. Reshef, R., Sbeit, W., Tur-Kaspa, R. N. Engl. J. Med. (2000) [Pubmed]
  2. Lamivudine for chronic hepatitis B. Bernasconi, E., Battegay, M. N. Engl. J. Med. (1998) [Pubmed]
  3. Treatment with lamivudine, zidovudine, or both in HIV-positive patients with 200 to 500 CD4+ cells per cubic millimeter. North American HIV Working Party. Eron, J.J., Benoit, S.L., Jemsek, J., MacArthur, R.D., Santana, J., Quinn, J.B., Kuritzkes, D.R., Fallon, M.A., Rubin, M. N. Engl. J. Med. (1995) [Pubmed]
  4. Lamivudine in the treatment of polyarteritis nodosa associated with acute hepatitis B. Gupta, S., Piraka, C., Jaffe, M. N. Engl. J. Med. (2001) [Pubmed]
  5. Interferon-lamivudine combination is no better than lamivudine alone in anti-HBe-positive chronic hepatitis B. Akarca, U.S., Ersoz, G., Gunsar, F., Karasu, Z., Saritas, E., Yuce, G., Batur, Y. Antivir. Ther. (Lond.) (2004) [Pubmed]
  6. Short-term corticosteroid therapy in combination with lamivudine: A case of déjà vu? Perrillo, R.P. Hepatology (2000) [Pubmed]
  7. Prenatal AZT or 3TC and mouse development of locomotor activity and hot-plate responding upon administration of the GABA(A) receptor agonist muscimol. Ricceri, L., Venerosi, A., Valanzano, A., Sorace, A., Alleva, E. Psychopharmacology (Berl.) (2001) [Pubmed]
  8. Pharmacokinetic interaction between rifampicin and the once-daily combination of saquinavir and low-dose ritonavir in HIV-infected patients with tuberculosis. Ribera, E., Azuaje, C., Lopez, R.M., Domingo, P., Curran, A., Feijoo, M., Pou, L., Sánchez, P., Sambeat, M.A., Colomer, J., Lopez-Colomes, J.L., Crespo, M., Falcó, V., Ocaña, I., Pahissa, A. J. Antimicrob. Chemother. (2007) [Pubmed]
  9. Monitoring drug resistance in chronic hepatitis B virus (HBV)-infected patients during lamivudine therapy: evaluation of performance of INNO-LiPA HBV DR assay. Lok, A.S., Zoulim, F., Locarnini, S., Mangia, A., Niro, G., Decraemer, H., Maertens, G., Hulstaert, F., De Vreese, K., Sablon, E. J. Clin. Microbiol. (2002) [Pubmed]
  10. Lamivudine for the treatment of chronic hepatitis B. Verhelst, D., Goffin, E. N. Engl. J. Med. (2000) [Pubmed]
  11. Lamivudine as initial treatment for chronic hepatitis B in the United States. Dienstag, J.L., Schiff, E.R., Wright, T.L., Perrillo, R.P., Hann, H.W., Goodman, Z., Crowther, L., Condreay, L.D., Woessner, M., Rubin, M., Brown, N.A. N. Engl. J. Med. (1999) [Pubmed]
  12. Maintenance antiretroviral therapies in HIV infected patients with undetectable plasma HIV RNA after triple-drug therapy. AIDS Clinical Trials Group Study 343 Team. Havlir, D.V., Marschner, I.C., Hirsch, M.S., Collier, A.C., Tebas, P., Bassett, R.L., Ioannidis, J.P., Holohan, M.K., Leavitt, R., Boone, G., Richman, D.D. N. Engl. J. Med. (1998) [Pubmed]
  13. Lamivudine-zidovudine combination for prevention of maternal-infant transmission of HIV-1. Mandelbrot, L., Landreau-Mascaro, A., Rekacewicz, C., Berrebi, A., Bénifla, J.L., Burgard, M., Lachassine, E., Barret, B., Chaix, M.L., Bongain, A., Ciraru-Vigneron, N., Crenn-Hébert, C., Delfraissy, J.F., Rouzioux, C., Mayaux, M.J., Blanche, S. JAMA (2001) [Pubmed]
  14. Treatment with indinavir, zidovudine, and lamivudine in adults with human immunodeficiency virus infection and prior antiretroviral therapy. Gulick, R.M., Mellors, J.W., Havlir, D., Eron, J.J., Gonzalez, C., McMahon, D., Richman, D.D., Valentine, F.T., Jonas, L., Meibohm, A., Emini, E.A., Chodakewitz, J.A. N. Engl. J. Med. (1997) [Pubmed]
  15. Safety and efficacy of lamivudine-zidovudine combination therapy in antiretroviral-naive patients. A randomized controlled comparison with zidovudine monotherapy. Lamivudine European HIV Working Group. Katlama, C., Ingrand, D., Loveday, C., Clumeck, N., Mallolas, J., Staszewski, S., Johnson, M., Hill, A.M., Pearce, G., McDade, H. JAMA (1996) [Pubmed]
  16. Adefovir dipivoxil added to ongoing lamivudine in chronic hepatitis B with YMDD mutant hepatitis B virus. Perrillo, R., Hann, H.W., Mutimer, D., Willems, B., Leung, N., Lee, W.M., Moorat, A., Gardner, S., Woessner, M., Bourne, E., Brosgart, C.L., Schiff, E. Gastroenterology (2004) [Pubmed]
  17. 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]
  18. Tenofovir disoproxil fumarate exhibits strong antiviral effect in a patient with lamivudine-resistant severe hepatitis B reactivation. Van Bömmel, F., Schernick, A., Hopf, U., Berg, T. Gastroenterology (2003) [Pubmed]
  19. Safety and efficacy of lamivudine-zidovudine combination therapy in zidovudine-experienced patients. A randomized controlled comparison with zidovudine monotherapy. Lamivudine European HIV Working Group. Staszewski, S., Loveday, C., Picazo, J.J., Dellarnonica, P., Skinhøj, P., Johnson, M.A., Danner, S.A., Harrigan, P.R., Hill, A.M., Verity, L., McDade, H. JAMA (1996) [Pubmed]
  20. Effect of trimethoprim on lamivudine bioavailability. Hudson, M., Nash, C. JAMA (1996) [Pubmed]
  21. Susceptibility of lamivudine-resistant hepatitis B virus to other reverse transcriptase inhibitors. Ono-Nita, S.K., Kato, N., Shiratori, Y., Lan, K.H., Yoshida, H., Carrilho, F.J., Omata, M. J. Clin. Invest. (1999) [Pubmed]
  22. Predominance of hepatitis B virus YMDD mutants is prognostic of viral DNA breakthrough. Lee, C.H., Kim, S.O., Byun, K.S., Moon, M.S., Kim, E.O., Yeon, J.E., Yoo, W., Hong, S.P. Gastroenterology (2006) [Pubmed]
  23. Lamivudine therapy for chronic hepatitis B: a six-month randomized dose-ranging study. Nevens, F., Main, J., Honkoop, P., Tyrrell, D.L., Barber, J., Sullivan, M.T., Fevery, J., De Man, R.A., Thomas, H.C. Gastroenterology (1997) [Pubmed]
  24. Lamivudine treatment can restore T cell responsiveness in chronic hepatitis B. Boni, C., Bertoletti, A., Penna, A., Cavalli, A., Pilli, M., Urbani, S., Scognamiglio, P., Boehme, R., Panebianco, R., Fiaccadori, F., Ferrari, C. J. Clin. Invest. (1998) [Pubmed]
  25. Hepatitis-B-virus resistance to lamivudine given for recurrent infection after orthotopic liver transplantation. Bartholomew, M.M., Jansen, R.W., Jeffers, L.J., Reddy, K.R., Johnson, L.C., Bunzendahl, H., Condreay, L.D., Tzakis, A.G., Schiff, E.R., Brown, N.A. Lancet (1997) [Pubmed]
  26. Reduction of HIV-1 in blood and lymph nodes following potent antiretroviral therapy and the virologic correlates of treatment failure. Wong, J.K., Günthard, H.F., Havlir, D.V., Zhang, Z.Q., Haase, A.T., Ignacio, C.C., Kwok, S., Emini, E., Richman, D.D. Proc. Natl. Acad. Sci. U.S.A. (1997) [Pubmed]
  27. Cross-resistance testing of next-generation nucleoside and nucleotide analogues against lamivudine-resistant HBV. Yang, H., Qi, X., Sabogal, A., Miller, M., Xiong, S., Delaney, W.E. Antivir. Ther. (Lond.) (2005) [Pubmed]
  28. Pre-emptive use of lamivudine in bone marrow transplantation with chronic hepatitis B virus infection. Deschênes, M., Laneuville, P. Hepatology (2004) [Pubmed]
  29. A controlled trial of two nucleoside analogues plus indinavir in persons with human immunodeficiency virus infection and CD4 cell counts of 200 per cubic millimeter or less. AIDS Clinical Trials Group 320 Study Team. Hammer, S.M., Squires, K.E., Hughes, M.D., Grimes, J.M., Demeter, L.M., Currier, J.S., Eron, J.J., Feinberg, J.E., Balfour, H.H., Deyton, L.R., Chodakewitz, J.A., Fischl, M.A. N. Engl. J. Med. (1997) [Pubmed]
  30. Safety and efficacy of adefovir dipivoxil in patients co-infected with HIV-1 and lamivudine-resistant hepatitis B virus: an open-label pilot study. Benhamou, Y., Bochet, M., Thibault, V., Calvez, V., Fievet, M.H., Vig, P., Gibbs, C.S., Brosgart, C., Fry, J., Namini, H., Katlama, C., Poynard, T. Lancet (2001) [Pubmed]
  31. Reduced replication of 3TC-resistant HIV-1 variants in primary cells due to a processivity defect of the reverse transcriptase enzyme. Back, N.K., Nijhuis, M., Keulen, W., Boucher, C.A., Oude Essink, B.O., van Kuilenburg, A.B., van Gennip, A.H., Berkhout, B. EMBO J. (1996) [Pubmed]
  32. Predictors of virologic and clinical outcomes in HIV-1-infected patients receiving concurrent treatment with indinavir, zidovudine, and lamivudine. AIDS Clinical Trials Group Protocol 320. Demeter, L.M., Hughes, M.D., Coombs, R.W., Jackson, J.B., Grimes, J.M., Bosch, R.J., Fiscus, S.A., Spector, S.A., Squires, K.E., Fischl, M.A., Hammer, S.M. Ann. Intern. Med. (2001) [Pubmed]
  33. Lamivudine plus zidovudine compared with zalcitabine plus zidovudine in patients with HIV infection. A randomized, double-blind, placebo-controlled trial. North American HIV Working Party. Bartlett, J.A., Benoit, S.L., Johnson, V.A., Quinn, J.B., Sepulveda, G.E., Ehmann, W.C., Tsoukas, C., Fallon, M.A., Self, P.L., Rubin, M. Ann. Intern. Med. (1996) [Pubmed]
  34. Impaired 2',3'-dideoxy-3'-thiacytidine accumulation in T-lymphoblastoid cells as a mechanism of acquired resistance independent of multidrug resistant protein 4 with a possible role for ATP-binding cassette C11. Turriziani, O., Schuetz, J.D., Focher, F., Scagnolari, C., Sampath, J., Adachi, M., Bambacioni, F., Riva, E., Antonelli, G. Biochem. J. (2002) [Pubmed]
  35. Hepatitis B virus enhances tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) cytotoxicity by increasing TRAIL-R1/death receptor 4 expression. Janssen, H.L., Higuchi, H., Abdulkarim, A., Gores, G.J. J. Hepatol. (2003) [Pubmed]
  36. In vitro immunotoxicity of +/- 2'-deoxy-3'-thiacytidine, a new anti-HIV agent. Lisignoli, G., Monaco, M.C., Degrassi, A., Toneguzzi, S., Ricchi, E., Costigliola, P., Facchini, A. Clin. Exp. Immunol. (1993) [Pubmed]
  37. Antisense oligodeoxynucleotides targeted against molecular chaperonin Hsp60 block human hepatitis B virus replication. Park, S.G., Lee, S.M., Jung, G. J. Biol. Chem. (2003) [Pubmed]
  38. Selection of a multiple drug-resistant hepatitis B virus strain in a liver-transplanted patient. Villet, S., Pichoud, C., Villeneuve, J.P., Tr??po, C., Zoulim, F. Gastroenterology (2006) [Pubmed]
  39. Lamivudine plus low-dose hepatitis B immunoglobulin to prevent recurrent hepatitis B following liver transplantation. Gane, E.J., Angus, P.W., Strasser, S., Crawford, D.H., Ring, J., Jeffrey, G.P., McCaughan, G.W. Gastroenterology (2007) [Pubmed]
  40. Preemptive lamivudine in hepatitis B patients undergoing chemotherapy. Del Poggio, P., Jamoletti, C., Zaccanelli, M. Gastroenterology (2004) [Pubmed]
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