Research Topics
| R J ColonnoSummaryAffiliation: Bristol-Myers Squibb Country: USA Publications
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Publications
Entecavir resistance is rare in nucleoside naïve patients with hepatitis BRichard J Colonno
Bristol Myers Squibb Pharmaceutical Research Institute, Wallingford, CT 06492, USA
Hepatology 44:1656-65. 2006..These findings suggest that the rapid, sustained suppression of HBV replication, combined with a requirement for multiple substitutions, creates a high genetic barrier to ETVr in nucleoside naïve patients...
Identification of I50L as the signature atazanavir (ATV)-resistance mutation in treatment-naive HIV-1-infected patients receiving ATV-containing regimensRichard Colonno
Bristol Myers Squibb Pharmaceutical Research Institute, Wallingford, Connecticut, USA
J Infect Dis 189:1802-10. 2004..The unique I50L substitution is the signature mutation for resistance to ATV...
Long-term entecavir treatment results in sustained antiviral efficacy and prolonged life span in the woodchuck model of chronic hepatitis infectionR J Colonno
Bristol Myers Squibb Pharmaceutical Research Institute, Wallingford, Connecticut 06492 7660, USA
J Infect Dis 184:1236-45. 2001..ETV was well tolerated, and there was no evidence of resistant variants. On the basis of historical data, long-term ETV treatment appeared to significantly prolong the life of treated animals and delay the emergence of HCC...
Efficacy of the carbocyclic 2'-deoxyguanosine nucleoside BMS-200475 in the woodchuck model of hepatitis B virus infectionE V Genovesi
Pharmaceutical Research Institute, Bristol Myers Squibb, Wallingford, Connecticut 06492, USA
Antimicrob Agents Chemother 42:3209-17. 1998..These results indicate that BMS-200475 should be evaluated in clinical trials for the therapy of chronic human hepatitis B virus infections...
Antiviral efficacy of lobucavir (BMS-180194), a cyclobutyl-guanosine nucleoside analogue, in the woodchuck (Marmota monax) model of chronic hepatitis B virus (HBV) infectionE V Genovesi
Bristol Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, Connecticut, CT 06492 7660, USA
Antiviral Res 48:197-203. 2000..These results indicated that the minimally effective antiviral daily per os dose of lobucavir in WHV-carrier woodchucks was approximately 5 mg/kg...
Lobucavir is phosphorylated in human cytomegalovirus-infected and -uninfected cells and inhibits the viral DNA polymeraseD J Tenney
Department of Virology, Bristol Myers Squibb Pharmaceutical Research Institute, Wallingford, Connecticut 06492, USA
Antimicrob Agents Chemother 41:2680-5. 1997..Furthermore, LBV may be effective in the treatment of GCV-resistant HCMV...
Clinical emergence of entecavir-resistant hepatitis B virus requires additional substitutions in virus already resistant to LamivudineD J Tenney
Bristol Myers Squibb Pharmaceutical Research Institute, 5 Research Pkwy, Wallingford, CT 06492, USA
Antimicrob Agents Chemother 48:3498-507. 2004..In summary, infrequent ETV resistance can emerge during prolonged therapy, with selection of additional RT substitutions within a 3TC(r) HBV background, leading to reduced ETV susceptibility and treatment failure...
Metabolic studies on BMS-200475, a new antiviral compound active against hepatitis B virusG Yamanaka
Bristol Myers Squibb Pharmaceutical Research Institute, Wallingford, Connecticut 06492 7660, USA
Antimicrob Agents Chemother 43:190-3. 1999..Compared with five other nucleoside analogs of medical interest (lamivudine, penciclovir, ganciclovir, acyclovir, and lobucavir), BMS-200475 was most efficiently phosphorylated to the triphosphate in HepG2 cells...
Efficacies of entecavir against lamivudine-resistant hepatitis B virus replication and recombinant polymerases in vitroS Levine
Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA
Antimicrob Agents Chemother 46:2525-32. 2002..These findings are predictive of potent antiviral activity of ETV against both wild-type and 3TC-resistant HBV...
De novo initiation of RNA synthesis by the RNA-dependent RNA polymerase (NS5B) of hepatitis C virusG Luo
Department of Virology, Bristol Myers Squibb Pharmaceutical Research Institute, Wallingford, Connecticut 06492 7660, USA
J Virol 74:851-63. 2000..These findings suggest that HCV NS5B is able to initiate RNA synthesis de novo...
Separate functional domains of the herpes simplex virus type 1 protease: evidence for cleavage inside capsidsB J Robertson
Department of Virology, Bristol Myers Squibb Pharmaceutical Research Institute, Wallingford, Connecticut 06492 7660, USA
J Virol 70:4317-28. 1996..Our results demonstrate that the HSV-1 protease has distinct functional domains and some of these functions can complement in trans...
Stavudine resistance: an update on susceptibility following prolonged therapyP F Lin
Bristol Myers Squibb, Wallingford, Conn, USA
Antivir Ther 4:21-8. 1999..This low incidence of stavudine resistance is in striking contrast to that observed with other nucleoside analogues and further supports the use of stavudine in first-line combination therapy for HIV patients...
Entecavir for treatment of hepatitis B virus displays no in vitro mitochondrial toxicity or DNA polymerase gamma inhibitionCharles E Mazzucco
Bristol Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA
Antimicrob Agents Chemother 52:598-605. 2008..In summary, cell culture and enzymatic studies yielded no evidence that would predict mitochondrial toxicity of ETV at exposure levels in excess of those expected to be achieved clinically...
Inhibition of hepatitis B virus polymerase by entecavirDavid R Langley
Bristol Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06443, USA
J Virol 81:3992-4001. 2007..Overall, these studies explain the potency, mechanism, and cross-resistance profile of ETV against HBV and account for the successful treatment of naive and LVD- or ADV-experienced chronic HBV patients...
Two-year assessment of entecavir resistance in Lamivudine-refractory hepatitis B virus patients reveals different clinical outcomes depending on the resistance substitutions presentDaniel J Tenney
Bristol Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA
Antimicrob Agents Chemother 51:902-11. 2007..In summary, ETV was effective in LVD-refractory patients, with resistant sequences arising from a subset of patients harboring preexisting LVDr/ETVr variants and with approximately half of the patients experiencing a virologic rebound...
The effects of the Roche AMPLICOR HIV-1 MONITOR UltraSensitive Test versions 1.0 and 1.5 viral load assays and plasma collection tube type on determination of response to antiretroviral therapy and the inappropriateness of cross-study comparisonsMichael Giordano
Pharmaceutical Research Institute, Bristol Myers Squibb Company, 3 rue Joseph Monier, 92500 Rueil Malmaison, Paris, France
J Clin Virol 35:420-5. 2006..However, a variety of factors can confound these comparisons, resulting in misleading or invalid conclusions...
Hepatitis B virus quasispecies susceptibility to entecavir confirms the relationship between genotypic resistance and patient virologic responseCarl J Baldick
Bristol Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA
J Hepatol 48:895-902. 2008..Using >500 patient HBV isolates from several entecavir clinical trials, we show that phenotypic susceptibility correlates with genotypic resistance and patient virologic responses...
Protection of macaques from vaginal SHIV challenge by vaginally delivered inhibitors of virus-cell fusionRonald S Veazey
Tulane National Primate Research Center, Covington, Louisiana 70433, USA
Nature 438:99-102. 2005..In vivo, significant protection was achieved using each compound alone and in combinations. CMPD167 and BMS-378806 were protective even when applied 6 h before challenge...
A dose-ranging study of the efficacy and tolerability of entecavir in Lamivudine-refractory chronic hepatitis B patientsTing Tsung Chang
National Cheng Kung University Medical College, Tainan, Taiwan
Gastroenterology 129:1198-209. 2005..This randomized, dose-ranging, phase 2 study compared the efficacy and safety of entecavir with lamivudine in lamivudine-refractory patients...
Molecular basis for increased susceptibility of isolates with atazanavir resistance-conferring substitution I50L to other protease inhibitorsJoseph Yanchunas
Gene Expression and Protein Biochemistry Department, Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA
Antimicrob Agents Chemother 49:3825-32. 2005..The results of this study provide a molecular understanding of the novel hypersusceptibility of atazanavir-resistant I50L/A71V-containing clinical isolates to other currently approved PIs...
Potent efficacy of entecavir (BMS-200475) in a duck model of hepatitis B virus replicationPatricia L Marion
Division of Gastroenterology, Stanford University School of Medicine, Stanford, California 94305 5187, USA
Antimicrob Agents Chemother 46:82-8. 2002..ETV and 3TC were both well tolerated in all treated animals. These results show that ETV is a highly potent and effective antiviral in the DHBV duck model...
Activities of atazanavir (BMS-232632) against a large panel of human immunodeficiency virus type 1 clinical isolates resistant to one or more approved protease inhibitorsRichard J Colonno
Bristol Myers Squibb Pharmaceutical Research Institute, Wallingford, Connecticut 06492, USA
Antimicrob Agents Chemother 47:1324-33. 2003..0-fold), the presence of at least five of these substitutions correlated strongly with loss of atazanavir susceptibility. Mutations associated with reduced susceptibility to each of the other six PIs were also determined...
Entecavir therapy combined with DNA vaccination for persistent duck hepatitis B virus infectionWendy K Foster
School of Molecular and Biomedical Science, University of Adelaide, Adelaide, South Australia 5005, Australia
Antimicrob Agents Chemother 47:2624-35. 2003....
Characterization of antiviral activity of entecavir in transgenic mice expressing hepatitis B virusJustin G Julander
Institute for Antiviral Research, Animal, Dairy, and Veterinary Sciences Department and Biotechnology Center, Utah State University, 4700 Old Main Hill, Logan, UT 84322-4700, USA
Antiviral Res 59:155-61. 2003..ETV was well tolerated and no morbidity or mortality was observed during the 10-day study. Similar to other animal models, ETV displayed potent anti-HBV activity in this transgenic mouse model...
Comprehensive evaluation of hepatitis B virus reverse transcriptase substitutions associated with entecavir resistanceCarl J Baldick
Bristol Myers Squibb Research and Development, Wallingford, CT 06492, USA
Hepatology 47:1473-82. 2008....
Respiratory syncytial virus fusion inhibitors. Part 4: optimization for oral bioavailabilityKuo Long Yu
Department of Chemistry, The Bristol Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA
Bioorg Med Chem Lett 17:895-901. 2007....
Biochemical and genetic characterizations of a novel human immunodeficiency virus type 1 inhibitor that blocks gp120-CD4 interactionsQi Guo
Department of Virology, Bristol Myers Squibb Pharmaceutical Research Institute, Wallingford, Connecticut 06492, USA
J Virol 77:10528-36. 2003..BMS-378806 therefore serves as a prototype for this new class of antiretroviral agents and validates gp120 as a viable target for small-molecule inhibitors...
Effect of antiviral treatment with entecavir on age- and dose-related outcomes of duck hepatitis B virus infectionWendy K Foster
Hepatitis Virus Research Laboratory, Infectious Diseases Laboratories, Institute of Medical and Veterinary Science, Frome Rd, Box 14 Rundle Mall, Adelaide, SA 5000, Australia
J Virol 79:5819-32. 2005..Since DHBV infection of ducks provides a good model system for HBV infection in humans, it seems likely that ETV may be useful in postexposure therapy for HBV infection aimed at preventing the development of persistent infection...
Discovery of 4-benzoyl-1-[(4-methoxy-1H- pyrrolo[2,3-b]pyridin-3-yl)oxoacetyl]-2- (R)-methylpiperazine (BMS-378806): a novel HIV-1 attachment inhibitor that interferes with CD4-gp120 interactionsTao Wang
Department of Discovery Chemistry, The Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, Connecticut 06492, USA
J Med Chem 46:4236-9. 2003..The 7-azaindole derivative 3, BMS-378806, exhibited improved pharmaceutical properties while retaining the HIV-1 inhibitory profile of 2...
