Page last updated: 2024-11-13

entecavir

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Description

entecavir (anhydrous) : Guanine substituted at the 9 position by a 4-hydroxy-3-(hydroxymethyl)-2-methylidenecyclopentyl group. A synthetic analogue of 2'-deoxyguanosine, it is a nucleoside reverse transcriptase inhibitor with selective antiviral activity against hepatitis B virus. Entecavir is phosphorylated intracellularly to the active triphosphate form, which competes with deoxyguanosine triphosphate, the natural substrate of hepatitis B virus reverse transcriptase, inhibiting every stage of the enzyme's activity, although it has no activity against HIV. It is used for the treatment of chronic hepatitis B. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID135398508
CHEMBL ID713
CHEBI ID59902
CHEBI ID473990
SCHEMBL ID28648
SCHEMBL ID15198001
MeSH IDM0370336
PubMed CID57339144
CHEMBL ID2426364
CHEBI ID95086
SCHEMBL ID19730381
MeSH IDM0370336

Synonyms (130)

Synonym
AC-1593
2-amino-9-[(1s,3r,4s)-4-hydroxy-3-(hydroxymethyl)-2-methylidenecyclopentyl]-6,9-dihydro-1h-purin-6-one
bms-200475
baraclude
2-amino-9-[(1s,3r,4s)-4-hydroxy-3-(hydroxymethyl)-2-methylene-cyclopentyl]-1h-purin-6-one
142217-69-4
entecavir
6-h-purin-6-one-,2-amino-1,9-dihydro-9-[(1s,3r,4s)-4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]
sq-34676
209216-23-9
entecavir (anhydrous)
entecavir anhydrous
DB00442
anhydrous entecavir
NCGC00164563-01
hsdb 7334
6h-purin-6-one, 2-amino-1,9-dihydro-9-((1s,3r,4s)-4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl)-
sq 34676
entecavir [usan:inn]
bms 200475
CHEMBL713
sq34676
bms-200475-01
CHEBI:59902 ,
2-amino-9-[(1s,3r,4s)-4-hydroxy-3-(hydroxymethyl)-2-methylidenecyclopentyl]-3h-purin-6-one
D07896
entecavir (inn)
QDGZDCVAUDNJFG-FXQIFTODSA-N
chebi:473990 ,
2-amino-9-[(1s,3r,4s)-4-hydroxy-3-(hydroxymethyl)-2-methylidenecyclopentyl]-1,9-dihydro-6h-purin-6-one
A807868
2-amino-9-[(1r,3r,4s)-4-hydroxy-3-(hydroxymethyl)-2-methylene-cyclopentyl]-3h-purin-6-one hydrate;entecavir
2-amino-1,9-dihydro-9-[(1s,3r,4s)-4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]-6h-purin-6-one
nnu2o4609d ,
unii-nnu2o4609d
cas-142217-69-4
dtxcid2026446
dtxsid4046446 ,
tox21_112192
bms 200475-01
unii-5968y6h45m
AKOS015920226
2-amino-9-((1s,3r,4s)-4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl)-1,9-dihydro-6h-purin-6-one
entecavir [who-dd]
entecavir [hsdb]
entecavir [inn]
entecavir [mi]
AKOS015854916
6h-purin-6-one, 2-amino-1,9-dihydro-9-[(1s,3r,4s)-4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]-
AM20080880
(1r,3s,4s)-entecavir
BRD-K08206212-001-01-2
CS-3160
HY-13623
SCHEMBL28648
SCHEMBL15198001
E0899
9-[(1s,3r,4s)-4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]guanine
mfcd00907887
sq 34,676
2-amino-9-[(1s,3r,4s)-4-hydroxy-3-hydroxymethyl-2-methylene-cyclopentyl]-3,9-dihydro-purin-6-one
AKOS025312554
2-amino-9-[(1s,3r,4s)-4-hydroxy-3-(hydroxymethyl)-2-methylidenecyclopentyl]-6,9-dihydro-3h-purin-6-one
bms200475
GS-6386
entecavir, >=98% (hplc)
2-amino-9-((1s,3r,4s)-4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl)-1h-purin-6(9h)-one
NCGC00164563-09
bdbm50248008
Q418586
1333204-94-6
AR-270/43507901
2-amino-9-[4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]-1,9-dihydro-6h-purin-6-one
CCG-267218
NCGC00164563-04
NCGC00164563-13
2-amino-9-[(1s,3r,4s)-4-hydroxy-3-hydroxymethyl-2-methylenecyclopentyl]-1,9-dihydro-6h-purin-6-one
2-amino-9-[(1s,3r,4s)-4-hydroxy-3-(hydroxymethyl)-2-methylidenecyclopentyl]-1h-purin-6-one
S5246
NCGC00164563-06
EN300-37158607
entecavir (mart.)
entecavirum
j05af10
entecavir (usp monograph)
entecavir monohydrate (ep monograph)
entecavir monohydrate (usp-rs)
[2-(phenylamino)benzene-1,4-diyl]bis{[4-(pyrrolidin-1-yl)piperidin-1-yl]methanone}
NCGC00344623-02
2-phenylamino-1,4-bis(4-(pyrrolidinyl)piperidinyl)benzamide
S7088
(2-(phenylamino)-1,4-phenylene)bis((4-(pyrrolidin-1-yl)piperidin-1-yl)methanone)
BP-21087
gtpl8232
n-phenyl-2,5-bis[4-(pyrrolidin-1-yl)piperidine-1-carbonyl]aniline
bdbm50440614
chembl2426364 ,
unc1215 ,
CS-1646
HY-15649
MLS006011024
smr004702819
1415800-43-9
2-phenylamino-1,4-bis[4-(pyrrolidinyl)-piperidinyl)benzamide]
unc 1215
2-phenylamino-1,4-[4-(pyrrolidinyl)piperidinyl)benzamide
AC-32715
AKOS024458279
unc-1215
[3-anilino-4-(4-pyrrolidin-1-ylpiperidine-1-carbonyl)phenyl]-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone
EX-A193
CHEBI:95086
HMS3652P22
unc1215, >=98% (hplc)
mfcd22683289
NCGC00344623-12
SCHEMBL19730381
n-phenyl-2,5-bis({[4-(pyrrolidin-1-yl)piperidin-1-yl]carbonyl})aniline
SW220042-1
FT-0713405
BCP07393
Q27089089
AS-16797
methanone, 1,1'-[2-(phenylamino)-1,4-phenylene]bis[1-[4-(1-pyrrolidinyl)-1-piperidinyl]-
SB19337
HMS3426E15
HMS3744C05
CCG-269911
A857599
DTXSID301026044

Research Excerpts

Toxicity

Entecavir (ETV) has been shown to be safe and efficacious in randomised controlled trials in highly selected patients with hepatitis B virus (HBV) infection. Tenofovir and entecvir are effective and safe for long-term use in patients with compensated or decompensated cirrhosis.

ExcerptReferenceRelevance
" Entecavir was well tolerated, with no patients discontinuing study drug due to adverse events."( Efficacy and safety of entecavir in lamivudine-refractory patients with chronic hepatitis B: randomized controlled trial in Japanese patients.
Imazeki, F; Kage, M; Katano, Y; Kumada, H; Moriyama, M; Omata, M; Sata, M; Seriu, T; Suzuki, F; Toyoda, J, 2008
)
0.35
" The frequency of adverse events with entecavir and placebo was comparable."( Efficacy and safety of entecavir for chronic HBV in HIV/HBV coinfected patients receiving lamivudine as part of antiretroviral therapy.
Brandão-Mello, CE; Brett-Smith, H; Cassetti, I; Gazzard, B; Hall, A; Huang, AK; Mendes-Corrêa, MC; Pessôa, MG; Phiri, P; Soriano, V, 2008
)
0.35
" There were no significant adverse effects from these drugs and no alteration of renal function during the follow-up period."( Efficacy and safety of entecavir and/or tenofovir for prophylaxis and treatment of hepatitis B recurrence post-liver transplant.
de la Cruz-Lombardo, J; Jiménez-Pérez, M; Lozano-Rey, JM; Mongil Poce, L; Rodrigo-López, JM; Sáez-Gómez, AB, 2010
)
0.36
"Therapy with ETV and/or TDF seems to be efficient and safe when used in the prophylaxis and treatment of HBV recurrence after liver transplantation."( Efficacy and safety of entecavir and/or tenofovir for prophylaxis and treatment of hepatitis B recurrence post-liver transplant.
de la Cruz-Lombardo, J; Jiménez-Pérez, M; Lozano-Rey, JM; Mongil Poce, L; Rodrigo-López, JM; Sáez-Gómez, AB, 2010
)
0.36
" There were no serious adverse events."( Three years of continuous entecavir therapy in treatment-naïve chronic hepatitis B patients: VIRAL suppression, viral resistance, and clinical safety.
Fung, J; Lai, CL; Seto, WK; Wong, DK; Yuen, JC; Yuen, MF, 2011
)
0.37
" Adverse event rates were comparable between groups."( Efficacy and safety of entecavir versus adefovir in chronic hepatitis B patients with hepatic decompensation: a randomized, open-label study.
Beebe, S; Bialkowska, J; Brown, RS; Cheinquer, H; Cooney, E; Jeffers, L; Leung, N; Liaw, YF; Myers, RP; Peng, CY; Raptopoulou-Gigi, M; Sarin, SK; Tang, S; Tanwandee, T; Tsai, N, 2011
)
0.37
"To review long-term safety data from the rollover study ETV-901, focusing on adverse events (AEs) with a potential nucleos(t)ide association."( Long-term safety and tolerability of entecavir in patients with chronic hepatitis B in the rollover study ETV-901.
Akarca, US; Beebe, S; Chang, TT; Manns, MP; Min, A; Pangerl, A; Sievert, W; Tsai, N; Wongcharatrawee, S; Yoon, SK; Yu, M, 2012
)
0.38
" No patients discontinued treatment due to adverse events."( Efficacy and safety of entecavir in clinical practice in treatment-naive Caucasian chronic hepatitis B patients.
Bonet, L; Buti, M; Diago, M; García-Samaniego, J; Morillas, RM; Palau, A; Pérez, J; Prieto, M; Rodríguez, M; Solà, R; Testillano, M, 2012
)
0.38
" Several studies suggest that NAs long-term administration have been associated with low rates of serious adverse events (AEs), including lactic acidosis, renal function impairment, osteopenia and osteoporosis."( Safety of long-term nucleos(t)ide treatment in chronic hepatitis B.
Ridruejo, E; Silva, MO, 2012
)
0.38
" Laboratory test results, clinical outcomes, and drug-related adverse events were compared among groups."( Long-term efficacy and safety of lamivudine, entecavir, and tenofovir for treatment of hepatitis B virus-related cirrhosis.
Akbal, E; Akin, E; Alkan, E; Ataseven, H; Aygün, C; Başar, O; Baykal, O; Coban, S; Demir, M; Gülşen, MT; Ibiş, M; Koçkar, MC; Köklü, S; Köksal, AŞ; Küçükazman, M; Nadir, I; Ozdil, K; Pürnak, T; Tuna, Y; Yildirim, B; Yüksel, I; Yüksel, O, 2013
)
0.39
"Tenofovir and entecavir are effective and safe for long-term use in patients with compensated or decompensated cirrhosis from HBV infection."( Long-term efficacy and safety of lamivudine, entecavir, and tenofovir for treatment of hepatitis B virus-related cirrhosis.
Akbal, E; Akin, E; Alkan, E; Ataseven, H; Aygün, C; Başar, O; Baykal, O; Coban, S; Demir, M; Gülşen, MT; Ibiş, M; Koçkar, MC; Köklü, S; Köksal, AŞ; Küçükazman, M; Nadir, I; Ozdil, K; Pürnak, T; Tuna, Y; Yildirim, B; Yüksel, I; Yüksel, O, 2013
)
0.39
" No severe adverse events associated with entecavir or tenofovir were reported."( Efficacy and safety of entecavir and/or tenofovir in hepatitis B compensated and decompensated cirrhotic patients in clinical practice.
Arenas, J; Canós, AP; Díaz-Sánchez, A; Jiménez, M; Miquel, M; Núñez, Ó; Trapero-Marugán, M,
)
0.13
" In addition, no obvious adverse reactions were observed during ETV treatment."( The efficacy and safety of entecavir in patients with advanced schistosomiasis co-infected with hepatitis B virus.
Hua, HY; Huang, LH; Li, YG; Niu, XH; Qiu, YW; Wu, HY; Wu, PF; Yang, XJ; Yao, SZ; Zhu, HY, 2013
)
0.39
"ETV is safe and effective in patients with advanced schistosomiasis and HBV co-infection."( The efficacy and safety of entecavir in patients with advanced schistosomiasis co-infected with hepatitis B virus.
Hua, HY; Huang, LH; Li, YG; Niu, XH; Qiu, YW; Wu, HY; Wu, PF; Yang, XJ; Yao, SZ; Zhu, HY, 2013
)
0.39
" Adverse event rates were comparable between treatment-na€ıve and treatment-experienced patients with compensated liver disease, but were higher in decompensated than in compensated patients, consistent with previous reports in these patients with more advanced disease."( Efficacy and safety of entecavir treatment in a heterogeneous CHB population from a ‘real-world’ clinical practice setting in China.
Cheng, M; Cohen, D; Hou, JL; Jia, JD; Llamoso, C; Ren, H; Tan, DM; Tang, H; Tang, X; Wang, YM; Wei, L; Zhao, W, 2013
)
0.39
"Entecavir (ETV) is effective and safe in patients with chronic hepatitis B in the short term, but its long term efficacy and safety has not been established."( Efficacy and safety of long term entecavir in chronic hepatitis B treatment naïve patients in clinical practice.
Adrover, R; Cocozzella, D; Estepo, C; Fainboim, H; Fernandez, N; Gadano, AC; Galdame, O; Levi, D; Mandó, OG; Marciano, S; Mendizabal, M; Muñoz, AE; Paz, S; Reggiardo, MV; Ridruejo, E; Romero, GA; Schroder, T; Silva, MO,
)
0.13
" No serious adverse events were reported."( Efficacy and safety of long term entecavir in chronic hepatitis B treatment naïve patients in clinical practice.
Adrover, R; Cocozzella, D; Estepo, C; Fainboim, H; Fernandez, N; Gadano, AC; Galdame, O; Levi, D; Mandó, OG; Marciano, S; Mendizabal, M; Muñoz, AE; Paz, S; Reggiardo, MV; Ridruejo, E; Romero, GA; Schroder, T; Silva, MO,
)
0.13
"TDF and ETV are similarly effective and safe in chronic HBV patients after 24 weeks and 48 weeks of anti-viral therapy."( Comparison of efficacy and safety of tenofovir and entecavir in chronic hepatitis B virus infection: a systematic review and meta-analysis.
Gao, Y; Ke, W; Liu, L; Yang, Y; Ye, X; Zhang, C; Zhou, S, 2014
)
0.4
" Entecavir as a potent and safe agent leading to continuous viral suppression proved to be safe and well tolerated therapy."( Four-year study of entecavir efficacy and safety in nucleos(t)ide-naïve HBeAg positive chronic hepatitis B patients.
Ayaz, C; Bayan, K; Celen, MK; Dal, T; Devecil, O; Mert, D; Oruc, EK, 2014
)
0.4
" Combination therapy with tenofovir plus entecavir in this setting with multidrug resistance is safe and effective."( Efficacy and safety of tenofovir in a kidney transplant patient with chronic hepatitis B and nucleos(t)ide multidrug resistance: a case report.
Shan, C; Wu, P; Yin, GQ, 2014
)
0.4
"This retrospective investigation carried out in Guangdong Province indicated that not only are anti-HBV drugs efficacious for blocking vertical transmission of HBV but also are safe for both mothers and infants when taken by fathers or mothers during the reproduction phases of insemination and pregnancy."( [Retrospective analysis of the efficacy and safety of anti-hepatitis B virus drugs taken during pregnancy in women from the Guangdong Province].
Chen, X; Gao, W; Li, D; Peng, J; Wen, F; Xia, J; Xu, C; Xu, M; Yao, Z, 2014
)
0.4
" There were no treatment discontinuations due to adverse events."( Entecavir has high efficacy and safety in white patients with chronic hepatitis B and comorbidities.
Andrade, R; Arenas, JI; Bonet, L; Buti, M; Calleja, JL; Castellano, G; Delgado, M; Diago, M; Gallego, A; García-Buey, L; García-Samaniego, J; Gila, A; González-Guirado, A; Gutiérrez, ML; Mas, A; Morillas, RM; Palau, A; Pérez, J; Prieto, M; Rodríguez, M; Romero-Gómez, M; Solà, R; Testillano, M, 2015
)
0.42
" No adverse effect was identified in the examined studies."( The efficacy and safety of entecavir in patients with chronic hepatitis B- associated liver failure: a meta-analysis.
An, Y; Chen, S; Du, Y; Gao, S; Liu, L; Zhang, M; Zhang, X,
)
0.13
" There was no case with serious adverse event."( Virologic response and safety of tenofovir versus entecavir in treatment-naïve chronic Hepatitis B patients.
An, SH; Choe, WH; Chung, HA; Jeong, GW; Jeong, TG; Kim, J; Kim, JH; Kwon, SW; Kwon, SY; Min, JK; Yu, HM; Yun, SU,
)
0.13
" ETV, IFN, and the combination of the two are safe in CHB treatment."( The Efficacy and Safety of Entecavir and Interferon Combination Therapy for Chronic Hepatitis B Virus Infection: A Meta-Analysis.
Fu, LL; Wu, LH; Xiang, Y; Xie, QL; Zhu, Y, 2015
)
0.42
" No adverse effects were observed or dose reductions required associated with ETV or TDF."( Tenofovir/entecavir monotherapy after hepatitis B immunoglobulin withdrawal is safe and effective in the prevention of hepatitis B in liver transplant recipients.
Abradelo, M; Calvo, J; Cambra, F; Castellano, G; Fernández, I; García, A; Hernández, O; Jiménez, C; Loinaz, C; Manrique, A; Manzano, M, 2015
)
0.42
"Maintenance therapy with newer NAs, after discontinuation of HBIG prophylaxis, was safe and effective, with a low rate of serological recurrence and no evident clinical, biochemical, or virological consequences."( Tenofovir/entecavir monotherapy after hepatitis B immunoglobulin withdrawal is safe and effective in the prevention of hepatitis B in liver transplant recipients.
Abradelo, M; Calvo, J; Cambra, F; Castellano, G; Fernández, I; García, A; Hernández, O; Jiménez, C; Loinaz, C; Manrique, A; Manzano, M, 2015
)
0.42
"Entecavir (ETV) has been shown to be safe and efficacious in randomised controlled trials in highly selected patients with hepatitis B virus (HBV) infection."( Entecavir safety and effectiveness in a national cohort of treatment-naïve chronic hepatitis B patients in the US - the ENUMERATE study.
Ahn, J; Chu, D; Do, S; Lee, HM; Lim, JK; Lok, AS; Mannalithara, A; Min, A; Nguyen, MH; Pan, CQ; Ray Kim, W; Reddy, KR; Te, H; Tran, T; Trinh, H, 2016
)
0.43
" Rates of ALT normalisation, undetectable HBV DNA, HBeAg and HBsAg loss/seroconversion, adverse events (AE) and clinical outcomes were evaluated."( Entecavir safety and effectiveness in a national cohort of treatment-naïve chronic hepatitis B patients in the US - the ENUMERATE study.
Ahn, J; Chu, D; Do, S; Lee, HM; Lim, JK; Lok, AS; Mannalithara, A; Min, A; Nguyen, MH; Pan, CQ; Ray Kim, W; Reddy, KR; Te, H; Tran, T; Trinh, H, 2016
)
0.43
"Entecavir treatment was safe in a large cohort of US patients, but ALT normalisation and hepatitis B virus DNA suppression rates were lower than previously reported in clinical trials."( Entecavir safety and effectiveness in a national cohort of treatment-naïve chronic hepatitis B patients in the US - the ENUMERATE study.
Ahn, J; Chu, D; Do, S; Lee, HM; Lim, JK; Lok, AS; Mannalithara, A; Min, A; Nguyen, MH; Pan, CQ; Ray Kim, W; Reddy, KR; Te, H; Tran, T; Trinh, H, 2016
)
0.43
" The adverse responses were recorded."( Safety and efficacy of mizoribine treatment in nephrotic syndrome complicated with hepatitis B virus infection: a clinical study.
Ji, Y; Li, W; Liu, J; Sun, J; Wang, J; Yong, Q; Zhang, H; Zhang, K; Zhang, W, 2016
)
0.43
"This study indicates that newer antivirals are effective and safe in HTR with CHB."( Efficacy and safety of tenofovir, entecavir, and telbivudine for chronic hepatitis B in heart transplant recipients.
Andini, R; Durante-Mangoni, E; Falco, E; Iossa, D; Maiello, C; Parrella, A; Ragone, E; Utili, R; Vitrone, M; Zampino, R, 2016
)
0.43
" Monitoring viral and liver markers combined with hepatologist consultations may ensure safe follow-up in LDKT recipients with prior resolved HBV infection."( Safety of Monitoring Viral and Liver Function Markers in Patients With Prior Resolved Hepatitis B Infection After Kidney Transplantation.
Chikaraishi, T; Imai, N; Kawarazaki, H; Koitabashi, K; Maekawa, H; Nakazawa, R; Sasaki, H; Shibagaki, Y; Yazawa, M,
)
0.13
" The incidence of serious adverse events was low and unrelated to the study medications."( Efficacy and safety of entecavir versus lamivudine over 5 years of treatment: A randomized controlled trial in Korean patients with hepatitis B e antigen-negative chronic hepatitis B.
Byun, KS; Heo, J; Kim, BH; Kim, D; Kim, DJ; Kim, TH; Kweon, YO; Lee, HJ; Lee, KS; Lee, MS; Lee, YS; Lim, YS; Paik, SW; Suh, DJ; Um, SH; Yu, K, 2017
)
0.46
"Entecavir (ETV) is effective and safe antiviral agent against hepatitis B virus (HBV) in clinical and real-world setting but, most studies were performed in single institute or have limitation in patient's number."( Large-scale surveillance study of the safety and effectiveness of entecavir in Korean patients with chronic hepatitis B.
Kim, CS; Kim, CW; Kim, HY; Lee, CD; Lee, HJ; Llamoso, C; Yu, K, 2018
)
0.48
" For the safety assessment, investigators recorded the occurrence of observed and patient-reported adverse events (AEs), as well as laboratory abnormalities."( Large-scale surveillance study of the safety and effectiveness of entecavir in Korean patients with chronic hepatitis B.
Kim, CS; Kim, CW; Kim, HY; Lee, CD; Lee, HJ; Llamoso, C; Yu, K, 2018
)
0.48
"57%), and 67 adverse drug reactions in 54 cases (1."( Large-scale surveillance study of the safety and effectiveness of entecavir in Korean patients with chronic hepatitis B.
Kim, CS; Kim, CW; Kim, HY; Lee, CD; Lee, HJ; Llamoso, C; Yu, K, 2018
)
0.48
" Death, acute pancreatitis, lactic acidosis and kidney function impairment were considered as major adverse events."( Efficacy and safety of long-term entecavir therapy in a European population.
Belci, P; Collo, A; Durazzo, M; Fagoonee, S; Gariglio, V; Loreti, L; Magistroni, P; Parise, R, 2018
)
0.48
" No major adverse events were recorded."( Efficacy and safety of long-term entecavir therapy in a European population.
Belci, P; Collo, A; Durazzo, M; Fagoonee, S; Gariglio, V; Loreti, L; Magistroni, P; Parise, R, 2018
)
0.48
" Finally, ETV is a safe drug, substantially free of major side effects."( Efficacy and safety of long-term entecavir therapy in a European population.
Belci, P; Collo, A; Durazzo, M; Fagoonee, S; Gariglio, V; Loreti, L; Magistroni, P; Parise, R, 2018
)
0.48
" None of our patients reported NUCs-related complications or adverse effects."( Entecavir and other nucleos(t)ide analogs prophylaxis in hepatitis B virus-related liver transplantation: long-term efficacy and safety.
Akroof, K; Darweesh, SK; ElLatif, ZA; Gad, AA, 2019
)
0.51
"ETV and other NUCs were effective and safe as a long-term prophylaxis of HBV recurrence after LTx, leading to a good graft function."( Entecavir and other nucleos(t)ide analogs prophylaxis in hepatitis B virus-related liver transplantation: long-term efficacy and safety.
Akroof, K; Darweesh, SK; ElLatif, ZA; Gad, AA, 2019
)
0.51
" Entecavir and tenofovir were safe and well tolerated, while treatment with telbivudine was associated with development of myopathy in 13% of cases."( Efficacy and safety of long-term therapy with nucleos(t)ide analogues in chronic hepatitis B.
Abdurakhmanov, DT; Ibragimov, EK; Moiseev, SV; Nikulkina, EN; Odintsov, AV; Panevkina, SV; Rozina, TP; Tanaschuk, EL, 2019
)
0.51
" However, less attention has been put on their adverse events."( Bayesian Network Meta-Analysis for Assessing Adverse Effects of Anti-hepatitis B Drugs.
Ji, J; Jia, Y; Shen, Y; Xun, P; Zhou, J, 2019
)
0.51
" Poisson-prior-based Bayesian NMA was performed to synthesize both direct and indirect evidence with reporting hazard ratios (HRs) and 95% credible intervals (CrIs) for serious adverse events (SAEs) and hepatic/renal impairments."( Bayesian Network Meta-Analysis for Assessing Adverse Effects of Anti-hepatitis B Drugs.
Ji, J; Jia, Y; Shen, Y; Xun, P; Zhou, J, 2019
)
0.51
"The combination of hepatitis B virus RNA and hepatitis B core-related antigen performed satisfactorily in predicting clinical relapse and hepatitis B surface antigen loss after stopping nucleos(t)ide analogue treatment among noncirrhotic hepatitis B e antigen-positive patients with chronic hepatitis B and could be used to guide safe discontinuation."( Combining Hepatitis B Virus RNA and Hepatitis B Core-Related Antigen: Guidance for Safely Stopping Nucleos(t)ide Analogues in Hepatitis B e Antigen-Positive Patients With Chronic Hepatitis B.
Bai, X; Chen, X; Fan, R; Hou, J; Niu, J; Peng, J; Ren, H; Sheng, J; Sun, J; Tan, D; Tang, H; Wang, H; Wang, M; Wu, Y; Xie, Q; Xu, M; Zhou, B, 2020
)
0.56
" In addition, the number of adverse events was significantly reduced by ETV plus Tα1, compared to ETV alone (RR = 0."( The clinical efficacy and adverse effects of Entecavir plus Thymosin alpha-1 combination therapy versus Entecavir Monotherapy in HBV-related cirrhosis: a systematic review and meta-analysis.
Chen, JH; Hou, M; Li, B; Li, C; Peng, D; Wang, XF; Xing, HY, 2020
)
0.56
"ETV plus Tα1 might lead to a higher clinical response and a lower comprehensive adverse reaction rate in HBV-related patients with cirrhosis, compared to ETV alone."( The clinical efficacy and adverse effects of Entecavir plus Thymosin alpha-1 combination therapy versus Entecavir Monotherapy in HBV-related cirrhosis: a systematic review and meta-analysis.
Chen, JH; Hou, M; Li, B; Li, C; Peng, D; Wang, XF; Xing, HY, 2020
)
0.56
" The treatment using NAs was well-tolerated and there was no serious drug-related adverse event reported."( Short-term and long-term safety and efficacy of tenofovir alafenamide, tenofovir disoproxil fumarate and entecavir treatment of acute-on-chronic liver failure associated with hepatitis B.
Chen, T; Chen, Y; Fu, M; Fu, S; Gao, Z; He, Y; Hu, C; Li, J; Liu, J; Yan, T; Yang, Y; Zhang, R; Zhao, Y; Zhou, M, 2021
)
0.62
"ETV, TDF, and TAF were safe antiviral agents and showed similar antiviral effect for CHB at 48 weeks."( Real-World Single-Center Comparison of the Safety and Efficacy of Entecavir, Tenofovir Disoproxil Fumarate, and Tenofovir Alafenamide in Patients with Chronic Hepatitis B.
Jeong, S; Kim, HI; Shin, HP, 2022
)
0.72
" The safety endpoints were the incidence of HBV virologic breakthrough and adverse events."( The efficacy and safety of tacrolimus and entecavir combination therapy in the treatment of hepatitis B virus-associated glomerulonephritis: a multi-center, placebo controlled, and single-blind randomized trial.
Hou, JH; Li, RZ; Li, ZL; Liu, DL; Xie, BY; Xie, XF; Xu, LX; Ye, ZM; Zhang, L; Zhang, WH, 2022
)
0.72
" 10 patients occurred adverse reaction, most of them were mild, and all recovered or achieved remission."( Efficacy and safety of Fuzheng Huayu tablet on persistent advanced liver fibrosis following 2 years entecavir treatment: A single arm clinical objective performance criteria trial.
Huang, JQ; Jiang, XG; Li, XD; Liang, J; Liu, CH; Liu, P; Lv, YH; Sun, KW; Xie, Q; Xing, HC; Zhang, B; Zhang, KJ; Zhang, W; Zhang, Y; Zhang, YX; Zhao, ZM; Zhu, CW; Zong, YL, 2022
)
0.72
"The combination therapy of FZHY, TCM granules and ETV could regress the liver fibrosis in the patients with HBV cirrhosis, who experienced 2 years of ETV treatment, and it is safe and well tolerated."( Efficacy and safety of Fuzheng Huayu tablet on persistent advanced liver fibrosis following 2 years entecavir treatment: A single arm clinical objective performance criteria trial.
Huang, JQ; Jiang, XG; Li, XD; Liang, J; Liu, CH; Liu, P; Lv, YH; Sun, KW; Xie, Q; Xing, HC; Zhang, B; Zhang, KJ; Zhang, W; Zhang, Y; Zhang, YX; Zhao, ZM; Zhu, CW; Zong, YL, 2022
)
0.72
"This retrospective study explored whether entecavir is effective and safe for the treatment of HBV-GN with renal insufficiency."( Efficacy and safety of entecavir for hepatitis B virus-associated glomerulonephritis with renal insufficiency.
Bu, Q; Jiang, W; Xu, L; Xu, T; Xu, Y; Yang, C; Yu, Y; Zhang, W; Zhao, L, 2023
)
0.91
" However, greater adverse effects on renal function were observed for TDF than ETV at 60 months compared to 12 months."( Renal and bone side effects of long-term use of entecavir, tenofovir disoproxil fumarate, and tenofovir alafenamide fumarate in patients with Hepatitis B: a network meta-analysis.
Liu, S; Liu, Z; Ma, X; Xin, Y; Zhao, Z, 2023
)
0.91
"Long-term administration of TDF has resulted in stronger adverse effects than TAF and ETV in regard to both renal function and bone tissue in CHB patients."( Renal and bone side effects of long-term use of entecavir, tenofovir disoproxil fumarate, and tenofovir alafenamide fumarate in patients with Hepatitis B: a network meta-analysis.
Liu, S; Liu, Z; Ma, X; Xin, Y; Zhao, Z, 2023
)
0.91

Pharmacokinetics

The absorption of entecavir from dispersible tablets was altered significantly with food intake, as evidenced by a decrease in Cm,, of 63%. The objectives were to identify significant and clinically meaningful covariate effects on entecvir population pharmacokinetic parameters.

ExcerptReferenceRelevance
" Blood and urine samples were collected for pharmacokinetic analyses."( Entecavir pharmacokinetics, safety, and tolerability after multiple ascending doses in healthy subjects.
Bifano, M; Grasela, DM; LaCreta, F; Olsen, S; Smith, RA; Yan, JH; Zhang, D, 2006
)
0.33
" Pharmacokinetic assessments were performed on days 4 and 24 for adefovir and on days 14 and 24 for entecavir."( Absence of a pharmacokinetic interaction between entecavir and adefovir.
Bifano, M; Grasela, DM; LaCreta, F; Smith, RA; Yan, JH; Zhang, D, 2007
)
0.34
" Blood samples were collected and determined for pharmacokinetic analyses."( Food effect on the pharmacokinetics of entecavir from dispersible tablets following oral administration in healthy Chinese volunteers.
Davey, AK; He, Y; Liu, F; Wang, JP; Yang, J; Zhang, QH, 2010
)
0.36
" The objectives were to identify significant and clinically meaningful covariate effects on entecavir population pharmacokinetic parameters and assess whether differences exist between Japanese and non-Japanese patients."( Pooled model-based approach to compare the pharmacokinetics of entecavir between Japanese and non-Japanese chronic hepatitis B patients.
Bifano, M; Hiraoka, M; Ishikawa, H; Pfister, M; Roy, A; Sakurai, T; Seriu, T; Yoshitsugu, H, 2011
)
0.37
"Pretreatment with glycyrrhizin resulted in no significant alterations in the main pharmacokinetic parameters of ETV in the short-term and long-term administration experiments."( Effect of diammonium glycyrrhizinate on entecavir pharmacokinetics in rats.
Hao, HP; Hao, K; Li, FY; Wang, GJ; Yan, TT, 2013
)
0.39
" The validated method was used for a pharmacokinetic study of entecavir in rats and dogs."( A validated method for quantifying entecavir in biological matrices and its application in a pharmacokinetic study in rats and dogs.
Huang, X; Jiang, ZZ; Tang, WW; Xiao, Y; Zhang, LY; Zhang, ZJ, 2013
)
0.39
"Data from recent clinical trials were used to develop a population pharmacokinetic (PPK) model, which allowed us to estimate entecavir exposures in children and compare them to ranges known to be efficacious in adults."( Using Population Pharmacokinetic and Pharmacodynamic Analyses of Entecavir in Pediatric Subjects to Simplify Dosing Recommendations.
Bertz, R; Bifano, M; Chan, P; LaCreta, F; Mould, DR; Reynolds, L; Tarif, MA, 2016
)
0.43
" The ETV-HQD group exhibited a decrease in the maximum plasma concentration (Cmax), and a delay in time to achieve Cmax (tmax) following single- and multi-dose administrations, and decreased area under the concentration- time curve (AUC0–t) following single dosing."( [Effect of Huangqi decoction on entecavir pharmacokinetics in rat plasma].
Li, YY; Liu, P; Ma, YM; Zeng, JK; Zhang, H; Zhang, XY, 2016
)
0.43

Compound-Compound Interactions

Entecavir combined with Chinese patent medicine shows superior efficiency compared with entecvir alone for the treatment of chronic HBV-related liver fibrosis.

ExcerptReferenceRelevance
"This study was designed to test the efficacy of antiviral treatment with entecavir (ETV) in combination with DNA vaccines expressing duck hepatitis B virus (DHBV) antigens as a therapy for persistent DHBV infection in ducks."( Entecavir therapy combined with DNA vaccination for persistent duck hepatitis B virus infection.
Colonno, RJ; Foster, WK; Jilbert, AR; Kotlarski, I; Marion, PL; Miller, DS, 2003
)
0.32
" These findings suggest that ETV treatment combined with post-exposure "prime-boost" vaccination induced immune responses that eliminated DHBV-infected hepatocytes and prevented the development of persistent DHBV infection."( Antiviral therapy with entecavir combined with post-exposure "prime-boost" vaccination eliminates duck hepatitis B virus-infected hepatocytes and prevents the development of persistent infection.
Boyle, D; Colonno, R; Feng, F; Jilbert, AR; Kotlarski, I; Miller, DS; Reaiche, GY, 2008
)
0.35
" We investigated the activity of clevudine (CLV) in combination with other nucleoside/nucleotide analogues to determine if these combinations were compatible in vitro."( Evaluation of the in vitro anti-HBV activity of clevudine in combination with other nucleoside/nucleotide inhibitors.
Bao, H; Furman, PA; Korba, B; Micolochick Steuer, HM; Murakami, E; Niu, C; Tolstykh, T, 2010
)
0.36
"Using the HepAD38 cell line, which expresses wild-type HBV, and a real-time PCR assay, we tested the anti-HBV activity of CLV in combination with entecavir, lamivudine, adefovir, tenofovir and telbivudine (TBV)."( Evaluation of the in vitro anti-HBV activity of clevudine in combination with other nucleoside/nucleotide inhibitors.
Bao, H; Furman, PA; Korba, B; Micolochick Steuer, HM; Murakami, E; Niu, C; Tolstykh, T, 2010
)
0.36
"When CLV was combined with entecavir, lamivudine, adefovir or tenofovir, a synergistic antiviral effect was observed; however, the combination of CLV and TBV gave an antagonistic antiviral response."( Evaluation of the in vitro anti-HBV activity of clevudine in combination with other nucleoside/nucleotide inhibitors.
Bao, H; Furman, PA; Korba, B; Micolochick Steuer, HM; Murakami, E; Niu, C; Tolstykh, T, 2010
)
0.36
"Entecavir combined with adefovir is an effective rescue therapy in CHB patients after failure of treatment with nucleoside analogs."( [Safety and efficacy of Entecavir combined with Adefovir in patients with chronic hepatitis B who fail to respond to nucleoside analog treatment].
Guo, YB; Hou, JL; Peng, J; Sun, J; Wang, ZH; Yan, L; Yang, J; Zhou, B, 2011
)
0.37
" We aimed to elucidate whether entecavir was a substrate of OAT1, OAT3, OCT, and PEPT1 and to investigate the targets of drug-drug interactions between entecavir and JBP485."( OAT1 and OAT3: targets of drug-drug interaction between entecavir and JBP485.
Kaku, T; Liu, K; Liu, Q; Ma, X; Meng, Q; Peng, J; Sun, H; Wang, C; Xu, Q, 2013
)
0.39
"Inoculation with different WHV doses had a strong influence on the course of WHV infection; NA alone or in combination with a DNA vaccine completely prevented viremia after a high dose of WHV inoculation in Chinese woodchucks and induced partial or complete protective immunity, respectively."( Nucleoside analogues alone or combined with vaccination prevent hepadnavirus viremia and induce protective immunity: alternative strategy for hepatitis B virus post-exposure prophylaxis.
Fan, W; Huang, S; Lu, M; Song, Z; Tao, Y; Wang, B; Wang, H; Wang, J; Wang, Z; Yang, D; Zhu, B; Zhu, Z, 2014
)
0.4
"NA-based PEP strategies (NA alone or in combination with vaccine) may be an alternative of HBV PEP, especially in those living in the remote and rural areas of the developing countries and the non-responders to the current vaccine, and may be valuable in the PEP of HBV and HIV co-infection after occupational and non-occupational exposure."( Nucleoside analogues alone or combined with vaccination prevent hepadnavirus viremia and induce protective immunity: alternative strategy for hepatitis B virus post-exposure prophylaxis.
Fan, W; Huang, S; Lu, M; Song, Z; Tao, Y; Wang, B; Wang, H; Wang, J; Wang, Z; Yang, D; Zhu, B; Zhu, Z, 2014
)
0.4
" The influence of furin suppression on HBV replication and the effect of CMK combined with nucleoside analog entecavir (ETV) on HBV replication and HBeAg secretion was investigated in HepG2."( Entecavir combined with furin inhibitor simultaneously reduces hepatitis B virus replication and e antigen secretion.
Gu, L; Li, DM; Peng, XM; Yang, HY; Zheng, NQ, 2014
)
0.4
" Moreover, the viral replication-enhancing effect of CMK was abrogated by ETV and ETV combined with CMK reduced HBV replication and HBeAg secretion simultaneously."( Entecavir combined with furin inhibitor simultaneously reduces hepatitis B virus replication and e antigen secretion.
Gu, L; Li, DM; Peng, XM; Yang, HY; Zheng, NQ, 2014
)
0.4
" Nucleotide/nucleoside analogs combined with furin inhibitors may be a potential easy way to realize the dual goals of the antiviral therapy for chronic hepatitis B in the future."( Entecavir combined with furin inhibitor simultaneously reduces hepatitis B virus replication and e antigen secretion.
Gu, L; Li, DM; Peng, XM; Yang, HY; Zheng, NQ, 2014
)
0.4
" This study suggests the proof-of-concept that the lower dose of NA in combination with other NA might be the theoretical option for rescue combination therapy in patients with CHB who had failed on prior multiple NA treatments in order to reduce systemic exposure and possible side effects of NA."( Comparison of the efficacies of entecavir 0.5 and 1.0 mg combined with adefovir in patients with chronic hepatitis B who had failed on prior nucleos(t)ide analogue treatments.
Cho, Y; Kim, YJ; Lee, HS; Lee, JH; Yoon, JH; Yu, SJ, 2015
)
0.42
"Infusion of two high doses of HBIG during surgery in combination with entecavir significantly prevented HBV recurrence and improved the 3-year survival after liver transplantation."( A new scheme with infusion of hepatitis B immunoglobulin combined with entecavir for prophylaxis of hepatitis B virus recurrence among liver transplant recipients.
Bai, JH; Chen, G; Gan, XM; Hu, ZQ; Li, L; Liu, H; Liu, QY; Ma, LJ; Wang, DD; Wang, F; Zhao, YP, 2015
)
0.42
" We evaluated the therapeutic efficacy of HBV-pulsed DCs in combination with the antiviral drug entecavir in patients with CHB."( Efficacy of HBV-pulsed DCs in combination with entecavir in patients with chronic hepatitis B infection.
Jiang, YL; Li, XH; Liu, XL; Pan, XN; Shen, JK; Wei, KP; Wei, MJ; Zhang, CY; Zhang, XM, 2015
)
0.42
" We determined the in vivo antiviral efficacy and effects on innate and endoplasmic reticulum (ER) stress responses of NVR3-778 alone or in combination with pegylated interferon alpha (peg-IFN) and compared with entecavir."( Efficacy of NVR 3-778, Alone and In Combination With Pegylated Interferon, vs Entecavir In uPA/SCID Mice With Humanized Livers and HBV Infection.
Allweiss, L; Dandri, M; Flores, OA; Hartman, G; Klumpp, K; Lam, AM; Lütgehetmann, M; Shimada, T; Volz, T, 2018
)
0.48
"The aim of this study was to investigate the reactivation of the hepatitis B virus (HBV) following transarterial chemoembolization (TACE) in primary hepatocellular carcinoma (HCC) patients with HBV-DNA negative and to evaluate the effects of TACE combined with antiviral therapy."( Effects of transarterial chemoembolization combined with antiviral therapy on HBV reactivation and liver function in HBV-related hepatocellular carcinoma patients with HBV-DNA negative.
Jia, Z; Jiang, G; Ni, C; Wang, K; Zhu, X, 2018
)
0.48
" However, the development of HBVr combined with NS after allo-HSCT is uncommon."( Reactivation of resolved hepatitis B virus infection combined with nephrotic syndrome in a patient after allogeneic haematopoietic stem cell transplantation.
Li, XD; Long, B; Sun, YL; Wang, XZ; Zhang, JW; Zhang, XZ, 2019
)
0.51
" However, she developed HBVr combined with nephrotic syndrome (NS) 16 months after HSCT."( Reactivation of resolved hepatitis B virus infection combined with nephrotic syndrome in a patient after allogeneic haematopoietic stem cell transplantation.
Li, XD; Long, B; Sun, YL; Wang, XZ; Zhang, JW; Zhang, XZ, 2019
)
0.51
"Entecavir combined with immunosuppression has efficacy in the treatment of HBVr combined with NS after allo-HSCT, but long course of treatment is needed."( Reactivation of resolved hepatitis B virus infection combined with nephrotic syndrome in a patient after allogeneic haematopoietic stem cell transplantation.
Li, XD; Long, B; Sun, YL; Wang, XZ; Zhang, JW; Zhang, XZ, 2019
)
0.51
"The network meta-analysis (NMA) is to evaluate whether entecavir combined with Chinese patent medicine, such as "fuzhenghuayu capsules," "anluohuaxian pills," "fufangbiejiaruangan tablets," shows superior efficiency compared with entecavir alone for the treatment of chronic HBV-related liver fibrosis or cirrhosis."( The efficacy of Chinese patent medicine combined with entecavir for the treatment of chronic HBV-related liver fibrosis or cirrhosis: Protocol for a systematic review and meta-analysis of randomized controlled trials or prospective cohort studies.
Hong, J; Huang, H; Huo, S; Song, Y; Wang, S; Zhao, J; Zuo, J, 2019
)
0.51
" We will search PubMed, EMbase, Medline, Cochrane, China Network Knowledge Infrastructure (CNKI), and Wanfang for randomized controlled trials (RCTs) or "prospective cohort studies" of "fuzhenghuayu capsules," "anluohuaxian pills," "fufangbiejiaruangan tablets" respectively combined with entecavir in the treatment of chronic HBV-related liver fibrosis or cirrhosis from their inception to September 30, 2018."( The efficacy of Chinese patent medicine combined with entecavir for the treatment of chronic HBV-related liver fibrosis or cirrhosis: Protocol for a systematic review and meta-analysis of randomized controlled trials or prospective cohort studies.
Hong, J; Huang, H; Huo, S; Song, Y; Wang, S; Zhao, J; Zuo, J, 2019
)
0.51
"To investigate the effects of radiofrequency ablation (RFA) combined with transarterial chemoembolization (TACE) and antiviral therapy on the prognosis and quality of life in primary chronic hepatitis B virus (HBV)-related liver cancer."( Effects of radiofrequency ablation combined with transarterial chemoembolization and antiviral therapy on the prognosis and quality of life in primary chronic HBV-related liver cancer.
Cheng, Y; Fan, J; Lu, B; Wang, X; Yu, L; Zhong, L; Zhu, L,
)
0.13
" The patients in the control group were treated with RFA combined with TACE, while those in the observation group were additionally treated with entecavir."( Effects of radiofrequency ablation combined with transarterial chemoembolization and antiviral therapy on the prognosis and quality of life in primary chronic HBV-related liver cancer.
Cheng, Y; Fan, J; Lu, B; Wang, X; Yu, L; Zhong, L; Zhu, L,
)
0.13
"The RFA combined with TACE and regular antiviral therapy for HBV-related liver cancer is of significance in reducing the HBV-DNA load and tumor markers, improving the liver function, promoting the overall clinical therapeutic effect and prolonging the survival of patients."( Effects of radiofrequency ablation combined with transarterial chemoembolization and antiviral therapy on the prognosis and quality of life in primary chronic HBV-related liver cancer.
Cheng, Y; Fan, J; Lu, B; Wang, X; Yu, L; Zhong, L; Zhu, L,
)
0.13
" Traditional Chinese medicine combined with antiviral therapy has become the first choice for clinical treatment of hepatitis b Cirrhosis."( Meta-analysis of influences of Biejiajian Pill combined with entecavir on serum liver fibrosis markers of compensatory period of hepatitis b cirrhosis: Protocol of systematic review and meta-analysis.
Cao, N; Feng, X; Li, G; Shi, J; Wang, B; Wang, L; Yang, Y; Zhang, T; Zheng, X, 2019
)
0.51
" Randomized controlled trials (RCTs) on Biejiajian Pill combined with Entecavir and Entecavir alone against Compensatory period of hepatitis b cirrhosis will be included; inclusion and exclusion criteria will be used to screen the trials."( Meta-analysis of influences of Biejiajian Pill combined with entecavir on serum liver fibrosis markers of compensatory period of hepatitis b cirrhosis: Protocol of systematic review and meta-analysis.
Cao, N; Feng, X; Li, G; Shi, J; Wang, B; Wang, L; Yang, Y; Zhang, T; Zheng, X, 2019
)
0.51
"This study protocol will be used to evaluate the efficacy and safety of Biejia Pill in combination with entecavir in the treatment of Compensatory period of hepatitis b cirrhosis, as well as the adjuvant treatment of Biejia Pill in combination."( Meta-analysis of influences of Biejiajian Pill combined with entecavir on serum liver fibrosis markers of compensatory period of hepatitis b cirrhosis: Protocol of systematic review and meta-analysis.
Cao, N; Feng, X; Li, G; Shi, J; Wang, B; Wang, L; Yang, Y; Zhang, T; Zheng, X, 2019
)
0.51
"Randomized controlled trials (RCTs) of KS combined with ETV for CHB will be identified from PubMed, EMBASE, Web of Science, The Cochrane Library, Chinese Biomedical Database, China National Knowledge Infrastructure, Chongqing VIP, Wangfang Data."( Kushenin combined with entecavir for chronic hepatitis B: A protocol for a systematic review and meta-analysis.
Jin, Y; Wang, Y; Xiao, X; Zhang, J; Zhang, Q, 2020
)
0.56
"A high-quality synthesis of current evidence on the efficacy and safety of KS combined with ETV for CHB will be provided in this study."( Kushenin combined with entecavir for chronic hepatitis B: A protocol for a systematic review and meta-analysis.
Jin, Y; Wang, Y; Xiao, X; Zhang, J; Zhang, Q, 2020
)
0.56
"This systematic review will aim to evaluate the efficacy and safety of KS combined with ETV for CHB."( Kushenin combined with entecavir for chronic hepatitis B: A protocol for a systematic review and meta-analysis.
Jin, Y; Wang, Y; Xiao, X; Zhang, J; Zhang, Q, 2020
)
0.56
"A 55-year-old MM patient with a family history of MM, who was also a chronic HBV carrier, achieved HBV clearance after treatment with a bortezomib-based regimen in combination with anti-HBV drugs."( Clearance of HBsAg in a patient with familial multiple myeloma after a bortezomib-based regimen combined with anti-HBV drug: A case report.
Li, X; Liang, Y; Tong, J; Wang, W; Xu, Y; Zhang, X, 2020
)
0.56
"This is the first case of MM with HBV clearance after receiving a bortezomib-based regimen combined with anti-HBV drug."( Clearance of HBsAg in a patient with familial multiple myeloma after a bortezomib-based regimen combined with anti-HBV drug: A case report.
Li, X; Liang, Y; Tong, J; Wang, W; Xu, Y; Zhang, X, 2020
)
0.56
" The present study evaluated long-term AIC649 treatment in combination with Entecavir for potency and safety in woodchucks."( Treatment with the Immunomodulator AIC649 in Combination with Entecavir Produces Antiviral Efficacy in the Woodchuck Model of Chronic Hepatitis B.
Huang, X; Kallakury, BV; Korolowicz, KE; Leng, X; Li, B; Menne, S; Suresh, M; Tucker, RD; Yon, C, 2021
)
0.62
"The objective of this study was to assess whether entecavir (ETV) in combination with interferon-α (IFN-α) could reduce hepatocellular cancer (HCC) and extrahepatic cancers (EHCs) in patients with chronic hepatitis B (CHB)."( Entecavir combined with interferon-α Is superior to entecavir monotherapy in reducing hepatic and extrahepatic cancer in patients with chronic hepatitis B.
Chen, Y; Cheng, K; Duan, X; Duan, Z; Liao, W; Sun, Y; Wang, L; Wang, X; Xu, M; Zhao, X, 2022
)
0.72
"The cohort consisted of 4194 patients with CHB treated with ETV combined with IFN-α or ETV monotherapy at a tertiary hospital in Beijing, China, from January 2009 to December 2017."( Entecavir combined with interferon-α Is superior to entecavir monotherapy in reducing hepatic and extrahepatic cancer in patients with chronic hepatitis B.
Chen, Y; Cheng, K; Duan, X; Duan, Z; Liao, W; Sun, Y; Wang, L; Wang, X; Xu, M; Zhao, X, 2022
)
0.72
"0854) were observed in the group receiving ETV combined with IFN-α in comparison with the ETV monotherapy group."( Entecavir combined with interferon-α Is superior to entecavir monotherapy in reducing hepatic and extrahepatic cancer in patients with chronic hepatitis B.
Chen, Y; Cheng, K; Duan, X; Duan, Z; Liao, W; Sun, Y; Wang, L; Wang, X; Xu, M; Zhao, X, 2022
)
0.72
"ETV combined with IFN-α therapy is superior to ETV monotherapy in reducing the risk of HCC and EHCs for patients with CHB."( Entecavir combined with interferon-α Is superior to entecavir monotherapy in reducing hepatic and extrahepatic cancer in patients with chronic hepatitis B.
Chen, Y; Cheng, K; Duan, X; Duan, Z; Liao, W; Sun, Y; Wang, L; Wang, X; Xu, M; Zhao, X, 2022
)
0.72
" Renal excretion played an important role in the elimination of Y101 and its metabolites, M8 and M9, in healthy Chinese subjects, although the molecular mechanisms of renal excretion and potential drug-drug interactions (DDIs) remain unclear."( OAT3 Participates in Drug-Drug Interaction between Bentysrepinine and Entecavir through Interactions with M8-A Metabolite of Bentysrepinine-In Rats and Humans In Vitro.
Dong, S; Fan, H; Huo, X; Li, C; Li, W; Liu, J; Peng, Y; Yang, F; Yuan, Y; Zhang, A; Zhang, N; Zheng, J; Zhou, S, 2023
)
0.91
" The aim of this study was to evaluate the effect of nucleoside analogs entecavir combined with short-term HBIG in preventing HBV recurrence after LT."( Entecavir Combined With Short-term Hepatitis B Immunoglobulin in Preventing Hepatitis B Virus Recurrence in Liver Transplant Recipients.
Guo, Y; Li, X; Liu, L; Nashan, B; Qi, C; Qin, J; Wang, J; Wang, N; Wu, W; Xu, Z; Yuan, X; Zheng, H; Zhu, Z, 2023
)
0.91
" All patients received entecavir treatment combined with HBIG for the prevention of hepatitis B recurrence, and HBIG treatment was withdrawn within 1 month."( Entecavir Combined With Short-term Hepatitis B Immunoglobulin in Preventing Hepatitis B Virus Recurrence in Liver Transplant Recipients.
Guo, Y; Li, X; Liu, L; Nashan, B; Qi, C; Qin, J; Wang, J; Wang, N; Wu, W; Xu, Z; Yuan, X; Zheng, H; Zhu, Z, 2023
)
0.91
"Entecavir combined with short-term HBIG can exert a good effect for the prevention of HBV reinfection post-LT."( Entecavir Combined With Short-term Hepatitis B Immunoglobulin in Preventing Hepatitis B Virus Recurrence in Liver Transplant Recipients.
Guo, Y; Li, X; Liu, L; Nashan, B; Qi, C; Qin, J; Wang, J; Wang, N; Wu, W; Xu, Z; Yuan, X; Zheng, H; Zhu, Z, 2023
)
0.91
"To evaluate the effects of Zhenggan Huayu decoction (, ZGHY) combined with entecavir (ETV) on the gut microbiota in patients with chronic hepatitis B (CHB) fibrosis."( Effects of Zhenggan Huayu decoction combined with entecavir on gut microbiota in patients with chronic hepatitis B fibrosis.
Daguo, Y; Fang, L; Jinzhen, LV; Wenlin, C; Yuncheng, Z, 2023
)
0.91
"A total of 59 CHB-related fibrosis patients were enrolled and treated with ZGHY combined with ETV (ZGHY + ETV) and ETV alone."( Effects of Zhenggan Huayu decoction combined with entecavir on gut microbiota in patients with chronic hepatitis B fibrosis.
Daguo, Y; Fang, L; Jinzhen, LV; Wenlin, C; Yuncheng, Z, 2023
)
0.91

Bioavailability

ExcerptReferenceRelevance
" The lead candidates, both 1a (PBHBV-001) and 3c (PBHBV-2-15), were well-tolerated in both normal and HBV-transgenic mice and exhibited acceptable pharmacokinetics and bioavailability in Sprague-Dawley rats."( Design, synthesis, and biological evaluation of triazolo-pyrimidine derivatives as novel inhibitors of hepatitis B virus surface antigen (HBsAg) secretion.
Block, TM; Clearfield, E; Cuconati, A; Goddard, C; Guo, H; Mills, C; Morrey, JD; Motter, NE; Xiao, T; Xu, X; Yu, W; Zhao, K, 2011
)
0.37
" In particular, the (2S,4S)-4,4-difluoroproline substituted analogue 34a demonstrated high oral bioavailability and liver exposure and achieved over 2 log viral load reduction in a hydrodynamic injected (HDI) HBV mouse model."( Design and Synthesis of Orally Bioavailable 4-Methyl Heteroaryldihydropyrimidine Based Hepatitis B Virus (HBV) Capsid Inhibitors.
Chen, W; Guo, L; Huang, M; Jiang, M; Lin, X; Liu, H; Liu, Y; Mao, Y; Mayweg, AV; Qin, N; Qiu, H; Qiu, Z; Ren, S; Shen, F; Shen, HC; Shi, L; Tang, G; Wu, G; Wu, JZ; Wu, X; Xu, Z; Yang, G; Yang, W; Zhang, W; Zhang, Y; Zhong, S; Zhou, M; Zhou, X; Zhou, Z; Zhu, W, 2016
)
0.43
"SB 9200, an orally bioavailable dinucleotide, activates the viral sensor proteins, retinoic acid-inducible gene 1 (RIG-I) and nucleotide-binding oligomerization domain-containing protein 2 (NOD2) causing the induction of the interferon (IFN) signaling cascade for antiviral defense."( Antiviral Efficacy and Host Immune Response Induction during Sequential Treatment with SB 9200 Followed by Entecavir in Woodchucks.
Afdhal, N; Balarezo, M; Cleary, D; Gimi, R; Iyer, RP; Kallakury, BV; Korolowicz, KE; Menne, S; Padmanabhan, S; Sheri, A; Suresh, M; Tucker, RD; Yon, C, 2017
)
0.46
" In particular, it demonstrated a good systemic exposure and high oral bioavailability and achieved a viral-load reduction greater than 2 log in a hydrodynamic-injected (HDI) HBV mouse model and has now been selected for further development."( 3-((R)-4-(((R)-6-(2-Bromo-4-fluorophenyl)-5-(ethoxycarbonyl)-2-(thiazol-2-yl)-3,6-dihydropyrimidin-4-yl)methyl)morpholin-2-yl)propanoic Acid (HEC72702), a Novel Hepatitis B Virus Capsid Inhibitor Based on Clinical Candidate GLS4.
Chen, Y; Goldmann, S; Gu, B; Huang, J; Li, J; Liu, X; Luo, Z; Nie, B; Ren, Q; Wei, Y; Yan, G; Zhang, J; Zhang, Y; Zou, Z, 2018
)
0.48
" The absorption rate and extent of EV after SC injection of 12."( Design and in vivo evaluation of entecavir-3-palmitate microcrystals for subcutaneous sustained delivery.
Choi, YW; Han, YT; Ho, MJ; Im, SH; Jang, SW; Kang, MJ; Kim, HJ; Lee, DR; Shin, CY; Yoon, JA, 2018
)
0.48
" RG7834, a compound from the dihydroquinolizinone (DHQ) chemical series, is a first-in-class highly selective and orally bioavailable HBV inhibitor which can reduce both viral antigens and viral DNA with a novel mechanism of action."( Discovery of RG7834: The First-in-Class Selective and Orally Available Small Molecule Hepatitis B Virus Expression Inhibitor with Novel Mechanism of Action.
Cheng, Z; Han, X; Javanbakht, H; Jiang, M; Liang, C; Liu, Y; Luangsay, S; Lv, W; Mayweg, AV; Shen, HC; Wang, J; Wang, M; Wang, Y; Wang, Z; Weikert, R; Xie, J; Yang, S; Yu, X; Zhou, C; Zhou, X, 2018
)
0.48
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
"Cell membrane permeability is an important determinant for oral absorption and bioavailability of a drug molecule."( Highly predictive and interpretable models for PAMPA permeability.
Jadhav, A; Kerns, E; Nguyen, K; Shah, P; Sun, H; Xu, X; Yan, Z; Yu, KR, 2017
)
0.46
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

Entecavir (ETV) dosage in patients with chronic hepatitis B (CHB) who partially responded to ETV after 1 year. Treatment of patients with lamivudine failure requires a higher dosage of entecvir. The higher doses showed significantly greater viral suppression.

ExcerptRelevanceReference
" A clear dose-response relationship was observed for entecavir with the higher doses showing significantly greater viral suppression."( Entecavir is superior to lamivudine in reducing hepatitis B virus DNA in patients with chronic hepatitis B infection.
Anderson, FH; Dehertogh, D; Lai, CL; Lao, J; Rosmawati, M; Thomas, N; Van Vlierberghe, H, 2002
)
0.31
" Preemptive post-transplant lamivudine monotherapy is associated with progressively increasing HBV recurrence rates, but combined therapy with lamivudine and HBIG at relatively low dosage is currently the most effective approach in this setting, even in HBV-DNA-positive patients, who also receive lamivudine in the pretransplant period."( Prevention of and treatment for hepatitis B virus infection after liver transplantation in the nucleoside analogues era.
Burroughs, AK; Papatheodoridis, GV; Sevastianos, V, 2003
)
0.32
"5 mg as a better dosage for a further large scale clinical trial."( [A study of the dosage and efficacy of entecavir for treating hepatitis B virus].
Lei, BJ; Wang, BE; Xu, DZ; Yao, GB; Zhang, DF; Zhou, XQ, 2005
)
0.33
" There were no clinically meaningful differences in the incidence of any adverse events between the entecavir dosing and the placebo groups."( [A study of the dosage and efficacy of entecavir for treating hepatitis B virus].
Lei, BJ; Wang, BE; Xu, DZ; Yao, GB; Zhang, DF; Zhou, XQ, 2005
)
0.33
" Treatment of patients with lamivudine failure requires a higher dosage of entecavir and induces a significant decline in viraemia levels."( Entecavir: a new treatment option for chronic hepatitis B.
Zoulim, F, 2006
)
0.33
" At steady state, the mean area under the plasma concentration-time curve over 1 dosing interval, increased approximately proportional to dose."( Entecavir pharmacokinetics, safety, and tolerability after multiple ascending doses in healthy subjects.
Bifano, M; Grasela, DM; LaCreta, F; Olsen, S; Smith, RA; Yan, JH; Zhang, D, 2006
)
0.33
" Genotyping all additional ETV patients with PCR-detectable HBV DNA at Weeks 48, 96, or end of dosing identified seven additional patients with LVDr substitutions, including one with simultaneous emergence of LVDr/ETVr."( Entecavir resistance is rare in nucleoside naïve patients with hepatitis B.
Baldick, CJ; Colonno, RJ; Eggers, B; Fang, J; Hsu, M; Klesczewski, K; Levine, S; Mazzucco, C; Plym, M; Pokornowski, K; Rose, R; Tenney, DJ; Walsh, A; Yu, CF; Zhang, S, 2006
)
0.33
"5 mg and 1 mg, respectively, with 33% of patients in each dosing group achieving <400 copies/mL."( Efficacy and safety of entecavir in lamivudine-refractory patients with chronic hepatitis B: randomized controlled trial in Japanese patients.
Imazeki, F; Kage, M; Katano, Y; Kumada, H; Moriyama, M; Omata, M; Sata, M; Seriu, T; Suzuki, F; Toyoda, J, 2008
)
0.35
" To attain a better antiviral response the dosage of entecavir was increased to 2mg daily in two patients, resulting in further viral load decline for both of them."( Entecavir shows limited efficacy in HBeAg-positive hepatitis B patients with a partial virologic response to adefovir therapy.
de Man, RA; Janssen, HL; Pas, SD; Reijnders, JG; Schutten, M, 2009
)
0.35
"Entecavir monotherapy dosed at 1mg resulted in a slow reduction of viral load in both lamivudine-experienced and -naïve patients with persistently high HBV DNA during adefovir therapy."( Entecavir shows limited efficacy in HBeAg-positive hepatitis B patients with a partial virologic response to adefovir therapy.
de Man, RA; Janssen, HL; Pas, SD; Reijnders, JG; Schutten, M, 2009
)
0.35
" Developing optimal treatment regimens requires understanding how to best measure anti-HIV activity in vitro and how drug dose-response curves generated in vitro correlate with in-vivo efficacy."( New approaches for quantitating the inhibition of HIV-1 replication by antiviral drugs in vitro and in vivo.
McMahon, MA; Shen, L; Siliciano, RF, 2009
)
0.35
" Recent studies using a single-round infectivity assay have shown that a previously neglected parameter, the dose-response curve slope, is an extremely important determinant of antiviral activity."( New approaches for quantitating the inhibition of HIV-1 replication by antiviral drugs in vitro and in vivo.
McMahon, MA; Shen, L; Siliciano, RF, 2009
)
0.35
"5 mg orally, daily) or lamivudine (100 mg orally, daily) together with a long-term low dosage of HBIG to prevent hepatitis B recurrence after transplantation."( The role of entecavir in preventing hepatitis B recurrence after liver transplantation.
Chen, XS; Han, LZ; Luo, Y; Qiu, DK; Shen, CH; Wang, SY; Wang, X; Xi, ZF; Xia, Q; Xin, TY; Zhang, JJ, 2009
)
0.35
"An RP-HPLC method was validated for the determination of entecavir in tablet dosage form."( Validation of a stability-indicating RP-HPLC method for the determination of entecavir in tablet dosage form.
da Silva, LM; Dalmora, SL; Nogueira, DR; Sangoi, Mda S,
)
0.13
"9999), and was applied for the analysis of entecavir in tablet dosage forms."( Development and validation of a stability-indicating capillary zone electrophoretic method for the assessment of entecavir and its correlation with liquid chromatographic methods.
D'Avila, FB; Dalmora, SL; Leal, DP; Nogueira, DR; Souto, RB, 2011
)
0.37
" Entecavir provides sustained viral suppression and histological benefit with minimal resistance during long-term treatment of chronic hepatitis B, it is well-tolerable and has good safety profile, simple dosing and simple monitoring requirements."( [Long-term therapy with nucleoside analog entecavir (baraclude) in patients with chronic hepatitis B].
Halota, W; Pawłowska, M, 2011
)
0.37
" Entecavir was given at a dosage of 1 mg/d for 1 year."( Entecavir treatment of chronic hepatitis D.
Bozdayi, AM; Idilman, R; Kabaçam, G; Karatayli, E; Karatayli, SC; Onder, FO; Savas, B; Seven, G; Yakut, M; Yurdaydin, C, 2012
)
0.38
"NAs are cleared by kidneys and their dosage should be adjusted in patients with creatinine clearance <50 mL/min."( Review article: nucleos(t)ide analogues in patients with chronic hepatitis B virus infection and chronic kidney disease.
Cholongitas, E; Papatheodoridis, G; Pipili, C, 2014
)
0.4
" Antiviral treatments were withdrawn in patients who met all of the following 7 criteria: (i) no clinical and histologic evidence of cirrhosis, (ii) normal liver biochemistry, (iii) negative for both HBV DNA and hepatitis B envelope antigen (HBeAg), (iv) no resistance to antiviral agent, (v) antiviral therapy > 9 months, (vi) maintenance dosage of immunosuppressant for > 3 months, and (vii) no history of acute rejection during recent 6 months."( Successful withdrawal of antiviral treatment in kidney transplant recipients with chronic hepatitis B viral infection.
Cho, JH; Choi, JY; Huh, S; Kang, YJ; Kim, CD; Kim, HK; Kim, JS; Kim, YL; Kwon, O; Lim, JH; Park, GY; Park, SH, 2014
)
0.4
"To analyze the effect of increasing Entecavir (ETV) dosage in patients with chronic hepatitis B (CHB) who partially responded to ETV after 1 year."( Is increasing the dose of Entecavir effective in partial virological responders?
Akdogan, RA; Cumhur Cure, M; Cure, E; Erturk, A; Ozturk, C; Parlak, E, 2014
)
0.4
"Using non-linear regression models, dose-response curves of cloned HBV strains from patients pre-treated with RT inhibitors were established in human hepatoma cell lines after transfection with HBV genomes containing HBV polymerase genes from patient isolates."( Entecavir allows an unexpectedly high residual replication of HBV mutants resistant to lamivudine.
Geipel, A; Gerlich, WH; Glebe, D; Kaiser, R; Neumann-Fraune, M; Niekamp, H; Protzer, U; Seiz, PL; Zhang, K, 2015
)
0.42
"The entecavir dose-response curve of lamivudine-resistant HBV RT mutants rtM204 for the replication of HBV decreased less than expected with increasing drug dose."( Entecavir allows an unexpectedly high residual replication of HBV mutants resistant to lamivudine.
Geipel, A; Gerlich, WH; Glebe, D; Kaiser, R; Neumann-Fraune, M; Niekamp, H; Protzer, U; Seiz, PL; Zhang, K, 2015
)
0.42
"Multidrug resistance protein 4 is a critical protein associated with the antiviral efficacy of NAs, and combination therapy of NA and MRP inhibitors could reduce the dosage for long-term NA use."( Multidrug resistance protein 4 is a critical protein associated with the antiviral efficacy of nucleos(t)ide analogues.
Chen, Q; Liu, W; Liu, Y; Lu, M; Song, H; Wang, B; Xu, C; Xu, D; Yang, D; Zhang, W; Zheng, X, 2016
)
0.43
"To develop simplified entecavir dosing recommendations for young children infected with CHB."( Using Population Pharmacokinetic and Pharmacodynamic Analyses of Entecavir in Pediatric Subjects to Simplify Dosing Recommendations.
Bertz, R; Bifano, M; Chan, P; LaCreta, F; Mould, DR; Reynolds, L; Tarif, MA, 2016
)
0.43
"Model-estimated, steady-state entecavir area under the concentration-time curve, in both the original (15 weight groups) and simplified (eight weight groups) pediatric dosing regimens, provided entecavir exposures consistent with those observed to be efficacious in adults, and resulted in the simplified dose algorithm for pediatric patients that is approved for the current entecavir label."( Using Population Pharmacokinetic and Pharmacodynamic Analyses of Entecavir in Pediatric Subjects to Simplify Dosing Recommendations.
Bertz, R; Bifano, M; Chan, P; LaCreta, F; Mould, DR; Reynolds, L; Tarif, MA, 2016
)
0.43
" The virologic response was determined by the dosage of serum HBV-DNA, HBsAg, HBeAg, anti-HBs and anti-HBe antibodies."( Efficacy and safety of long-term entecavir therapy in a European population.
Belci, P; Collo, A; Durazzo, M; Fagoonee, S; Gariglio, V; Loreti, L; Magistroni, P; Parise, R, 2018
)
0.48
" The dose-response analyses of adherence rates showed that the risk of LREs increased progressively as medication adherence declined."( Medication Nonadherence Increases Hepatocellular Carcinoma, Cirrhotic Complications, and Mortality in Chronic Hepatitis B Patients Treated With Entecavir.
Jung, SW; Lee, BU; Lee, SB; Park, BR; Park, EJ; Park, NH; Shin, JW, 2018
)
0.48
" The sirolimus dosage was increased to 2 mg daily without causing HBV reactivation."( Successful Sirolimus Treatment of Lymphangioleiomyomatosis in a Hepatitis B Virus Carrier.
Akira, M; Arai, T; Hirose, M; Inoue, Y; Kasai, T; Kitaichi, M; Sonobe, S; Sugimoto, C; Tanimoto, Y, 2019
)
0.51
" The concentration of ETV in the liver was not obviously altered during pregnancy, which indicates that dosage adjustment in pregnancy is not necessary."( Roles of organic anion transporter 2 and equilibrative nucleoside transporter 1 in hepatic disposition and antiviral activity of entecavir during non-pregnancy and pregnancy.
Bai, M; Jiang, H; Jiang, T; Lin, N; Lu, S; Ma, Z; Sun, D; Zeng, S; Zhou, H, 2019
)
0.51
" Because 70% of orally dosed ETV is eliminated by kidney, the effects of estradiol (E2) and progesterone (P4), 2 important hormones during pregnancy, on ETV-related renal transporters were investigated."( Pregnancy Impacts Entecavir Pharmacokinetics but Does Not Alter Its Renal Excretion.
Jiang, H; Jiang, T; Lin, N; Lu, S; Ma, Z; Wang, W; Yang, X; Zeng, S; Zhou, H, 2020
)
0.56
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitorA DNA polymerase inhibitor that interferes with the activity of reverse transcriptase, EC 2.7.7.49, a viral DNA polymerase enzyme that retroviruses need in order to reproduce.
antiviral drugA substance used in the prophylaxis or therapy of virus diseases.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (6)

ClassDescription
2-aminopurinesAny aminopurine having the amino substituent at the 2-position.
oxopurine
primary alcoholA primary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has either three hydrogen atoms attached to it or only one other carbon atom and two hydrogen atoms attached to it.
secondary alcoholA secondary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has two other carbon atoms attached to it.
benzamides
N-acylpiperidine
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (25)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
TDP1 proteinHomo sapiens (human)Potency0.00680.000811.382244.6684AID686978; AID686979
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.81070.009610.525035.4813AID1479145
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency26.83700.01237.983543.2770AID1645841
EWS/FLI fusion proteinHomo sapiens (human)Potency12.90070.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
cytochrome P450 2D6Homo sapiens (human)Potency37.90830.00108.379861.1304AID1645840
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)133.00000.11007.190310.0000AID1473738
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki0.07200.00000.690210.0000AID1915119
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki0.40000.00000.79519.1201AID1915121
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC50 (µMol)3.50000.00001.403910.0000AID771606
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki0.09700.00000.59729.1201AID1915118
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.86000.00030.483410.0000AID1915123
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki0.89000.00000.54057.7600AID1915120
Lysine-specific demethylase 5AHomo sapiens (human)IC50 (µMol)20.00000.13002.374710.0000AID1077871; AID771611
MBT domain-containing protein 1Homo sapiens (human)IC50 (µMol)43.50009.00009.00009.0000AID1077875; AID771615
Lethal(3)malignant brain tumor-like protein 3Homo sapiens (human)IC50 (µMol)0.13540.02401.40964.7000AID1077877; AID1912836; AID1913327; AID771620; AID771621
Lethal(3)malignant brain tumor-like protein 1Homo sapiens (human)IC50 (µMol)5.60000.09804.29968.9000AID1077876; AID771619
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Capsid protein Hepatitis B virusEC50 (µMol)5.00010.00020.26030.8194AID1363957; AID1377846
Lethal(3)malignant brain tumor-like protein 3Homo sapiens (human)Kd0.12000.12000.12000.1200AID1578927; AID1915126; AID771609
Lethal(3)malignant brain tumor-like protein 1Homo sapiens (human)Kd9.40005.00008.133310.0000AID771608
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (139)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIChromobox protein homolog 7Homo sapiens (human)
chromatin organizationChromobox protein homolog 7Homo sapiens (human)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M2Homo sapiens (human)
regulation of heart contractionMuscarinic acetylcholine receptor M2Homo sapiens (human)
response to virusMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
presynaptic modulation of chemical synaptic transmissionMuscarinic acetylcholine receptor M2Homo sapiens (human)
regulation of smooth muscle contractionMuscarinic acetylcholine receptor M2Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M2Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M2Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M4Homo sapiens (human)
cell surface receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
regulation of locomotionMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M4Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M4Homo sapiens (human)
positive regulation of monoatomic ion transportMuscarinic acetylcholine receptor M1Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
neuromuscular synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of locomotionMuscarinic acetylcholine receptor M1Homo sapiens (human)
saliva secretionMuscarinic acetylcholine receptor M1Homo sapiens (human)
cognitionMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of postsynaptic membrane potentialMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of glial cell proliferationMuscarinic acetylcholine receptor M1Homo sapiens (human)
positive regulation of intracellular protein transportMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of smooth muscle contractionAlpha-2C adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2C adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2C adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2C adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2C adrenergic receptorHomo sapiens (human)
calcium-mediated signalingMuscarinic acetylcholine receptor M3Homo sapiens (human)
regulation of monoatomic ion transmembrane transporter activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
smooth muscle contractionMuscarinic acetylcholine receptor M3Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
synaptic transmission, cholinergicMuscarinic acetylcholine receptor M3Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M3Homo sapiens (human)
positive regulation of insulin secretionMuscarinic acetylcholine receptor M3Homo sapiens (human)
protein modification processMuscarinic acetylcholine receptor M3Homo sapiens (human)
positive regulation of smooth muscle contractionMuscarinic acetylcholine receptor M3Homo sapiens (human)
saliva secretionMuscarinic acetylcholine receptor M3Homo sapiens (human)
acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
ion channel modulating, G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
ligand-gated ion channel signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
regulation of smooth muscle contractionMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M3Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M3Homo sapiens (human)
negative regulation of transcription by RNA polymerase IILysine-specific demethylase 5AHomo sapiens (human)
circadian regulation of gene expressionLysine-specific demethylase 5AHomo sapiens (human)
positive regulation of DNA-templated transcriptionLysine-specific demethylase 5AHomo sapiens (human)
regulation of DNA-binding transcription factor activityLysine-specific demethylase 5AHomo sapiens (human)
facultative heterochromatin formationLysine-specific demethylase 5AHomo sapiens (human)
regulation of DNA-templated transcriptionLysine-specific demethylase 5AHomo sapiens (human)
chromatin remodelingLysine-specific demethylase 5AHomo sapiens (human)
double-strand break repair via homologous recombinationMBT domain-containing protein 1Homo sapiens (human)
chromatin organizationMBT domain-containing protein 1Homo sapiens (human)
regulation of apoptotic processMBT domain-containing protein 1Homo sapiens (human)
positive regulation of DNA-templated transcriptionMBT domain-containing protein 1Homo sapiens (human)
embryonic skeletal system developmentMBT domain-containing protein 1Homo sapiens (human)
regulation of cell cycleMBT domain-containing protein 1Homo sapiens (human)
positive regulation of double-strand break repair via homologous recombinationMBT domain-containing protein 1Homo sapiens (human)
regulation of double-strand break repairMBT domain-containing protein 1Homo sapiens (human)
negative regulation of DNA-templated transcriptionMBT domain-containing protein 1Homo sapiens (human)
DNA damage responseTP53-binding protein 1Homo sapiens (human)
double-strand break repair via nonhomologous end joiningTP53-binding protein 1Homo sapiens (human)
chromatin organizationTP53-binding protein 1Homo sapiens (human)
DNA damage responseTP53-binding protein 1Homo sapiens (human)
positive regulation of isotype switchingTP53-binding protein 1Homo sapiens (human)
positive regulation of DNA-templated transcriptionTP53-binding protein 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IITP53-binding protein 1Homo sapiens (human)
positive regulation of DNA-binding transcription factor activityTP53-binding protein 1Homo sapiens (human)
protein homooligomerizationTP53-binding protein 1Homo sapiens (human)
cellular response to X-rayTP53-binding protein 1Homo sapiens (human)
double-strand break repair via classical nonhomologous end joiningTP53-binding protein 1Homo sapiens (human)
protein localization to site of double-strand breakTP53-binding protein 1Homo sapiens (human)
negative regulation of double-strand break repair via homologous recombinationTP53-binding protein 1Homo sapiens (human)
DNA damage checkpoint signalingTP53-binding protein 1Homo sapiens (human)
chromatin organizationLethal(3)malignant brain tumor-like protein 4Homo sapiens (human)
negative regulation of DNA-templated transcriptionLethal(3)malignant brain tumor-like protein 4Homo sapiens (human)
chromatin organizationLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
macrophage differentiationLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
granulocyte differentiationLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
erythrocyte maturationLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
negative regulation of DNA-templated transcriptionLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
regulation of DNA methylation-dependent heterochromatin formationLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
positive regulation of ubiquitin-dependent protein catabolic processLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
double-strand break repair via homologous recombinationE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
ubiquitin-dependent protein catabolic processE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
DNA damage responseE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
heterochromatin formationE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
homologous recombinationE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
epigenetic regulation of gene expressionE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
negative regulation of gene expression via chromosomal CpG island methylationE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
regulation of epithelial cell proliferationE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
positive regulation of protein metabolic processE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
protein autoubiquitinationE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
mitotic spindle assemblyE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
positive regulation of DNA topoisomerase (ATP-hydrolyzing) activityE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
protein ubiquitinationE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
autophagyPHD finger protein 23Homo sapiens (human)
positive regulation of protein ubiquitinationPHD finger protein 23Homo sapiens (human)
negative regulation of autophagosome maturationPHD finger protein 23Homo sapiens (human)
negative regulation of autophagosome assemblyPHD finger protein 23Homo sapiens (human)
chromatin organizationScm-like with four MBT domains protein 1Homo sapiens (human)
spermatogenesisScm-like with four MBT domains protein 1Homo sapiens (human)
cell differentiationScm-like with four MBT domains protein 1Homo sapiens (human)
negative regulation of DNA-templated transcriptionScm-like with four MBT domains protein 1Homo sapiens (human)
negative regulation of muscle organ developmentScm-like with four MBT domains protein 1Homo sapiens (human)
chromatin organizationLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
regulation of mitotic nuclear divisionLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
hemopoiesisLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
heterochromatin formationLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
regulation of megakaryocyte differentiationLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
negative regulation of DNA-templated transcriptionLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
regulation of cell cycleLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (70)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
protein bindingChromobox protein homolog 7Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M2Homo sapiens (human)
arrestin family protein bindingMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M4Homo sapiens (human)
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2C adrenergic receptorHomo sapiens (human)
alpha-2A adrenergic receptor bindingAlpha-2C adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2C adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2C adrenergic receptorHomo sapiens (human)
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
signaling receptor activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
acetylcholine bindingMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
transcription cis-regulatory region bindingLysine-specific demethylase 5AHomo sapiens (human)
DNA bindingLysine-specific demethylase 5AHomo sapiens (human)
transcription coactivator activityLysine-specific demethylase 5AHomo sapiens (human)
enzyme inhibitor activityLysine-specific demethylase 5AHomo sapiens (human)
protein bindingLysine-specific demethylase 5AHomo sapiens (human)
zinc ion bindingLysine-specific demethylase 5AHomo sapiens (human)
chromatin DNA bindingLysine-specific demethylase 5AHomo sapiens (human)
histone demethylase activityLysine-specific demethylase 5AHomo sapiens (human)
histone H3K4me/H3K4me2/H3K4me3 demethylase activityLysine-specific demethylase 5AHomo sapiens (human)
methylated histone bindingLysine-specific demethylase 5AHomo sapiens (human)
histone bindingLysine-specific demethylase 5AHomo sapiens (human)
protein bindingMBT domain-containing protein 1Homo sapiens (human)
zinc ion bindingMBT domain-containing protein 1Homo sapiens (human)
methylated histone bindingMBT domain-containing protein 1Homo sapiens (human)
NuA4 histone acetyltransferase complex bindingMBT domain-containing protein 1Homo sapiens (human)
chromatin bindingMBT domain-containing protein 1Homo sapiens (human)
p53 bindingTP53-binding protein 1Homo sapiens (human)
damaged DNA bindingTP53-binding protein 1Homo sapiens (human)
transcription coregulator activityTP53-binding protein 1Homo sapiens (human)
protein bindingTP53-binding protein 1Homo sapiens (human)
methylated histone bindingTP53-binding protein 1Homo sapiens (human)
telomeric DNA bindingTP53-binding protein 1Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingTP53-binding protein 1Homo sapiens (human)
ubiquitin-modified histone reader activityTP53-binding protein 1Homo sapiens (human)
histone reader activityTP53-binding protein 1Homo sapiens (human)
histone bindingTP53-binding protein 1Homo sapiens (human)
protein bindingLethal(3)malignant brain tumor-like protein 4Homo sapiens (human)
zinc ion bindingLethal(3)malignant brain tumor-like protein 4Homo sapiens (human)
histone bindingLethal(3)malignant brain tumor-like protein 4Homo sapiens (human)
chromatin bindingLethal(3)malignant brain tumor-like protein 4Homo sapiens (human)
chromatin bindingLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
protein bindingLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
zinc ion bindingLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
identical protein bindingLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
methylation-dependent protein bindingLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
histone bindingLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
nucleic acid bindingE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
ubiquitin-protein transferase activityE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
protein bindingE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
zinc ion bindingE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
methyl-CpG bindingE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
methylated histone bindingE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
histone bindingE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
identical protein bindingE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
hemi-methylated DNA-bindingE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
ubiquitin protein ligase activityE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
H3K9me3 modified histone bindingE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
DNA damage sensor activityE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
histone H3 ubiquitin ligase activityE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
protein bindingPHD finger protein 23Homo sapiens (human)
metal ion bindingPHD finger protein 23Homo sapiens (human)
transcription corepressor activityScm-like with four MBT domains protein 1Homo sapiens (human)
protein bindingScm-like with four MBT domains protein 1Homo sapiens (human)
histone bindingScm-like with four MBT domains protein 1Homo sapiens (human)
chromatin bindingScm-like with four MBT domains protein 1Homo sapiens (human)
chromatin bindingLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
protein bindingLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
zinc ion bindingLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
nucleosome bindingLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
SAM domain bindingLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
methylated histone bindingLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
histone bindingLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
identical protein bindingLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (53)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
nucleusChromobox protein homolog 7Homo sapiens (human)
nucleoplasmChromobox protein homolog 7Homo sapiens (human)
cytosolChromobox protein homolog 7Homo sapiens (human)
chromatinChromobox protein homolog 7Homo sapiens (human)
PcG protein complexChromobox protein homolog 7Homo sapiens (human)
PRC1 complexChromobox protein homolog 7Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
clathrin-coated endocytic vesicle membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
asymmetric synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
symmetric synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
presynaptic membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
neuronal cell bodyMuscarinic acetylcholine receptor M2Homo sapiens (human)
axon terminusMuscarinic acetylcholine receptor M2Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
glutamatergic synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
cholinergic synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M2Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M4Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M4Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M4Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M4Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M4Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
presynaptic membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
axon terminusMuscarinic acetylcholine receptor M1Homo sapiens (human)
Schaffer collateral - CA1 synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
postsynaptic density membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
glutamatergic synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
cholinergic synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M1Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
cytoplasmAlpha-2C adrenergic receptorHomo sapiens (human)
endosomeAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
endoplasmic reticulum membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
basal plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
basolateral plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M3Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M3Homo sapiens (human)
nucleusLysine-specific demethylase 5AHomo sapiens (human)
nucleoplasmLysine-specific demethylase 5AHomo sapiens (human)
nucleolusLysine-specific demethylase 5AHomo sapiens (human)
nucleusLysine-specific demethylase 5AHomo sapiens (human)
chromatinLysine-specific demethylase 5AHomo sapiens (human)
site of double-strand breakMBT domain-containing protein 1Homo sapiens (human)
nucleosomeMBT domain-containing protein 1Homo sapiens (human)
NuA4 histone acetyltransferase complexMBT domain-containing protein 1Homo sapiens (human)
nucleusMBT domain-containing protein 1Homo sapiens (human)
chromosome, telomeric regionTP53-binding protein 1Homo sapiens (human)
site of double-strand breakTP53-binding protein 1Homo sapiens (human)
kinetochoreTP53-binding protein 1Homo sapiens (human)
nucleusTP53-binding protein 1Homo sapiens (human)
nucleoplasmTP53-binding protein 1Homo sapiens (human)
replication forkTP53-binding protein 1Homo sapiens (human)
cytoplasmTP53-binding protein 1Homo sapiens (human)
nuclear bodyTP53-binding protein 1Homo sapiens (human)
site of double-strand breakTP53-binding protein 1Homo sapiens (human)
DNA repair complexTP53-binding protein 1Homo sapiens (human)
nucleusTP53-binding protein 1Homo sapiens (human)
nucleusLethal(3)malignant brain tumor-like protein 4Homo sapiens (human)
nucleusLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
nucleoplasmLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
nucleolusLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
spindleE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
nucleusE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
nucleoplasmE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
replication forkE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
nuclear matrixE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
chromatinE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
euchromatinE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
heterochromatinE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
nucleoplasmPHD finger protein 23Homo sapiens (human)
cytoplasmPHD finger protein 23Homo sapiens (human)
nucleusPHD finger protein 23Homo sapiens (human)
nucleusScm-like with four MBT domains protein 1Homo sapiens (human)
nucleoplasmScm-like with four MBT domains protein 1Homo sapiens (human)
nucleusScm-like with four MBT domains protein 1Homo sapiens (human)
nucleolusLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
condensed chromosomeLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
nucleusLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
nucleoplasmLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
chromatin lock complexLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
chromatinLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
nucleusLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (354)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID519968Antiviral activity against HIV1 NL4-3 harboring M184L mutant RT infected in human MT2 cellssmeasured after 7 passages on day 34 postinfection2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID525238Toxicity in HBeAg-positive chronic hepatitis B patient assessed as nausea at 0.5 mg/day2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B.
AID322841Antiviral activity against Lamivudine -adenofir-resistant HBV with reverse transcriptase V173L/L180M/A181V/M204V/N236T mutant2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activity of 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]-pyrimidine against multidrug-resistant hepatitis B virus mutants.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID519876Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1693340Antiviral activity against wild type HBV infected in human HepG2 2.2.15 cells assessed as inhibition of viral DNA replication at 10 uM measured after incubation of 72 hrs by RT-PCR analysis relative to control2021Bioorganic & medicinal chemistry, 01-01, Volume: 29Synthesis and evaluation of new phenyl acrylamide derivatives as potent non-nucleoside anti-HBV agents.
AID322839Antiviral activity against lamivudine-adenofir-resistant HBV with reverse transcriptase V173L/L180M/A181V mutant2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activity of 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]-pyrimidine against multidrug-resistant hepatitis B virus mutants.
AID1859028Antiviral activity against HBV infected in human HepDES19 cells assessed as effect on levels of intracellular core protein 1 uM measured by Western blot assay2022Bioorganic & medicinal chemistry letters, 02-15, Volume: 584-Oxooctahydroquinoline-1(2H)-carboxamides as hepatitis B virus (HBV) capsid core protein assembly modulators.
AID322831Fold resistance, ratio of EC50 for adenofir-resistant HBV with reverse transcriptase N236T mutant to EC50 for wild-type HBV2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activity of 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]-pyrimidine against multidrug-resistant hepatitis B virus mutants.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID283270Inhibition of HBV replication with RT L228P substitution and M204I background from Lamivudine refractory patient transfected into HepG2 cells2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Two-year assessment of entecavir resistance in Lamivudine-refractory hepatitis B virus patients reveals different clinical outcomes depending on the resistance substitutions present.
AID1694161Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by MTT assay2021Bioorganic & medicinal chemistry, 02-01, Volume: 31Discovery and structure activity relationship of glyoxamide derivatives as anti-hepatitis B virus agents.
AID322845Fold resistance, ratio of lamivudine-resistant HBV with reverse transcriptase L180M/A181V mutant to wild-type HBV genotype E2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activity of 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]-pyrimidine against multidrug-resistant hepatitis B virus mutants.
AID1533172Cytotoxicity against human HepG2.2.15 cells after 7 days by MTT assay2018ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12
Synthesis, Anti-HBV, and Anti-HIV Activities of 3'-Halogenated Bis(hydroxymethyl)-cyclopentenyladenines.
AID1617348Antiviral activity against HBV infected in BALB/c mouse hydrodynamic injection model hydrodynamically injected with replication-competent HBV DNA plasmid assessed as reduction in HBV DNA level in plasma at 0.1 mg/kg, po QD for 5 days by RT-qPCR analysis2019Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
A New Approach of Mitigating CYP3A4 Induction Led to the Discovery of Potent Hepatitis B Virus (HBV) Capsid Inhibitor with Optimal ADMET Profiles.
AID519967Antiviral activity against 0.005 MOI HIV1 NL4-3 harboring M184V mutant RT infected in human MT2 cells by phenosense assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1457761Antiviral activity against HBV ayw1 infected in human HepG2(2.2.15) cells assessed as reduction in viral replication by measuring extracellular viral DNA copy number after 6 days by real-time qPCR method2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Expanding the Antiviral Spectrum of 3-Fluoro-2-(phosphonomethoxy)propyl Acyclic Nucleoside Phosphonates: Diamyl Aspartate Amidate Prodrugs.
AID1228485Antiviral activity against Hepatitis B virus in HepG2.2.15 cells assessed as inhibition of intracellular viral DNA replication at 0.1 uM after 3 days by real-time FQ-PCR analysis2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Synthesis and biological evaluation of 4-substituted fluoronucleoside analogs for the treatment of hepatitis B virus infection.
AID283259Inhibition of HBV replication with RT A200V substitution and M204I background from Lamivudine refractory patient transfected into HepG2 cells2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Two-year assessment of entecavir resistance in Lamivudine-refractory hepatitis B virus patients reveals different clinical outcomes depending on the resistance substitutions present.
AID517932Cytotoxicity against human HEK293 cells at 100 uM2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Telbivudine exhibits no inhibitory activity against HIV-1 clinical isolates in vitro.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID519855Antiviral activity against pseudotype HIV1 LAI-Luc infected in human PBMC measured on day 3 postinfection by luciferase reporter gene assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID519873Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1678334Antiviral activity against adenovirus AdH294-WT harboring wild-type HBV genotype D accession #V01460 infected in human HepG2 cells assessed as reduction in viral replicative intermediate DNAs at 4 to 1000 nM incubated for 5 days by Southern blot analysis2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Scalable Synthesis, In Vitro cccDNA Reduction, and In Vivo Antihepatitis B Virus Activity of a Phosphonomethoxydeoxythreosyl Adenine Prodrug.
AID283263Inhibition of HBV replication with RT I53F substitution and V173F, L180M, M204V background from Lamivudine refractory patient transfected into HepG2 cells2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Two-year assessment of entecavir resistance in Lamivudine-refractory hepatitis B virus patients reveals different clinical outcomes depending on the resistance substitutions present.
AID1599889Antiviral activity against HBV genotype D hydrodynamically infected as pHBV1.3 mer plasmid carrying viral genome in C57BL/6 mouse assessed as reduction in serum viral DNA level at 0.1 to 1 mg/kg, po once daily and measured upto 6 days post treatment by qR2019ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6
Design, Synthesis, and Anti-HBV Activity of New Bis(l-amino acid) Ester Tenofovir Prodrugs.
AID519857Antiviral activity against pseudotype HIV1 NL-Luc infected in 24 hrs pretreated HEK293 cells by phenosense assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID322849Fold resistance, ratio of lamivudine -adenofir-resistant with HBV reverse transcriptase V173L/L180M/A181V/M204V/N236T mutant to wild-type HBV genotype E2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activity of 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]-pyrimidine against multidrug-resistant hepatitis B virus mutants.
AID525047Antiviral activity against Hepatitis B virus in HBeAg-positive chronic hepatitis B patient assessed as mean viral clearance rate at 0.5 mg/day2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B.
AID525226Toxicity in HBeAg-positive chronic hepatitis B patient assessed as gingival bleeding at 0.5 mg/day2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B.
AID519881Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1854350Drug elimination in human urine assessed as unchanged drug administered po relative to control2022European journal of medicinal chemistry, Oct-05, Volume: 240HIV nucleoside reverse transcriptase inhibitors.
AID1422426Antiviral activity against Hepatitis B virus infected in po dosed human liver chimeric uPA-SCID mouse assessed as reduction in serum HBeAg levels administered bid and measured for 21 days during compound dosing and follow-up period up to 35 days2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Discovery of RG7834: The First-in-Class Selective and Orally Available Small Molecule Hepatitis B Virus Expression Inhibitor with Novel Mechanism of Action.
AID322835Antiviral activity against wild type HBV genotype E assessed as inhibition of replication2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activity of 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]-pyrimidine against multidrug-resistant hepatitis B virus mutants.
AID517935Antiviral activity against HIV1 subtype A isolate 1 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Telbivudine exhibits no inhibitory activity against HIV-1 clinical isolates in vitro.
AID519969Antiviral activity against HIV infected in CD4+ lymphocyte by fluorescence-activated cell sorter assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID283264Inhibition of HBV replication with RT S78T substitution from Lamivudine refractory patient transfected into HepG2 cells2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Two-year assessment of entecavir resistance in Lamivudine-refractory hepatitis B virus patients reveals different clinical outcomes depending on the resistance substitutions present.
AID519867Antiviral activity against HIV1 subtype B-ASM 034 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625938Antiviral activity against lamivudine-resistant Hepatitis B virus harboring reverse transcriptase M204I mutant infected in human HepG2(2.2.15) cells assessed as inhibition of virus replication treated daily for 9 days by quantitative blot hybridization me2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Antiviral activity of novel 2'-fluoro-6'-methylene-carbocyclic adenosine against wild-type and drug-resistant hepatitis B virus mutants.
AID519879Antiviral activity against 0.006 MOI HIV1 NL4-3 infected in 1 hr-pretreated human MT2 cells measured after 5 days by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID322825Inhibition of wild type HBV replication in Huh7 cells2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activity of 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]-pyrimidine against multidrug-resistant hepatitis B virus mutants.
AID625935Antiviral activity against lamivudine-resistant Hepatitis B virus harboring reverse transcriptase M204V mutant infected in human HepG2(2.2.15) cells assessed as inhibition of virus replication treated daily for 9 days by quantitative blot hybridization me2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Antiviral activity of novel 2'-fluoro-6'-methylene-carbocyclic adenosine against wild-type and drug-resistant hepatitis B virus mutants.
AID519878Antiviral activity against 0.006 MOI HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID322832Fold resistance, ratio of EC50 for lamivudine-resistant HBV with reverse transcriptase L180M/M204V mutant to EC50 for wild-type HBV2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activity of 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]-pyrimidine against multidrug-resistant hepatitis B virus mutants.
AID519851Cytotoxicity against human CEM-SS cells after 10 days by MTT assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID517936Antiviral activity against HIV1 subtype A isolate 2 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Telbivudine exhibits no inhibitory activity against HIV-1 clinical isolates in vitro.
AID517937Antiviral activity against HIV1 subtype B isolate 3 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Telbivudine exhibits no inhibitory activity against HIV-1 clinical isolates in vitro.
AID283258Inhibition of HBV replication with RT A200V substitution from Lamivudine refractory patient transfected into HepG2 cells2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Two-year assessment of entecavir resistance in Lamivudine-refractory hepatitis B virus patients reveals different clinical outcomes depending on the resistance substitutions present.
AID1457762Cytotoxicity against human HepG2.2.15 cells assessed as cell viability by tetrazolium dye uptake assay2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Expanding the Antiviral Spectrum of 3-Fluoro-2-(phosphonomethoxy)propyl Acyclic Nucleoside Phosphonates: Diamyl Aspartate Amidate Prodrugs.
AID625939Antiviral activity against lamivudine-resistant Hepatitis B virus harboring reverse transcriptase M204I mutant infected in human HepG2(2.2.15) cells assessed as reduction of infectious virus titer treated daily for 9 days by quantitative Southern blot hyb2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Antiviral activity of novel 2'-fluoro-6'-methylene-carbocyclic adenosine against wild-type and drug-resistant hepatitis B virus mutants.
AID519868Antiviral activity against HIV1 subtype B-92US076 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID519852Cmax in human at 1 mg/kg, po2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID283275Inhibition of HBV replication with RT M309L substitution from Lamivudine refractory patient transfected into HepG2 cells2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Two-year assessment of entecavir resistance in Lamivudine-refractory hepatitis B virus patients reveals different clinical outcomes depending on the resistance substitutions present.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID525234Toxicity in HBeAg-positive chronic hepatitis B patient assessed as thrombocytopenia at 0.5 mg/day2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B.
AID322837Antiviral activity against lamivudine-resistant HBV with reverse transcriptase L180M/A181V mutant2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activity of 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]-pyrimidine against multidrug-resistant hepatitis B virus mutants.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1678352Antiviral activity against adenovirus AdH294-WT harboring wild-type HBV genotype D accession #V01460 infected in human HepG2 cells assessed as reduction in viral replicative intermediate DNA level at 10000 nM incubated for 5 days by Southern blot analysis2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Scalable Synthesis, In Vitro cccDNA Reduction, and In Vivo Antihepatitis B Virus Activity of a Phosphonomethoxydeoxythreosyl Adenine Prodrug.
AID1694157Antiviral activity against Hepatitis B virus infected in human HePAD38 cells assessed as reduction in viral DNA replication incubated for 7 days by RT-PCR analysis2021Bioorganic & medicinal chemistry, 02-01, Volume: 31Discovery and structure activity relationship of glyoxamide derivatives as anti-hepatitis B virus agents.
AID525045Hepatotoxicity in HBeAg-positive chronic hepatitis B patient assessed as reduction in alanine aminotransferase level at 0.5 mg/day after 12 weeks (Rvb = 170.2 IU/liter)2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B.
AID1457764Antiviral activity against HBV ayw1 infected in human HepG2(2.2.15) cells assessed as reduction in viral replication by measuring intracellular viral DNA copy number after 6 days byr by real-time qPCR assay2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Expanding the Antiviral Spectrum of 3-Fluoro-2-(phosphonomethoxy)propyl Acyclic Nucleoside Phosphonates: Diamyl Aspartate Amidate Prodrugs.
AID322828Antiviral activity against adenofir-resistant HBV with reverse transcriptase N236T mutant assessed as inhibition of replication2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activity of 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]-pyrimidine against multidrug-resistant hepatitis B virus mutants.
AID525252Toxicity in HBeAg-positive chronic hepatitis B patient assessed as proteinuria at 0.5 mg/day2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B.
AID525242Toxicity in HBeAg-positive chronic hepatitis B patient assessed as headache at 0.5 mg/day2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B.
AID1555316Inhibition of capsid protein in lamivudine/entecavir-resistant Hepatitis B virus harboring rtL180M/rtM204V/rt184L mutant infected in human HepG2.2.15 cells assessed as reduction in viral DNA level at 10 uM measured after 72 hrs by PCR analysis relative to2019European journal of medicinal chemistry, Aug-15, Volume: 176Assessment of quinazolinone derivatives as novel non-nucleoside hepatitis B virus inhibitors.
AID525218Toxicity in HBeAg-positive chronic hepatitis B patient assessed as upper abdominal pain at 0.5 mg/day2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B.
AID519883Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID322851Fold resistance, ratio of entecavir-resistant HBV with reverse transcriptase L180M/S202G/M204V mutant to wild-type HBV genotype H2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activity of 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]-pyrimidine against multidrug-resistant hepatitis B virus mutants.
AID1228493Antiviral activity against Hepatitis B virus in HepG2.2.15 cells assessed as inhibition of intracellular viral DNA replication at 0.1 uM after 9 days by real-time FQ-PCR analysis2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Synthesis and biological evaluation of 4-substituted fluoronucleoside analogs for the treatment of hepatitis B virus infection.
AID1649795Cytotoxicity in human HepG2 cells assessed as induction of cell killing2020Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11
Discovery of (1
AID1678339Antiviral activity against ETV-resistant and adenovirus AdH294-7LR harboring wild-type HBV infected in human HepG2 cells assessed as viral replicative intermediate DNA level at 40 nM incubated for 5 days by Southern blot analysis (Rvb = 100%)2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Scalable Synthesis, In Vitro cccDNA Reduction, and In Vivo Antihepatitis B Virus Activity of a Phosphonomethoxydeoxythreosyl Adenine Prodrug.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID525212Toxicity in HBeAg-positive chronic hepatitis B patient assessed as upper respiratory tract infection at 0.5 mg/day2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B.
AID322827Antiviral activity against wild type HBV assessed as inhibition of replication2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activity of 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]-pyrimidine against multidrug-resistant hepatitis B virus mutants.
AID283262Inhibition of HBV replication with RT V27A substitution and L180M, M204V background from Lamivudine refractory patient transfected into HepG2 cells2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Two-year assessment of entecavir resistance in Lamivudine-refractory hepatitis B virus patients reveals different clinical outcomes depending on the resistance substitutions present.
AID519889Selectivity ratio of EC50 for 0.005 MOI HIV1 NL4-3 infected in human MT2 cells by MTS assay to EC50 for 0.005 MOI HIV1 NL4-3 infected in human MT2 cells by RT assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1377839Inhibition of capsid in HBV infected in human HepAD38 cells assessed as reduction in cccDNA formation by measuring reduction in HBe antigen secretion at 10 uM after 14 days by ELISA relative to control2017European journal of medicinal chemistry, Sep-29, Volume: 138Synthesis of sulfamoylbenzamide derivatives as HBV capsid assembly effector.
AID1555318Inhibition of capsid protein in wild type Hepatitis B virus infected in human HepG2.2.15 cells assessed as reduction of viral DNA level at 10 uM measured after 72 hrs by PCR analysis relative to control2019European journal of medicinal chemistry, Aug-15, Volume: 176Assessment of quinazolinone derivatives as novel non-nucleoside hepatitis B virus inhibitors.
AID525220Toxicity in HBeAg-positive chronic hepatitis B patient assessed as increase in AST level at 0.5 mg/day2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B.
AID283268Inhibition of HBV replication with RT C188S substitution and L80I, L180T, M204V background from Lamivudine refractory patient transfected into HepG2 cells2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Two-year assessment of entecavir resistance in Lamivudine-refractory hepatitis B virus patients reveals different clinical outcomes depending on the resistance substitutions present.
AID283271Inhibition of HBV replication with RT L229W substitution and L180M, M204V background from Lamivudine refractory patient transfected into HepG2 cells2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Two-year assessment of entecavir resistance in Lamivudine-refractory hepatitis B virus patients reveals different clinical outcomes depending on the resistance substitutions present.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1473613Antiviral activity against HBV infected in hydrodynamic injection Balb/c mouse model assessed as log reduction in viral DNA load in liver at 0.1 mg/kg, po qd measured on day 8 post infection by RT-PCR method relative to control2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
3-((R)-4-(((R)-6-(2-Bromo-4-fluorophenyl)-5-(ethoxycarbonyl)-2-(thiazol-2-yl)-3,6-dihydropyrimidin-4-yl)methyl)morpholin-2-yl)propanoic Acid (HEC72702), a Novel Hepatitis B Virus Capsid Inhibitor Based on Clinical Candidate GLS4.
AID322847Fold resistance, ratio of Lamivudine -adenofir-resistant HBV with reverse transcriptase V173L/L180M/A181V mutant to wildtype HBV genotype E2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activity of 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]-pyrimidine against multidrug-resistant hepatitis B virus mutants.
AID1228497Antiviral activity against Hepatitis B virus in HepG2.2.15 cells assessed as inhibition of extracellular viral DNA replication at 0.1 uM after 3 days by real-time FQ-PCR analysis2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Synthesis and biological evaluation of 4-substituted fluoronucleoside analogs for the treatment of hepatitis B virus infection.
AID1377851Antiviral activity against HBV infected in human HepAD38 cells assessed as reduction in extracellular viral DNA level by RT-PCR method2017European journal of medicinal chemistry, Sep-29, Volume: 138Synthesis of sulfamoylbenzamide derivatives as HBV capsid assembly effector.
AID1678338Antiviral activity against ETV-resistant and adenovirus AdH294-7LR harboring wild-type HBV infected in human HepG2 cells assessed as viral replicative intermediate DNA level at 13 nM incubated for 5 days by Southern blot analysis (Rvb = 100%)2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Scalable Synthesis, In Vitro cccDNA Reduction, and In Vivo Antihepatitis B Virus Activity of a Phosphonomethoxydeoxythreosyl Adenine Prodrug.
AID1661467Antiviral activity against HBV in AAV8-HBV-transduced Balb/c mouse assessed as reduction in HBV DNA level in plasma at 0.1 mg/kg, po QD for 4 weeks relative to control
AID525224Toxicity in HBeAg-positive chronic hepatitis B patient assessed as dyspnea at 0.5 mg/day2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B.
AID625941Antiviral activity against lamivudine-resistant Hepatitis B virus harboring reverse transcriptase L180M mutant infected in human HepG2(2.2.15) cells assessed as inhibition of virus replication treated daily for 9 days by quantitative blot hybridization me2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Antiviral activity of novel 2'-fluoro-6'-methylene-carbocyclic adenosine against wild-type and drug-resistant hepatitis B virus mutants.
AID519971Selectivity ratio of EC50 for 0.005 MOI HIV1 NL4-3 harboring M184V mutant RT to EC50 for 0.005 MOI HIV1 NL4-3 harboring wild type RT infected in human MT2 cells2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID519854Antiviral activity against pseudotype HIV1 LAI-Luc infected in human MT2 cells measured on day 3 postinfection by luciferase reporter gene assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1694158Cytotoxicity against human PBMC cells assessed as reduction in cell viability by MTT assay2021Bioorganic & medicinal chemistry, 02-01, Volume: 31Discovery and structure activity relationship of glyoxamide derivatives as anti-hepatitis B virus agents.
AID322833Fold resistance, ratio of EC50 for lamivudine-adefovir-resistant HBV with reverse transcriptase L180M/M204V/N236T mutant to EC50 for wild-type HBV2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activity of 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]-pyrimidine against multidrug-resistant hepatitis B virus mutants.
AID322846Fold resistance, ratio of lamivudine-resistant HBV with reverse transcriptase V173L/L180/M204V mutant to wild-type HBV genotype H2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activity of 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]-pyrimidine against multidrug-resistant hepatitis B virus mutants.
AID625932Antiviral activity against wild type Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of virus replication treated daily for 9 days by quantitative blot hybridization method2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Antiviral activity of novel 2'-fluoro-6'-methylene-carbocyclic adenosine against wild-type and drug-resistant hepatitis B virus mutants.
AID517934Antiviral activity against HIV1 NL4-3 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Telbivudine exhibits no inhibitory activity against HIV-1 clinical isolates in vitro.
AID525256Toxicity in HBeAg-positive chronic hepatitis B patient assessed as vomiting at 0.5 mg/day2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1228489Antiviral activity against Hepatitis B virus in HepG2.2.15 cells assessed as inhibition of intracellular viral DNA replication at 0.1 uM after 6 days by real-time FQ-PCR analysis2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Synthesis and biological evaluation of 4-substituted fluoronucleoside analogs for the treatment of hepatitis B virus infection.
AID283265Inhibition of HBV replication with RT L80I substitution and L180M, M204I background from Lamivudine refractory patient transfected into HepG2 cells2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Two-year assessment of entecavir resistance in Lamivudine-refractory hepatitis B virus patients reveals different clinical outcomes depending on the resistance substitutions present.
AID625998Antiviral activity against lamivudine-resistant Hepatitis B virus harboring reverse transcriptase L180M/M204V double mutant infected in human HepG2(2.2.15) cells assessed as inhibition of virus replication treated daily for 9 days by quantitative blot hyb2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Antiviral activity of novel 2'-fluoro-6'-methylene-carbocyclic adenosine against wild-type and drug-resistant hepatitis B virus mutants.
AID525232Toxicity in HBeAg-positive chronic hepatitis B patient assessed as neutropenia at 0.5 mg/day2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B.
AID1364073Antiviral activity against entecavir-resistant wild type hepatitis B virus infected in human Huh7 cells assessed as reduction in intracellular DNA levels measured on day 7 by real-time PCR analysis2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Discovery of hepatitis B virus capsid assembly inhibitors leading to a heteroaryldihydropyrimidine based clinical candidate (GLS4).
AID1678347Antiviral activity against adenovirus AdH294-WT harboring wild-type HBV genotype D accession #V01460 infected in human HepG2 cells assessed as reduction in viral replicative intermediate DNA level at 40 nM incubated for 5 days by Southern blot analysis (R2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Scalable Synthesis, In Vitro cccDNA Reduction, and In Vivo Antihepatitis B Virus Activity of a Phosphonomethoxydeoxythreosyl Adenine Prodrug.
AID1422422Antiviral activity against Hepatitis B virus infected in human dHepaRG cells assessed as reduction in extracellular viral DNA levels after 6 days by qPCR/TaqMan assay2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Discovery of RG7834: The First-in-Class Selective and Orally Available Small Molecule Hepatitis B Virus Expression Inhibitor with Novel Mechanism of Action.
AID519856Antiviral activity against pseudotype HIV1 NL-RLuc infected in human MT2 cells measured on day 5 postinfection by luciferase reporter gene assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID525042Antiviral activity against Hepatitis B virus in HBeAg-positive chronic hepatitis B patient assessed as HBV DNA level in serum at 600 mg/day after 12 weeks (Rvb = 10.29 log10copies/ml)2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B.
AID283272Inhibition of HBV replication with RT D263G substitution from Lamivudine refractory patient transfected into HepG2 cells2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Two-year assessment of entecavir resistance in Lamivudine-refractory hepatitis B virus patients reveals different clinical outcomes depending on the resistance substitutions present.
AID519877Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID519864Antiviral activity against HIV1 subtype B-NL4-3 infected in 2 hrs pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1742101Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as inhibition of DNA replication at 10 uM supplemented with fresh medium containing compound every 2 days for 6 days by RT-PCR analysis relative to control2020European journal of medicinal chemistry, Nov-01, Volume: 205Discovery of novel quinazolinone derivatives as potential anti-HBV and anti-HCC agents.
AID1661461Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as reduction in capsid associated DNAs at 0.1 uM by agarose gel electrophoresis method
AID519875Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1617347Antiviral activity against HBV infected in BALB/c mouse hydrodynamic injection model hydrodynamically injected with replication-competent HBV DNA plasmid assessed as reduction in HBV DNA level in liver at 0.1 mg/kg, po QD for 5 days by RT-qPCR analysis2019Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
A New Approach of Mitigating CYP3A4 Induction Led to the Discovery of Potent Hepatitis B Virus (HBV) Capsid Inhibitor with Optimal ADMET Profiles.
AID283269Inhibition of HBV replication with RT V224A substitution and V173L, L180M, M204V background from Lamivudine refractory patient transfected into HepG2 cells2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Two-year assessment of entecavir resistance in Lamivudine-refractory hepatitis B virus patients reveals different clinical outcomes depending on the resistance substitutions present.
AID369218Antiviral activity against woodchuck hepatitis virus infected woodchucks assessed as log reduction of serum viral DNA per ml of serum after 4 weeks2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Antiviral effect of orally administered (-)-beta-D-2-aminopurine dioxolane in woodchucks with chronic woodchuck hepatitis virus infection.
AID519869Antiviral activity against HIV1 subtype B-ASM 044 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID519871Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID283266Inhibition of HBV replication with RT K168E substitution and M204I background from Lamivudine refractory patient transfected into HepG2 cells2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Two-year assessment of entecavir resistance in Lamivudine-refractory hepatitis B virus patients reveals different clinical outcomes depending on the resistance substitutions present.
AID1678350Antiviral activity against adenovirus AdH294-WT harboring wild-type HBV genotype D accession #V01460 infected in human HepG2 cells assessed as reduction in viral replicative intermediate DNA level at 1100 nM incubated for 5 days by Southern blot analysis 2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Scalable Synthesis, In Vitro cccDNA Reduction, and In Vivo Antihepatitis B Virus Activity of a Phosphonomethoxydeoxythreosyl Adenine Prodrug.
AID517941Antiviral activity against HIV1 subtype C isolate 7 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Telbivudine exhibits no inhibitory activity against HIV-1 clinical isolates in vitro.
AID519888Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1351361Antiviral activity against lamivudine/entecavir resistant HBV harboring reverse transcriptase L180M/M204V/T184L mutant infected in human HepG2(2.2.15) cells assessed as inhibition of viral DNA replication at 10 uM after 72 hrs by RT-PCR method relative to2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis and evaluation of novel phenyl propionamide derivatives as non-nucleoside hepatitis B virus inhibitors.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID283260Inhibition of HBV replication with RT A200V substitution and L180M, M204I background from Lamivudine refractory patient transfected into HepG2 cells2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Two-year assessment of entecavir resistance in Lamivudine-refractory hepatitis B virus patients reveals different clinical outcomes depending on the resistance substitutions present.
AID1694159Cytotoxicity against human CEM cells assessed as reduction in cell viability by MTT assay2021Bioorganic & medicinal chemistry, 02-01, Volume: 31Discovery and structure activity relationship of glyoxamide derivatives as anti-hepatitis B virus agents.
AID519859Antiviral activity against HIV1 subtype B-RF infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID727269Cytotoxicity against human HuH7 cells2013Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
2'-Fluoro-6'-methylene-carbocyclic adenosine phosphoramidate (FMCAP) prodrug: in vitro anti-HBV activity against the lamivudine-entecavir resistant triple mutant and its mechanism of action.
AID525236Toxicity in HBeAg-positive chronic hepatitis B patient assessed as increase in blood CK level at 0.5 mg/day2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B.
AID523463Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as decrease in intracellular viral DNA level at 2.16 uM after 72 hrs by RT-PCR analysis2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Heat stress cognate 70 host protein as a potential drug target against drug resistance in hepatitis B virus.
AID1649793Antiviral activity against multidrug-resistant HBV infected in human HepG2.1403F cells assessed as reduction in viral replication incubated for 6 days by PCR analysis2020Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11
Discovery of (1
AID1533171Antiviral activity against HBV genotype D infected in human HepG2.2.15 cells assessed as reduction in viral DNA level after 7 days by RT-PCR assay2018ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12
Synthesis, Anti-HBV, and Anti-HIV Activities of 3'-Halogenated Bis(hydroxymethyl)-cyclopentenyladenines.
AID1351359Antiviral activity against HBV infected in human HepG2(2.2.15) cells assessed as inhibition of viral DNA replication at 10 uM after 72 hrs by RT-PCR method relative to control2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis and evaluation of novel phenyl propionamide derivatives as non-nucleoside hepatitis B virus inhibitors.
AID525246Toxicity in HBeAg-positive chronic hepatitis B patient assessed as insomnia at 0.5 mg/day2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B.
AID322843Antiviral activity against entecavir-resistant HBV with reverse transcriptase L180M/S202G/M204V mutant2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activity of 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]-pyrimidine against multidrug-resistant hepatitis B virus mutants.
AID1631968Antiviral activity against Hepatitis B virus genotype D infected in Balb/c mouse assessed as reduction in viral DNA level in liver at 0.1 mg/kg, po qd for 5 days by RT-PCR method2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
Design and Synthesis of Orally Bioavailable 4-Methyl Heteroaryldihydropyrimidine Based Hepatitis B Virus (HBV) Capsid Inhibitors.
AID1364074Antiviral activity against entecavir-resistant wild type hepatitis B virus infected in human Huh7 cells assessed as reduction in secreted DNA levels measured on day 7 by real-time PCR analysis2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Discovery of hepatitis B virus capsid assembly inhibitors leading to a heteroaryldihydropyrimidine based clinical candidate (GLS4).
AID519966Antiviral activity against 0.005 MOI HIV1 NL4-3 harboring wild type RT infected in human MT2 cells by phenosense assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID519853Antiviral activity against pseudotype HIV1 LAI-Luc infected in CD4-positive human HeLa cells measured on day 3 postinfection by luciferase reporter gene assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID519887Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID322840Antiviral activity against Lamivudine -adenofir-resistant HBV with reverse transcriptase V173L/L180M/A181V/M204V mutant2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activity of 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]-pyrimidine against multidrug-resistant hepatitis B virus mutants.
AID1377854Antiviral activity against HBV infected in human HepAD38 cells assessed as reduction in intracellular viral DNA level at 10 uM by RT-PCR method relative to control2017European journal of medicinal chemistry, Sep-29, Volume: 138Synthesis of sulfamoylbenzamide derivatives as HBV capsid assembly effector.
AID626001Antiviral activity against adefovir-resistant Hepatitis B virus harboring reverse transcriptase N236T mutant infected in human HepG2(2.2.15) cells assessed as inhibition of virus replication treated daily for 9 days by quantitative blot hybridization meth2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Antiviral activity of novel 2'-fluoro-6'-methylene-carbocyclic adenosine against wild-type and drug-resistant hepatitis B virus mutants.
AID727270Antiviral activity against wild type Hepatitis B virus infected in human HuH7 cells2013Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
2'-Fluoro-6'-methylene-carbocyclic adenosine phosphoramidate (FMCAP) prodrug: in vitro anti-HBV activity against the lamivudine-entecavir resistant triple mutant and its mechanism of action.
AID322842Antiviral activity against lamivudine-adenofir-resistant HBV with reverse transcriptase V173L/L180M/A181V/N236T mutant2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activity of 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]-pyrimidine against multidrug-resistant hepatitis B virus mutants.
AID519874Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1678340Antiviral activity against ETV-resistant and adenovirus AdH294-7LR harboring wild-type HBV infected in human HepG2 cells assessed as viral replicative intermediate DNA level at 120 nM incubated for 5 days by Southern blot analysis (Rvb = 100%)2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Scalable Synthesis, In Vitro cccDNA Reduction, and In Vivo Antihepatitis B Virus Activity of a Phosphonomethoxydeoxythreosyl Adenine Prodrug.
AID1859031Antiviral activity against HBV infected in human HepDES19 cells assessed as reduction of capsid associated HBV DNA 1 uM measured by agarose gel electrophoresis-based particle gel assay2022Bioorganic & medicinal chemistry letters, 02-15, Volume: 584-Oxooctahydroquinoline-1(2H)-carboxamides as hepatitis B virus (HBV) capsid core protein assembly modulators.
AID525254Toxicity in HBeAg-positive chronic hepatitis B patient assessed as vaginal hemorrhage at 0.5 mg/day2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B.
AID322826Effect on cell viability in human Huh7 cells2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activity of 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]-pyrimidine against multidrug-resistant hepatitis B virus mutants.
AID1695272Cytotoxicity against human HepG2.2.15.7 cells assessed as reduction in cell viability2020RSC medicinal chemistry, May-01, Volume: 11, Issue:5
Synthesis and anti-HBV activity of carbocyclic nucleoside hybrids with salient features of entecavir and aristeromycin.
AID519860Antiviral activity against HIV1 subtype B-SF-2 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1678337Antiviral activity against ETV-resistant and adenovirus AdH294-7LR harboring wild-type HBV infected in human HepG2 cells assessed as viral replicative intermediate DNA level at 4 nM incubated for 5 days by Southern blot analysis (Rvb = 100%)2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Scalable Synthesis, In Vitro cccDNA Reduction, and In Vivo Antihepatitis B Virus Activity of a Phosphonomethoxydeoxythreosyl Adenine Prodrug.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1678342Antiviral activity against ETV-resistant and adenovirus AdH294-7LR harboring wild-type HBV infected in human HepG2 cells assessed as viral replicative intermediate DNA level at 1100 nM incubated for 5 days by Southern blot analysis (Rvb = 100%)2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Scalable Synthesis, In Vitro cccDNA Reduction, and In Vivo Antihepatitis B Virus Activity of a Phosphonomethoxydeoxythreosyl Adenine Prodrug.
AID322838Antiviral activity against lamivudine-resistant HBV with reverse transcriptase V173L/L180/M204V mutant2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activity of 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]-pyrimidine against multidrug-resistant hepatitis B virus mutants.
AID1228505Antiviral activity against Hepatitis B virus in HepG2.2.15 cells assessed as inhibition of extracellular viral DNA replication at 0.1 uM after 9 days by real-time FQ-PCR analysis2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Synthesis and biological evaluation of 4-substituted fluoronucleoside analogs for the treatment of hepatitis B virus infection.
AID1678358Toxicity in HBV infected hydrodynamic injection C57BL/6 mouse model assessed as effect on body weight at 0.6 to 60 mg/kg, po QD for 6 days2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Scalable Synthesis, In Vitro cccDNA Reduction, and In Vivo Antihepatitis B Virus Activity of a Phosphonomethoxydeoxythreosyl Adenine Prodrug.
AID517943Antiviral activity against HIV1 expressing reverse transcriptase D67N/K70R/T215F/K219E/M184V mutant infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Telbivudine exhibits no inhibitory activity against HIV-1 clinical isolates in vitro.
AID1678345Antiviral activity against adenovirus AdH294-WT harboring wild-type HBV genotype D accession #V01460 infected in human HepG2 cells assessed as reduction in viral replicative intermediate DNA level at 4 nM incubated for 5 days by Southern blot analysis (Rv2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Scalable Synthesis, In Vitro cccDNA Reduction, and In Vivo Antihepatitis B Virus Activity of a Phosphonomethoxydeoxythreosyl Adenine Prodrug.
AID525222Toxicity in HBeAg-positive chronic hepatitis B patient assessed as conjunctival hypermia at 0.5 mg/day2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B.
AID519862Antiviral activity against HIV1 subtype B-LAI infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID283273Inhibition of HBV replication with RT Q267Stop substitution and L180M, M204V background from Lamivudine refractory patient transfected into HepG2 cells2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Two-year assessment of entecavir resistance in Lamivudine-refractory hepatitis B virus patients reveals different clinical outcomes depending on the resistance substitutions present.
AID1228501Antiviral activity against Hepatitis B virus in HepG2.2.15 cells assessed as inhibition of extracellular viral DNA replication at 0.1 uM after 6 days by real-time FQ-PCR analysis2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Synthesis and biological evaluation of 4-substituted fluoronucleoside analogs for the treatment of hepatitis B virus infection.
AID519870Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID525049Antiviral activity against Hepatitis B virus in HBeAg-positive chronic hepatitis B patient assessed as mean rate of infected cell loss at 0.5 mg/day2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B.
AID1363957Inhibition of hepatitis B virus capsid assembly infected in human HepG2.215 cells assessed as reduction in viral DNA replication measured on day 7 by real time PCR analysis2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Discovery of hepatitis B virus capsid assembly inhibitors leading to a heteroaryldihydropyrimidine based clinical candidate (GLS4).
AID517939Antiviral activity against HIV1 subtype BF isolate 5 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Telbivudine exhibits no inhibitory activity against HIV-1 clinical isolates in vitro.
AID1678348Antiviral activity against adenovirus AdH294-WT harboring wild-type HBV genotype D accession #V01460 infected in human HepG2 cells assessed as reduction in viral replicative intermediate DNA level at 120 nM incubated for 5 days by Southern blot analysis (2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Scalable Synthesis, In Vitro cccDNA Reduction, and In Vivo Antihepatitis B Virus Activity of a Phosphonomethoxydeoxythreosyl Adenine Prodrug.
AID1678335Antiviral activity against ETV-resistant and adenovirus AdH294-7LR harboring wild-type HBV infected in human HepG2 cells assessed as reduction in viral replicative intermediate DNAs up to 100 uM incubated for 5 days by Southern blot analysis2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Scalable Synthesis, In Vitro cccDNA Reduction, and In Vivo Antihepatitis B Virus Activity of a Phosphonomethoxydeoxythreosyl Adenine Prodrug.
AID727268Antiviral activity against entecavir-resistant Hepatitis B virus harboring L180M/M204V/S202G triple mutant infected in human HuH7 cells2013Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
2'-Fluoro-6'-methylene-carbocyclic adenosine phosphoramidate (FMCAP) prodrug: in vitro anti-HBV activity against the lamivudine-entecavir resistant triple mutant and its mechanism of action.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID519884Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1363962Cytotoxicity in human HepG2.215 cells assessed as reduction in cell viability after 5 days by CCK8 assay2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Discovery of hepatitis B virus capsid assembly inhibitors leading to a heteroaryldihydropyrimidine based clinical candidate (GLS4).
AID525230Toxicity in HBeAg-positive chronic hepatitis B patient assessed as myalgia at 0.5 mg/day2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B.
AID1695271Antiviral activity against Hepatitis B virus infected in human HepG2.2.15.7 assessed as reduction in HBV DNA level incubated for 9 days media replaced every 3 days once with test compound by RT-PCR analysis2020RSC medicinal chemistry, May-01, Volume: 11, Issue:5
Synthesis and anti-HBV activity of carbocyclic nucleoside hybrids with salient features of entecavir and aristeromycin.
AID519863Antiviral activity against HIV1 subtype B-NL4-3 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1228457Cytotoxicity against human HepG2.2.15 cells by MTT assay2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Synthesis and biological evaluation of 4-substituted fluoronucleoside analogs for the treatment of hepatitis B virus infection.
AID626004Antiviral activity against lamivudine/entecavir-resistant Hepatitis B virus harboring reverse transcriptase L180M/M204V/S202G infected in human HepG2(2.2.15) cells assessed as inhibition of virus replication treated daily for 9 days by quantitative blot h2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Antiviral activity of novel 2'-fluoro-6'-methylene-carbocyclic adenosine against wild-type and drug-resistant hepatitis B virus mutants.
AID525250Toxicity in HBeAg-positive chronic hepatitis B patient assessed as nasophayngitis at 0.5 mg/day2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID525240Toxicity in HBeAg-positive chronic hepatitis B patient assessed as facial edema at 0.5 mg/day2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B.
AID322829Antiviral activity against lamivudine-resistant HBV with reverse transcriptase L180M/M204V mutant assessed as inhibition of replication2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activity of 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]-pyrimidine against multidrug-resistant hepatitis B virus mutants.
AID519861Antiviral activity against HIV1 subtype B-3B infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID525214Toxicity in HBeAg-positive chronic hepatitis B patient assessed as chest discomfort at 0.5 mg/day2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B.
AID1649792Antiviral activity against HBV infected in human HepG2.A64 cells containing reverse transcriptase L180M/T184L/M204V mutant assessed as reduction in viral replication incubated for 6 days by PCR analysis2020Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11
Discovery of (1
AID1473614Antiviral activity against HBV infected in hydrodynamic injection Balb/c mouse model assessed as log reduction in viral DNA load in plasma at 0.1 mg/kg, po qd measured up to day 8 post infection by RT-PCR method relative to control2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
3-((R)-4-(((R)-6-(2-Bromo-4-fluorophenyl)-5-(ethoxycarbonyl)-2-(thiazol-2-yl)-3,6-dihydropyrimidin-4-yl)methyl)morpholin-2-yl)propanoic Acid (HEC72702), a Novel Hepatitis B Virus Capsid Inhibitor Based on Clinical Candidate GLS4.
AID1457763Selectivity index, ratio of CC50 for HepG2.2.15 cells to EC50 for HBV ayw1 infected in human HepG2(2.2.15) cells assessed as reduction in viral replication by measuring extracellular viral DNA copy2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Expanding the Antiviral Spectrum of 3-Fluoro-2-(phosphonomethoxy)propyl Acyclic Nucleoside Phosphonates: Diamyl Aspartate Amidate Prodrugs.
AID525216Toxicity in HBeAg-positive chronic hepatitis B patient assessed as abdominal discomfort at 0.5 mg/day2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID727267Selectivity ratio of EC50 for entecavir-resistant Hepatitis B virus harboring L180M/M204V/S202G triple mutant to EC50 for wild type Hepatitis B virus2013Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
2'-Fluoro-6'-methylene-carbocyclic adenosine phosphoramidate (FMCAP) prodrug: in vitro anti-HBV activity against the lamivudine-entecavir resistant triple mutant and its mechanism of action.
AID1377853Antiviral activity against HBV infected in human HepAD38 cells assessed as reduction in intracellular viral DNA level by RT-PCR method2017European journal of medicinal chemistry, Sep-29, Volume: 138Synthesis of sulfamoylbenzamide derivatives as HBV capsid assembly effector.
AID525053Toxicity in HBeAg-positive chronic hepatitis B patient assessed as increase in ALT level at 0.5 mg/day2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B.
AID1678344Antiviral activity against ETV-resistant and adenovirus AdH294-7LR harboring wild-type HBV infected in human HepG2 cells assessed as viral replicative intermediate DNA level at 10000 nM incubated for 5 days by Southern blot analysis (Rvb = 100%)2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Scalable Synthesis, In Vitro cccDNA Reduction, and In Vivo Antihepatitis B Virus Activity of a Phosphonomethoxydeoxythreosyl Adenine Prodrug.
AID625996Antiviral activity against lamivudine-resistant Hepatitis B virus harboring reverse transcriptase L180M mutant infected in human HepG2(2.2.15) cells assessed as reduction of infectious virus titer treated daily for 9 days by quantitative Southern blot hyb2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Antiviral activity of novel 2'-fluoro-6'-methylene-carbocyclic adenosine against wild-type and drug-resistant hepatitis B virus mutants.
AID1661464Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as reduction in capsid formation
AID519858Antiviral activity against HIV1 subtype B-HXB2 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1678343Antiviral activity against ETV-resistant and adenovirus AdH294-7LR harboring wild-type HBV infected in human HepG2 cells assessed as viral replicative intermediate DNA level at 3300 nM incubated for 5 days by Southern blot analysis (Rvb = 100%)2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Scalable Synthesis, In Vitro cccDNA Reduction, and In Vivo Antihepatitis B Virus Activity of a Phosphonomethoxydeoxythreosyl Adenine Prodrug.
AID322830Antiviral activity against lamivudine-adefovir-resistant HBV with reverse transcriptase L180M/M204V/N236T mutant assessed as inhibition of replication2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activity of 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]-pyrimidine against multidrug-resistant hepatitis B virus mutants.
AID525051Antiviral activity against Hepatitis B virus in HBeAg-positive chronic hepatitis B patient assessed as mean efficiency factor of blocking virus production at 0.5 mg/day2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B.
AID1678351Antiviral activity against adenovirus AdH294-WT harboring wild-type HBV genotype D accession #V01460 infected in human HepG2 cells assessed as reduction in viral replicative intermediate DNA level at 3300 nM incubated for 5 days by Southern blot analysis 2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Scalable Synthesis, In Vitro cccDNA Reduction, and In Vivo Antihepatitis B Virus Activity of a Phosphonomethoxydeoxythreosyl Adenine Prodrug.
AID519849Antiviral activity against Hepatitis B virus2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1693342Antiviral activity against lamivudine/entecavir-resistant HBV rtL180M/rtM204V/rtT184L mutant infected in human HepG2 2.2.15 cells assessed as inhibition of viral DNA replication at 10 uM measured after incubation of 72 hrs by RT-PCR analysis relative to c2021Bioorganic & medicinal chemistry, 01-01, Volume: 29Synthesis and evaluation of new phenyl acrylamide derivatives as potent non-nucleoside anti-HBV agents.
AID1678357Antiviral activity against HBV infected hydrodynamic injection C57BL/6 mouse model assessed as reduction in serum HBV DNA level at 0.6 to 60 mg/kg, po QD for 6 days by qPCR analysis2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Scalable Synthesis, In Vitro cccDNA Reduction, and In Vivo Antihepatitis B Virus Activity of a Phosphonomethoxydeoxythreosyl Adenine Prodrug.
AID283274Inhibition of HBV replication with RT G295S substitution and L80I, M204I background from Lamivudine refractory patient transfected into HepG2 cells2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Two-year assessment of entecavir resistance in Lamivudine-refractory hepatitis B virus patients reveals different clinical outcomes depending on the resistance substitutions present.
AID1678349Antiviral activity against adenovirus AdH294-WT harboring wild-type HBV genotype D accession #V01460 infected in human HepG2 cells assessed as reduction in viral replicative intermediate DNA level at 370 nM incubated for 5 days by Southern blot analysis (2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Scalable Synthesis, In Vitro cccDNA Reduction, and In Vivo Antihepatitis B Virus Activity of a Phosphonomethoxydeoxythreosyl Adenine Prodrug.
AID519880Antiviral activity against 0.006 MOI HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1859022Antiviral activity against HBV infected in human HepDES19 cells assessed effect on intracellular total HBV RNA at 1 uM measured after 24 hrs by northern blot hybridization assay2022Bioorganic & medicinal chemistry letters, 02-15, Volume: 584-Oxooctahydroquinoline-1(2H)-carboxamides as hepatitis B virus (HBV) capsid core protein assembly modulators.
AID1854349Elimination half life in human administered po2022European journal of medicinal chemistry, Oct-05, Volume: 240HIV nucleoside reverse transcriptase inhibitors.
AID1678346Antiviral activity against adenovirus AdH294-WT harboring wild-type HBV genotype D accession #V01460 infected in human HepG2 cells assessed as reduction in viral replicative intermediate DNA level at 13 nM incubated for 5 days by Southern blot analysis (R2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Scalable Synthesis, In Vitro cccDNA Reduction, and In Vivo Antihepatitis B Virus Activity of a Phosphonomethoxydeoxythreosyl Adenine Prodrug.
AID322834Antiviral activity against wild type HBV genotype H assessed as inhibition of replication2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activity of 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]-pyrimidine against multidrug-resistant hepatitis B virus mutants.
AID525260Toxicity in HBeAg-positive chronic hepatitis B patient assessed as muscular weakness at 0.5 mg/day2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B.
AID1859025Antiviral activity against HBV infected in human HepDES19 cells assessed reduction of amounts of encapsidated pgRNA 1 uM measured after 24 hrs by northern blot hybridization assay2022Bioorganic & medicinal chemistry letters, 02-15, Volume: 584-Oxooctahydroquinoline-1(2H)-carboxamides as hepatitis B virus (HBV) capsid core protein assembly modulators.
AID519970Cmax in human blood2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID519882Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1363984Antiviral activity against entecavir-resistant hepatitis B virus harboring reverse transcriptase M204I/S202G/M250V triple mutant infected in human Huh7 cells assessed as reduction in intracellular DNA levels measured on day 7 by real-time PCR analysis2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Discovery of hepatitis B virus capsid assembly inhibitors leading to a heteroaryldihydropyrimidine based clinical candidate (GLS4).
AID1678341Antiviral activity against ETV-resistant and adenovirus AdH294-7LR harboring wild-type HBV infected in human HepG2 cells assessed as viral replicative intermediate DNA level at 370 nM incubated for 5 days by Southern blot analysis (Rvb = 100%)2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Scalable Synthesis, In Vitro cccDNA Reduction, and In Vivo Antihepatitis B Virus Activity of a Phosphonomethoxydeoxythreosyl Adenine Prodrug.
AID519964Antiviral activity against 0.005 MOI HIV1 NL4-3 harboring wild type RT infected in human MT2 cells2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID625936Antiviral activity against lamivudine-resistant Hepatitis B virus harboring reverse transcriptase M204V mutant infected in human HepG2(2.2.15) cells assessed as reduction of infectious virus titer treated daily for 9 days by quantitative Southern blot hyb2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Antiviral activity of novel 2'-fluoro-6'-methylene-carbocyclic adenosine against wild-type and drug-resistant hepatitis B virus mutants.
AID626005Antiviral activity against lamivudine/entecavir-resistant Hepatitis B virus harboring reverse transcriptase L180M/M204V/S202G infected in human HepG2(2.2.15) cells assessed as reduction of infectious virus titer treated daily for 9 days by quantitative So2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Antiviral activity of novel 2'-fluoro-6'-methylene-carbocyclic adenosine against wild-type and drug-resistant hepatitis B virus mutants.
AID519865Antiviral activity against HIV1 subtype B-NL4-3 infected in 3 hrs pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID519972Selectivity ratio of EC50 for 0.005 MOI HIV1 NL4-3 harboring M184V mutant RT to EC50 for 0.005 MOI HIV1 NL4-3 harboring wild type RT infected in human MT2 cells by phenosense assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1422421Antiviral activity against Hepatitis B virus infected in human dHepaRG cells assessed as reduction in HBeAg secretion after 10 mins by chemiluminescence immunoassay2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Discovery of RG7834: The First-in-Class Selective and Orally Available Small Molecule Hepatitis B Virus Expression Inhibitor with Novel Mechanism of Action.
AID519890Selectivity ratio of EC50 for 0.01 MOI HIV1 NL4-3 infected in human MT2 cells by MTS assay to EC50 for 0.01 MOI HIV1 NL4-3 infected in human MT2 cells by RT assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID525248Toxicity in HBeAg-positive chronic hepatitis B patient assessed as myringitis at 0.5 mg/day2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID519886Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1854347Antiviral activity against HIV-12022European journal of medicinal chemistry, Oct-05, Volume: 240HIV nucleoside reverse transcriptase inhibitors.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID519973Antiviral activity against HIV1 NL4-3 harboring M184V mutant RT at 2.5 uM after 6 days2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID322848Fold resistance, ratio of Lamivudine -adenofir-resistant with HBV reverse transcriptase V173L/L180M/A181V/M204V mutant to wildtype HBV genotype E2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activity of 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]-pyrimidine against multidrug-resistant hepatitis B virus mutants.
AID626002Antiviral activity against adefovir-resistant Hepatitis B virus harboring reverse transcriptase N236T mutant infected in human HepG2(2.2.15) cells assessed as reduction of infectious virus titer treated daily for 9 days by quantitative Southern blot hybri2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Antiviral activity of novel 2'-fluoro-6'-methylene-carbocyclic adenosine against wild-type and drug-resistant hepatitis B virus mutants.
AID1363983Antiviral activity against entecavir-resistant hepatitis B virus harboring reverse transcriptase M204I/S202G double mutant infected in human Huh7 cells assessed as reduction in intracellular DNA levels measured on day 7 by real-time PCR analysis2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Discovery of hepatitis B virus capsid assembly inhibitors leading to a heteroaryldihydropyrimidine based clinical candidate (GLS4).
AID517938Antiviral activity against HIV1 subtype B isolate 4 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Telbivudine exhibits no inhibitory activity against HIV-1 clinical isolates in vitro.
AID322836Antiviral activity against lamivudine-resistant HBV with reverse transcriptase L180M/M204V mutant2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activity of 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]-pyrimidine against multidrug-resistant hepatitis B virus mutants.
AID525244Toxicity in HBeAg-positive chronic hepatitis B patient assessed as hordeolum at 0.5 mg/day2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B.
AID322844Fold resistance, ratio of lamivudine-resistant HBV with reverse transcriptase L180M/M204V mutant to wild-type HBV genotype E2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activity of 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]-pyrimidine against multidrug-resistant hepatitis B virus mutants.
AID1228456Antiviral activity against Hepatitis B virus in HepG2.CW cells assessed as inhibition of viral DNA replication at 1 uM after 9 days by real-time FQ-PCR analysis2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Synthesis and biological evaluation of 4-substituted fluoronucleoside analogs for the treatment of hepatitis B virus infection.
AID519866Antiviral activity against HIV1 subtype B-93US143 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1457789Selectivity index, ratio of CC50 for HepG2.2.15 cells to EC50 for HBV ayw1 infected in human HepG2(2.2.15) cells assessed as reduction in viral replication by measuring intracellular viral DNA copy2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Expanding the Antiviral Spectrum of 3-Fluoro-2-(phosphonomethoxy)propyl Acyclic Nucleoside Phosphonates: Diamyl Aspartate Amidate Prodrugs.
AID1859030Antiviral activity against HBV infected in human HepDES19 cells assessed as effect on levels of intracellular core capsid 1 uM measured by Western blot assay2022Bioorganic & medicinal chemistry letters, 02-15, Volume: 584-Oxooctahydroquinoline-1(2H)-carboxamides as hepatitis B virus (HBV) capsid core protein assembly modulators.
AID283267Inhibition of HBV replication with RT A181T substitution and V173L, L180M, M204V background from Lamivudine refractory patient transfected into HepG2 cells2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Two-year assessment of entecavir resistance in Lamivudine-refractory hepatitis B virus patients reveals different clinical outcomes depending on the resistance substitutions present.
AID1422428Antiviral activity against Hepatitis B virus infected in po dosed human liver chimeric uPA-SCID mouse assessed as log reduction in serum viral DNA levels administered bid and measured for 21 days during compound dosing and follow-up period up to 35 days2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Discovery of RG7834: The First-in-Class Selective and Orally Available Small Molecule Hepatitis B Virus Expression Inhibitor with Novel Mechanism of Action.
AID1363985Antiviral activity against entecavir-resistant hepatitis B virus harboring reverse transcriptase M204I/S202G double mutant infected in human Huh7 cells assessed as reduction in secreted DNA levels measured on day 7 by real-time PCR analysis2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Discovery of hepatitis B virus capsid assembly inhibitors leading to a heteroaryldihydropyrimidine based clinical candidate (GLS4).
AID1742103Antiviral activity against lamivudine and entecavir-resistant HBV harboring rtL180 M/rtM204V/rtT184L mutant infected in human HepG2.2.15 cells assessed as inhibition of DNA replication at 10 uM supplemented with fresh medium containing compound every 2 da2020European journal of medicinal chemistry, Nov-01, Volume: 205Discovery of novel quinazolinone derivatives as potential anti-HBV and anti-HCC agents.
AID1363986Antiviral activity against entecavir-resistant hepatitis B virus harboring reverse transcriptase M204I/S202G/M250V triple mutant infected in human Huh7 cells assessed as reduction in secreted DNA levels measured on day 7 by real-time PCR analysis2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Discovery of hepatitis B virus capsid assembly inhibitors leading to a heteroaryldihydropyrimidine based clinical candidate (GLS4).
AID1599886Toxicity against C57BL/6 mouse hydrodynamically infected with pHBV1.3 mer plasmid carrying HBV genotype D assessed as change in body weight at 0.1 to 1 mg/kg, po once daily and measured upto 6 days post treatment2019ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6
Design, Synthesis, and Anti-HBV Activity of New Bis(l-amino acid) Ester Tenofovir Prodrugs.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1649794Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as reduction in viral DNA levels incubated for 6 days by PCR analysis2020Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11
Discovery of (1
AID525258Toxicity in HBeAg-positive chronic hepatitis B patient assessed as peripheral neuropathy at 0.5 mg/day2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B.
AID517942Antiviral activity against HIV1 subtype D isolate 8 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Telbivudine exhibits no inhibitory activity against HIV-1 clinical isolates in vitro.
AID517940Antiviral activity against HIV1 subtype C isolate 6 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Telbivudine exhibits no inhibitory activity against HIV-1 clinical isolates in vitro.
AID517944Antiviral activity against HIV1 expressing reverse transcriptase K103N/Y181C/G190A mutant infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Telbivudine exhibits no inhibitory activity against HIV-1 clinical isolates in vitro.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625934Cytotoxicity against human HepG2(2.2.15) cells after 24 hrs by neutral red dye uptake assay2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Antiviral activity of novel 2'-fluoro-6'-methylene-carbocyclic adenosine against wild-type and drug-resistant hepatitis B virus mutants.
AID1377846Inhibition of capsid in HBV infected in human HepAD38 cells assessed as reduction in tetracycline-induced cccDNA formation by measuring reduction in HBe antigen secretion after 14 days by ELISA2017European journal of medicinal chemistry, Sep-29, Volume: 138Synthesis of sulfamoylbenzamide derivatives as HBV capsid assembly effector.
AID1422425Antiviral activity against Hepatitis B virus infected in po dosed human liver chimeric uPA-SCID mouse assessed as reduction in serum HBsAg levels administered bid and measured for 21 days during compound dosing and follow-up period up to 35 days2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Discovery of RG7834: The First-in-Class Selective and Orally Available Small Molecule Hepatitis B Virus Expression Inhibitor with Novel Mechanism of Action.
AID1422420Antiviral activity against Hepatitis B virus infected in human dHepaRG cells assessed as reduction in HBsAg secretion after 10 mins by chemiluminescence immunoassay2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Discovery of RG7834: The First-in-Class Selective and Orally Available Small Molecule Hepatitis B Virus Expression Inhibitor with Novel Mechanism of Action.
AID625999Antiviral activity against lamivudine-resistant Hepatitis B virus harboring reverse transcriptase L180M/M204V double mutant infected in human HepG2(2.2.15) cells assessed as reduction of infectious virus titer treated daily for 9 days by quantitative Sout2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Antiviral activity of novel 2'-fluoro-6'-methylene-carbocyclic adenosine against wild-type and drug-resistant hepatitis B virus mutants.
AID625933Antiviral activity against wild type Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as reduction of infectious virus titer treated daily for 9 days by quantitative Southern blot hybridization assay2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Antiviral activity of novel 2'-fluoro-6'-methylene-carbocyclic adenosine against wild-type and drug-resistant hepatitis B virus mutants.
AID1659438Antiviral activity against Hepatitis B virus infected in C57BL/6 mouse assessed as reduction in viral DNA at 0.1 mg/kg, po measured upto 6 days by qRT-PCR analysis
AID519885Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1694160Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability by MTT assay2021Bioorganic & medicinal chemistry, 02-01, Volume: 31Discovery and structure activity relationship of glyoxamide derivatives as anti-hepatitis B virus agents.
AID1649770Antiviral activity against HBV infected in human HepAD38 cells assessed as reduction in viral DNA levels incubated for 6 days by PCR analysis2020Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11
Discovery of (1
AID519963Antiviral activity against HIV1 3B infected in MOLT-4/3B cells assessed as inhibition of mature virus release measured after 4 days of infection by RT assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1350670Antiviral activity against HBV genotype D infected in chimeric mouse with humanized liver assessed as log reduction in viral DNA level in serum at 0.03 mg/kg, po qd for 28 days by RT-PCR method2018Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
Synthesis and Evaluation of N-Phenyl-3-sulfamoyl-benzamide Derivatives as Capsid Assembly Modulators Inhibiting Hepatitis B Virus (HBV).
AID283261Inhibition of HBV replication with RT L80V substitution and L180M, M204V background from Lamivudine refractory patient transfected into HepG2 cells2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Two-year assessment of entecavir resistance in Lamivudine-refractory hepatitis B virus patients reveals different clinical outcomes depending on the resistance substitutions present.
AID519872Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID519965Antiviral activity against 0.005 MOI HIV1 NL4-3 harboring M184V mutant RT infected in human MT2 cells2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID519850Antiviral activity against HIV1 infected in human CEM-SS cells after 10 days by MTT assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID322850Fold resistance, ratio of Lamivudine -adenofir-resistant with HBV reverse transcriptase V173L/L180M/A181V/N236T mutant to wildtype HBV genotype E2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activity of 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]-pyrimidine against multidrug-resistant hepatitis B virus mutants.
AID525228Toxicity in HBeAg-positive chronic hepatitis B patient assessed as hyperphosphatemia at 0.5 mg/day2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B.
AID1854348Oral bioavailability in human relative to control2022European journal of medicinal chemistry, Oct-05, Volume: 240HIV nucleoside reverse transcriptase inhibitors.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1745855NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay2023Disease models & mechanisms, 03-01, Volume: 16, Issue:3
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID1745854NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS2023Disease models & mechanisms, 03-01, Volume: 16, Issue:3
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508612NCATS Parallel Artificial Membrane Permeability Assay (PAMPA) Profiling2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Highly predictive and interpretable models for PAMPA permeability.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1508591NCATS Rat Liver Microsome Stability Profiling2020Scientific reports, 11-26, Volume: 10, Issue:1
Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1645848NCATS Kinetic Aqueous Solubility Profiling2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID771610Selectivity ratio of IC50 for L3MBTL1 (unknown origin) to IC50 for L3MBTL3 (unknown origin) by AlphaScreen assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
AID771603Displacement of mero76 from GFP-L3MBTL3 (unknown origin) expressed in HEK293 cells at 5 uM after 3 hrs by immunofluorescence assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
AID771608Binding affinity to L3MBTL1 (unknown origin) by isothermal titration calorimetric assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
AID771612Inhibition of PHF23 (unknown origin) after 30 mins by AlphaScreen assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
AID771611Inhibition of JARID1A (unknown origin) after 30 mins by AlphaScreen assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
AID771615Inhibition of MBTD1 (unknown origin) after 30 mins by AlphaScreen assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
AID771619Inhibition of L3MBTL1 (unknown origin) after 30 mins by AlphaScreen assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
AID771607Selectivity ratio of Kd for L3MBTL1 (unknown origin) to Kd for L3MBTL3 (unknown origin) by isothermal titration calorimetric assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
AID1077873Inhibition of CBX7 (8 to 62) (unknown origin) expressed in Escherichia coli BL21 Rosetta DE3 using H3K9Me3 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay2013MedChemComm, Nov, Volume: 4, Issue:11
The structure-activity relationships of L3MBTL3 inhibitors: flexibility of the dimer interface.
AID1578927Inhibition of L3MBTL3 (unknown origin) assessed as dissociation constant by isothermal titration calorimetry2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Discovery of a Potent and Selective Fragment-like Inhibitor of Methyllysine Reader Protein Spindlin 1 (SPIN1).
AID1077870Inhibition of GST-tagged PHF23 (unknown origin) using H3K4Me3 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay2013MedChemComm, Nov, Volume: 4, Issue:11
The structure-activity relationships of L3MBTL3 inhibitors: flexibility of the dimer interface.
AID771623Cytotoxicity against HEK293T/17 cells assessed as cell viability up to 100 uM after 24 hrs by CellTiter-Glo luminescence assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
AID771604Displacement of mero76-UNC1215 from GFP-L3MBTL3 (unknown origin) expressed in HEK293 cells at 1 equivalent dose after 3 hrs by immunofluorescence assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
AID771618Inhibition of L3MBTL4 (unknown origin) after 30 mins by AlphaScreen assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
AID771606Antagonist activity at muscarinic M1 receptor (unknown origin) expressed in HEK293T cells assessed as inhibition of UNC1679 calcium mobilization2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
AID1077875Inhibition of MBTD1 (130 to 566) (unknown origin) expressed in Escherichia coli BL21 Rosetta DE3 using H4K20Me1 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay2013MedChemComm, Nov, Volume: 4, Issue:11
The structure-activity relationships of L3MBTL3 inhibitors: flexibility of the dimer interface.
AID771617Inhibition of SFMBT1 (unknown origin) after 30 mins by AlphaScreen assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
AID1077872Inhibition of UHRF1 tandem tudor domain (121 to 286) (unknown origin) expressed in Escherichia coli BL21 Rosetta DE3 using H3K9Me3 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScree2013MedChemComm, Nov, Volume: 4, Issue:11
The structure-activity relationships of L3MBTL3 inhibitors: flexibility of the dimer interface.
AID1077876Inhibition of His-tagged L3MBTL1 (unknown origin) using H4K20Me1 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay2013MedChemComm, Nov, Volume: 4, Issue:11
The structure-activity relationships of L3MBTL3 inhibitors: flexibility of the dimer interface.
AID1077874Inhibition of 53BP1 (1485 to 1611) (unknown origin) expressed in Escherichia coli BL21 Rosetta DE3 using H4K20Me2 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay2013MedChemComm, Nov, Volume: 4, Issue:11
The structure-activity relationships of L3MBTL3 inhibitors: flexibility of the dimer interface.
AID771602Binding affinity to L3MBTL3 in human G401 cells by Western blot based pulldown assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
AID771614Inhibition of UHRF1 (unknown origin) after 30 mins by AlphaScreen assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
AID771621Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
AID771620Inhibition of L3MBTL3 (unknown origin) after 30 mins by AlphaScreen assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
AID1077877Inhibition of His-tagged L3MBTL3 (unknown origin) using H4K20Me2 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay2013MedChemComm, Nov, Volume: 4, Issue:11
The structure-activity relationships of L3MBTL3 inhibitors: flexibility of the dimer interface.
AID771616Inhibition of CBX7 (unknown origin) after 30 mins by AlphaScreen assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
AID771609Binding affinity to L3MBTL3 (unknown origin) by isothermal titration calorimetric assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
AID1077871Inhibition of GST-tagged Jarid1A (unknown origin) using H3K4Me3 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay2013MedChemComm, Nov, Volume: 4, Issue:11
The structure-activity relationships of L3MBTL3 inhibitors: flexibility of the dimer interface.
AID771601Ratio of Kd for L3MBTL1 L361F mutant (unknown origin) to Kd for wild type L3MBTL1 (unknown origin) by isothermal titration calorimetric assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
AID771613Inhibition of 53BP1 (unknown origin) after 30 mins by AlphaScreen assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346246Human L3MBTL3, histone methyl-lysine binding protein (Methyllysine reader proteins)2013Nature chemical biology, Mar, Volume: 9, Issue:3
Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,787)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's5 (0.28)18.2507
2000's257 (14.38)29.6817
2010's1169 (65.42)24.3611
2020's356 (19.92)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 87.63

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index87.63 (24.57)
Research Supply Index2.89 (2.92)
Research Growth Index4.53 (4.65)
Search Engine Demand Index150.96 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (87.63)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials248 (13.33%)5.53%
Trials0 (0.00%)5.53%
Reviews276 (14.84%)6.00%
Reviews0 (0.00%)6.00%
Case Studies177 (9.52%)4.05%
Case Studies0 (0.00%)4.05%
Observational43 (2.31%)0.25%
Observational0 (0.00%)0.25%
Other1,116 (60.00%)84.16%
Other17 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (237)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
An, Open-label, Multicenter, Randomized, Active Control Study, Comparing P1101 Monotherapy to Entecavir Monotherapy in Patients With HBeAg-negative Chronic Hepatitis B Under Long-term Nucleos(t)Ide Analogue Therapy [NCT05494528]90 participants (Anticipated)Interventional2021-05-04Recruiting
Study of the Antiviral Activity of Entecavir in Patients Receiving Liver Transplant Due to Chronic Hepatitis B Virus Infection [NCT00395018]Phase 3109 participants (Actual)Interventional2007-04-30Completed
The Curative Effect and Security of Entecavir Combined Thymosin or Resveratrol on HBeAg Positive Chronic Hepatitis B Patients - a Multi-center, Random, Control, Open Clinical Trial [NCT03509688]312 participants (Actual)Interventional2014-11-30Completed
Efficacy of HBV Therapeutic Vaccine in Consolidation of Nucleos(t)Ide Analogues Therapy: a Pilot Study [NCT02505009]Phase 4116 participants (Actual)Interventional2015-05-01Completed
Study on Three Types of Nucleotide/Nucleoside Analogues Treatment in Patients With Hepatitis b Virus Related Acute-on-chronic Liver Failure [NCT03920618]150 participants (Anticipated)Interventional2019-02-01Recruiting
Influence of Hepatic Steatosis on the Therapeutic Effect of Entecavir in Chronic Hepatitis B Patients-A Randomized, Double-Blinded, Controlled Trial [NCT01148576]Phase 41,200 participants (Anticipated)Interventional2010-06-30Recruiting
Comparison of Antiviral Efficacy of Entecavir Monotherapy and Combination Treatment With Poly IC for Chronic Hepatitis B [NCT02532413]Phase 4180 participants (Anticipated)Interventional2015-07-31Recruiting
Induction of Fibrosis Regression on Patients With Chronic Hepatitis B Infection [NCT01341106]Phase 47 participants (Actual)Interventional2011-04-30Terminated(stopped due to insufficient patient numbers have been recruited)
A Phase 2 Open-label Trial to Evaluate Safety, Efficacy, Tolerability, and Pharmacodynamics of a Combination of JNJ-73763989, Nucleos(t)Ide Analogs, and a PD-1 Inhibitor in Chronic Hepatitis B Patients [NCT05275023]Phase 237 participants (Actual)Interventional2022-06-30Active, not recruiting
A Phase 2 Randomized, Open-label, Parallel-group, Multicenter Study to Assess Intrahepatic and Peripheral Changes of Immunologic and Virologic Markers in Response to Combination Regimens Containing JNJ-73763989 and Nucleos(t)Ide Analog With or Without JNJ [NCT04585789]Phase 224 participants (Actual)Interventional2021-03-11Active, not recruiting
A Phase 2, Multicenter, Randomized, Double-blind, Placebo-Controlled Study With Deferred Active Treatment to Investigate the Efficacy, Safety, and Pharmacokinetics of JNJ-73763989 + Nucleos(t)Ide Analog in Participants Co-Infected With Hepatitis B and Hep [NCT04535544]Phase 252 participants (Actual)Interventional2020-09-17Active, not recruiting
A Phase 2a, Multicenter, Single-Blind, Placebo-Controlled, Multiple Cohort Study Evaluating ABI-H2158-Containing Regimens in Chronic Hepatitis B Infection [NCT04398134]Phase 288 participants (Actual)Interventional2020-08-28Terminated(stopped due to Study stopped due to a safety signal of drug-induced liver injury in subjects receiving 2158)
A Phase IIa Study to Evaluate the Efficacy and Safety of ZM-H1505R in Combination With Entecavir (ETV) Compared With ETV Monotherapy in Patients With Chronic Hepatitis B Who Have Received ETV Monotherapy for at Least 12 Months [NCT05484466]Phase 290 participants (Anticipated)Interventional2022-11-11Recruiting
Pilot Study of First Line Combination Treatment With Low Dose Pegylated Interferon and Entecavir in Treatment-naïve Patients With Chronic Hepatitis B. [NCT01589952]Phase 1/Phase 220 participants (Anticipated)Interventional2012-03-31Recruiting
A Phase 1, Double-Blind, Randomized, Placebo-Controlled, First-in-Human Study of Orally Administered ALG-000184 to Evaluate Safety, Tolerability, Pharmacokinetics and Pharmacodynamics After Single-Ascending Doses (Part 1) and Multiple-Ascending Doses in H [NCT04536337]Phase 1336 participants (Anticipated)Interventional2020-10-22Recruiting
A Phase IV, 2x2 Factorial, Double Blind Study of 48 Versus 96 Weeks of PEGASYS 180µg, With or Without 24 Weeks of Entecavir in Adult Patients With HBeAg Negative Chronic Hepatitis B. [NCT01179594]Phase 40 participants (Actual)Interventional2010-09-18Withdrawn(stopped due to This study was canceled for operational reasons.)
A Phase 2a, Multi-center, Double-blind, Placebo-controlled Study Evaluating ABI-H0731 as Adjunctive Therapy in Virally-suppressed Patients With Chronic Hepatitis B [NCT03576066]Phase 273 participants (Actual)Interventional2018-06-11Completed
A Study of the Safety and Efficacy of Entecavir Plus Tenofovir in Adults With Chronic Hepatitis B Virus Infection With Previous Nucleoside/Nucleotide Treatment Failure [NCT01063036]Phase 3144 participants (Actual)Interventional2010-05-31Completed
Efficacies of Entecavir Add on HBeAg Negative Chronic Hepatitis B Patients With HBV DNA Load ≥1000 Copies/ml After 3 Months of Peginterferon Alpha 2a Treatment [NCT02365402]Phase 4180 participants (Anticipated)Interventional2013-01-31Recruiting
Efficacies of Entecavir Add on Chronic Hepatitis B Patients With HBV DNA Load ≥1000 Copies/ml After 6 Months Treatment of Peginterferon Alpha 2a [NCT02368288]Phase 4200 participants (Anticipated)Interventional2013-01-31Recruiting
A Prospective Randomized Clinical Trial of Combination Sequential Treatment With Y Peginterferon Alfa-2b and ETV (Entecavir) in CHB (Chronic Hepatitis B) Patients NAs (Nucleotides or Nucleosides) Experienced (Anchor Study) [NCT02327416]Phase 3300 participants (Anticipated)Interventional2014-10-31Recruiting
Continuation of Lamivudine Plus Adefovir Versus Switching to Entecavir Plus Adefovir in Adults With Chronic Hepatitis B Who Have Resistant Mutants to Lamivudine and Show Suboptimal Response to Combination of Lamivudine Plus Adefovir [NCT01023217]Phase 490 participants (Actual)Interventional2009-11-30Completed
A Open-label, Single Center Drug Interaction Study of Morphothiadine Mesilate/Ritonavir , Entecavir and Tenofovir Disoproxil Fumarate in Healthy Subjects [NCT03662568]Phase 156 participants (Actual)Interventional2018-06-26Completed
A Sequential Phase 1a/1b Dose-Escalating Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Antiviral Activity of ARC-521 in Normal Adult Volunteers and Patients With Chronic Hepatitis B [NCT02797522]Phase 147 participants (Actual)Interventional2016-06-30Terminated(stopped due to Company decision to discontinue trial)
Phase4, to Compare Efficacy and Safety of Therapeutic Vaccination With Intensified Schedule Plus Pegylated Interferon Dual Therapy on Seroclearance of HBS Antigen in Patients With Complete Virological Response Induced by Entecavir [NCT02097004]Phase 4111 participants (Actual)Interventional2014-04-30Completed
A Multi-center, Randomized, Controlled Study to Evaluate the Efficacy and Safety of Generic Entecavir Monotherapy or in Combination With Adefovir for Chronic Hepatitis B Patients With Inadequate Response to NUC Therapy [NCT01341743]Phase 4360 participants (Anticipated)Interventional2010-12-31Active, not recruiting
Efficacy and Safety Study of Adefovir and Entecavir for Elderly With Chronic Hepatitis B [NCT02075294]242 participants (Actual)Observational2010-01-31Completed
A Phase 2a, Randomized, Double-blind, Placebo-controlled Study of Oral FXR Modulator EYP001a Combined With Nucleos(t)Ide Analogues (NA) in Virologically Suppressed Chronic Hepatitis B Patients to Improve Functional Cure Rates [NCT04465916]Phase 226 participants (Actual)Interventional2020-05-12Terminated(stopped due to DSMC reviewed results of 26 subjects. New randomizations were stopped. Already randomized subjects were followed up to W40.)
A Study in Reversing Hepatic Fibrosis or Cirrhosis Related to Hepatitis B Virus and Finding Biomarkers [NCT03568578]450 participants (Anticipated)Interventional2018-01-28Recruiting
A Prospective Open Label Control Study to Evaluate the Efficacy and Safety of Entecavir Treatment of Patients With Acute on Chronic Hepatitis B Liver Failure [NCT01254994]Phase 2108 participants (Actual)Interventional2007-08-31Completed
A Single-Center, Open-Label, Randomized, Single-Dose, Two-Period, Two-Sequence, Crossover Study to Assess the Bioequivalence of Entecavir Tablets 1.0 mg With Baraclude® 1.0 mg in Healthy Adult Subjects Under Fasting Conditions [NCT03847246]26 participants (Actual)Interventional2018-12-04Completed
A Prospective, Randomized, Multicenter, Open-label, Exploratory Study of Utilizing of Peginterferon Alfa-2a on the Relapse Rate of the Subjects With Hepatocellular Carcinoma Who Have Been Treated by Resection [NCT03253250]Phase 4432 participants (Anticipated)Interventional2017-09-01Recruiting
Metformin as Add-on to the Standard Therapy in Patients With Chronic Hepatitis B: A Randomized, Double-Blind, Placebo-Controlled Trial [NCT04182321]60 participants (Actual)Interventional2020-03-13Completed
Randomized, Open-Label, Comparative Study to Evaluate Early Viral Load Reductions and Exploratory Viral Kinetics Following Administration of Entecavir or Adefovir in Nucleoside-Naive Adults With Chronic Hepatitis B Infection [NCT00096785]Phase 369 participants (Actual)Interventional2004-12-31Completed
Clinical Pharmacokinetics of Tyrosine Kinase Inhibitors in Chinese Patients of Hepatitis B [NCT03680183]300 participants (Anticipated)Observational [Patient Registry]2018-05-22Recruiting
A Phase II Study of Durvalumab (MEDI 4736) for Advanced Hepatocellular Carcinoma in Patients With Active Chronic Hepatitis B Virus Infection [NCT04294498]Phase 243 participants (Anticipated)Interventional2020-11-02Recruiting
A Phase II Study of the Safety and Efficacy of Adding Entecavir to Current Lamivudine Therapy in HIV and HBV Co-Infected Patients Who Have Hepatitis B Viremia While Being Treated With Lamivudine [NCT00051038]Phase 2/Phase 30 participants Interventional2002-09-30Completed
[NCT00036608]Phase 30 participants Interventional2002-01-31Completed
A Randomized Phase 2a, Multicenter, Open-Label, Multiple-Cohort Study Evaluating Regimens Containing Vebicorvir in Subjects With Chronic Hepatitis B Virus Infection [NCT04820686]Phase 265 participants (Actual)Interventional2021-05-07Terminated(stopped due to Sponsor decision)
A Phase 1b/2a, Dose-Ranging Study of the Safety, Tolerability, Pharmacokinetics, and Initial Efficacy of ABI-H0731 in Patients With Chronic Hepatitis B [NCT03109730]Phase 1/Phase 238 participants (Actual)Interventional2017-06-15Completed
A Study to Describe the Antiviral Effect of Entecavir (ETV) in Blacks/African Americans and Hispanics With Chronic Hepatitis B Virus (HBV) Infection Who Are Nucleoside-Naive [NCT00371150]Phase 4131 participants (Actual)Interventional2006-11-30Completed
A Phase II Study in Japan of the Safety And Antiviral Activity of Entecavir (BMS-200475) in Adults With Chronic Hepatitis B With Incomplete Response to Current Lamivudine Therapy [NCT01037166]Phase 284 participants (Actual)Interventional2002-12-31Completed
Investigator Initiated Study of Thymosin in HBV-related HCC [NCT02281266]Phase 4360 participants (Anticipated)Interventional2015-01-31Not yet recruiting
Phase 1, Randomized, Double-Blind, Placebo-Controlled, Multiple Ascending Dose, Safety, Tolerability and Pharmacokinetics Study of Birinapant in Subjects With Chronic Hepatitis B [NCT02288208]Phase 17 participants (Actual)Interventional2014-11-30Terminated(stopped due to Due to cranial nerve palsies observed)
A Phase 2, Double-Blind, Randomized, Placebo-Controlled Study of FG-3019 in Subjects With Liver Fibrosis Due to Chronic Hepatitis B Infection [NCT01217632]Phase 2114 participants (Actual)Interventional2010-08-31Terminated(stopped due to Study terminated due to an unexpected prominent effect of entecavir alone in this patient population.)
A Randomized, Multi Center, Phase IIIb Open-label Study to Evaluate the Efficacy of Sequential Therapy of Peginterferon Alfa-2a(Pegasys(TM)) Following Entercavir Compared With Peginterferon Alfa-2a Monotherapy in Patient With HBeAg Positive Chronic Hepati [NCT01220596]Phase 3228 participants (Anticipated)Interventional2010-06-30Recruiting
The Beneficial Effect of Vitamin D Supplement to Peg Interferon Alpha 2a or to Telbivudine Monotherapy in Patients With Chronic HBV Viral Infection [NCT01083251]120 participants (Anticipated)Interventional2010-03-31Recruiting
Effect of Entecavir Treatment on Regression and Long-term Disease Outcome in Patients With HBV-induced Liver Fibrosis and Cirrhosis (Regress Extension Study) [NCT02849132]Phase 4800 participants (Anticipated)Interventional2016-01-31Active, not recruiting
Comparison of the Efficacy and Safety of Entecavir Versus Adefovir in Subjects Chronically Infected With Hepatitis B Virus and Evidence of Hepatic Decompensation [NCT00065507]Phase 3195 participants (Actual)Interventional2003-08-31Completed
Dose-Ranging Study to Evaluate the Safety, Efficacy and Pharmacokinetics of Pegylated Interferon Lambda (BMS-914143) Monotherapy in Interferon-Naive Patients With Chronic Hepatitis B Virus Infection Who Are HBeAg-positive [NCT01204762]Phase 2197 participants (Actual)Interventional2010-11-30Completed
An Open-Label Rollover Study of Entecavir (BMS-200475) in Adults With Chronic Hepatitis B Infection Who Have Completed Previous Phase II Studies in Japan But Who Require Further Treatment [NCT01037062]Phase 2282 participants (Actual)Interventional2003-12-31Completed
[NCT01139203]300 participants (Anticipated)Interventional2009-08-31Recruiting
Induction of HBsAg Decline Using an add-on Treatment of Peginterferon Alfa-2a in HBeAg-negative Chronic Hepatitis B Patients Treated With Nucleos(t)Ide Analogous (PAS) [NCT01373684]Phase 490 participants (Actual)Interventional2012-05-25Completed
A Multinational, Multi-center, Open, Comparative, Paralleled, Roll-over Study to Assess the Safety and Antiviral Activity of LB80380 Tablet Compared to Entecavir 0.5 mg After Additional 48 Weeks of Treatment in Chronic Hepatitis B Patients Who Have Comple [NCT01242787]Phase 2115 participants (Anticipated)Interventional2010-08-31Active, not recruiting
A Multicenter, Extension Study of the Safety and Efficacy of Multi-dose Intravenous ARC-520 in Combination With Entecavir or Tenofovir in Patients With Chronic Hepatitis B Virus (HBV) Infection [NCT02738008]Phase 212 participants (Actual)Interventional2016-03-31Terminated(stopped due to Company decision to discontinue trial)
A Multicenter, Randomized, Open-label Control Study to Evaluate Efficacy and Safety of Combination Therapy of Thymalfasin and Entecavir in HBeAg-positive ETV-experienced Patients [NCT03448744]Phase 4240 participants (Anticipated)Interventional2017-10-25Recruiting
A Study to Compare and Evaluate Intrahepatic cccDNA Reduction After Administrating Clevudine or Entecavir in the Chronic HBV Patients [NCT01266005]Phase 475 participants (Anticipated)Interventional2009-08-31Terminated
The Effect of Entecavir Consolidation on Post-TDF Treatment Durability [NCT03308890]Phase 4156 participants (Anticipated)Interventional2017-11-01Not yet recruiting
A Comparative Study of the Antiviral Efficacy and Safety of Entecavir (ETV) Versus Placebo in Pediatric Subjects With Chronic Hepatitis B Virus (HBV) Infection Who Are HBeAg-Positive [NCT01079806]Phase 3180 participants (Actual)Interventional2010-06-30Completed
Randomized, Open-Labeled Study Evaluating the Antiviral Efficacy, Safety, and Tolerability of Continuing Lamivudine Therapy or Switching to Entecavir in Subjects With Chronic Hepatitis B Who Achieved Undetectable HBV DNA [NCT00637663]Phase 472 participants (Actual)Interventional2008-02-29Completed
A Randomized, Parallel, Single-Dose Study to Evaluate the Pharmacokinetics of a Test Formulation of Entigin Film Coated Tablet 0.5mg (Entecavir 0.5 mg), Compared to an Equivalent Dose of a Reference Drug Product (Baraclude 0.5mg Tablets) in Healthy Adult [NCT02850848]Phase 439 participants (Actual)Interventional2015-12-31Completed
Efficacy of Switch or Sequential Combination Therapy of Pegylated Interferon Alfa-2a in Chronic Hepatitis B Patients With Low HBsAg and HBeAg Titers After Long-term Entecavir Therapy: A Multicenter, Prospective Cohort Study [NCT02589652]294 participants (Anticipated)Observational2015-10-31Not yet recruiting
Efficacy of Antiviral Therapy With Lamivudine or Entecavir After Radical Resection for Hepatitis B Virus-Related Hepatocellular Carcinoma [NCT00768157]Phase 4200 participants (Anticipated)Interventional2007-04-30Recruiting
A Randomized, Controlled Study to Evaluate the Efficacy and Significant of the Anti-virus Therapy for the Unresectable Hepatitis B Virus-related Primary Liver Cancer [NCT00824707]200 participants (Actual)Interventional2008-12-31Completed
A Phase II Study in Japan of the Safety and Antiviral Activity of Entecavir (BMS-200475) in Adults With Chronic Hepatitis B Infection [NCT01020565]Phase 260 participants (Anticipated)Interventional2003-02-28Completed
A Study of the Safety and Antiviral Activity of Open-Label Entecavir (BMS-200475) in Adults With Chronic Hepatitis B Infection Who Have Completed Dosing in a Previous Phase II/III Study in China [NCT00975091]Phase 3600 participants (Actual)Interventional2004-05-31Completed
Combination Entecavir and Peginterferon Therapy in HBeAg-Positive Immune-Tolerant Adults With Chronic Hepatitis B [NCT01369199]Phase 328 participants (Actual)Interventional2012-05-31Terminated
A Multicenter, Randomized, Double-blind, Placebo-controlled Multi-dose Study to Determine the Depth of Hepatitis B Surface Antigen (HBsAg) Reduction Following Intravenous ARC-520 in Combination With Entecavir or Tenofovir in Patients With HBeAg Positive, [NCT02604212]Phase 232 participants (Actual)Interventional2015-11-30Terminated(stopped due to Company decision to discontinue trial)
Clinical Trial of Entecavir/Pegylated Interferon in Immune Tolerant Children With Chronic HBV Infection (HBRN) [NCT01368497]Phase 360 participants (Actual)Interventional2012-09-30Completed
A Single and Repeated Dose Escalation, Phase I Clinical Study to Evaluate the Safety, Pharmacokinetics and Preliminary Pharmacodynamics of RBD1016 in Subjects With Chronic Hepatitis B Virus (HBV) Infection [NCT05017116]Phase 140 participants (Actual)Interventional2021-08-09Completed
A Phase IIb, Open, Multinational, Multi-center, Randomised, Comparative, Parallel Study to Assess the Safety and Antiviral Activity of LB80380 Compared to Entecavir 0.5 mg in Chronic Hepatitis B Patients for 48 Weeks With a Planned Analysis of Efficacy an [NCT01026610]Phase 2115 participants (Actual)Interventional2009-08-31Completed
A Clinical Study to Evaluate the Steady State Pharmacokinetics of Baraclude in Participants With Hepatitis B Virus Infection [NCT03083821]Phase 16 participants (Actual)Interventional2017-05-16Completed
A Randomized, Prospective, Multicenter, Open-label Study to Evaluate the Efficacy of Telbivudine With or Without add-on Tenofovir According to Roadmap Strategy Compare With Entecavir in HBeAg-positive Chronic Hepatitis B Patients [NCT01588912]Phase 4104 participants (Anticipated)Interventional2012-04-30Recruiting
A Comparative Study of Entecavir vs Adefovir Plus Lamivudine vs Combination Entecavir Plus Adefovir in Lamivudine-Resistant Chronic Hepatitis B Chinese Subjects [NCT00986778]Phase 40 participants (Actual)Interventional2009-12-31Withdrawn(stopped due to Business Objectives Changed)
"A Prospective, Randomized, Multicenter, Open-label, Exploratory Study of Utilizing of Response-Guided-Therapy (RGT) Strategy on Optimal Nucleoside Analogue (NUC)-Experienced Patients" [NCT02560649]Phase 4324 participants (Anticipated)Interventional2015-05-31Active, not recruiting
A Phase IV Study of the Antiviral Activity and Safety of Entecavir Versus Lamivudine in Adults With Chronic Hepatitis B Infection Who Are Negative for Hepatitis B e Antigen in Korea [NCT00393484]Phase 4122 participants (Actual)Interventional2007-02-28Completed
"A Phase Randomized Open Labelled Controlled Dose Escalation Study of Repeated Administration of CYT107 (Glyco-r-hIL-7) Added on Antiviral Treatment and Vaccination in HBeAg-negative Chronic Hepatitis B-infected Patients" [NCT01027065]Phase 1/Phase 224 participants (Anticipated)Interventional2009-12-31Active, not recruiting
Evaluation of the Pharmacokinetics, Safety, Tolerability and Efficacy of Entecavir (ETV) in Pediatric Subjects With Chronic Hepatitis B Virus (HBV) Infection Who Are HBeAg-Positive [NCT00423891]Phase 1/Phase 264 participants (Actual)Interventional2007-06-30Completed
An Open, Randomized Controlled Clinical Trial to Compare the Prophylactic Use or Preemptive Use of an Anti-viral Drug Entecavir in Patients With Colorectal Cancer Who Are Inactive Hepatitis B Carriers [NCT02777814]Phase 250 participants (Anticipated)Interventional2015-05-01Recruiting
A Randomized, Prospective, Comparative Study of the Effectiveness of Prophylactic Entecavir Treatment for HBV Reactivation in Past HBV Infected Patients With Hematopoietic Stem Cell Transplantation [NCT04942886]164 participants (Anticipated)Interventional2021-08-21Enrolling by invitation
Effects of Antiviral Therapy on HBV Reactivation and Liver Function After Hepatectomy for HBV-DNA Negative HBV-related Hepatocellular Carcinoma [NCT02829359]Phase 2/Phase 3200 participants (Actual)Interventional2012-07-31Completed
An Exploratory Study to Evaluate The Efficacy And Safety of HLX10, A Humanized Monoclonal Antibody Targeting Programmed Death-1 (PD-1) Protein In Chronic Hepatitis B Patients [NCT04133259]Phase 244 participants (Anticipated)Interventional2019-12-31Recruiting
An Open, Randomized Controlled Clinical Trial to Compare the Prophylactic Use or Preemptive Use of an Anti-viral Drug Entecavir in Patients With Gastric Cancer Who Are Inactive Hepatitis B Carriers [NCT02777801]Phase 250 participants (Anticipated)Interventional2015-06-30Recruiting
Maintaining Antiviral Efficacy After Switching to Generic Entecavir, Baracle® in Patients Taking Baraclude® 1 mg for Antiviral Resistant Chronic Hepatitis B; A Noninferiority Study Assessing Non-detection Rate of Hepatitis B Virus DNA [NCT04069858]Phase 440 participants (Actual)Interventional2016-12-01Active, not recruiting
The Different Effects of Nucleotide and Nucleoside Analogues on the Prognosis of Hepatitis B Virus-Related Hepatocellular Carcinoma Patients After Curative Resection:a Randomized Controlled Trial [NCT04032860]Phase 4104 participants (Actual)Interventional2017-07-01Active, not recruiting
Incidence of Hepatitis B Reactivation in Non-Hodgkin's Lymphoma Patients Who Receive Rituximab-containing Chemotherapy and Are Previously Infected With Hepatitis B Virus [NCT00931229]202 participants (Actual)Interventional2009-06-30Active, not recruiting
Prevention of HBV Reinfection After Liver Transplantation Using Entecavir Monotherapy After Short-term HBIg Administration: A Pilot Study [NCT01046799]Phase 320 participants (Anticipated)Interventional2008-03-31Completed
Randomized Clinical Study of Arabinoxylan Rice Bran (MGN-3/Biobran) for the Treatment of Hepatocellular Carcinoma and Hepatitis B and C Infection [NCT01018381]130 participants (Actual)Interventional2006-06-30Completed
A Phase 2, Open-label, Single-arm, Multicenter Study to Assess Efficacy, Safety, Tolerability, and Pharmacokinetics of Treatment With JNJ-73763989, JNJ-56136379, Nucleos(t)Ide Analogs, and Pegylated Interferon Alpha-2a in Virologically Suppressed Patients [NCT04667104]Phase 248 participants (Actual)Interventional2021-02-01Completed
A Randomized, Placebo-Controlled, Open-label, Multi-Center Study to Assess the Efficacy and Safety of Fuzheng Huayu Combined With Entecavir and Carvedilol in Moderate and Severe Cirrhotic Portal Hypertension Due to Hepatitis B Virus [NCT02945982]Phase 4184 participants (Anticipated)Interventional2018-04-05Recruiting
A Comparative Study of the Week 12 Antiviral Efficacy and Safety of Switching to Entecavir vs. Continuing Adefovir Treatment in Adults With Chronic Hepatitis B and Suboptimal Response to Adefovir [NCT00718887]Phase 4228 participants (Actual)Interventional2008-07-31Completed
Risk of Hepatocellular Carcinoma in Patients Treated With ETV vs TDF for Chronic Hepatitis B With Compensated Cirrhosis: A Multicenter, Real-world and Respective Study [NCT04160897]4,000 participants (Anticipated)Observational2019-10-22Enrolling by invitation
[NCT02588937]Phase 476 participants (Anticipated)Interventional2015-10-31Active, not recruiting
A Randomized, Open-label, 3-way Crossover Clinical Trial to Evaluate the Food Effect on the Pharmacokinetics and Safety of Single-dose Cavir Tab. 0.5mg With Baraclude Tab. 0.5mg in Healthy Male Volunteers [NCT02586363]Phase 130 participants (Anticipated)Interventional2015-11-30Active, not recruiting
A Clinical Trial on Hepatitis B Vaccine Activated-Dendritic Cells Combined With Anti-HBV Drugs in Chronic Hepatitis B [NCT02615639]Phase 1/Phase 2450 participants (Anticipated)Interventional2015-11-30Not yet recruiting
Direct Antiviral Agents for the Treatment of Chronic HCV/HBV Co-infection Patients [NCT02555943]Phase 2/Phase 323 participants (Actual)Interventional2015-02-28Completed
Randomized, Open-Labelled Study Evaluating the Antiviral Efficacy, Safety, and Tolerability of Continuing Lamivudine Therapy or Switching to Entecavir in Subjects With Chronic Hepatitis B With Detectable HBV DNA [NCT00625560]Phase 472 participants (Actual)Interventional2008-02-29Completed
A Phase 1, Randomized, Double-blind, Placebo-controlled, Single- and Multiple-dose Study in Healthy Subjects and Chronic Hepatitis B Subjects to Evaluate the Safety, Tolerability, Pharmacokinetics and Antiviral Activity of Freethiadine [NCT05391360]Phase 1128 participants (Actual)Interventional2021-10-11Completed
A Single-center, Randomized, Double-blind, Single and Multiple Dosing, Evaluation HEC121120 Tolerance in Healthy Subjects and Patients With Chronic Hepatitis B, Pharmacokinetics Characteristics and Antiviral Activity of Ⅰ Phase of Study [NCT04536532]Phase 1/Phase 2126 participants (Anticipated)Interventional2020-10-12Suspended(stopped due to New investigational drug on the same target already in clinical trials)
Evaluate the Safety, Tolerability, and Antiviral Activity of GLS4 With Ritonavir in Combination With Entecavir in Comparison With Entecavir Alone in Patients With Chronic HBV Who Are HBeAg Positive [NCT04147208]Phase 2250 participants (Anticipated)Interventional2019-02-28Recruiting
An Open-Label Phase 2 Study to Evaluate Safety and Efficacy of QL-007 Tablets in Combination With Entecavir or Tenofovir in Patients With Chronic Hepatitis b Who Have Received Nucleoside (Acid) Therapy : a Multicenter, Randomized, Positive Controlled Clin [NCT04157257]Phase 260 participants (Anticipated)Interventional2019-07-26Recruiting
Entecavir and Peginterferon Alfa-2a Sequential Therapy Versus Peginterferon Alfa-2a Monotherapy for HBeAg Positive Chronic Hepatitis B [NCT00921180]Phase 4148 participants (Anticipated)Interventional2007-02-28Recruiting
Clinical Investigation About Therapeutic Effects and Long-term Follow-up After Ending Anti-hepatitis B Virus Therapy With Nucleos(t)Ide Analogs in Patients With Chronic Hepatitis b [NCT02883647]100 participants (Anticipated)Observational2014-01-31Recruiting
A Study on Optimizing HBeAg Seroconversion in HBeAg Positive CHB Patients With Combination or Sequential Treatment of Pegylated Interferon Alpha-2a and Entecavir [NCT00940485]Phase 4200 participants (Actual)Interventional2009-04-30Completed
Exploratory Study on Antiviral Therapy for Patients With Chronic Hepatitis B Virus Infection (Immune Tolerance Period) [NCT05382351]Phase 2238 participants (Anticipated)Interventional2022-05-10Recruiting
Randomed and Double-blinded Phase II Clinical Trial of Hydronidone Capsules(F351) in Patients With Liver Fibrosis Induced by HBV Chronic Hepatitis [NCT02499562]Phase 2168 participants (Actual)Interventional2015-06-25Completed
A Phase II Multi-center, Randomized, Single-blind, Placebo-controlled to Evaluate Safety and Efficacy of ASC42 Tablets in Combination With Entecavir and Pegylated Interferon α-2a in Subjects With Chronic Hepatitis B Virus [NCT05107778]Phase 243 participants (Actual)Interventional2022-01-10Active, not recruiting
Pegasys Plus Entecavir Versus Entecavir Alone for Hepatitis Be Antigen-Positive Chronic Hepatitis B [NCT00597259]Phase 4294 participants (Anticipated)Interventional2008-01-31Recruiting
Augmenting Response to Entecavir Using a Temporary Peginterferon Alpha-2a add-on Strategy for the Treatment of HBeAg-positive Chronic Hepatitis B [NCT00877760]Phase 4184 participants (Actual)Interventional2009-08-31Completed
A Pilot Trial of Simvastatin Alone and Added to Tenofovir or Entecavir for the Treatment of Chronic Hepatitis B [NCT00994773]Phase 132 participants (Actual)Interventional2009-12-31Completed
Prophylactic Use of Entecavir for Chemotherapy Associated With Hepatitis B Reactivation in HBsAg (-), Anti-HBc (+) Non-Hodgkin's Lymphoma Patients: a Randomized Controlled Trial [NCT00926757]Phase 480 participants (Actual)Interventional2009-04-30Completed
Randomized, Double-blind, Placebo-controlled Phase Ib/IIa Clinical Trial to Evaluate the Efficacy and Safety of TQA3605 Tablets Monotherapy or in Combination With Nucleoside (Acid) Analogues in Treatment-naïve Patients and Treated Patients With Chronic He [NCT06150014]Phase 1/Phase 264 participants (Anticipated)Interventional2023-12-07Recruiting
Entecavir and Peginterferon Alfa-2a Sequential Therapy Versus Peginterferon Alfa-2a Monotherapy for HBeAg Negative Chronic Hepatitis B [NCT00917761]Phase 4300 participants (Anticipated)Interventional2007-02-28Recruiting
A Phase 2, Double-Blind, Multi-center, Randomized Study Comparing Tenofovir Disoproxil Fumarate, Emtricitabine Plus Tenofovir Disoproxil Fumarate, and Entecavir in the Treatment of Chronic Hepatitis B Subjects With Decompensated Liver Disease and in the P [NCT00298363]Phase 2112 participants (Actual)Interventional2006-04-30Completed
Combination or Sequential Therapy of Peginterferon Alfa-2a and Entecavir for Hepatitis B e Antigen-positive Patients With Chronic Hepatitis B [NCT01906580]Phase 4105 participants (Anticipated)Interventional2011-07-31Recruiting
A Randomized Phase 2a, Multicenter, Open-label Study Evaluating ABI-H0731-Containing Regimens in Patients With Chronic Hepatitis B [NCT04781647]Phase 254 participants (Actual)Interventional2021-02-18Terminated(stopped due to Study ABI-H0731-203 was terminated early by the study Sponsor for strategic reasons to prioritize research and development efforts on finite and curative HBV therapies.)
A Randomized, Placebo-Controlled, Open-label, Multi-Center Study to Assess the Efficacy and Safety of Fuzheng Huayu Combined With Entecavir in Low-grade Cirrhotic Portal Hypertension Due to Hepatitis B Virus [NCT02945956]Phase 4192 participants (Anticipated)Interventional2018-04-05Recruiting
A Randomized, Open Label, Phase IV, Multicenter Study for Efficacy and Safety of Lamivudine Versus Entecarvir Therapy in HBV-related Advanced Liver Disease Patients With High Viral Load and Normal or Slightly Elevated Transaminase [NCT00823550]Phase 4462 participants (Anticipated)Interventional2009-01-31Active, not recruiting
A Phase Ib Dose-Escalation Study to Assess the Safety and Tolerability of DV-601 in Subjects With Chronic Hepatitis B on Concurrent Treatment With a Nucleoside Analogue [NCT01023230]Phase 114 participants (Actual)Interventional2009-09-30Completed
A Comparative Study of Entecavir vs. Adefovir Plus Lamivudine vs Combination Entecavir Plus Adefovir in Lamivudine-resistant Chronic Hepatitis B Subjects: The DEFINE Study [NCT00410202]Phase 3629 participants (Actual)Interventional2008-03-31Completed
The Antiviral Efficacy of Entecavir in Chronic Hepatitis B Within the European Network of Excellence (VIRGIL) [NCT01323452]418 participants (Actual)Observational2010-11-30Completed
Randomized, Observational Study of Entecavir to Assess Long-term Outcomes Associated With Nucleoside/Nucleotide Monotherapy for Patients With Chronic HBV Infection: The REALM Study [NCT00388674]12,522 participants (Actual)Observational2006-12-18Completed
A Comparative Study of Chronic Hepatitis B Subjects Treated With Entecavir Plus Tenofovir Combination Therapy vs. Entecavir Monotherapy in Adults Who Are Treatment-Naive to Nucleosides and Nucleotides: The BE-LOW Study [NCT00410072]Phase 3669 participants (Actual)Interventional2007-04-30Completed
Chemoembolization With or Without Antiviral Therapy for Unresectable HBV-related Hepatocellular Carcinoma With Low HBV DNA Replication: Effectiveness and Safety. A Prospective and Randomized Clinical Trial [NCT01894269]Phase 4200 participants (Anticipated)Interventional2013-07-31Recruiting
Propylactic Use of Entecavir for Biological Agents Associated Hepatitis B Virus Reactivation in Inflammatory Arthritis Patients: a Randomized Controlled Trial [NCT01907230]Phase 4115 participants (Actual)Interventional2013-09-10Active, not recruiting
A Multicenter, Double-blind, Active-controlled, Randomized, Parallel Group Study to Demonstrate the Comparison and Evaluation of Baracle Tab.® and Baraclude Tab.® for HBeAG Chronic Hepatitis B [NCT01913431]Phase 4118 participants (Actual)Interventional2013-09-12Completed
Entecavir Versus Lamivudine for Preventing the Risk of Hepatitis B Virus Reactivation in Patients With Non-Hodgkin Lymphoma on CHOP/R-CHOP: a Randomized Phase II Study [NCT01914744]Phase 282 participants (Anticipated)Interventional2013-02-28Recruiting
[NCT01918631]36 participants (Actual)Interventional2013-08-31Completed
Optimized Treatment and Regression of HBV-induced Liver Fibrosis [NCT01938781]Phase 4400 participants (Actual)Interventional2013-06-30Completed
Optimized Treatment and Regression of HBV-induced Early Cirrhosis [NCT01938820]Phase 482 participants (Actual)Interventional2013-06-30Completed
Optimized Treatment and Regression of HBV-induced Compensated Liver Cirrhosis [NCT01943617]Phase 4606 participants (Actual)Interventional2013-06-30Completed
A Multicenter, Open-label, Phase II Clinical Study to Evaluate the Safety and Efficacy of APG-1387 in Combination With Entecavir in Patients With Chronic Hepatitis B [NCT04568265]Phase 2122 participants (Anticipated)Interventional2020-06-03Recruiting
Randomized, Open-Labeled Study Evaluating the Antiviral Efficacy, Safety, and Tolerability of Continuing Lamivudine Therapy or Switching to Entecavir in Subjects With Chronic Hepatitis B Who Achieved Undetectable HBV DNA [NCT00625339]Phase 472 participants (Actual)Interventional2008-02-29Completed
A Comparative Study of the Efficacy and Safety of Entecavir and Tenofovir Versus Entecavir Alone in the Treatment of Hepatitis B DNA-positive Patients With Lymphomas [NCT04539119]Phase 3120 participants (Anticipated)Interventional2020-07-03Recruiting
An Open-label, Dose-escalating Clinical Study to Evaluate the Tolerability, Immunogenicity and Efficacy of HB-110 Administered by Electroporation (EP) in an Add-on Therapy With Entecavir in Chronic Hepatitis B Patients [NCT01641536]Phase 19 participants (Actual)Interventional2011-11-30Completed
A Randomized, Open Labeled, Multicenter Study Comparing Entecavir Versus Lamivudine as Antiviral Prophylaxis for Patients With Hepatitis B Infection Undergoing Cytotoxic Chemotherapy for Malignant Tumors [NCT01580202]Phase 3180 participants (Actual)Interventional2012-04-30Completed
A Randomized, Double-blind, Multicenter Phase II Clinical Trial to Evaluate the Efficacy and Safety of Therapeutic Hepatitis B Vaccine (Mimogen-based) Joint Entecavir in Treating HBeAg Positive Chronic Hepatitis B Patients [NCT01326546]Phase 2378 participants (Actual)Interventional2010-06-30Completed
A Randomized, Open Label Study of the Effect of Peginterferon Alfa-2a (40KD) (PEGASYS®) Plus Entecavir (Baraclude®) Combination Therapy on Quantitative Changes in HBeAg in Treatment-naive Patients With HBeAg Positive Chronic Hepatitis B [NCT00614471]Phase 4219 participants (Actual)Interventional2007-08-31Completed
Entecavir for Patients With Decompensated HBV-Related Cirrhosis:a Prospective Randomized Controlled Trial [NCT00663182]Phase 4200 participants (Anticipated)Interventional2008-01-31Enrolling by invitation
A Randomized, Double-blinded, Placebo-controlled, Phase IIa Study of TQ-A3334 Combined With Entecavir in the Treatment of Untreated or HBV DNA Negative Subjects With Chronic Hepatitis B [NCT04180150]Phase 212 participants (Anticipated)Interventional2019-11-18Recruiting
Pharmacokinetic Interactions Between Hydronidone and Entecavir Capsules in Healthy Chinese Subjects(Single Center, Single Arm, Open, Self - Control) [NCT04124081]Phase 112 participants (Actual)Interventional2019-05-15Completed
A Treatment Use Protocol of Entecavir in Subjects With Chronic Hepatitis B Infection Who Have Failed or Who Are Intolerant of Available Therapies [NCT00096811]0 participants Expanded Access2003-09-30No longer available
Lamivudine Therapy in Patients With Prior Entecavir Treatment and Undetectable Viral Load [NCT01013272]50 participants (Actual)Interventional2007-06-30Completed
A Phase Ib, Open Label Study to Assess the Safety and Efficacy of Sequential Administration of P1101 and Anti-PD1 in Interferon-Naive Adults With Chronic Hepatitis B or D Infection [NCT04638439]Phase 120 participants (Anticipated)Interventional2021-12-31Recruiting
A Phase 1a/1b, Dose-Ranging Study of the Safety, Tolerability, Pharmacokinetics, and Initial Efficacy of ABI-H0731 in Healthy Volunteers and Patients With Chronic Hepatitis B [NCT02908191]Phase 186 participants (Actual)Interventional2016-11-30Completed
The Use of Novel Hepatitis B Virus (HBV) Biomarkers to Detect Occult HBV Infection in Liver Donors Positive for Antibody to Hepatitis B Core Antigen (Anti-HBc) in Liver Transplantation [NCT04199819]100 participants (Anticipated)Interventional2022-01-01Recruiting
A Phase 1b/2a Randomized, Open-label Clinical Trial of Daily Myrcludex B Versus Entecavir in Patients With HBeAg Negative Chronic Hepatitis B [NCT02881008]Phase 1/Phase 248 participants (Actual)Interventional2012-11-14Completed
Phase IV Study of the Efficacy of Entecavir in Patients With Chronic Hepatitis B Virus Infection and Persistently Normal Alanine Aminotransferase [NCT01833611]Phase 4130 participants (Anticipated)Interventional2008-09-30Active, not recruiting
A Randomized Design Study to Compare the Efficacy of Pegylated Interferon Alpha-2b Monotherapy Versus Combination With Entecavir in HBeAg-negative Chronic Hepatitis B: Role of Host and Viral Factors Associated With Treatment Response [NCT01243281]126 participants (Anticipated)Interventional2011-03-31Recruiting
A Multicenter, Open-label, Prospective Study to Evaluate Antiviral Efficacy and Safety of Entecavir Plus Tenofovir Combination in Subjects With Multi-drug Resistant Chronic Hepatitis B Virus Infection [NCT01594905]Phase 490 participants (Anticipated)Interventional2012-08-31Active, not recruiting
Prospective Randomized Study for the Comparison of Adding Adefovir Dipivoxil and Switching to Entecavir in Patients With Lamivudine-resistant Chronic Hepatitis B [NCT00531167]Phase 4219 participants (Actual)Interventional2007-04-30Completed
A Randomized, Double-blinded, Phase 3, Multicenter, Investigator-initiated Trial for Entecavir for Prophylaxis of Hepatitis B Virus (HBV) Reactivation in HBV Surface Antigen or Anti-HBc Positive Patients Undergoing Anti-TNFα Treatment [NCT01694264]Phase 343 participants (Actual)Interventional2012-09-01Terminated(stopped due to Delayed recruitment, unable to meet calculated sample size)
Prophylactic Use of Entecavir to Reduce Hepatitis Flare in Highly Viremic HBV Patients With Active Tuberculosis Receiving Anti-tuberculous Treatment [NCT01724723]Phase 450 participants (Anticipated)Interventional2012-12-31Not yet recruiting
Clinical and Basic Research of Relationship Between Hepatitis B Virus Quasi-Species Evolution and Function of Natural Killer Cells With Antiviral Therapy Response in Chronic Hepatitis B Patients [NCT03164889]80 participants (Actual)Interventional2017-01-31Terminated(stopped due to no enough participant can be enrolled)
The Efficacy and Safety of Switching to Vemliver Tab (Tenofovir Alafenamide Hemitartrate) From Entecavir in Chronic Hepatitis B Patients Who Pretreated With Entecavir; A Multi-Center, Randomized, Open-Label, Active-Controlled, Non-Inferiority, Phase IV Cl [NCT06000657]Phase 4196 participants (Anticipated)Interventional2023-07-28Recruiting
Study of the Immunogenicity and Efficacy of HBsAg Vaccine in Combination With Standard Antiviral Therapy in Patients Who Have Been Treated With HB110E Hepatitis B DNA Vaccine [NCT01813487]6 participants (Actual)Interventional2013-02-28Completed
Combination Therapy of Interferon Alfa-2b Plus Interleukin 2 and Hepatitis B Vaccine in Entecavir-experienced Chronic Hepatitis B Patients With HBeAg Seroclearance: a Prospective, Randomized Open-label Trial (Endeavor Study, a Pilot Study) [NCT02360592]Phase 494 participants (Actual)Interventional2013-06-30Completed
HBV Viral Suppression by Entecavir in Adefovir Partial Responders [NCT00704106]60 participants (Actual)Observational2008-05-31Completed
Nucleoid as an Adjuvant Therapy After Radiofrequency Ablation for Hepatocellular Carcinoma [NCT00555334]Phase 4200 participants (Anticipated)Interventional2007-11-30Recruiting
A Randomized, Open-label Study of the Effect of Peginterferon Alfa-2a (40KD)(PEGASYS) in Combination With Adefovir or Entecavir on HBeAg Seroconversion in Patients With HBeAg Positive Chronic Hepatitis B [NCT00922207]Phase 4280 participants (Actual)Interventional2010-05-07Completed
A Randomized, Double-blind, Placebo-controlled Study to Determine the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of the FXR-agonist EYP001a in Chronically HBV Infected Subjects [NCT03272009]Phase 173 participants (Actual)Interventional2017-09-21Completed
Entecavir Prophylaxis for Hepatitis B Reactivation for CD20 Positive B-cell Lymphoma Patients With Resolved Hepatitis B (Negative Hepatitis B Surface Antigen, Positive Hepatitis B Core Antibody) (REHEB):a Single Arm, Open Label, Multi-center Phase II Stud [NCT05453435]Phase 284 participants (Anticipated)Interventional2022-07-15Not yet recruiting
A Randomized, Open-label, Controlled, Multicenter, Exploratory Trial to Characterize the Results of Daily Oral Administration of Telbivudine (LDT600) 600 mg or Entecavir (ETV) 0.5 mg Given Over 12 Weeks on the Kinetics of Hepatitis B Virus (HBV) DNA in Ad [NCT00412529]Phase 344 participants (Actual)Interventional2006-12-31Completed
Entecavir Intensification for Persistent Hepatitis B Virus (HBV) Viremia in HIV-HBV Infection [NCT00662545]Phase 410 participants (Actual)Interventional2008-04-30Completed
A Randomized, Double Blind, Placebo-controlled Phase 2b Study to Evaluate Efficacy, Pharmacokinetics, and Safety of 48-week Study Intervention With JNJ 73763989+JNJ 56136379+Nucleos(t)Ide Analog (NA) Regimen Compared to NA Alone in e Antigen Negative Viro [NCT04129554]Phase 2130 participants (Actual)Interventional2019-11-06Completed
Study on Screening, Verification and Intervention of High-risk Patients With Liver Cancer [NCT05721300]2,215 participants (Anticipated)Interventional2023-02-10Recruiting
A Multicenter Controlled Open-label Trial of Evaluating Tenofovir Alafenamide, Tenofovir Disoproxil Fumarate and Entecavir in Acute-on-chronic Liver Failure of Chronic Hepatitis B Patients [NCT03640728]200 participants (Anticipated)Observational2019-01-25Recruiting
Higher Risk of Kidney Function Decline With Entecavir Than Tenofovir Alafenamide in Patients With HBV Related Acute-on-chronic Liver Failure: Real-World Study [NCT05453448]272 participants (Actual)Interventional2022-05-01Completed
A Phase III Randomized Trial of Prophylactic Antiviral Therapy in Patients With Current or Past Hepatitis B Virus (HBV) Infection Receiving Anti-Cancer Therapy for Solid Tumors [NCT03887702]Phase 3444 participants (Anticipated)Interventional2020-01-17Active, not recruiting
Comparison Between Lamivudine and Entecavir Treatment in Patients With Spontaneous Severe Acute Exacerbation of Chronic Hepatitis B. [NCT01627223]Phase 417 participants (Actual)Interventional2012-07-31Terminated(stopped due to Slow progress in recruiting study patients)
A Multicenter Randomized Controlled Open-label Trial of Tenofovir Plus Entecavir Combination vs. Tenofovir Monotherapy in Chronic Hepatitis B Patients With Genotypic Resistance to Adefovir and Partial Virologic Response to Ongoing Treatment [NCT01639066]Phase 4102 participants (Actual)Interventional2012-09-25Completed
A Multicenter Randomized Controlled Open-label Trial of Tenofovir vs. Tenofovir Plus Entecavir in Chronic Hepatitis B Patients With Genotypic Resistance to Entecavir and Partial Virologic Response to Ongoing Treatment [NCT01639092]Phase 488 participants (Actual)Interventional2012-09-28Completed
A Phase 1, Blinded, Randomized, Placebo-controlled, First-in-human Study of Orally Administered JNJ-64457744 to Evaluate the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics After Single and Multiple Ascending Doses [NCT05423106]Phase 160 participants (Actual)Interventional2022-07-04Terminated(stopped due to Strategic business decision, not due to safety concerns)
Switching to Tenofovir Disoproxil Fumarate vs. Continuing Entecavir in Chronic Hepatitis B Patients With Partial Virologic Response During Entecavir Therapy: STEEP Study [NCT01711567]Phase 460 participants (Actual)Interventional2013-04-30Completed
A Prospective and Open-Label Study of the Effect on Proximal Tubular Function in Asian-American Patients Receiving Tenofovir Disoproxil Fumarate (TDF) or Entecavir (ETV) for HBV Treatment [NCT01715987]48 participants (Actual)Observational2012-10-31Terminated
Prophylactic Use of Entecavir for HBsAg Negative/HBcAb Positive/Hepatitis B Virus DNA Negative Patients With Lymphoma [NCT01765231]Phase 4190 participants (Anticipated)Interventional2013-01-31Recruiting
Prophylactic Use of Entecavir for HBsAg Positive Lymphoma Patients Treated With Rituximab-based Immunochemotherapy [NCT01768195]Phase 480 participants (Anticipated)Interventional2013-01-31Recruiting
A 3-year, Open-lable, Multi-center Extension Trial of Entecavir Therapy for Patients Previously Treated in Dragon Study [NCT01829685]Phase 4360 participants (Anticipated)Interventional2013-03-31Active, not recruiting
The Incidence of Lactic Acidosis During Entecavir Treatment in Chronic Hepatitis B Patients With Severe Cirrhosis or Hepatic Failure [NCT01354652]Phase 45 participants (Actual)Interventional2011-05-31Terminated(stopped due to Tenofovir has become available in Korea.)
A Prospective Study to Investigate the Relationship Between Hepatitis B Surface Antigen (HBsAg) Loss and the Dynamics in Host and Viral Markers After Discontinuation of Nucleos(t)Ide Analog (NA) Treatment in Chronic Hepatitis B E-antigen Negative Patients [NCT05550519]Early Phase 10 participants (Actual)Interventional2022-10-31Withdrawn(stopped due to Sponsor decision after reevaluation of strategy in the context of recruitment timelines projection)
Study on Therapeutic Effects and Safety of Three Types of Nucleotide/Nucleoside Analogues in Patients With Chronic Hepatitis b [NCT04195074]300 participants (Anticipated)Interventional2019-01-01Recruiting
Investigation on Antiviral Therapy of Peginterferon Alfa-2b in HBeAg Positive Chronic Hepatitis B Patients Based on Detection of Interferon Gene Mutation and Interferon Receptor [NCT02973646]Phase 4100 participants (Anticipated)Interventional2016-01-31Recruiting
Efficacy Comparison Between Two Kind of Chinese Herbal Formulas on Traditional Chinese Medicine Syndromes Among Chronic Hepatitis Patients [NCT03018821]250 participants (Anticipated)Interventional2017-01-31Recruiting
A Phase II Study in Japan of the Safety and Antiviral Activity of Entecavir (BMS-200475) vs Lamivudine in Adults With Chronic Hepatitis B Infection [NCT01022801]Phase 2120 participants (Anticipated)Interventional2003-08-31Completed
Stopping Antiviral Treatment and Subsequent Flare in Chronic Hepatitis B Infection: Immunological and Virological Profiling [NCT04431245]54 participants (Anticipated)Observational2021-06-01Active, not recruiting
Safety and Efficacy of Finite Versus Continuous Nucleos(t)Ide Analogues Therapy in Patients With Chronic Hepatitis B: A Multicenter Randomized Controlled Trial [NCT05793268]360 participants (Anticipated)Interventional2022-12-20Active, not recruiting
A Phase 1, Randomized, Partially-Blind, Parallel-Group, Active and Placebo Controlled Study to Evaluate the Safety and Pharmacokinetics of Single Oral Doses of Entecavir Extended Release (XR) in Healthy Subjects [NCT03239353]Phase 140 participants (Actual)Interventional2017-10-20Completed
A Preliminary Assessment of Safety and Antiviral Activity of Open-label Entecavir in Subjects With Chronic Hepatitis B Following Monotherapy in Other Entecavir Trials [NCT01438424]Phase 21,053 participants (Actual)Interventional2001-01-31Completed
A Multicenter, Randomized, Double-blind, Placebo-controlled, Multi-dose Study to Determine the Depth of Hepatitis B Surface Antigen (HBsAg) Reduction Following Intravenous ARC-520 in Combination With Entecavir or Tenofovir in Patients With HBeAg Positive, [NCT02452528]Phase 24 participants (Actual)Interventional2015-08-31Terminated(stopped due to Company decision to discontinue trial)
A Multicenter, Open-Label Study to Evaluate ARC-520 Administered Alone and in Combination With Other Therapeutics in Patients With Chronic Hepatitis B Virus (HBV) Infection (MONARCH) [NCT02577029]Phase 279 participants (Actual)Interventional2015-12-31Terminated(stopped due to Company decision to discontinue trial)
A Multicenter, Randomized, Double-blind, Placebo-controlled, Multi-dose Study to Determine the Depth of Hepatitis B Surface Antigen (HBsAg) Reduction Following Intravenous ARC-520 in Combination With Entecavir or Tenofovir in Patients With HBeAg Negative, [NCT02604199]Phase 258 participants (Actual)Interventional2015-09-30Terminated(stopped due to Company decision to discontinue trial)
A Randomized, Open-label Trial Comparing Telbivudine vs, Entecavir in Reducing Serum HBsAg Levels in Patients With HBeAg-positive Chronic Hepatitis B Who Have Achieved Serum HBV DNA Undetectability by Preceding Entecavir Treatment [NCT01595685]Phase 398 participants (Actual)Interventional2012-05-31Completed
A Randomized, Multicenter, Prospective Study to Compare Antiviral Efficacy and Safety of Switching to ETV Plus TDF Versus Maintaining LAM/LDT Plus ADF Combination in CHC With PVR to LAM/LDF Plus ADF Combination Rescue Therapy for YMDD Mutation [NCT01597934]Phase 4104 participants (Anticipated)Interventional2012-08-31Active, not recruiting
The Efficacy of Peg-interferon α-2a in HBeAg (+) Chronic Hepatitis B Patients Who Have Been Treated by Entecavir for 48 Weeks But Without HBeAg Loss [NCT01599130]60 participants (Anticipated)Interventional2012-07-31Not yet recruiting
Adjuvant Entecavir or Tenofovir for Hepatitis B Virus Related Hepatocellular Carcinoma After Curative Hepatic Resection [NCT02650271]Phase 3240 participants (Anticipated)Interventional2021-02-02Recruiting
Pegasys Plus Entecavir Versus Entecavir Versus Pegasys for Hepatitis B e Antigen-Negative Chronic Hepatitis B [NCT01925820]Phase 4540 participants (Anticipated)Interventional2013-01-31Recruiting
Efficacy and Safety of Entecavir Maleate Tablets in Chinese Patients With Hepatitis B [NCT01926288]Phase 4287 participants (Actual)Interventional2008-10-31Completed
SWITCH OR ADD PEGYLATED-INTERFERON IN CHRONIC HEPATITIS B PATIENTS ON LONG TERM NUCLEOS(T)IDE THERAPY (SWAP TRIAL) [NCT01928511]Phase 4254 participants (Actual)Interventional2014-01-31Completed
Therapeutic Safety and Efficacy of Combination Treatment With REP 2139-Ca and Pegasys in Patients With Chronic Hepatitis B [NCT02726789]Phase 25 participants (Actual)Interventional2012-10-31Completed
Chronic Kidney Disease Progression in Chronic Hepatitis B Patients on Tenofovir Alafenamide (TAF) Versus Entecavir [NCT05423834]1,800 participants (Anticipated)Observational [Patient Registry]2022-09-01Active, not recruiting
The Therapy of Tacrolimus Combined With Entecavir on HBV Associated Glomerulonephritis : A Multicenter, Prospective, Randomized, Controlled, Single-blind Trial. [NCT03062813]Phase 4112 participants (Anticipated)Interventional2017-02-01Recruiting
A Phase 2a, Multi-center, Double-blind, Placebo-controlled Study Evaluating ABI-H0731+ Entecavir vs Entecavir Alone for the Treatment of Viremic HBeAg-positive Patients With Chronic Hepatitis B [NCT03577171]Phase 225 participants (Actual)Interventional2018-06-19Completed
A Phase 2a Open-label Study of the Oral Farnesoid X Receptor (FXR) Modulator EYP001a to Assess Its Safety and Anti-viral Effect in Chronic Hepatitis B (CHB) Patients in Combination With Pegylated Interferon alpha2a (Peg-IFN) Alone and With Entecavir (ETV) [NCT04365933]Phase 220 participants (Actual)Interventional2020-05-25Completed
A Multicenter, Randomized, Double-blind, Placebo-controlled, Dose-escalation Study to Determine the Depth and Duration of Hepatitis B Surface Antigen (HBsAg) Reduction After a Single Intravenous Dose of ARC-520 in Combination With Entecavir in Patients Wi [NCT02065336]Phase 258 participants (Actual)Interventional2014-03-31Terminated(stopped due to Company decision to discontinue trial)
Entecavir Combined Short-term Intravenous Hepatitis B Immune Globulin (HBIG) to Prevent Hepatitis B Recurrence After Liver Transplantation [NCT02417207]Phase 460 participants (Anticipated)Interventional2015-04-30Not yet recruiting
A Multiple-Center, Randomized, Partially Double-Blind, Placebo-Controlled Study to Investigate the Safety, Tolerability, Pharmacokinetics, Pharmacodynamics, and Antiviral Effects of 12-Week Treatment With RO6864018 in Virologically Suppressed Patients Wit [NCT02391805]Phase 231 participants (Actual)Interventional2015-05-17Completed
A 3-year, Open-lable, Multi-center Extension Trial of Entecavir Plus Adefovir Combination Treatment for Patients Previously Treated in EXPLORE, EXCEL and EFFORT Ex Study [NCT01834508]Phase 4600 participants (Anticipated)Interventional2013-03-31Active, not recruiting
Clinical Effects and Cost-effectiveness Analysis of Early Anti-viral Therapy on HBV-related Compensated Liver Cirrhosis [NCT01720238]621 participants (Actual)Observational2012-03-31Active, not recruiting
A Randomized, Placebo-Controlled, Double-Blind, Multi-Center Study to Assess the Efficacy and Safety of Fuzheng Huayu Combined With Entecavir in Liver Cirrhosis Patients Due to Hepatitis B Virus [NCT02241590]Phase 4700 participants (Anticipated)Interventional2014-09-30Recruiting
Study on Therapeutic Effects and Safety of Three Types of Nucleotide/Nucleoside Analogues in Patients With Hepatitis b Virus Related Compensated Cirrhosis [NCT04196998]150 participants (Anticipated)Interventional2019-01-01Recruiting
A Prospective, Randomized, Open-label Study of the Investigation of Peginterferon Alfa-2a on Optimal in Chronic Hepatitis B Patients Who Have a High Risk of HCC [NCT03084250]Phase 4150 participants (Anticipated)Interventional2017-03-10Active, not recruiting
Hellenic Multicenter Real-life Clinical Study for Bulevirtide Therapy in Chronic Hepatitis D: HERACLIS-BLV [NCT05928000]80 participants (Anticipated)Observational [Patient Registry]2023-05-01Recruiting
A Prospective Randomized Controlled Trial of Tenofovir and Entecavir in the Treatment of Long-term Prognosis in Patients With Hepatitis B-related Hepatocellular Carcinoma After Curative Resection [NCT04392700]Phase 3706 participants (Anticipated)Interventional2019-07-25Recruiting
A Multi Center, Phase IIIb Study to Evaluate the Efficacy of Response Guided Therapy Using Quantitative HBsAg Measurement in Patient With HBeAg Positive Chronic Hepatitis B: [NCT01456312]Phase 4200 participants (Anticipated)Interventional2012-09-30Recruiting
A Multi-center, Open-label, Long-term Extension Study of ABI-H0731 + Nucleos(t)Ide as Finite Treatment for Chronic Hepatitis B Patients [NCT03780543]Phase 292 participants (Actual)Interventional2018-12-20Terminated(stopped due to Sponsor decision)
Role of Nucleoside Analogue in Preventing Clinical Reactivation of HBV in HCV/HBV Co-infected Patients Receiving DAA Therapy for Chronic Hepatitis C [NCT04405011]60 participants (Anticipated)Interventional2018-08-01Recruiting
A Multi-Center Study to Assess the Efficacy and Safety of Traditional Chinese Medicine Combined With Entecavir for Patients With Refractory Liver Fibrosis in Liver Cirrhosis Due to HBV [NCT02241616]Phase 4350 participants (Anticipated)Interventional2014-09-30Recruiting
A Randomized, Open-label, Multi-part Study of the Relative Oral Bioavailability of AL-3778 Tablets and Drug Interaction With Entecavir or Tenofovir Disoproxil Fumarate in Healthy Volunteers [NCT03032536]Phase 154 participants (Actual)Interventional2017-01-31Terminated(stopped due to Sponsor decision.)
Alterations in the Intestinal Microbiome and Metabolic Profile of Patients With Cirrhosis Supplemented With Lactulose, Clostridium Butyricum, and Bifidobacterium Longum Infantis: a Randomized Placebo-controlled Trial [NCT05687409]Phase 4120 participants (Actual)Interventional2019-11-24Completed
A Comparative Study of the Antiviral Efficacy and Safety of Entecavir Plus Tenofovir Versus Adefovir Added to Continuing Lamivudine in Adults With Lamivudine- Resistant Chronic Hepatitis B Virus Infection [NCT00605384]Phase 34 participants (Actual)Interventional2008-08-31Terminated(stopped due to Business Objectives Have Changed)
Prospective Trial of Entecavir for Chronic Hepatitis B in Hepatocellular Carcinoma Patients Underwent Radiofrequency Ablation Therapy [NCT01270178]420 participants (Anticipated)Observational2011-01-31Not yet recruiting
A Real-World Study of Sequential Combination Therapy With Pegylated Interferon In Nucleoside-treated Patients With Chronic Hepatitis B [NCT03357822]Phase 42,000 participants (Anticipated)Interventional2018-01-25Recruiting
The Efficacy and Safety Study of Magnesium Isoglycyrrhizinate Injection Followed by Diammonium Glycyrrhizinate Enteric-coated Capsules and Combined With Entecavir on the Treatment of Chronic Hepatitis B [NCT03349008]Phase 4480 participants (Anticipated)Interventional2017-11-25Not yet recruiting
The Efficacy and Safety of Tenofovir Alafenamide Fumarate Compared With Other Nucleoside Analogues (Acid) to Treat Patients With Low-level Viremia of HBV [NCT04501224]200 participants (Anticipated)Interventional2020-08-03Recruiting
Study to Compare Virological Response to 0.5 mg Daily Versus 1.0 mg Daily Oral Doses of Entecavir in Chronic Hepatitis B Virus Infection Related Decompensated Cirrhosis [NCT03345498]32 participants (Actual)Observational2017-01-01Completed
Efficacy and Safety of Continuing Lamivudine Plus Adefovir or Adefovir Versus Switching to Entecavir Plus Adefovir in Patients With Chronic Hepatitis B Who Have Resistant Mutants to Lamivudine and Show Suboptimal Response to Combination of Lamivudine Plus [NCT02482272]Phase 490 participants (Anticipated)Interventional2015-05-31Recruiting
[NCT01892241]Phase 374 participants (Actual)Interventional2010-01-31Completed
PhaseIVstudy to Evaluate the Non-inferiority of Cavir®Tab. in Terms of Hepatitis B Virus(HBV)DNA Undetectability Comparing Baraclude® Tab. in Hepatitis B e Antigen(HBeAg)(+) Chronic Hepatitis B Patients Treated With Long-term Baraclude® Tab [NCT02523547]Phase 4134 participants (Anticipated)Interventional2015-01-31Recruiting
[NCT00035789]Phase 30 participants Interventional2001-11-30Completed
[NCT00035633]Phase 30 participants Interventional2001-12-31Completed
Study of the Drug Interaction of EYP001a With Entecavir in Healthy Subjects [NCT03469583]Phase 116 participants (Actual)Interventional2018-02-12Completed
Improvement of Hard Endpoint in Chronic Hepatitis B Patients Treated With Antiviral Therapy [NCT03366571]600 participants (Anticipated)Observational2016-01-31Active, not recruiting
Efficacy and Safety of Combination Therapy With Entecavir, Peginterferon Alfa-2b and Immunomodulators in Nucleoside or Nucleotide Analogue (NA)-Suppressed Chronic Hepatitis B Patients [NCT03332329]Phase 415 participants (Actual)Interventional2015-12-01Active, not recruiting
Utilization of Hepatitis B Virus Nucleic Acid Test Positive Donors for Hepatitis B Vaccinated Lung Transplant Candidates [NCT05404919]Phase 210 participants (Anticipated)Interventional2022-09-06Recruiting
Investigation of Efficacy of Tenofovir Monotherapy in Comparison With Entecavir Plus Tenofovir in Patients With Chronic Hepatitis B Patients Who Had Achieved Complete Viral Suppression on Entecavir Plus Tenofovir Combination Therapy-Multicenter Randomized [NCT03236610]Phase 3112 participants (Anticipated)Interventional2016-01-01Recruiting
Tenofovir Alafenamide Versus Entecavir for the Treatment of Chronic Hepatitis B: An Open Label, Randomized Controlled Trial [NCT03933384]Phase 4420 participants (Anticipated)Interventional2019-08-19Recruiting
A Phase IIIb, Randomized, Open-Label Study of Pegylated Interferon Alfa-2A in Combination With Lamivudine or Entecavir Compared With Untreated Control Patients in Children With HBeAg Positive Chronic Hepatitis B in the Immune-Tolerant Phase [NCT02263079]Phase 362 participants (Actual)Interventional2014-06-16Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00065507 (26) [back to overview]Number of Subjects Achieving Composite Endpoint (HBV DNA < 10*4 Copies/mL by PCR Assay and Normal ALT [≤ 1.0 x ULN]) Through Week 48
NCT00065507 (26) [back to overview]Number of Participants With Improvement or No Worsening in Child-Pugh Score From Baseline to Week 48
NCT00065507 (26) [back to overview]Number of Participants With Malignant Neoplasms - On Treatment or During 24-Week Follow-up Period
NCT00065507 (26) [back to overview]Number of Participants With Treatment-Emergent Grade 3/4 Laboratory Abnormalities - Week 48 and Cumulative Data
NCT00065507 (26) [back to overview]Number of Participants With HBV DNA < 300 Copies/mL by PCR At Week 48
NCT00065507 (26) [back to overview]Number of Participants With HBV DNA < 300 Copies/mL by PCR At Week 24
NCT00065507 (26) [back to overview]Mean Change From Baseline in Total Bilirubin Through Week 48
NCT00065507 (26) [back to overview]Mean Change From Baseline in Prothrombin Time Through Week 48
NCT00065507 (26) [back to overview]Mean Change From Baseline in Model for End-Stage Liver Disease (MELD) Scores From Baseline Through Week 48
NCT00065507 (26) [back to overview]Improvement or No Worsening in MELD Score Through Week 48
NCT00065507 (26) [back to overview]Cumulative Number of Participants With Adverse Events (AEs), Serious Adverse Events (SAEs), Deaths, HCC, Discontinuations Due to AEs, and Confirmed Creatinine Increase >=0.5 mg/dL
NCT00065507 (26) [back to overview]Change From Baseline in Platelet Count Through Week 48
NCT00065507 (26) [back to overview]Change From Baseline in Child-Pugh Score Through Week 48
NCT00065507 (26) [back to overview]Change From Baseline in Albumin Through Week 48
NCT00065507 (26) [back to overview]>=2-Point Reduction From Baseline in Child-Pugh Score Through Week 48
NCT00065507 (26) [back to overview]Change From Baseline in HBV DNA by PCR at Week 48
NCT00065507 (26) [back to overview]Change From Baseline in Hepatitis B Virus (HBV) DNA by Polymerase Chain Reaction (PCR) at Week 24
NCT00065507 (26) [back to overview]Participants Achieving Albumin Normalization Through Week 48
NCT00065507 (26) [back to overview]Participants Achieving Platelet Count Normalization Through Week 48
NCT00065507 (26) [back to overview]Participants Achieving Prothrombin Time Normalization Through Week 48
NCT00065507 (26) [back to overview]Participants Achieving Total Bilirubin Normalization Through Week 48
NCT00065507 (26) [back to overview]Number of Hepatocellular Carcinoma (HCC) Events at Different Time Points Through Week 48
NCT00065507 (26) [back to overview]Number of Participants Achieving Alanine Transaminase (ALT) Normalization (≤1.0 x Upper Limit of Normal [ULN]) at Weeks 24 and 48
NCT00065507 (26) [back to overview]Number of Participants Undergoing Liver Transplant - On-Treatment or 24-Week Follow-Up
NCT00065507 (26) [back to overview]Number of Participants With Alanine Aminotransferase (ALT) Flares - On Treatment
NCT00065507 (26) [back to overview]Number of Participants With Improvement in Child-Pugh Class at Week 24 and Week 48
NCT00096785 (10) [back to overview]HBV DNA Viral Kinetics - Spline Model
NCT00096785 (10) [back to overview]HBV DNA Viral Kinetics Estimates of Exponential Decay Model - Efficacy in Blocking Virus Production and de Novo Infections
NCT00096785 (10) [back to overview]HBV DNA Viral Kinetics Estimates of Exponential Decay Model - Viral Clearance Rate and Infected Cell Death Rate
NCT00096785 (10) [back to overview]Summary of Safety - Laboratory Abnormalities Reported as Clinical AEs
NCT00096785 (10) [back to overview]Summary of Safety - Most Frequent (> 10%) Adverse Events (AEs), Serious Adverse Events (SAEs), Discontinuations Due to AEs, and Deaths
NCT00096785 (10) [back to overview]Alanine Aminotransferase (ALT) Normalization
NCT00096785 (10) [back to overview]Change From Baseline in HBV DNA by PCR Assay at Week 48
NCT00096785 (10) [back to overview]Change From Baseline in Hepatitis B Virus DNA (HBV DNA) by Polymerase Chain Reaction (PCR) Assay at Week 12
NCT00096785 (10) [back to overview]HBV DNA Viral Kinetics Estimates of Exponential Decay Model - Half-Life of Free Virus
NCT00096785 (10) [back to overview]Viral Load Undetectable (HBV DNA <300 Copies/mL)
NCT00298363 (38) [back to overview]Percentage of Participants With HBeAg Loss and HBeAg Seroconversion at Week 96 (for Participants Who Were HBeAg Positive at Baseline)
NCT00298363 (38) [back to overview]Median Change in MELD Score From Baseline at Week 96
NCT00298363 (38) [back to overview]Median Change in MELD Score From Baseline at Week 168
NCT00298363 (38) [back to overview]Median Change in MELD Score From Baseline at Week 144
NCT00298363 (38) [back to overview]In the Subset of Participants Undergoing Liver Transplantation, Time to Recurrence of Hepatitis B, Defined as 2 Consecutive Plasma HBV DNA Concentrations ≥ 400 Copies/mL or 2 Consecutive HBsAg(+) Results
NCT00298363 (38) [back to overview]Median DAVG in Plasma HBV DNA Levels at 144 Weeks Relative to Baseline
NCT00298363 (38) [back to overview]Median DAVG in Plasma HBV DNA Levels at 168 Weeks Relative to Baseline
NCT00298363 (38) [back to overview]Median DAVG in Plasma HBV DNA Levels at 96 Weeks Relative to Baseline
NCT00298363 (38) [back to overview]Median Time-averaged Change (DAVG) in Plasma Hepatitis B Virus (HBV) Deoxyribonucleic Acid (DNA) Levels at 48 Weeks Relative to Baseline
NCT00298363 (38) [back to overview]Percent Probability of a Confirmed Increase in Serum Creatinine of ≥ 0.5 mg/dL From Baseline or a Confirmed Serum Phosphorus Level < 2.0 mg/dL
NCT00298363 (38) [back to overview]Percent Probability of Tolerability Failure
NCT00298363 (38) [back to overview]Percentage of Participants With a Decrease in CPT Score of ≥ 2 Points From Baseline at Week 144
NCT00298363 (38) [back to overview]Percentage of Participants With a Decrease in CPT Score of ≥ 2 Points From Baseline at Week 168
NCT00298363 (38) [back to overview]Percentage of Participants With a Decrease in CPT Score of ≥ 2 Points From Baseline at Week 48
NCT00298363 (38) [back to overview]Percentage of Participants With a Decrease in CPT Score of ≥ 2 Points From Baseline at Week 96
NCT00298363 (38) [back to overview]Percentage of Participants With an Increase in Child-Pugh Turcotte (CPT) Score of ≥ 2 Points at Weeks 48
NCT00298363 (38) [back to overview]Percentage of Participants With an Increase in CPT Score of ≥ 2 Points at Week 144
NCT00298363 (38) [back to overview]Percentage of Participants With an Increase in CPT Score of ≥ 2 Points at Week 168
NCT00298363 (38) [back to overview]Percentage of Participants With an Increase in CPT Score of ≥ 2 Points at Week 96
NCT00298363 (38) [back to overview]Percentage of Participants With Baseline ADV-R + LAM-R Mutations Achieving HBV DNA < 400 Copies/mL by 168 Weeks
NCT00298363 (38) [back to overview]Percentage of Participants With Normalized Alanine Aminotransferase (ALT) (for Subjects With Elevated ALT at Baseline) at Week 48
NCT00298363 (38) [back to overview]Percentage of Participants With Normalized ALT (for Subjects With Elevated ALT at Baseline) at Week 144
NCT00298363 (38) [back to overview]Percentage of Participants With Normalized ALT (for Subjects With Elevated ALT at Baseline) at Week 168
NCT00298363 (38) [back to overview]Percentage of Participants With Hepatitis B Surface Antigen (HBsAg) Loss and HBsAg Seroconversion at Week 48
NCT00298363 (38) [back to overview]Percentage of Participants With Normalized ALT (for Subjects With Elevated ALT at Baseline) at Week 96
NCT00298363 (38) [back to overview]Percentage of Participants With Hepatitis B Early Antigen (HBeAg) Loss and HBeAg Seroconversion at Week 48 (for Participants Who Were HBeAg Positive at Baseline)
NCT00298363 (38) [back to overview]Percentage of Participants With Only Baseline Adefovir Dipivoxil Resistance (ADV-R) Mutations Achieving HBV DNA < 400 Copies/mL by 168 Weeks
NCT00298363 (38) [back to overview]Percentage of Participants With Only Baseline Lamivudine-resistance (LAM-R) Mutations Achieving HBV DNA < 400 Copies/mL by 168 Weeks
NCT00298363 (38) [back to overview]Percentage of Participants With Plasma HBV DNA < 400 Copies/mL at Week 144
NCT00298363 (38) [back to overview]Percentage of Participants With Plasma HBV DNA < 400 Copies/mL at Week 168
NCT00298363 (38) [back to overview]Percentage of Participants With Plasma HBV DNA < 400 Copies/mL at Week 48
NCT00298363 (38) [back to overview]Percentage of Participants With Plasma HBV DNA < 400 Copies/mL at Week 96
NCT00298363 (38) [back to overview]Percentage of Participants With HBeAg Loss and HBeAg Seroconversion at Week 144 (for Participants Who Were HBeAg Positive at Baseline)
NCT00298363 (38) [back to overview]Percentage of Participants With HBeAg Loss and HBeAg Seroconversion at Week 168 (for Participants Who Were HBeAg Positive at Baseline)
NCT00298363 (38) [back to overview]Percentage of Participants With HBsAg Loss and HBsAg Seroconversion at Week 144
NCT00298363 (38) [back to overview]Percentage of Participants With HBsAg Loss and HBsAg Seroconversion at Week 168
NCT00298363 (38) [back to overview]Percentage of Participants With HBsAg Loss and HBsAg Seroconversion at Week 96
NCT00298363 (38) [back to overview]Median Change in Model for End-Stage Liver Disease (MELD) Score From Baseline at Week 48
NCT00371150 (13) [back to overview]Percentage of Participants With HBeAg Seroconversion at Week 48 (for HBeAg-positive Participants Only)
NCT00371150 (13) [back to overview]Percentage of Participants With HBV DNA by PCR Category at Week 48
NCT00371150 (13) [back to overview]Percentage of Participants Who Achieve HBV DNA < Lower Limit of Quantitation (LOQ = 29 IU/mL [Approximately 169 Copies/mL]) at Week 48
NCT00371150 (13) [back to overview]Percentage of Participants With Confirmed HBeAg Loss at Week 48 (for HBeAg-positive Participants Only)
NCT00371150 (13) [back to overview]Number of Participants With Adverse Events (AE), Serious Adverse Events (SAE), and Discontinuations From Study Drug Due to Adverse Events
NCT00371150 (13) [back to overview]Percentage of Participants With HBsAg Seroconversion at Week 48
NCT00371150 (13) [back to overview]Percentage of Participants With HBV Deoxyribonucleic Acid (DNA) < 50 IU/mL by Polymerase Chain Reaction (PCR) at Week 48
NCT00371150 (13) [back to overview]Percentage of Participants With Hepatitis B Surface Antigen (HBsAg) Loss at Week 48
NCT00371150 (13) [back to overview]Percentage of Participants With Virologic Rebound Through Week 48 While on Continued Dosing With ETV
NCT00371150 (13) [back to overview]Mean log10 Reduction From Baseline in HBV DNA at Week 48
NCT00371150 (13) [back to overview]Percentage of Participants With Alanine Aminotransferase (ALT) Normalization at Week 48
NCT00371150 (13) [back to overview]Number of Participants With Laboratory Abnormalities On-treatment (OT) and Off-Treatment (OF) : Serum Chemistry
NCT00371150 (13) [back to overview]Number of Participants With Laboratory Abnormalities On-treatment (OT) and Off-Treatment (OF): Hematology
NCT00388674 (6) [back to overview]Number of Participants With Liver-related HBV Disease Progression
NCT00388674 (6) [back to overview]Number of Participants With HCC Malignant Neoplasm
NCT00388674 (6) [back to overview]Number of Participants With Adjudicated Overall Malignant Neoplasms
NCT00388674 (6) [back to overview]Number of Participants With Non-HCC Malignant Neoplasm
NCT00388674 (6) [back to overview]Number of Deaths
NCT00388674 (6) [back to overview]Number of Participants With Liver-related Death
NCT00393484 (14) [back to overview]Number of Participants With Grade 3 or 4 Abnormalities in Laboratory Test Results by World Health Organization (WHO) Criteria at Week 96
NCT00393484 (14) [back to overview]Number of Participants With Hepatitis B Virus (HBV) DNA <10^3, <10^4, or < 10^5 Copies/mL by Polymerase Chain Reaction (PCR) Assy at Weeks 24, 48, and 96
NCT00393484 (14) [back to overview]Number of Participants With Normalization of Serum Alanine Aminotransferase (ALT) Levels at Weeks 24, 48, and 96
NCT00393484 (14) [back to overview]Number of Participants With Viral Rebound and Drug-resistant Hepatitis B Virus (HBV) DNA Mutations at Week 96
NCT00393484 (14) [back to overview]Percentage of Participants With a Virologic Response as Defined by Undetectable Hepatitis B Virus DNA at Weeks 48, 96, 144, 192, and 240
NCT00393484 (14) [back to overview]Number of Participants With Death as Outcome, Serious Adverse Events (SAEs), Discontinuations Due to Adverse Events (AEs), Most Common AEs, and Grade 3/4 AEs at Week 240
NCT00393484 (14) [back to overview]Mean Laboratory Test Values for Alanine Aminotransferase (ALT) at Week 24
NCT00393484 (14) [back to overview]Number of Participants With Clinically or Statistically Significant Changes in Vital Sign Measurements at Week 24
NCT00393484 (14) [back to overview]Number of Participants With Virologic Rebound at Week 24
NCT00393484 (14) [back to overview]Percentage of Participants Who Achieved a Virologic Response at Week 24
NCT00393484 (14) [back to overview]Mean Log10 Reduction From Baseline in Hepatitis B Virus (HBV) DNA at Weeks 24, 48, 96, 144, 192, and 240
NCT00393484 (14) [back to overview]Number of Participants With Death as Outcome, Serious Adverse Events (SAEs), Discontinuations Due to Adverse Events (AEs), Most Common AEs, and Grade 3/4 AEs at Week 24
NCT00393484 (14) [back to overview]Number of Participants With Elevations in Alanine Transaminase (ALT) and Aspartate Aminoaminase (AST) Levels, Elevations in ALT and AST Levels,Simultaneous Elevations in ALT and Total Bilirubin Levels, and ALT Flares at Week 24
NCT00393484 (14) [back to overview]Number of Participants With Grade 3 or 4 Abnormalities in Laboratory Test Results by World Health Organization (WHO) Criteria at Week 24
NCT00395018 (15) [back to overview]Percentage of Participants With HBeAg Loss at Week 72 (for HBeAg-positive Participants)
NCT00395018 (15) [back to overview]Percentage of Participants With HBeAg Seroconversion at Week 72 (for HBeAg-positive Participants)
NCT00395018 (15) [back to overview]Percentage of Participants With HBsAg Loss at Week 72
NCT00395018 (15) [back to overview]Percentage of Participants With HBsAg Recurrence At Week 72
NCT00395018 (15) [back to overview]Percentage of Participants With HBV Deoxyribonucleic Acid (DNA) => 50 IU/mL by Polymerase Chain Reaction (PCR) at Week 72
NCT00395018 (15) [back to overview]Percentage of Participants With HBsAg Seroconversion at Week 72
NCT00395018 (15) [back to overview]Number of Participants With HBV DNA by PCR >= 50 IU/mL Through Week 72
NCT00395018 (15) [back to overview]Distribution of ALT Levels Through 72 Weeks: Overall
NCT00395018 (15) [back to overview]Number of Participants With Liver Rejection Through Week 72
NCT00395018 (15) [back to overview]Number of Participants With Laboratory Abnormalities On-treatment (OT) and Off-Treatment (OF) Follow-up: Serum Chemistry (All Grades)
NCT00395018 (15) [back to overview]Number of Participants With Laboratory Abnormalities On-treatment (OT) and Off-Treatment Follow-up(OF): Hematology (All Grades)
NCT00395018 (15) [back to overview]Participants With Adverse Events (AE), Serious Adverse Events (SAE), and Discontinuations From Study Drug Due to AEs (On-treatment [OT] and Off-treatment Follow-up [OF])
NCT00395018 (15) [back to overview]Number of Participants With Re-transplantation Through Week 72
NCT00395018 (15) [back to overview]Total Bilirubin at Week 72
NCT00395018 (15) [back to overview]Prothrombin Time (PT) at Week 72
NCT00410072 (16) [back to overview]Percentage of Participants With HBeAg Seroconversion [( at Weeks 48 and 96
NCT00410072 (16) [back to overview]Percentage of Participants With Alanine Aminotransferase (ALT) Normalization at Weeks 48 and 96
NCT00410072 (16) [back to overview]Percentage of Participants Who Achieved HBV DNA Levels
NCT00410072 (16) [back to overview]Percentage of Participants Who Achieved HBV DNA Levels
NCT00410072 (16) [back to overview]Percentage of Participants Who Achieved HBV DNA Levels <50 IU/mL by PCR at Week 48 and Week 96 by Hepatitis B e Antigen (HBeAg) Status
NCT00410072 (16) [back to overview]Number of Participants With Virologic Breakthrough at Week 48
NCT00410072 (16) [back to overview]Number of Participants With HBV Resistance Through Week 48
NCT00410072 (16) [back to overview]Number of Participants With HBV Resistance at Week 96
NCT00410072 (16) [back to overview]Number of Participants With HBV DNA in Relevant Categories at Weeks 48 and 96
NCT00410072 (16) [back to overview]Number of Participants With Adverse Events, Serious Adverse Events, and Discontinuations From Study Drug Due to Adverse Events or Laboratory Abnormalities
NCT00410072 (16) [back to overview]Mean Log 10 HBV DNA at Weeks 48 and 96
NCT00410072 (16) [back to overview]Percentage of Participants Who Achieved Hepatitis B Virus DNA (HBV DNA) Levels <50 IU/mL by Polymerase Chain Reaction (PCR) at Week 96
NCT00410072 (16) [back to overview]Number of Participants With Virologic Breakthrough at Week 96
NCT00410072 (16) [back to overview]Percentage of Participants With Hepatitis B Surface Antigen (HBsAg) Loss at Weeks 48 and 96
NCT00410072 (16) [back to overview]Percentage of Participants With Hepatitis B e Antigen (HBeAg) Loss at Weeks 48 and 96
NCT00410072 (16) [back to overview]Percentage of Participants With HBsAg Seroconversion at Weeks 48 and 96
NCT00410202 (25) [back to overview]Percentage of Participants With Alanine Aminotransferase (ALT) > 1 x Upper Limit of Normal (ULN) at Baseline Who Achieve ALT Normalization at Week 96
NCT00410202 (25) [back to overview]Percentage of Participants With Alanine Aminotransferase (ALT) > 1 x Upper Limit of Normal (ULN) at Baseline Who Achieve ALT Normalization at Week 48
NCT00410202 (25) [back to overview]Percentage of Participants Who Achieve HBV DNA < Lower Limit of Quantitation (LOQ = 29 IU/mL [Approximately 169 Copies/mL]) at Week 96
NCT00410202 (25) [back to overview]Percentage of Participants Who Achieve HBV DNA < Lower Limit of Quantitation (LOQ = 29 IU/mL [Approximately 169 Copies/mL]) at Week 48
NCT00410202 (25) [back to overview]Percentage of Participants Who Achieve HBV DNA < Lower Limit of Detection (LOD = 10 IU/mL [Approximately 58 Copies/mL]) at Week 96
NCT00410202 (25) [back to overview]Percentage of Participants Who Achieve HBV DNA < Lower Limit of Detection (LOD = 10 IU/mL [Approximately 58 Copies/mL]) at Week 48
NCT00410202 (25) [back to overview]Change in Mean log10 From Baseline in HBV DNA at Week 96
NCT00410202 (25) [back to overview]Percentage of Participants With HBV DNA < 50 IU/mL (Approximately 300 Copies/mL) by PCR at Week 96
NCT00410202 (25) [back to overview]Percentage of Participants With Hepatitis B Surface Antigen (HBsAg) Loss at Week 48
NCT00410202 (25) [back to overview]Percentage of Participants With HBsAg Seroconversion at Week 96
NCT00410202 (25) [back to overview]Percentage of Participants With Hepatitis B Surface Antigen (HBsAg) Loss at Week 96
NCT00410202 (25) [back to overview]Percentage of Participants With Hepatitis B Virus (HBV) Deoxyribonucleic Acid (DNA) < 50 IU/mL (Approximately 300 Copies/mL) by Polymerase Chain Reaction (PCR) at Week 48
NCT00410202 (25) [back to overview]Change in Mean log10 From Baseline in HBV DNA at Week 48
NCT00410202 (25) [back to overview]Cumulative Probability of Emergent Genotypic Resistance at Year 1
NCT00410202 (25) [back to overview]Cumulative Probability of Emergent Genotypic Resistance at Year 2
NCT00410202 (25) [back to overview]Number of Participants With Laboratory Abnormalities: Hematology
NCT00410202 (25) [back to overview]Number of Participants With Laboratory Abnormalities: Serum Chemistry
NCT00410202 (25) [back to overview]Participants With Adverse Events (AE), Serious Adverse Events (SAE), and Discontinuations Due to Adverse Events or Laboratory Abnormalities During Treatment
NCT00410202 (25) [back to overview]Percentage of Participants With HBV DNA by PCR Category at Week 48
NCT00410202 (25) [back to overview]Percentage of Participants With HBV DNA by PCR Category at Week 96
NCT00410202 (25) [back to overview]Percentage of Participants With Confirmed HBeAg Loss at Week 48 (Treated HBeAg Positive Participants Only)
NCT00410202 (25) [back to overview]Percentage of Participants With Confirmed HBeAg Loss at Week 96 (Treated HBeAg Positive Participants Only)
NCT00410202 (25) [back to overview]Percentage of Participants With HBsAg Seroconversion at Week 48
NCT00410202 (25) [back to overview]Percentage of Participants With HBeAg Seroconversion at Week 48 (Treated HBeAg-positive Participants Only)
NCT00410202 (25) [back to overview]Percentage of Participants With HBeAg Seroconversion at Week 96 (Treated HBeAg-positive Participants Only)
NCT00412529 (8) [back to overview]The Area Under the Curve (AUC) of HBV DNA Change.
NCT00412529 (8) [back to overview]Characterization of Very Early Viral Kinetics: Estimation of Viral Clearance
NCT00412529 (8) [back to overview]Characterization of Very Early Viral Kinetics: Estimation of the Rate of Infected Cell Loss
NCT00412529 (8) [back to overview]Characterization of Very Early Viral Kinetics: Estimation of the Efficiency Factor of Blocking Virus Production
NCT00412529 (8) [back to overview]Change in Alanine Aminotransferase (ALT) Levels
NCT00412529 (8) [back to overview]Number of Patients Who Are Polymerase Chain Reaction (PCR) Negative
NCT00412529 (8) [back to overview]Change in Mean Hepatitis B Virus (HBV) DNA Levels
NCT00412529 (8) [back to overview]Change in Mean HBV DNA Level
NCT00423891 (22) [back to overview]Number of Participants With HBV DNA Less Than 50 IU/mL Through Week 96 in Treated Participants
NCT00423891 (22) [back to overview]Number of Participants With HBV DNA Less Than Lower Limit of Quantification (LLQ) for the Roche COBAS TaqMan - HPS Assay Through Week 96 in Treated Participants
NCT00423891 (22) [back to overview]Number of Participants With HBV DNA Less Than Lower Limit of Detection (LLD) for the Roche COBAS TaqMan - HPS Assay at Week 96 in Treated Participants
NCT00423891 (22) [back to overview]Number of Participants Who Had a Protocol Defined Response (PDR) Through Week 96 in Treated Participants
NCT00423891 (22) [back to overview]Number of Participants With a Combination of ALT Normalization and HBV DNA Less Than 50 IU/mL Through Week 96 in Treated Participants
NCT00423891 (22) [back to overview]Number of Participants With a Combination of ALT Normalization and HBV DNA Less Than 50 IU/mL, Plus HBeAg Seroconversion Through Week 96 in Treated Participants
NCT00423891 (22) [back to overview]Number of Participants With Chemistry Laboratory Abnormalities (Grades 1 - 4) - On Treatment - Treated Participants
NCT00423891 (22) [back to overview]Number of Participants With Electrolyte Laboratory Abnormalities (Grades 1 - 4) - On Treatment - Treated Participants
NCT00423891 (22) [back to overview]Number of Participants With HB s Antigen (HBsAg) Seroconversion Through Week 96 in Treated Participants
NCT00423891 (22) [back to overview]Number of Participants With HBV DNA by PCR Categories at Weeks 48 and 96 in Treated Participants
NCT00423891 (22) [back to overview]Alanine Aminotransferase (ALT) Normalization From Baseline Through Week 96 in Treated Participants
NCT00423891 (22) [back to overview]Mean Apparent Total Body Clearance (CLT/F) of Entecavir in LVD-naive and LVD-experienced Participants, by Age Cohort
NCT00423891 (22) [back to overview]Mean Area Under the Concentration-Time Curve in One Dosing Interval [AUC(TAU)] of Entecavir in LVD-naive and LVD-experienced Participants, by Age Cohort
NCT00423891 (22) [back to overview]Mean Log10 Change From Baseline in HBV DNA Using Roche COBAS TaqMan - HPS Through Week 96 in Treated Participants
NCT00423891 (22) [back to overview]Mean Maximum Observed Plasma Concentration (Cmax) and Mean Trough Observed Plasma Concentration (Cmin) of Entecavir in LVD-naive and LVD-experienced Participants, by Age Cohort
NCT00423891 (22) [back to overview]Median Time of Maximum Observed Plasma Concentration (Tmax) in LVD-naive and LVD-experienced Participants, by Age Cohort
NCT00423891 (22) [back to overview]Number of Participants With a Combination of ALT Normalization and HBV DNA Less Than 50 IU/mL, Without HBeAg Seroconversion, Through Week 96 in Treated Participants
NCT00423891 (22) [back to overview]Number of Participants With Serious Adverse Events (SAE) and Discontinuations Due to Adverse Events (AEs) - On Treatment
NCT00423891 (22) [back to overview]Number of Participants With Hepatitis B s Antigen (HBsAg) Loss Through Week 96 in Treated Participants
NCT00423891 (22) [back to overview]Number of Participants With Hepatitis B e Antigen Seroconversion Through Week 96 in Treated Participants
NCT00423891 (22) [back to overview]Number of Participants With Hepatitis B e Antigen (HBeAg) Loss Through Week 96 in Treated Participants
NCT00423891 (22) [back to overview]Number of Participants With Hematology Laboratory Abnormalities (Grades 1 - 4) - On Treatment - Treated Participants
NCT00605384 (1) [back to overview]Number of Participants With Adverse Events (AEs), Serious Adverse Events (SAEs), and Discontinuations Due to AEs or Laboratory Abnormalities
NCT00662545 (5) [back to overview]Incidence of Permanent Discontinuation Due to Toxicity
NCT00662545 (5) [back to overview]Incidence of New Hepatic Decompensation( Ascites, Variceal Hemorrhage, Encephalopathy)
NCT00662545 (5) [back to overview]Incidence of ALT Flares
NCT00662545 (5) [back to overview]HIV RNA < 75 Copies/ml
NCT00662545 (5) [back to overview]Hepatitis B Virus (HBV) DNA
NCT00718887 (9) [back to overview]Mean log10 Reduction From Baseline in Serum HBV DNA Level by Polymerase Chain Reaction Testing
NCT00718887 (9) [back to overview]Percentage of Participants With Loss of Hepatitis B e Antigen (HBeAg) and Hepatitis B e (HBe) Seroconversion
NCT00718887 (9) [back to overview]Percentage of Participants With Grade 3 or 4 Abnormalities in Laboratory Test Results
NCT00718887 (9) [back to overview]Percentage of Participants Who Achieved Normalization of Alanine Aminotransferase (ALT)
NCT00718887 (9) [back to overview]Number of Participants With Hepatitis B s Surface Antibody (HBsAG) Loss and HBsAG Seroconversion
NCT00718887 (9) [back to overview]Number of Participants With Genotypic Resistance to Entecavir
NCT00718887 (9) [back to overview]Number of Participants With Adverse Events, Treatment-related AEs, Serious Adverse Events (SAEs), Treatment-related SAEs, Death as Outcome, Discontinuations Due to AEs, and Abnormalities in Laboratory Test Results (LTR) Leading to Discontinuation
NCT00718887 (9) [back to overview]Percentage of Participants Who Achieved an HBV DNA Level <50 IU/mL at Week 48 by Polymerase Chain Reaction Testing
NCT00718887 (9) [back to overview]Percentage of Participants Who Achieved a Hepatitis B Virus (HBV) DNA Level <50 IU/mL at Week 12 by Polymerase Chain Reaction Testing
NCT00922207 (7) [back to overview]Percentage of Participants Who Were HBeAg Negative
NCT00922207 (7) [back to overview]Percentage of Participants With Combined Response
NCT00922207 (7) [back to overview]Percentage of Participant Who Were Both Hepatitis B Surface Antigen (HBsAg) Negative and Hepatitis B Surface Antibody (Anti-HBs/HBsAb) Positive
NCT00922207 (7) [back to overview]Percentage of Participant With Normal Alanine Aminotransferase (ALT) Levels
NCT00922207 (7) [back to overview]Change From Baseline in Hepatitis B Virus Deoxyribonucleic Acid (HBV DNA) Levels at Weeks 4, 8, 16, 28, 40, 52, 64, 76, 88, and 100
NCT00922207 (7) [back to overview]Percentage of Participants With Hepatitis B e-Antigen (HBeAg) Seroconversion at 100 Weeks After Start of Treatment
NCT00922207 (7) [back to overview]Change From Baseline in HBsAg Levels at Weeks 4, 8, 16, 28, 40, 52, 64, 76, 88, and 100
NCT00940485 (10) [back to overview]Percentage of Participants With Hepatitis B Virus - Deoxyribonucleic Acid <1000 Copies/ Millilitre at Week 48
NCT00940485 (10) [back to overview]Percentage of Participants With Loss of Hepatitis B Envelope Antigen at Week 48
NCT00940485 (10) [back to overview]Quantitative Change in Mean Hepatitis B Envelope Antigen Over Time
NCT00940485 (10) [back to overview]Quantitative Change in Mean Hepatitis B Surface Antigen Change Over Time
NCT00940485 (10) [back to overview]Number of Participants With Laboratory Abnormalities Which Were Captured as an Adverse Event
NCT00940485 (10) [back to overview]Percentage of Participants With Normalized Alanine Aminotransferase at Week 48
NCT00940485 (10) [back to overview]Number of Participants With Incidence of Adverse Events and Serious Adverse Events
NCT00940485 (10) [back to overview]Percentage of Participants With Hepatitis B Envelope Antigen Seroconversion at Week 48
NCT00940485 (10) [back to overview]Percentage of Participants With Hepatitis B Surface Antigen Loss at Week 48
NCT00940485 (10) [back to overview]Percentage of Participants With Hepatitis B Surface Antigen Seroconversion at Week 48
NCT01023217 (1) [back to overview]Complete Virologic Response (CVR, Serum HBV DNA Undetectable by PCR or Less Than 60 IU/mL)
NCT01063036 (11) [back to overview]Percentage of Participants With Hepatitis B Surface Antigen (HBsAg) Seroconversion at Weeks 24, 48, and 96 - Treated Population Who Were HBsAg-Positive at Baseline
NCT01063036 (11) [back to overview]Percentage of Participants With Hepatitis B Surface Antigen (HBsAg) Loss at Weeks 24, 48, 96 - Treated Population Who Were HBsAg-Positive at Baseline
NCT01063036 (11) [back to overview]Percentage of Participants With Hepatitis B e Antigen (HBeAg) Loss at Weeks 24, 48, and 96 - Treated Population Who Were HBeAg Positive at Baseline
NCT01063036 (11) [back to overview]Percentage of Participants With HBV DNA Less Than the Lower Limit of Detection (LLD) at Weeks 24, 48, and 96 - Treated Population
NCT01063036 (11) [back to overview]Percentage of Participants With a Virologic Response at Week 24 and at Week 96 - Treated Population
NCT01063036 (11) [back to overview]Number of Participants With Treatment Emergent Serious Adverse Events (SAEs) on Treatment, and Discontinuation of Study Drug Due to Adverse Events (AE) - Treated Population
NCT01063036 (11) [back to overview]Number of Participants With Emergence of Genotypic Resistance to Study Drugs at Weeks 48 and 96- Treated Population
NCT01063036 (11) [back to overview]Percentage of Participants With HBe Seroconversion at Weeks 24, 48, and 96 - Treated Population Who Were HBeAg-positive at Baseline
NCT01063036 (11) [back to overview]Percentage of Participants With a Virologic Response at Week 48 - Treated Population
NCT01063036 (11) [back to overview]Change From Baseline in Mean log10 HBV DNA at Weeks 12, 24, 48, and 96 - Treated Evaluable Population
NCT01063036 (11) [back to overview]Number of Participants on Treatment With Study Drug With Laboratory Test Abnormalities Meeting Selected Criteria on Treatment - Treated Population
NCT01079806 (16) [back to overview]Percentage of Participants Who Achieved a Combination of Hepatitis B Virus (HBV) DNA Suppression and Hepatitis B e Antigen (HBeAg) Seroconversion at Week 48
NCT01079806 (16) [back to overview]Histological Analysis (Percentage) Among Participants With Available Liver Biopsy Data
NCT01079806 (16) [back to overview]Percentage of Participants With HBeAg Seroconversion (Undetectable HBeAg and Presence of Anti-HBeAb) up to Week 96
NCT01079806 (16) [back to overview]Percentage of Participants With HBeAg Seroconversion on ETV Over-time at Week 96 (All ETV Cohort)
NCT01079806 (16) [back to overview]Percentage of Participants With Hepatitis B e Antigen (HBeAg) Seroconversion at Week 48 (Undetectable HBeAg and Presence of Anti-HBeAb)
NCT01079806 (16) [back to overview]Percentage of Participants With Hepatitis B Virus (HBV) DNA <50 IU/mL at Week 48
NCT01079806 (16) [back to overview]Percentage of Participants With Hepatitis B Virus DNA
NCT01079806 (16) [back to overview]Percentage of Participants With Serum Alanine Aminotransferase ≤1*Upper Limit of Normal at Week 48
NCT01079806 (16) [back to overview]Number of Participants With Adverse Events (Including Palatability Issues), SAEs, Discontinuous Due to Adverse Events, and HBV Disease Progression Through Week 48
NCT01079806 (16) [back to overview]Number of Participants With Laboratory Test Results Meeting the Criteria for Abnormality (Grades 1-4)
NCT01079806 (16) [back to overview]Number of Participants With Laboratory Test Results Meeting the Criteria for Abnormality (Grades 1-4) (Continued)
NCT01079806 (16) [back to overview]Percentage of Participants Who Achieved Sustained HBeAg Seroconversion During Off-treatment Follow up Among Participants Who Achieved HBeAg Seroconversion at End of Dosing (EOD).
NCT01079806 (16) [back to overview]Percentage of Participants Who Maintained HBeAg Seroconversion at Week 96 (End of Blinded Therapy) Among Participants With HBeAg Seroconversion at Week 48
NCT01079806 (16) [back to overview]Percentage of Participants With Death as Outcome, Serious Adverse Events (SAEs), Discontinuations Due to Adverse Events (AEs), Related AEs, Grade 2-4 Related AEs, Grade 3-4 AEs, Malignancies, ALT Flares, and Hepatic Disease Progression Through Week 96
NCT01079806 (16) [back to overview]Percentage of Participants With HbeAg Loss at Weeks 48 and 96
NCT01079806 (16) [back to overview]Percentage of Participants With HbeAg Loss at Weeks 48 and 96
NCT01326546 (1) [back to overview]Percentage of Participants With HBeAg Seroconversion at Week 48
NCT01354652 (2) [back to overview]Overall OLT-free Survival
NCT01354652 (2) [back to overview]Incidence of Elevated Venous Lactate Levels More Than 2 mmol/L of Any Etiology
NCT01368497 (24) [back to overview]Proportion of Participants With Hepatitis B Surface Antigen (HBsAg) Loss
NCT01368497 (24) [back to overview]Proportion of Participants With Hepatitis B Surface Antigen (HBsAg) Loss
NCT01368497 (24) [back to overview]Proportion of Participants With Hepatitis B e Antigen (HBeAg) Loss & Hepatitis B Virus (HBV) Deoxyribonucleic Acid (DNA) Levels ≤1,000 International Units (IU) Per Milliliter (mL)
NCT01368497 (24) [back to overview]Proportion of Participants With Hepatitis B e Antigen (HBeAg) Loss
NCT01368497 (24) [back to overview]Proportion of Participants With Hepatitis B e Antigen (HBeAg) Loss
NCT01368497 (24) [back to overview]Proportion of Participants With HBV DNA ≤1000 IU/mL
NCT01368497 (24) [back to overview]Proportion of Participants With HBV DNA ≤1000 IU/mL
NCT01368497 (24) [back to overview]Proportion of Participants With HBV DNA < 20 IU/mL
NCT01368497 (24) [back to overview]Proportion of Participants With HBV DNA < 20 IU/mL
NCT01368497 (24) [back to overview]Proportion of Participants With HBsAg Seroconversion
NCT01368497 (24) [back to overview]Proportion of Participants With HBsAg Seroconversion
NCT01368497 (24) [back to overview]Proportion of Participants With HBeAg Seroconversion
NCT01368497 (24) [back to overview]Proportion of Participants With HBeAg Seroconversion
NCT01368497 (24) [back to overview]Proportion of Participants With ALT ≤ 40 U/L for Males, ≤ 35 U/L for Females
NCT01368497 (24) [back to overview]Proportion of Participants With Alanine Aminotransferase (ALT) ≤ 40 Units (U) Per Liter (L) for Males, ≤ 35 U/L for Females
NCT01368497 (24) [back to overview]Tanner Stages of Pubic Hair Growth
NCT01368497 (24) [back to overview]Proportion Without Detectable Antiviral Drug-resistance HBV Mutations
NCT01368497 (24) [back to overview]Tanner Stages of Pubic Hair Growth
NCT01368497 (24) [back to overview]Growth Measures: Z-scores Weight, Height, and Body Mass Index
NCT01368497 (24) [back to overview]Growth Measures: Z-scores Weight, Height, and Body Mass Index
NCT01368497 (24) [back to overview]Incidence of Adverse Events (AEs) Per Person-Year
NCT01368497 (24) [back to overview]Incidence of Serious Adverse Events (SAEs) Per Person-Year
NCT01368497 (24) [back to overview]Tanner Stages of Physical Growth
NCT01368497 (24) [back to overview]Tanner Stages of Physical Growth
NCT01369199 (20) [back to overview]Proportion of Participants With HBV DNA <20 IU/mL
NCT01369199 (20) [back to overview]Proportion of Participants With HBsAg Seroconversion
NCT01369199 (20) [back to overview]Proportion of Participants With HBsAg Seroconversion
NCT01369199 (20) [back to overview]Proportion of Participants With HBeAg Loss
NCT01369199 (20) [back to overview]Proportion of Participants With HBeAg Loss
NCT01369199 (20) [back to overview]Proportion of Participants With ALT Normalization (Men <30 U/L, Women <20 U/L)
NCT01369199 (20) [back to overview]Proportion of Participants With ALT Normalization (Men <30 U/L, Women <20 U/L)
NCT01369199 (20) [back to overview]Proportion of Participants With ALT <45 U/L for Men, <30 U/L for Women
NCT01369199 (20) [back to overview]Proportion of Participants With Alanine Aminotransferase (ALT) <45 U/L for Men, <30 U/L for Women
NCT01369199 (20) [back to overview]Absence of Detectable Antiviral Drug-resistance HBV Mutations
NCT01369199 (20) [back to overview]Proportion of Participants With HBsAg Loss
NCT01369199 (20) [back to overview]Proportion of Participants With HBsAg Loss
NCT01369199 (20) [back to overview]Proportion of Participants With HBeAg Seroconversion
NCT01369199 (20) [back to overview]Proportion of Participants With HBeAg Seroconversion
NCT01369199 (20) [back to overview]Proportion of Participants With HBeAg Loss (Lack of Detectable HBeAg) AND HBV DNA ≤1,000 IU/mL
NCT01369199 (20) [back to overview]Incidence of Serious Adverse Events (SAEs) Per Person-Year
NCT01369199 (20) [back to overview]Incidence of Adverse Events (AEs) Per Person-Year of Observation
NCT01369199 (20) [back to overview]Proportion of Participants With HBV DNA ≤1000 IU/mL
NCT01369199 (20) [back to overview]Proportion of Participants With HBV DNA ≤1000 IU/mL
NCT01369199 (20) [back to overview]Proportion of Participants With HBV DNA <20 IU/mL
NCT01438424 (26) [back to overview]Overall Study: Percentage of Participants With Sustained HBV DNA <10^4 Copies/mL by PCR Assay
NCT01438424 (26) [back to overview]Overall Study: Percentage of Participants With HBeAg Seroconversion
NCT01438424 (26) [back to overview]Overall Study: Percentage of Participants Who Achieved ALT Normalization
NCT01438424 (26) [back to overview]Overall Study: Percentage of Participants Who Achieved a Loss of Hepatitis B e Antigen (HBeAg)
NCT01438424 (26) [back to overview]Overall Study: Percentage of Participants by HBV DNA Category by PCR Assay
NCT01438424 (26) [back to overview]Overall Study: Number of Participants With Normal Pancreatic Enzyme and Renal Function Values at Baseline and Abnormalities in Pancreatic Enzyme and Renal Function Laboratory Test Results at End of Dosing
NCT01438424 (26) [back to overview]Overall Study: Number of Participants With Normal Hematology Values at Baseline and Abnormalities in Hematology Laboratory Test Results Through Week 240
NCT01438424 (26) [back to overview]Overall Study: Number of Participants With Normal Electrolyte and Fasting Glucose Values at Baseline and Abnormalities in Electrolyte and Fasting Glucose Laboratory Test Results at End of Dosing
NCT01438424 (26) [back to overview]Overall Study: Number of Participants With Death As Outcome, Any Adverse Event (AE), Grade 3-4 AEs, Serious Adverse Events (SAEs), and Discontinuations Due to AEs
NCT01438424 (26) [back to overview]Overall Study: Mean HBV DNA Level by PCR Assay
NCT01438424 (26) [back to overview]Overall Study: Mean Alanine Transaminase (ALT) Levels
NCT01438424 (26) [back to overview]Off-treatment Follow-up: Percentage of Participants With Sustained Hepatitis B Virus (HBV) DNA <10,000 Copies by Polymerase Chain Reaction (PCR) Assay (Amendment 11 Cohort)
NCT01438424 (26) [back to overview]Overall Study: Percentage of Participants With Sustained HBV DNA Level <300 Copies/mL by PCR Assay
NCT01438424 (26) [back to overview]Off-treatment Follow-up: Mean Change in HBV DNA (Amendment 11 Cohort)
NCT01438424 (26) [back to overview]Overall Study: Percentage of Participants With a Confirmed ≥1 log10 Increase From Nadir in HBV DNA by PCR Assay
NCT01438424 (26) [back to overview]Week 144: Number of Participants With Death As Outcome, Any AE, Grade 3-4 AEs, SAEs, Discontinuations Due to AEs, and Abnormalities in Selected Laboratory Test Results
NCT01438424 (26) [back to overview]Week 96: Percentage of Participants Who Achieved HBV DNA <300 Copies/mL by PCR Assay, Loss of HBeAg, HBeAg Seroconversion, and ALT ≤1.0*ULN (Lamivudine Continuous Switch Cohort)
NCT01438424 (26) [back to overview]Week 96: Percentage of Participants Who Achieved HBV DNA <300 Copies/mL by PCR Assay and ALT ≤1.0*ULN (Lamivudine Retreatment Switch Cohort)
NCT01438424 (26) [back to overview]Week 192: Percentage of Participants With Improvement in Fibrosis (Efficacy Evaluable Cohort)
NCT01438424 (26) [back to overview]Week 192: Percentage of Participants With Histologic Improvement (Efficacy Evaluable Cohort)
NCT01438424 (26) [back to overview]Week 192: Number of Participants With Death As Outcome, Any AE, Grade 3-4 AEs, SAEs, Discontinuations Due to AEs, and Abnormalities in Selected Laboratory Test Results
NCT01438424 (26) [back to overview]Off-treatment Follow-up: Percentage of Participants With Sustained HBV DNA <1,000, <300, and <10,000 Copies/mL by PCR Assay and With ALT ≤1*ULN (Amendment 11 Cohort)
NCT01438424 (26) [back to overview]Percentage of Participants Who Achieved HBV DNA <300 and <10^4 Copies/mL by PCR Assay and ALT ≤1.0*Upper Limit of Normal (ULN) (Entecavir Retreatment Cohort)
NCT01438424 (26) [back to overview]Week 144: Percentage of Participants Who Achieved HBV DNA <300 Copies/mL by PCR Assay and ALT ≤1.0*ULN (Lamivudine Retreatment Switch Cohort)
NCT01438424 (26) [back to overview]Percentage of Participants Who Achieved HBV DNA <300 Copies/mL by PCR Assay, Loss of HBeAG, Seroconversion, and ALT ≤1.0*Upper Limit of Normal (ULN) (Entecavir Continuous Treatment Cohort)
NCT01438424 (26) [back to overview]Week 144: Percentage of Participants Who Achieved HBV DNA <300 Copies/mL by PCR Assay and ALT ≤1.0*ULN (Lamivudine Continuous Switch Cohort)
NCT02065336 (16) [back to overview]Number of Participants With Treatment-Emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)
NCT02065336 (16) [back to overview]Number of Participants With Negative Bee Venom Allergy Test Results at Baseline, Day 29, and Day 85
NCT02065336 (16) [back to overview]Change From Baseline Over Time in Quantitative Hepatitis B Surface Antigen (HBsAG)
NCT02065336 (16) [back to overview]Change From Baseline Over Time in Quantitative Hepatitis B Surface Antigen (HBsAG)
NCT02065336 (16) [back to overview]Change From Baseline Over Time in Quantitative Hepatitis B Surface Antigen (HBsAG)
NCT02065336 (16) [back to overview]Change From Baseline Over Time in Quantitative Hepatitis B Surface Antigen (HBsAG)
NCT02065336 (16) [back to overview]Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Terminal Elimination Half-Life (t1/2), Cohorts 1-5
NCT02065336 (16) [back to overview]Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Area Under the Plasma Concentration-Time Curve From Time 0 Extrapolated to Infinity (AUCinf), Cohorts 1-5 Only
NCT02065336 (16) [back to overview]Pharmacokinetics of ARC-520 of ARC-520 Product Constituents AD0009 and AD0010: Area Under the Plasma Concentration-Time Curve From Time 0 to the Last Quantifiable Plasma Concentration (AUClast), Cohorts 1-5
NCT02065336 (16) [back to overview]Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Apparent Volume of Distribution During the Terminal Phase (Vz), Cohorts 1-5
NCT02065336 (16) [back to overview]Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Area Under the Plasma Concentration-Time Curve From Time 0 to 24 Hours (AUC0-24), Cohorts 1-5
NCT02065336 (16) [back to overview]Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Clearance (CL), Cohorts 1-5
NCT02065336 (16) [back to overview]Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Maximum Observed Plasma Concentration (Cmax), Cohorts 1-5
NCT02065336 (16) [back to overview]Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Terminal Elimination Rate Constant (Kel), Cohorts 1-5
NCT02065336 (16) [back to overview]Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Volume in Steady State (Vss), Cohorts 1-5
NCT02065336 (16) [back to overview]Change From Baseline in Entecavir Plasma Trough Concentration, Cohorts 1-7
NCT02263079 (19) [back to overview]Serum Concentration of Peg-INF-Alfa-2A
NCT02263079 (19) [back to overview]Percentage of Participants With AEs Leading to Dose Modification or Interruption
NCT02263079 (19) [back to overview]Percentage of Participants With Loss of HBsAg
NCT02263079 (19) [back to overview]Percentage of Participants With Loss of Hepatitis B Surface Antigen (HBsAg) at 24 Weeks Post-End of Treatment/End of Untreated Observation
NCT02263079 (19) [back to overview]Change From Baseline in HBV DNA Levels in the Peg-INF-Alfa-2A (Treated) Arm
NCT02263079 (19) [back to overview]Change From Baseline in HBV DNA Levels in the Untreated Control Participants
NCT02263079 (19) [back to overview]Percentage of Participants With Adverse Events (AEs)
NCT02263079 (19) [back to overview]Percentage of Participants With Combined Response for HBeAg Seroconversion (Defined as Loss of HBeAg and Presence of Anti-HBe) and HBV DNA Levels <20,000 IU/mL
NCT02263079 (19) [back to overview]Percentage of Participants With Combined Response for HBeAg Seroconversion (Defined as Loss of HBeAg and Presence of Anti-HBe) and HBV DNA Levels <20,000 IU/mL
NCT02263079 (19) [back to overview]Percentage of Participants With Combined Response for HBeAg Seroconversion (Defined as Loss of HBeAg and Presence of Anti-HBe) and HBV DNA Levels <2000 IU/mL
NCT02263079 (19) [back to overview]Percentage of Participants With Combined Response for HBeAg Seroconversion (Defined as Loss of HBeAg and Presence of Anti-HBe) and HBV DNA Levels <2000 IU/mL
NCT02263079 (19) [back to overview]Percentage of Participants With Different Hepatitis B Virus (HBV) Deoxyribonucleic Acid (DNA) Levels (Less Than [<] 20,000 International Units Per Milliliter [IU/mL], < 2000 IU/mL, or Undetectable HBV DNA)
NCT02263079 (19) [back to overview]Percentage of Participants With Different Hepatitis B Virus (HBV) Deoxyribonucleic Acid (DNA) Levels (Less Than [<] 20,000 International Units Per Milliliter [IU/mL], < 2000 IU/mL, or Undetectable HBV DNA)
NCT02263079 (19) [back to overview]Percentage of Participants With Loss of Hepatitis B Virus Envelope Antigen (HBeAg)
NCT02263079 (19) [back to overview]Percentage of Participants With Loss of Hepatitis B Virus Envelope Antigen (HBeAg)
NCT02263079 (19) [back to overview]Percentage of Participants With Seroconversion to Hepatitis B Envelope Antibody (Anti-HBe), Defined as Loss of HBeAg and Presence of Anti-HBe
NCT02263079 (19) [back to overview]Percentage of Participants With Seroconversion to Hepatitis B Envelope Antibody (Anti-HBe), Defined as Loss of HBeAg and Presence of Anti-HBe
NCT02263079 (19) [back to overview]Percentage of Participants With Seroconversion to Hepatitis B Surface Antibody (Anti-HBs), Defined as Loss of HBsAg and Presence of Anti-HBs
NCT02263079 (19) [back to overview]Percentage of Participants With Seroconversion to Hepatitis B Surface Antibody (Anti-HBs), Defined as Loss of HBsAg and Presence of Anti-HBs
NCT02452528 (1) [back to overview]Number of Participants With Treatment-Emergent Adverse Events (TEAEs), Serious Adverse Events (SAEs), Deaths, and Discontinuations Due to Adverse Events (AEs)
NCT02577029 (1) [back to overview]Number of Participants With Treatment-Emergent Adverse Events (TEAEs) and Serious TEAEs Considered Possibly or Probably Related to Treatment
NCT02604199 (3) [back to overview]Number of Participants With Adverse Events (AEs), Serious AEs (SAEs), Deaths and Discontinuations Due to AEs
NCT02604199 (3) [back to overview]Change From Baseline in Quantitative Hepatitis B Surface Antigen (Log qHBsAg) Over Time
NCT02604199 (3) [back to overview]Change From Baseline in Quantitative Hepatitis B Surface Antigen (Log qHBsAg) at Day 113
NCT02604212 (26) [back to overview]Change From Baseline at Day 99 in Log qHBsAg, by Category
NCT02604212 (26) [back to overview]Change From Baseline at Day 99 in Log qHBsAg, by Category
NCT02604212 (26) [back to overview]Change From Baseline at Day 99 in Log qHBsAg, by Category
NCT02604212 (26) [back to overview]Change From Baseline at Day 85 in Log qHBsAg, by Category
NCT02604212 (26) [back to overview]Change From Baseline at Day 85 in Log qHBsAg, by Category
NCT02604212 (26) [back to overview]Change From Baseline at Day 85 in Log qHBsAg, by Category
NCT02604212 (26) [back to overview]Change From Baseline at Day 71 in Log qHBsAg, by Category
NCT02604212 (26) [back to overview]Change From Baseline at Day 71 in Log qHBsAg, by Category
NCT02604212 (26) [back to overview]Change From Baseline at Day 71 in Log qHBsAg, by Category
NCT02604212 (26) [back to overview]Change From Baseline at Day 57 in Log qHBsAg, by Category
NCT02604212 (26) [back to overview]Change From Baseline at Day 57 in Log qHBsAg, by Category
NCT02604212 (26) [back to overview]Change From Baseline at Day 43 in Log qHBsAg, by Category
NCT02604212 (26) [back to overview]Change From Baseline at Day 43 in Log qHBsAg, by Category
NCT02604212 (26) [back to overview]Change From Baseline at Day 43 in Log qHBsAg, by Category
NCT02604212 (26) [back to overview]Change From Baseline at Day 29 in Log qHBsAg, by Category
NCT02604212 (26) [back to overview]Change From Baseline at Day 29 in Log qHBsAg, by Category
NCT02604212 (26) [back to overview]Change From Baseline at Day 15 in Log qHBsAg, by Category
NCT02604212 (26) [back to overview]Change From Baseline at Day 15 in Log qHBsAg, by Category
NCT02604212 (26) [back to overview]Change From Baseline at Day 15 in Log qHBsAg, by Category
NCT02604212 (26) [back to overview]Change From Baseline at Day 113 in Log qHBsAg, by Category
NCT02604212 (26) [back to overview]Change From Baseline at Day 113 in Log qHBsAg, by Category
NCT02604212 (26) [back to overview]Change From Baseline at Day 113 in Log qHBsAg, by Category
NCT02604212 (26) [back to overview]Change From Baseline in Quantitative Hepatitis B Surface Antigen (Log qHBsAg) at Day 113
NCT02604212 (26) [back to overview]Number of Participants With Adverse Events (AEs), Serious AEs (SAEs), Deaths, and Discontinuations Due to AEs
NCT02604212 (26) [back to overview]Change From Baseline at Day 57 in Log qHBsAg, by Category
NCT02604212 (26) [back to overview]Change From Baseline in Log qHBsAg Over Time
NCT02726789 (4) [back to overview]Number of Patients Experiencing Reductions in Serum HBsAg
NCT02726789 (4) [back to overview]Number of Patients Experiencing Reductions in Serum HBV DNA
NCT02726789 (4) [back to overview]Number of Patients Experiencing Serum Anti-HBs > 10 mIU / ml
NCT02726789 (4) [back to overview]Number of Patients Experiencing Treatment Emergent Laboratory Test Abnormalities or Adverse Events.
NCT02738008 (1) [back to overview]Number of Participants With Treatment Emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)
NCT02797522 (2) [back to overview]Number of Participants With TEAEs: CHB Participants
NCT02797522 (2) [back to overview]Number of Participants With Treatment-Emergent Adverse Events (TEAEs): Healthy Volunteers
NCT02881008 (7) [back to overview]Proportion of Patients With HBsAg Response at 24 Week of Therapy
NCT02881008 (7) [back to overview]Proportion of Patients With HBV DNA Response at Week 24 of Therapy
NCT02881008 (7) [back to overview]Proportion of Patients With HBV DNA Response at Week 12 of Therapy
NCT02881008 (7) [back to overview]Proportion of Patients With Biochemical Response at 24 Weeks of Therapy
NCT02881008 (7) [back to overview]Proportion of Patients With cccDNA Response at 24 Week of Therapy
NCT02881008 (7) [back to overview]Proportion of Patients With HBsAg Response at 12 Week of Therapy
NCT02881008 (7) [back to overview]Proportion of Patients With Biochemical Response at 12 Weeks of Therapy
NCT03083821 (6) [back to overview]Apparent Total Body Clearance (CLT/F)
NCT03083821 (6) [back to overview]Area Under the Concentration-time Curve in One Dosing Interval [AUC(TAU)]
NCT03083821 (6) [back to overview]Maximum Observed Plasma Concentration (Cmax)
NCT03083821 (6) [back to overview]Observed Plasma Concentration at 24 Hours Postdose (C24)
NCT03083821 (6) [back to overview]Time of Maximum Observed Plasma Concentration (Tmax)
NCT03083821 (6) [back to overview]Trough Observed Plasma (Predose) Concentration (Ctrough)
NCT03576066 (12) [back to overview]Trough Levels of Tenofovir Alafenamide (TAF) on ABI-H0731 + SOC NUC Therapy as Compared With Placebo + SOC NUC Therapy
NCT03576066 (12) [back to overview]Trough Levels of Tenofovir Disoproxil Fumarate (TDF) on ABI-H0731 + SOC NUC Therapy as Compared With Placebo + SOC NUC Therapy
NCT03576066 (12) [back to overview]Number of Participants With a Clinically-significant Change in Vital Signs
NCT03576066 (12) [back to overview]Number of Participants With Abnormal Alanine Aminotransferase (ALT) at Baseline Who Have Normal ALT at Week 24 on ABI-H0731 + NUC Therapy as Compared With Placebo + NUC Therapy
NCT03576066 (12) [back to overview]Number of Participants With One or More Abnormal Safety Laboratory Result
NCT03576066 (12) [back to overview]Number of Participants With One or More Adverse Events
NCT03576066 (12) [back to overview]Number of Participants With Premature Study Discontinuation
NCT03576066 (12) [back to overview]Change in Mean log10 Serum HBeAg From Baseline (Day 1) to Week 24 on ABI-H0731 + SOC NUC as Compared to Placebo + SOC NUC
NCT03576066 (12) [back to overview]Change in Mean log10 Serum HBsAg From Baseline (Day 1) to Week 24 on ABI-H0731 + SOC NUC as Compared to Placebo + SOC NUC
NCT03576066 (12) [back to overview]Trough Levels of ABI-H0731 on ABI-H0731 + SOC NUC Therapy
NCT03576066 (12) [back to overview]Trough Levels of Entecavir (ETV) on ABI-H0731 + SOC NUC Therapy as Compared With Placebo + SOC NUC Therapy
NCT03576066 (12) [back to overview]Number of Participants With a Clinically-significant Electrocardiogram Abnormality
NCT03577171 (10) [back to overview]Change in Mean log10 HBV DNA From Baseline (Day 1) to Week 12 or Week 24 on ABI H0731 + SOC ETV as Compared to Placebo + SOC ETV
NCT03577171 (10) [back to overview]Number of Participants With a Decline in Viral DNA to Below Limit of Quantitation on ABI-H0731 + SOC ETV as Compared to Placebo + SOC ETV
NCT03577171 (10) [back to overview]Number of Participants With One or More Abnormal Safety Laboratory Result
NCT03577171 (10) [back to overview]Trough Levels of ABI-H0731 on ABI-H0731 + SOC ETV Therapy
NCT03577171 (10) [back to overview]Number of Participants One or More Adverse Events
NCT03577171 (10) [back to overview]Number of Participants With a Clinically-significant Change in Vital Signs
NCT03577171 (10) [back to overview]Number of Participants With a Clinically-significant Electrocardiogram Abnormality
NCT03577171 (10) [back to overview]Number of Participants With Abnormal Alanine Aminotransferase (ALT) at Baseline Who Have Normal ALT at Week 24 on ABI-H0731 + SOC ETV as Compared to Placebo + SOC ETV
NCT03577171 (10) [back to overview]Number of Participants With Premature Study Discontinuation
NCT03577171 (10) [back to overview]Trough Levels of ETV on ABI-H0731 + ETV Therapy as Compared With Placebo + ETV Therapy
NCT03780543 (5) [back to overview]Number of Subjects With Adverse Events
NCT03780543 (5) [back to overview]Number of Subjects With Abnormal Alanine Aminotransferase (ALT) at Baseline Who Have Normal ALT at End of Treatment (EOT) and End of Study (EOS)
NCT03780543 (5) [back to overview]Sustained Viral Response (SVR) at 24 Weeks Off Treatment
NCT03780543 (5) [back to overview]Number of Subjects With Suppression/Loss of Viral HBeAg Antigen/DNA on Combination Treatment Whose Viral Antigens Rebound Off Therapy
NCT03780543 (5) [back to overview]Number of Subjects With Suppression/Loss of Viral Core-related Antigen/DNA on Combination Treatment Whose Viral Antigens Rebound Off Therapy
NCT04398134 (4) [back to overview]Percentage of Participants With Premature Treatment Discontinuation
NCT04398134 (4) [back to overview]Percentage of Participants With Adverse Events
NCT04398134 (4) [back to overview]Change From Baseline in Mean log10 HBV DNA
NCT04398134 (4) [back to overview]Percentage of Participants With Abnormal Laboratory Results
NCT04465916 (2) [back to overview]HBsAg Change (Δ log10) From Day 1 to Week 16 of Treatment
NCT04465916 (2) [back to overview]Virologic Failure Rate
NCT04781647 (10) [back to overview]Number of Participants With an Adverse Event
NCT04781647 (10) [back to overview]Number of Participants With a Laboratory Abnormality
NCT04781647 (10) [back to overview]Number of Participants With Premature Discontinuation of Treatment
NCT04781647 (10) [back to overview]Mean Change From Baseline in HBsAg
NCT04781647 (10) [back to overview]Plasma Concentration of ABI-H0731
NCT04781647 (10) [back to overview]Mean Change From Baseline in HBV pgRNA
NCT04781647 (10) [back to overview]Plasma Concentration of ABI-H0731
NCT04781647 (10) [back to overview]Mean Change From Baseline in HBeAg
NCT04781647 (10) [back to overview]Mean Change From Baseline in HBcrAg
NCT04781647 (10) [back to overview]Mean Change From Baseline HBV DNA
NCT04820686 (20) [back to overview]Change From Baseline in Mean log10 Hepatitis B Core-related Antigen (HBcrAg) On-Treatment
NCT04820686 (20) [back to overview]Number of Participants With One or More Abnormal Laboratory Result
NCT04820686 (20) [back to overview]Change From Baseline in Mean log10 HBV RNA Off-Treatment
NCT04820686 (20) [back to overview]Change From Baseline in Mean log10 Serum Hepatitis B Surface Antigen (HBsAg) Off-Treatment
NCT04820686 (20) [back to overview]Change From Baseline in Mean log10 Hepatitis B Core-related Antigen (HBcrAg) Off-Treatment
NCT04820686 (20) [back to overview]Number of Participants With Premature Treatment Discontinuation Due to AEs
NCT04820686 (20) [back to overview]Number of Participants With Premature Treatment Discontinuation Due to AEs
NCT04820686 (20) [back to overview]Change From Baseline in Mean log10 Hepatitis B Core-related Antigen (HBcrAg) Off-Treatment
NCT04820686 (20) [back to overview]Number of Participants With One or More Adverse Events (AEs)
NCT04820686 (20) [back to overview]Change From Baseline in Mean log10 HBV RNA Off-Treatment
NCT04820686 (20) [back to overview]Number of Participants With Premature Treatment Discontinuation Due to AEs
NCT04820686 (20) [back to overview]Change From Baseline in Mean log10 Serum Hepatitis B Surface Antigen (HBsAg) On-Treatment
NCT04820686 (20) [back to overview]Change From Baseline in Mean log10 Serum Hepatitis B Surface Antigen (HBsAg) On-Treatment
NCT04820686 (20) [back to overview]Change From Baseline in Mean log10 HBV RNA Off-Treatment
NCT04820686 (20) [back to overview]Change From Baseline in Mean log10 Serum Hepatitis B Surface Antigen (HBsAg) Off-Treatment
NCT04820686 (20) [back to overview]Change From Baseline in Mean log10 Serum Hepatitis B Surface Antigen (HBsAg) Off-Treatment
NCT04820686 (20) [back to overview]Change From Baseline in Mean log10 HBV RNA On-Treatment
NCT04820686 (20) [back to overview]Change From Baseline in Mean log10 HBV RNA Off-Treatment
NCT04820686 (20) [back to overview]Change From Baseline in Mean log10 HBV RNA On-Treatment
NCT04820686 (20) [back to overview]Change From Baseline in Mean log10 Serum Hepatitis B Surface Antigen (HBsAg) Off-Treatment

Number of Subjects Achieving Composite Endpoint (HBV DNA < 10*4 Copies/mL by PCR Assay and Normal ALT [≤ 1.0 x ULN]) Through Week 48

(NCT00065507)
Timeframe: Baseline, Week 4, Week 8, Week 12, Week 24, Week 48

,
InterventionParticipants (Number)
BaselineWeek 4Week 8Week 12Week 24Week 48
Adefovir (ADV) 10 mg1611162434
Entecavir (ETV) 1.0 mg32334374957

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Number of Participants With Improvement or No Worsening in Child-Pugh Score From Baseline to Week 48

Number of participants in each group with improvement or no worsening in Child-Pugh score from baseline to Week 48 as measured by improvement or no worsening in Child-Pugh score. Child-Pugh classification assesses the prognosis of chronic liver disease by 5 clinical measures, scored 1-3 each (most severe derangement=3). Score range: 5 (best prognosis) to 15 (worst prognosis). (NCT00065507)
Timeframe: Baseline, Week 4, Week 8, Week 12, Week 24, Week 48

,
InterventionParticipants (Number)
BaselineWeek 4Week 8Week 12Week 24Week 48
Adefovir (ADV) 10 mg06762626561
Entecavir (ETV) 1.0 mg06667686661

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Number of Participants With Malignant Neoplasms - On Treatment or During 24-Week Follow-up Period

Data includes type of malignant neoplasm. (NCT00065507)
Timeframe: On-treatment=up to Week 48 (Day 336); if discontinued early, all data up to 5 days after discontinuation date. 24-week follow-up=limited to end-of-dosing values and those from 6 days after last dose of study therapy to end of follow-up.

,
Interventionparticipants (Number)
Any Adverse EventsHepatic Neoplasm, MalignantBasal Cell CarcinomaLymph Node Cancer, MetastaticHepatic Mass
Adefovir (ADV) 10 mg1818000
Entecavir (ETV) 1.0 mg1412111

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Number of Participants With Treatment-Emergent Grade 3/4 Laboratory Abnormalities - Week 48 and Cumulative Data

Grade 3/4 laboratory abnormalities (hematology, electrolyte, lipase, liver function, metabolic, renal function, urinalysis). The Week 48 data set was used to evaluate the Week-48 on-treatment safety. The cumulative data set was used to evaluate the safety while on treatment. Common Terminology Criteria for Adverse Events v3.0 (CTCAE) Grades:1=Mild, 2=Moderate, 3=Severe, 4=Life-threatening/disabling, 5=Death. (NCT00065507)
Timeframe: Week 48=all on-treatment laboratory measurements up to Week 48. Cumulative data = on-treatment laboratory measurements obtained after the start of therapy and no more than 5 days after the last dose of study therapy.

,,,
Interventionparticipants (Number)
HemoglobinInternational Normalized RatioPlatelet CountProthrombin TimeBicarbonate, LowChloride, Serum, LowBicarbonate/Carbon Dioxide, LowPotassium, Serum, HighSodium, SerumSodium, Serum, LowLipase, Total (colorimetric assay)Alanine Aminotransferase (ALT)AlbuminAlkaline Phosphatase (ALP)Aspartate Aminotransferase (AST)Bilirubin, TotalG-Glutamyl Transferase (GGT)Glucose, Fasting Serum, HighCreatininePhosphorus, inorganicBlood, urineGlucose, urineProtein, urineNeutrophils (relative)Neutrophils + Bands (relative)Neutrophils (absolute)
Cumulative - Adefovir (ADV) 10 mg10322411424055254317251000622134187
Cumulative - Entecavir (ETV) 1.0 mg1140252542416623591924912018172045
Week 48 - Adefovir (ADV) 10 mg82221742403318131318600413112143
Week 48 - Entecavir (ETV) 1.0 mg830202032316617390719101013111022

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Number of Participants With HBV DNA < 300 Copies/mL by PCR At Week 48

(NCT00065507)
Timeframe: Week 48

InterventionParticipants (Number)
Entecavir (ETV) 1.0 mg57
Adefovir (ADV) 10 mg18

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Number of Participants With HBV DNA < 300 Copies/mL by PCR At Week 24

(NCT00065507)
Timeframe: Week 24

Interventionparticipants (Number)
Entecavir (ETV) 1.0 mg49
Adefovir (ADV) 10 mg15

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Mean Change From Baseline in Total Bilirubin Through Week 48

Mean total bilirubin levels, and mean change from baseline in total bilirubin, a measure of liver secretory function.Normal range for total bilirubin = 0.2 - 1.2 mg/dL. (NCT00065507)
Timeframe: Baseline, Week 4, Week 8, Week 12, Week 24, Week 36, Week 48

,
Interventionmg/dL (Mean)
Baseline Value (n=100; n=91)Change at Week 4 (n=98; n=88)Change at Week 8 (n=92; n=82)Change at Week 12 (n=88;l n=80)Change at Week 24 (n=81; n=77)Change at Week 36 (n=76; n=70)Change at Week 48 (n=72; n=63)
Adefovir (ADV) 10 mg2.500.21-0.17-0.28-0.14-0.09-0.10
Entecavir (ETV) 1.0 mg2.80-0.060.11-0.20-0.41-0.36-0.61

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Mean Change From Baseline in Prothrombin Time Through Week 48

Mean prothrombin time, and mean change from baseline in prothrombin time, a measure of synthetic liver function. Prothrombin time is the time it takes (in seconds) for a sample of blood to clot. Normal range for prothrombin time (PT) = 10-13 seconds. (NCT00065507)
Timeframe: Baseline, Week 4, Week 8, Week 12, Week 24, Week 36, Week 48

,
Interventionseconds (Mean)
Baseline Value (n=100; n=91)Change at Week 4 (n=98; n=87)Change at Week 8 (n=91; n=79)Change at Week 12 (n=88; n=80)Change at Week 24 (n=80; n=77)Change at Week 48 (n=72; n=63)
Adefovir (ADV) 10 mg15.350.030.06-0.05-0.18-0.52
Entecavir (ETV) 1.0 mg16.28-0.08-0.10-0.29-0.75-0.99

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Mean Change From Baseline in Model for End-Stage Liver Disease (MELD) Scores From Baseline Through Week 48

Adjusted mean change from baseline in MELD score through Week 48 (adjusted for baseline value). The Model for End-Stage Liver Disease (MELD), is a scoring system for assessing the severity of chronic liver disease. MELD uses the patient's values for serum bilirubin, serum creatinine, and the international normalized ratio for prothrombin time (INR) to predict survival. In interpreting the MELD Score in hospitalized patients, the 3 month mortality is: 40 or more=100% mortality; 30-39=83% mortality; 20-29=76% mortality; 10-19=27% mortality; <10=4% mortality. (NCT00065507)
Timeframe: Baseline, Week 4, Week 8, Week 12, Week 24, Week 36, Week 48

,
Interventionunits on a scale (Mean)
Baseline Value (n=100; n=91)Week 4 (n=97; n=87)Week 8 (n=90; n=79)Week 12 (n=88; n=80)Week 24 (n=80; n=77)Week 36 (n=75; n=70)Week 48 (n=72; n=62)
Adefovir (ADV) 10 mg15.30.1-0.4-0.9-0.9-1.2-1.7
Entecavir (ETV) 1.0 mg17.1-0.1-0.8-1.2-2.0-2.3-2.6

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Improvement or No Worsening in MELD Score Through Week 48

Participants with improvement or no worsening (any decrease or no change from baseline in score) in MELD score through Week 48. The Model for End-Stage Liver Disease (MELD), is a scoring system for assessing the severity of chronic liver disease. MELD uses the patient's values for serum bilirubin, serum creatinine, and the international normalized ratio for prothrombin time (INR) to predict survival. In interpreting the MELD Score in hospitalized patients, the 3 month mortality is: 40 or more=100% mortality; 30-39=83% mortality; 20-29=76% mortality; 10-19=27% mortality; <10=4% mortality. (NCT00065507)
Timeframe: Baseline, Week 4, Week 8, Week 12, Week 24, Week 48

,
InterventionParticipants (Number)
BaselineWeek 4Week 8Week 12Week 24Week 48
Adefovir (ADV) 10 mg05152605147
Entecavir (ETV) 1.0 mg05863676253

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Cumulative Number of Participants With Adverse Events (AEs), Serious Adverse Events (SAEs), Deaths, HCC, Discontinuations Due to AEs, and Confirmed Creatinine Increase >=0.5 mg/dL

AE=any new untoward medical occurrence/worsening of a pre-existing medical condition regardless of causal relationship. SAE=any untoward medical occurrence at any dose that: results in death; is life-threatening; requires/prolongs inpatient hospitalization; results in persistent/significant disability; is cancer; is congenital anomaly/birth defect; results in drug dependency/abuse; is an important medical event. Grades:1=Mild, 2=Moderate, 3=Severe, 4=Life-threatening/disabling, 5=Death. Confirmed increase in serum creatinine=values ≥0.5 mg/dL compared with baseline on 2 sequential measures. (NCT00065507)
Timeframe: on-treatment events obtained after the start of therapy and no more than 5 days after the last dose of study therapy.

,
Interventionparticipants (Number)
Any AEGrade 3/4 AEsSAEsDeathsHCCDiscontinuations due to AEsConfirmed creatinine increase >= 0.5 mg/dL
Adefovir (ADV) 10 mg8642592918521
Entecavir (ETV) 1.0 mg9155702312717

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Change From Baseline in Platelet Count Through Week 48

Mean baseline platelet count and mean change from baseline in platelet count at specific timepoints. Platelets are the smallest particles found in the blood, which play a major role in forming blood clots. Normal range for platelets = 140 - 450 X 10*9 c/L. (NCT00065507)
Timeframe: Baseline, Week 4, Week 8, Week 12, Week 24, Week 36, Week 48

,
Intervention10*9 c/L (Mean)
Baseline Value (n=97; n=91)Change at Week 4 (n=90; n=85)Change at Week 8 (n=82; n=76)Change at Week 12 (n=85; n=79)Change at Week 24 (n=77; n=76)Change at Week 36 (n=72; n=69)Change at Week 48 (n=68; n=63)
Adefovir (ADV) 10 mg93.31-2.143.88-0.81-2.891.323.05
Entecavir (ETV) 1.0 mg87.32-0.933.554.362.476.5610.19

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Change From Baseline in Child-Pugh Score Through Week 48

Mean change from baseline in Child-Pugh score through week 48. Child-Pugh classification assesses the prognosis of chronic liver disease by 5 clinical measures, scored 1-3 each (most severe derangement=3). Score range: 5 (best prognosis) to 15 (worst prognosis). (NCT00065507)
Timeframe: Baseline, Week 4, Week 8, Week 12, Week 24, Week 36, Week 48

,
Interventionunits on a scale (Mean)
Baseline Value (n=100, n=91)Change at Week 4 (n=90; n=85)Change at Week 8 (n=90; n=79)Change at Week 12 (n=87; n=80)Change at Week 24 (n=80; n=77)Change at Week 36 (n=75; n=70)Change at Week 48 (n=72; n=64)
Adefovir (ADV) 10 mg8.4-0.3-0.3-0.3-0.7-0.9-1.3
Entecavir (ETV) 1.0 mg8.8-0.4-0.4-0.6-1.2-1.6-1.7

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Change From Baseline in Albumin Through Week 48

Mean albumin levels, and mean change from baseline in albumin, a measure of synthetic liver function. Normal range for albumin = 3.5 - 5.3 g/dL. (NCT00065507)
Timeframe: Baseline, Week 4, Week 8, Week 12, Week 24, Week 36, Week 48

,
Interventiong/dL (Mean)
Baseline Value (n=100; n=91)Change at Week 4 (n=98; n=88)Change at Week 8 (n=92; n=82)Change at Week 12 (n=88; n=80)Change at Week 24 (n=81; n=77)Change at Week 36 (n=76; n=70)Change at Week 48 (n=72; n=63)
Adefovir (ADV) 10 mg3.10-0.01-0.030.030.200.250.34
Entecavir (ETV) 1.0 mg3.00-0.040.010.050.260.360.49

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>=2-Point Reduction From Baseline in Child-Pugh Score Through Week 48

Child-Pugh classification assesses the prognosis of chronic liver disease by 5 clinical measures, scored 1-3 each (most severe derangement=3). Score range: 5 (best prognosis) to 15 (worst prognosis). (NCT00065507)
Timeframe: Baseline, Week 4, Week 8, Week 12, Week 24, Week 36, Week 48

,
InterventionParticipants (Number)
BaselineWeek 4Week 8Week 12Week 24Week 36Week 48
Adefovir (ADV) 10 mg0111011221925
Entecavir (ETV) 1.0 mg0142322323535

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Change From Baseline in HBV DNA by PCR at Week 48

Mean change from baseline in HBV DNA by PCR at Week 48, adjusted for baseline HBV DNA and LVDr Status. (NCT00065507)
Timeframe: Baseline, Week 48

Interventionlog10 copies/mL (Mean)
Entecavir (ETV) 1.0 mg-4.66
Adefovir (ADV) 10 mg-3.90

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Change From Baseline in Hepatitis B Virus (HBV) DNA by Polymerase Chain Reaction (PCR) at Week 24

Mean reduction in serum HBV DNA determined by PCR assay (log10 copies/mL) at Week 24 adjusted for baseline HBV DNA and lamivudine resistance (LVDr) status, based on linear regression analysis. (NCT00065507)
Timeframe: Baseline, Week 24

Interventionlog10 copies/mL (Mean)
Entecavir (ETV) 1.0 mg-4.48
Adefovir (ADV) 10 mg-3.40

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Participants Achieving Albumin Normalization Through Week 48

Number of participants who achieved normalization of albumin (>= 1 x lower limit of normal [LLN]), a measure of liver function, at specific timepoints. (NCT00065507)
Timeframe: Baseline, Week 4, Week 8, Week 12, Week 24, Week 36, Week 48

,
Interventionparticipants (Number)
BaselineWeek 4Week 8Week 12Week 24Week 36Week 48
Adefovir (ADV) 10 mg07611141420
Entecavir (ETV) 1.0 mg0296202932

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Participants Achieving Platelet Count Normalization Through Week 48

Number of participants who achieved normalization of platelet count (>= 1 x lower limit of normal [LLN]), a measure of liver function, at specific timepoints. (NCT00065507)
Timeframe: Baseline, Week 4, Week 8, Week 12, Week 24, Week 36, Week 48

,
Interventionparticipants (Number)
BaselineWeek 4Week 8Week 12Week 24Week 36Week 48
Adefovir (ADV) 10 mg0453221
Entecavir (ETV) 1.0 mg0337256

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Participants Achieving Prothrombin Time Normalization Through Week 48

Number of participants who achieved normalization of prothrombin time (<= 1 x ULN), a measure of liver function, at specific timepoints. (NCT00065507)
Timeframe: Baseline, Week4, Week 8, Week 12, Week 24, Week 36, Week 48

,
Interventionparticipants (Number)
BaselineWeek 4Week 8Week 12Week 24Week 36Week 48
Adefovir (ADV) 10 mg0443657
Entecavir (ETV) 1.0 mg03549108

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Participants Achieving Total Bilirubin Normalization Through Week 48

Number of participants who achieved normalization of total bilirubin (<= 1 x ULN), a measure of liver function, at specific timepoints. (NCT00065507)
Timeframe: Baseline, Week 4, Week 8, Week 12, Week 24, Week 36, Week 48

,
Interventionparticipants (Number)
BaselineWeek 4Week 8Week 12Week 24Week 36Week 48
Adefovir (ADV) 10 mg0999101718
Entecavir (ETV) 1.0 mg0410812915

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Number of Hepatocellular Carcinoma (HCC) Events at Different Time Points Through Week 48

HCC-free survival was analyzed using life tables. Measured values show the number of HCC events among treated participants at given time points. (NCT00065507)
Timeframe: Week 48

,
InterventionHCC events (Number)
Weeks 0-4 (n=102; n=89)Weeks 4-8 (n=99; n=86)Weeks 8-12 (n=96; n=83)Weeks 12-16 (n=90; n=80)Weeks 16-20 (n=87; n=77)Weeks 20-24 (n=86; n=75)Weeks 24-28 (n=81; n=71)Weeks 28-32 (n=78; n=70)Weeks 32-36 (n=77; n=66)Weeks 36-40 (n=77; n=64)Weeks 40-44 (n=73; n=62)Weeks 44-48 (n=71; n=62)
Adefovir (ADV) 10 mg35691114151718202022
Entecavir (ETV) 1.0 mg2510111116171717192124

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Number of Participants Achieving Alanine Transaminase (ALT) Normalization (≤1.0 x Upper Limit of Normal [ULN]) at Weeks 24 and 48

Number of participants in each group who achieved ALT normalization (≤1.0 x upper limit of normal [ULN]) among those with baseline ALT >1.0 x ULN at Weeks 24 and 48 (NCT00065507)
Timeframe: Week 24, Week 48

,
InterventionParticipants (Number)
Week 24Week 48
Adefovir (ADV) 10 mg2833
Entecavir (ETV) 1.0 mg4649

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Number of Participants Undergoing Liver Transplant - On-Treatment or 24-Week Follow-Up

(NCT00065507)
Timeframe: On-treatment=up to Week 48 (Day 336); if discontinued early, all data up to 5 days after discontinuation date. 24-week follow-up=limited to end-of-dosing values and those from 6 days after last dose of study therapy to end of follow-up.

,
Interventionparticipants (Number)
Liver Transplant: YesLiver Transplant: No
Adefovir (ADV) 10 mg386
Entecavir (ETV) 1.0 mg1191

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Number of Participants With Alanine Aminotransferase (ALT) Flares - On Treatment

ALT flare=ALT > 2 x baseline and > 10 x upper limit of normal (ULN) by clinical laboratory evaluation. Table includes number of participants with selected clinical events and/or laboratory abnormalities during ALT flares. Selected clinical events during ALT flares=ascites, hepatic encephalopathy, jaundice, bacterial peritonitis. Selected Laboratory abnormalities during ALT flares=international normalized ratio > 1.5 or prothrombin time >= 1.2 x ULN and total bilirubin >2.5 mg/dL and > 1 mg/dL increase from baseline. (NCT00065507)
Timeframe: On-treatment=up to Week 48 (Day 336); if discontinued early, all data up to 5 days after discontinuation date.

,
Interventionparticipants (Number)
ALT flaresALT flares, no clinical events/lab abnormalitiesALT flares, with clinical events/lab abnormalities
Adefovir (ADV) 10 mg101
Entecavir (ETV) 1.0 mg211

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Number of Participants With Improvement in Child-Pugh Class at Week 24 and Week 48

Number of Participants in each group with improvement in Child-Pugh score from baseline to Week 48 as measured by improvement in Child-Pugh class. Improvement in Child-Pugh Class is defined as change from B to A or C to A. Evaluable subjects are subjects with Child-Pugh Class B or C at Baseline. Child-Pugh classification assesses the prognosis of chronic liver disease by 5 clinical measures, scored 1-3 each (most severe derangement=3). Score range: 5 (best prognosis) to 15 (worst prognosis). Child-Pugh class A to C employs the added score from above: 5-6=Class A; 7-9=Class B; 10-15=Class C. (NCT00065507)
Timeframe: Week 24, Week 48

,
InterventionParticipants (Number)
Week 24Week 48
Adefovir (ADV) 10 mg2229
Entecavir (ETV) 1.0 mg2535

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HBV DNA Viral Kinetics - Spline Model

This analysis uses a 3-parameter piece-wise linear model and describes the biphasic decline in HBV DNA (measured by PCR assay) through Week 12. The 3 parameters are the values for the 2 slopes, describing the first and second phase declines, respectively, and the estimated HBV DNA at the knot (at day 10; the time point where the 2 phases join). The biphasic viral decay kinetics for each treatment were obtained using a spline fitting procedure to estimate the 3 parameters for each subject; these estimates were then averaged within each treatment group. (NCT00096785)
Timeframe: Week 12

,
Interventionlog10 copies/mL (Number)
First slope (first phase of viral decay)Second slope (second phase of viral decay)
Adefovir-0.329-0.024
Entecavir-0.391-0.034

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HBV DNA Viral Kinetics Estimates of Exponential Decay Model - Efficacy in Blocking Virus Production and de Novo Infections

The biphasic decline of HBV DNA is characterized via a 4-parameter exponential decay model previously published for HBV compounds. The model parameters of interest are the effectiveness of the drug in blocking virus production from infected cells (efficacy, ε) and effectiveness of the study treatment in blocking de novo infection of susceptible cells (η). The model parameters reflect the biphasic pattern that is typically observed after initiation of antiviral therapy. Parameters were estimated for each subject separately and then averaged within each treatment group. (NCT00096785)
Timeframe: Week 12

,
Interventionpercent effective (Number)
Efficacy in blocking virus production - εEffectiveness in blocking de novo infections - η
Adefovir99.465.87
Entecavir99.876.07

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HBV DNA Viral Kinetics Estimates of Exponential Decay Model - Viral Clearance Rate and Infected Cell Death Rate

The biphasic decline of HBV DNA is characterized via a 4-parameter exponential decay model previously published for HBV compounds. The model parameters of interest are the clearance rate of the free virus (c), the death rate of productively infected cells (δ), The model parameters reflect the biphasic pattern that is typically observed after initiation of antiviral therapy. Parameters were estimated for each subject separately and then averaged within each treatment group. (NCT00096785)
Timeframe: Week 12

,
Interventionper day (Number)
Viral Clearance - cInfected cell death - δ
Adefovir0.910.04
Entecavir1.700.08

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Summary of Safety - Laboratory Abnormalities Reported as Clinical AEs

Laboratory abnormalities reported as clinical AEs (NCT00096785)
Timeframe: Week 48

,
InterventionParticipants (Number)
ALT increasedLipase increasedBlood phosphorus decreasedLiver function test abnormalPlatelet count decreasedProtein urine present
Adefovir221111
Entecavir110000

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Summary of Safety - Most Frequent (> 10%) Adverse Events (AEs), Serious Adverse Events (SAEs), Discontinuations Due to AEs, and Deaths

AE=new untoward medical occurrence or worsening of pre-existing medical condition regardless of causal relationship to treatment. SAE=untoward medical occurrence that is life-threatening, a congenital anomaly/birth defect, or an important medical event, or results in death, inpatient hospitalization/prolongation of hospitalization, or persistent/significant disability. AE grades: mild (1), moderate (2), severe (3), life-threatening (4), death (5). ALT flare= >2x baseline & >10x ULN up to end of therapy + 5 days. Hepatic SAE=SAEs consistent with worsening of hepatitis or hepatic decompensation. (NCT00096785)
Timeframe: cumulative through the end of on-treatment observation as available at the time of the Week 48 dataset

,
InterventionParticipants (Number)
DeathSerious AEDiscontinuation due to AEMalignant neoplasmOn Treatment: Any AEOn Treatment: HeadacheOn Treatment: Upper Respiratory InfectionOn Treatment: InfluenzaOn Treatment: NasopharyngitisOn Treatment: PyrexiaOn Treatment: Back PainOn Treatment: Grade 3-4 AEsALT FlareHepatic SAE
Adefovir031027684665512
Entecavir010028986440201

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Alanine Aminotransferase (ALT) Normalization

Number of participants with ALT ≤ 1 x upper limit of normal (ULN) (NCT00096785)
Timeframe: Week 48

Interventionparticipants (Number)
Entecavir25
Adefovir20

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Change From Baseline in HBV DNA by PCR Assay at Week 48

Antiviral efficacy, as measured by the mean reduction in serum HBV DNA levels by PCR (log10 copies/mL) at Week 48, adjusted for baseline (Week 48 - Baseline). A negative value = improvement. (NCT00096785)
Timeframe: Baseline, Week 48

Interventionlog10 c/mL (Mean)
Entecavir-7.28
Adefovir-5.08

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Change From Baseline in Hepatitis B Virus DNA (HBV DNA) by Polymerase Chain Reaction (PCR) Assay at Week 12

Antiviral efficacy, as measured by the mean reduction in serum HBV DNA levels by PCR (log10 copies/mL) at Week 12, adjusted for baseline (Week 12 - baseline). A negative value = improvement. (NCT00096785)
Timeframe: Baseline, Week 12

Interventionlog10 copies/mL (Mean)
Entecavir-6.23
Adefovir-4.52

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HBV DNA Viral Kinetics Estimates of Exponential Decay Model - Half-Life of Free Virus

The biphasic decline of HBV DNA is characterized via a 4-parameter exponential decay model previously published for HBV compounds. An important derived parameter is the half-life of free virus (ie, the average amount of time for HBV particles in plasma to be reduced to half the initial level), calculated as 24*ln(2)/c. The model parameters reflect the biphasic pattern that is typically observed after initiation of antiviral therapy. Parameters were estimated for each subject separately and then averaged within each treatment group. (NCT00096785)
Timeframe: Week 12

Interventionhours (Number)
Entecavir14.52
Adefovir32.46

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Viral Load Undetectable (HBV DNA <300 Copies/mL)

Number of Subjects with HBV DNA <300 copies/mL by Roche COBAS® Amplicor (limit of quantitation 300 copies/mL) (NCT00096785)
Timeframe: Week 48

InterventionParticipants (Number)
Entecavir19
Adefovir6

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Percentage of Participants With HBeAg Loss and HBeAg Seroconversion at Week 96 (for Participants Who Were HBeAg Positive at Baseline)

Loss of HBeAg was defined as change of detectable HBeAg from positive to negative. HBeAg seroconversion was defined as change of detectable antibody to HBeAg from negative to positive. (NCT00298363)
Timeframe: Baseline to Week 96

,,,
Interventionpercentage of participants (Number)
HBeAg LossHBeAg Seroconversion
Entecavir0.00.0
FTC/TDF33.313.3
Overall20.011.4
Tenofovir DF14.314.3

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Median Change in MELD Score From Baseline at Week 96

MELD scores, used to assess prognosis and suitability for transplant, are calculated based on laboratory values only and can range from 6 to 40, with higher scores indicating greater disease severity. (NCT00298363)
Timeframe: Baseline to Week 96

Interventionunits on a scale (Median)
Tenofovir DF-2.0
FTC/TDF-3.0
Entecavir-3.0
Overall-2.0

[back to top]

Median Change in MELD Score From Baseline at Week 168

MELD scores, used to assess prognosis and suitability for transplant, are calculated based on laboratory values only and can range from 6 to 40, with higher scores indicating greater disease severity. (NCT00298363)
Timeframe: Baseline to Week 168

Interventionunits on a scale (Median)
Tenofovir DF-2.0
FTC/TDF-2.0
Entecavir-2.0
Overall-2.0

[back to top]

Median Change in MELD Score From Baseline at Week 144

MELD scores, used to assess prognosis and suitability for transplant, are calculated based on laboratory values only and can range from 6 to 40, with higher scores indicating greater disease severity. (NCT00298363)
Timeframe: Baseline to Week 144

Interventionunits on a scale (Median)
Tenofovir DF-2.0
FTC/TDF-1.5
Entecavir-2.0
Overall-2.0

[back to top]

In the Subset of Participants Undergoing Liver Transplantation, Time to Recurrence of Hepatitis B, Defined as 2 Consecutive Plasma HBV DNA Concentrations ≥ 400 Copies/mL or 2 Consecutive HBsAg(+) Results

(NCT00298363)
Timeframe: Baseline to Week 168

InterventionDays (Number)
Tenofovir DFNA
FTC/TDFNA
EntecavirNA
OverallNA

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Median DAVG in Plasma HBV DNA Levels at 144 Weeks Relative to Baseline

Change from baseline was evaluated by subtracting baseline HBV DNA log_10 copies/mL from Week 144 HBV DNA log_10 copies/mL. DAVG is defined as the area of the trapezoid under the response-time curve divided by time to the last available evaluation of the patient minus the baseline value. (NCT00298363)
Timeframe: Baseline to 144 weeks

Interventionlog _10 copies/mL (Median)
Tenofovir DF-3.07
FTC/TDF-3.82
Entecavir-3.76
Overall-3.49

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Median DAVG in Plasma HBV DNA Levels at 168 Weeks Relative to Baseline

Change from baseline was evaluated by subtracting baseline HBV DNA log_10 copies/mL from Week 168 HBV DNA log_10 copies/mL. DAVG is defined as the area of the trapezoid under the response-time curve divided by time to the last available evaluation of the patient minus the baseline value. (NCT00298363)
Timeframe: Baseline to 168 weeks

Interventionlog_10 copies/mL (Median)
Tenofovir DF-3.16
FTC/TDF-4.06
Entecavir-3.77
Overall-3.66

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Median DAVG in Plasma HBV DNA Levels at 96 Weeks Relative to Baseline

Change from baseline was evaluated by subtracting baseline HBV DNA log_10 copies/mL from Week 96 HBV DNA log_10 copies/mL. DAVG is defined as the area of the trapezoid under the response-time curve divided by time to the last available evaluation of the patient minus the baseline value. (NCT00298363)
Timeframe: Baseline to 96 weeks

Interventionlog_10 copies/mL (Median)
Tenofovir DF-3.06
FTC/TDF-4.06
Entecavir-3.32
Overall-3.40

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Median Time-averaged Change (DAVG) in Plasma Hepatitis B Virus (HBV) Deoxyribonucleic Acid (DNA) Levels at 48 Weeks Relative to Baseline

Change from baseline was evaluated by subtracting baseline HBV DNA log_10 copies/mL from Week 48 HBV DNA log_10 copies/mL. DAVG is defined as the area of the trapezoid under the response-time curve divided by time to the last available evaluation of the patient minus the baseline value. (NCT00298363)
Timeframe: Baseline to 48 weeks

Interventionlog_10 copies/mL (Median)
Tenofovir DF-2.93
FTC/TDF-3.45
Entecavir-3.61
Overall-3.19

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Percent Probability of a Confirmed Increase in Serum Creatinine of ≥ 0.5 mg/dL From Baseline or a Confirmed Serum Phosphorus Level < 2.0 mg/dL

Results are expressed as proportions of participants who experience a confirmed increase in serum creatinine of ≥ 0.5 mg/dL from baseline or a confirmed serum phosphorus level < 2.0 mg/dL using the KM method of estimation. (NCT00298363)
Timeframe: Baseline to Week 168

Interventionpercent probability (KM estimate) (Number)
Tenofovir DF15
FTC/TDF14
TDF or FTC/TDF14
Entecavir10

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Percent Probability of Tolerability Failure

Tolerability failure was defined as permanent discontinuation of study drug due to a treatment-emergent adverse event (AE), including any subject who temporarily discontinued study drug due to an AE and did not restart. Results are expressed as proportions of participants who experience tolerability failure using the Kaplan-Meier (KM) method of estimation. (NCT00298363)
Timeframe: Baseline to Week 168

Interventionpercent probability (KM estimate) (Number)
Tenofovir DF18
FTC/TDF4
TDF or FTC/TDF11
Entecavir14

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Percentage of Participants With a Decrease in CPT Score of ≥ 2 Points From Baseline at Week 144

CPT scores, widely used to grade the severity of cirrhosis and to determine the need for liver transplantation, are calculated based on a combination of laboratory values and clinical features. CPT scores can range from 5 to 15, with higher scores indicating a greater severity of disease. (NCT00298363)
Timeframe: Baseline to Week 144

Interventionpercentage of participants (Number)
Tenofovir DF25.9
FTC/TDF51.9
Entecavir45.5
Overall40.0

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Percentage of Participants With a Decrease in CPT Score of ≥ 2 Points From Baseline at Week 168

CPT scores, widely used to grade the severity of cirrhosis and to determine the need for liver transplantation, are calculated based on a combination of laboratory values and clinical features. CPT scores can range from 5 to 15, with higher scores indicating a greater severity of disease. (NCT00298363)
Timeframe: Baseline to Week 168

Interventionpercentage of participants (Number)
Tenofovir DF24.0
FTC/TDF45.8
Entecavir45.5
Overall36.7

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Percentage of Participants With a Decrease in CPT Score of ≥ 2 Points From Baseline at Week 48

CPT scores, widely used to grade the severity of cirrhosis and to determine the need for liver transplantation, are calculated based on a combination of laboratory values and clinical features. CPT scores can range from 5 to 15, with higher scores indicating a greater severity of disease. (NCT00298363)
Timeframe: Baseline to Week 48

Interventionpercentage of participants (Number)
Tenofovir DF25.9
FTC/TDF48.0
Entecavir41.7
Overall37.5

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Percentage of Participants With a Decrease in CPT Score of ≥ 2 Points From Baseline at Week 96

CPT scores, widely used to grade the severity of cirrhosis and to determine the need for liver transplantation, are calculated based on a combination of laboratory values and clinical features. CPT scores can range from 5 to 15, with higher scores indicating a greater severity of disease. (NCT00298363)
Timeframe: Baseline to Week 96

Interventionpercentage of participants (Number)
Tenofovir DF23.1
FTC/TDF52.0
Entecavir50.0
Overall39.3

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Percentage of Participants With an Increase in Child-Pugh Turcotte (CPT) Score of ≥ 2 Points at Weeks 48

CPT scores, widely used to grade the severity of cirrhosis and to determine the need for liver transplantation, are calculated based on a combination of laboratory values and clinical features. CPT scores can range from 5 to 15, with higher scores indicating a greater severity of disease. (NCT00298363)
Timeframe: Baseline to Week 48

Interventionpercentage of participants (Number)
Tenofovir DF0.0
FTC/TDF2.6
Entecavir0.0
Overall1.0

[back to top]

Percentage of Participants With an Increase in CPT Score of ≥ 2 Points at Week 144

CPT scores, widely used to grade the severity of cirrhosis and to determine the need for liver transplantation, are calculated based on a combination of laboratory values and clinical features. CPT scores can range from 5 to 15, with higher scores indicating a greater severity of disease. (NCT00298363)
Timeframe: Baseline to Week 144

Interventionpercentage of participants (Number)
Tenofovir DF0.0
FTC/TDF2.5
Entecavir0.0
Overall1.0

[back to top]

Percentage of Participants With an Increase in CPT Score of ≥ 2 Points at Week 168

CPT scores, widely used to grade the severity of cirrhosis and to determine the need for liver transplantation, are calculated based on a combination of laboratory values and clinical features. CPT scores can range from 5 to 15, with higher scores indicating a greater severity of disease. (NCT00298363)
Timeframe: Baseline to Week 168

Interventionpercentage of participants (Number)
Tenofovir DF2.4
FTC/TDF0.0
Entecavir0.0
Overall1.0

[back to top]

Percentage of Participants With an Increase in CPT Score of ≥ 2 Points at Week 96

CPT scores, widely used to grade the severity of cirrhosis and to determine the need for liver transplantation, are calculated based on a combination of laboratory values and clinical features. CPT scores can range from 5 to 15, with higher scores indicating a greater severity of disease. (NCT00298363)
Timeframe: Baseline to Week 96

Interventionpercentage of participants (Number)
Tenofovir DF0.0
FTC/TDF0.0
Entecavir0.0
Overall0.0

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Percentage of Participants With Baseline ADV-R + LAM-R Mutations Achieving HBV DNA < 400 Copies/mL by 168 Weeks

ADV resistance mutation + LAM resistance mutations are defined as the presence of the rtA181T/V HBV gene mutation and/or the rtN236T HBV gene mutation, and the rtM204V/I HBV gene mutation with or without the rtL180M HBV gene mutation. (NCT00298363)
Timeframe: Baseline to Week 168

Interventionpercentage of participants (Number)
Tenofovir DF50

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Percentage of Participants With Normalized Alanine Aminotransferase (ALT) (for Subjects With Elevated ALT at Baseline) at Week 48

Normalized ALT is defined as having a baseline ALT value > the upper limit of the normal range (ULN), and a decrease in ALT value to ≤ ULN at the given time point. (NCT00298363)
Timeframe: Baseline to Week 48

Interventionpercentage of participants (Number)
Tenofovir DF46.2
FTC/TDF64.0
Entecavir41.2
Overall51.5

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Percentage of Participants With Normalized ALT (for Subjects With Elevated ALT at Baseline) at Week 144

Normalized ALT is defined as having a baseline ALT value > ULN, and a decrease in ALT value to ≤ ULN at the given time point. (NCT00298363)
Timeframe: Baseline to Week 144

Interventionpercentage of participants (Number)
Tenofovir DF34.6
FTC/TDF64.0
Entecavir37.5
Overall46.3

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Percentage of Participants With Normalized ALT (for Subjects With Elevated ALT at Baseline) at Week 168

Normalized ALT is defined as having a baseline ALT value > ULN, and a decrease in ALT value to ≤ ULN at the given time point. (NCT00298363)
Timeframe: Baseline to Week 168

Interventionpercentage of participants (Number)
Tenofovir DF29.2
FTC/TDF60.0
Entecavir37.5
Overall43.1

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Percentage of Participants With Hepatitis B Surface Antigen (HBsAg) Loss and HBsAg Seroconversion at Week 48

Loss of HBsAg was defined as change of detectable HBsAg from positive to negative. HBsAg seroconversion was defined as change of detectable antibody to HBsAg from negative to positive. (NCT00298363)
Timeframe: Baseline to Week 48

,,,
Interventionpercentage of participants (Number)
HBsAg LossHBsAg Seroconversion
Entecavir0.00.0
FTC/TDF0.00.0
Overall0.00.0
Tenofovir DF0.00.0

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Percentage of Participants With Normalized ALT (for Subjects With Elevated ALT at Baseline) at Week 96

Normalized ALT is defined as having a baseline ALT value > ULN, and a decrease in ALT value to ≤ ULN at the given time point. (NCT00298363)
Timeframe: Baseline to Week 96

Interventionpercentage of participants (Number)
Tenofovir DF50.0
FTC/TDF58.3
Entecavir31.3
Overall48.5

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Percentage of Participants With Hepatitis B Early Antigen (HBeAg) Loss and HBeAg Seroconversion at Week 48 (for Participants Who Were HBeAg Positive at Baseline)

Loss of HBeAg was defined as change of detectable HBeAg from positive to negative. HBeAg seroconversion was defined as change of detectable antibody to HBeAg from negative to positive. (NCT00298363)
Timeframe: Baseline to Week 48

,,,
Interventionpercentage of participants (Number)
HBeAg LossHBeAg Seroconversion
Entecavir0.00.0
FTC/TDF26.713.3
Overall19.413.9
Tenofovir DF21.421.4

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Percentage of Participants With Only Baseline Adefovir Dipivoxil Resistance (ADV-R) Mutations Achieving HBV DNA < 400 Copies/mL by 168 Weeks

ADV resistance mutations are defined as the presence of the rtA181T/V HBV gene mutation and/or the rtN236T HBV gene mutation. (NCT00298363)
Timeframe: Baseline to Week 168

Interventionpercentage of participants (Number)
Tenofovir DF100
FTC/TDF100

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Percentage of Participants With Only Baseline Lamivudine-resistance (LAM-R) Mutations Achieving HBV DNA < 400 Copies/mL by 168 Weeks

LAM resistance mutations are defined as the presence of the rtM204V/I HBV gene mutation with or without the rtL180M HBV gene mutation. (NCT00298363)
Timeframe: Baseline to Week 168

Interventionpercentage of participants (Number)
Tenofovir DF100
FTC/TDF100
Entecavir100

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Percentage of Participants With Plasma HBV DNA < 400 Copies/mL at Week 144

The percentage of participants with plasma HBV DNA < 400 copies/mL at Week 144 was summarized. (NCT00298363)
Timeframe: Week 144

Interventionpercentage of participants (Number)
Tenofovir DF50.0
FTC/TDF77.5
Entecavir52.4
Overall61.0

[back to top]

Percentage of Participants With Plasma HBV DNA < 400 Copies/mL at Week 168

The percentage of participants with plasma HBV DNA < 400 copies/mL at Week 168 was summarized. (NCT00298363)
Timeframe: Week 168

Interventionpercentage of participants (Number)
Tenofovir DF50.0
FTC/TDF75.7
Entecavir52.4
Overall60.0

[back to top]

Percentage of Participants With Plasma HBV DNA < 400 Copies/mL at Week 48

The percentage of participants with plasma HBV DNA < 400 copies/mL at Week 48 was summarized. (NCT00298363)
Timeframe: Week 48

Interventionpercentage of participants (Number)
Tenofovir DF70.5
FTC/TDF87.8
Entecavir72.7
Overall77.6

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Percentage of Participants With Plasma HBV DNA < 400 Copies/mL at Week 96

The percentage of participants with plasma HBV DNA < 400 copies/mL at Week 96 was summarized. (NCT00298363)
Timeframe: Week 96

Interventionpercentage of participants (Number)
Tenofovir DF59.1
FTC/TDF79.5
Entecavir57.1
Overall66.3

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Percentage of Participants With HBeAg Loss and HBeAg Seroconversion at Week 144 (for Participants Who Were HBeAg Positive at Baseline)

Loss of HBeAg was defined as change of detectable HBeAg from positive to negative. HBeAg seroconversion was defined as change of detectable antibody to HBeAg from negative to positive. (NCT00298363)
Timeframe: Baseline to Week 144

,,,
Interventionpercentage of participants (Number)
HBeAg LossHBeAg Seroconversion
Entecavir16.70.0
FTC/TDF33.313.3
Overall22.911.4
Tenofovir DF14.314.3

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Percentage of Participants With HBeAg Loss and HBeAg Seroconversion at Week 168 (for Participants Who Were HBeAg Positive at Baseline)

Loss of HBeAg was defined as change of detectable HBeAg from positive to negative. HBeAg seroconversion was defined as change of detectable antibody to HBeAg from negative to positive. (NCT00298363)
Timeframe: Baseline to Week 168

,,,
Interventionpercentage of participants (Number)
HBeAg LossHBeAg Seroconversion
Entecavir16.70.0
FTC/TDF35.721.4
Overall27.318.2
Tenofovir DF23.123.1

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Percentage of Participants With HBsAg Loss and HBsAg Seroconversion at Week 144

Loss of HBsAg was defined as change of detectable HBsAg from positive to negative. HBsAg seroconversion was defined as change of detectable antibody to HBsAg from negative to positive. (NCT00298363)
Timeframe: Baseline to Week 144

,,,
Interventionpercentage of participants (Number)
HBsAg LossHBsAg Seroconversion
Entecavir0.00.0
FTC/TDF0.00.0
Overall0.00.0
Tenofovir DF0.00.0

[back to top]

Percentage of Participants With HBsAg Loss and HBsAg Seroconversion at Week 168

Loss of HBsAg was defined as change of detectable HBsAg from positive to negative. HBsAg seroconversion was defined as change of detectable antibody to HBsAg from negative to positive. (NCT00298363)
Timeframe: Baseline to Week 168

,,,
Interventionpercentage of participants (Number)
HBsAg LossHBsAg Seroconversion
Entecavir0.00.0
FTC/TDF0.00.0
Overall0.00.0
Tenofovir DF0.00.0

[back to top]

Percentage of Participants With HBsAg Loss and HBsAg Seroconversion at Week 96

Loss of HBsAg was defined as change of detectable HBsAg from positive to negative. HBsAg seroconversion was defined as change of detectable antibody to HBsAg from negative to positive. (NCT00298363)
Timeframe: Baseline to Week 96

,,,
Interventionpercentage of participants (Number)
HBsAg LossHBsAg Seroconversion
Entecavir0.00.0
FTC/TDF0.00.0
Overall0.00.0
Tenofovir DF0.00.0

[back to top]

Median Change in Model for End-Stage Liver Disease (MELD) Score From Baseline at Week 48

MELD scores, used to assess prognosis and suitability for transplant, are calculated based on laboratory values only and can range from 6 to 40, with higher scores indicating greater disease severity. (NCT00298363)
Timeframe: Baseline to Week 48

Interventionunits on a scale (Median)
Tenofovir DF-2.0
FTC/TDF-2.0
Entecavir-2.0
Overall-2.0

[back to top]

Percentage of Participants With HBeAg Seroconversion at Week 48 (for HBeAg-positive Participants Only)

HBeAg is a hepatitis B viral protein. HBeAg Seroconversion = HBeAg Loss and Presence of Hepatitis B e Antibody (HBeAb). (NCT00371150)
Timeframe: Week 48

Interventionpercentage of participants (Number)
Black / African American40.9
Total46.2

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Percentage of Participants With HBV DNA by PCR Category at Week 48

HBV DNA assessments were performed using the Roche COBAS® TaqMan AmpliPrep assay. (NCT00371150)
Timeframe: Week 48

,
Interventionpercentage of participants (Number)
<50 IU/mL (< 300 copies/mL)50 to <172 IU/mL (300 to < 103 copies/mL)172 to <1720 IU/mL (103 to < 104 copies/mL)1720 to <17200 IU/mL (104 to < 105 copies/mL)≥17,200 IU/mL (≥105 copies/mL)Missing
Black / African American72.5010.05.0012.5
Total69.6010.94.3015.2

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Percentage of Participants Who Achieve HBV DNA < Lower Limit of Quantitation (LOQ = 29 IU/mL [Approximately 169 Copies/mL]) at Week 48

HBV DNA assessments were performed using the Roche COBAS® TaqMan AmpliPrep assay. LOQ is the level above which quantitative results may be obtained with a specified degree of confidence. The LOQ is mathematically defined as equal to 10 times the standard deviation of the results for a series of replicates used to determine a justifiable limit of detection. (NCT00371150)
Timeframe: Week 48

Interventionpercentage of participants (Number)
Black / African American12.5
Total13.0

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Percentage of Participants With Confirmed HBeAg Loss at Week 48 (for HBeAg-positive Participants Only)

HBeAg is a hepatitis B viral protein. HBeAg loss = HBeAg-negative at the specified analysis week (NCT00371150)
Timeframe: Week 48

Interventionpercentage of participants (Number)
Black / African American50.0
Total53.8

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Number of Participants With Adverse Events (AE), Serious Adverse Events (SAE), and Discontinuations From Study Drug Due to Adverse Events

AE: any new untoward medical occurrence/worsening of pre-existing medical condition, whether or not related to study drug. SAE: any AE that resulted in death; was life threatening; resulted in persistent/significant disability/incapacity; resulted in/prolonged an existing in-patient hospitalization; was a congenital anomaly/birth defect; or was an overdose. Participants who discontinued the study due to any AEs were recorded. (NCT00371150)
Timeframe: From enrollment through Week 52 + 5 days

,,
Interventionparticipants (Number)
DeathsSAEsDiscontinuations Due to AEsAny AEGrade 3 - 4 AEsRelated AEsGrade 2 - 4 Related AEs
Black / African American030335165
Hispanic0105100
Total040386165

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Percentage of Participants With HBsAg Seroconversion at Week 48

HBsAg = a part of the hepatitis B virus that, when in the blood, is a of infection. HBs seroconversion is defined as HBsAg loss with positive HBsAb. (NCT00371150)
Timeframe: Week 48

Interventionpercentage of participants (Number)
Black / African American2.5
Total4.3

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Percentage of Participants With HBV Deoxyribonucleic Acid (DNA) < 50 IU/mL by Polymerase Chain Reaction (PCR) at Week 48

HBV DNA assessments were performed using the Roche COBAS® TaqMan AmpliPrep assay. HBV DNA < 50 IU/mL = approximately <300 copies/mL. (NCT00371150)
Timeframe: Week 48 of ETV treatment

Interventionpercentage of participants (Number)
Black / African American72.5
Total69.6

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Percentage of Participants With Hepatitis B Surface Antigen (HBsAg) Loss at Week 48

HBsAg = a part of the hepatitis B virus that, when in the blood, is a marker of infection. HBsAg loss = HBsAg-negative at the specified analysis week. (NCT00371150)
Timeframe: Week 48

Interventionpercentage of participants (Number)
Black / African American5.0
Total6.5

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Percentage of Participants With Virologic Rebound Through Week 48 While on Continued Dosing With ETV

Virologic rebound is defined as a confirmed increase of ≥ 1 log10 in HBV DNA from the participant's nadir value (2 sequential HBV DNA measurements or last on-treatment measurement) (NCT00371150)
Timeframe: through Week 48

Interventionpercentage of participants (Number)
Black / African American0
Total0

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Mean log10 Reduction From Baseline in HBV DNA at Week 48

HBV DNA was analyzed by PCR, using the Roche COBAS®TaqMan TaqMan AmpliPrep assay. Reduction in log10 HBV count=reduced viral load. (NCT00371150)
Timeframe: baseline, Week 48

,
Interventionlog10 IU/mL (Mean)
BaselineHBV DNA at Week 48Change from baseline
Black / African American7.11.88-5.22
Total7.01.87-5.18

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Percentage of Participants With Alanine Aminotransferase (ALT) Normalization at Week 48

ALT normalization=ALT level being less than or equal to 1 times the upper limit of normal (ULN). ULN for ALT is 37 U/L. (NCT00371150)
Timeframe: Week 48

Interventionpercentage of participants (Number)
Black / African American67.5
Total67.4

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Number of Participants With Laboratory Abnormalities On-treatment (OT) and Off-Treatment (OF) : Serum Chemistry

The modified World Health Oranization(WHO)grading system was used to grade the abnormalities. ULN=upper limit of normal. Alanine aminotransferase:>1.25xULN, Aspartate aminotransferase:>1.25xULN, Alkaline Phosphatase:>1.25xULN, Total Bilirubin:>1.1xULN, Serum Lipase:>1.10xULN, Creatinine:>1.1xULN, Blood Urea Nitrogen:1.25xULN, Hyperglycemia:>116 mg/dL, Hypoglycemia:<64 mg/dL, Hyponatremia:<132meq/L, Hypokalemia:<3.4 meq/L, Albumin:≥1g/dL decrease from baseline, <3 g/dL; Hypernatremia:>148 meq/L, Hyperkalemia:>5.6 meq/L, Hypokalemia:<3.4 meq/L, Hyperchloremia:>113 meq/L, Hypochloremia:<93 meq/L (NCT00371150)
Timeframe: OT: From start of study therapy through Week 52 + 5 days; OF= End of OT period + 24-week follow-up

,
Interventionparticipants (Number)
Alanine aminotransferase-OTAlanine aminotransferase-OF; n=26 , 29Aspartate aminotransferase-OTAspartate aminotransferase-OF; n=26 , 29Alkaline Phosphatase-OTAlkaline Phosphatase-OF; n=26 , 29Albumin-OTAlbumin-OF; n=26 , 29Total Bilirubin-OTTotal Bilirubin-OF; n=26 , 29Serum Lipase-OTSerum Lipase-OF; n=26 , 29Creatinine-OTCreatinine-OF; n=26 , 29Blood Urea Nitrogen-OTBlood Urea Nitrogen-OF; n=26 , 29Hyperglycemia-OTHyperglycemia-OF; n=26 , 29Hypoglycemia-OTHypoglycemia-OF; n=26 , 29Hypernatremia-OTHypernatremia-OF; n=26 , 29Hyponatremia-OTHyponatremia-OF; n=26 , 29Hyperkalemia-OTHyperkalemia-OF; n=26 , 29Hypokalemia-OTHypokalemia-OF; n=26 , 29Hyperchloremia-OTHyperchloremia-OF; n=26 , 29Hypochloremia-OTHypochloremia-OF; n=26 , 29
Black / African American373332313073121302014551003000300000
Total434383315074141302015551003100300000

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Number of Participants With Laboratory Abnormalities On-treatment (OT) and Off-Treatment (OF): Hematology

Criteria for hematology abnormalities were graded using the modified WHO grading system. Hemoglobin: <=11.0 g/dL; White Blood Cells: <4000/mm^3; Absolute Neutrophils (includes absolute bands): <1500/mm^3; Platelets: <=99,000/mm^3; International Normalized Ratio: ≥ 1.5 and ≥ 0.5 from baseline. (NCT00371150)
Timeframe: OT: From start of study therapy through Week 52 + 5 days; OF= End of OT period + 24-week follow-up

,
Interventionparticipants (Number)
Hemoglobin-OTHemoglobin-OF; n=26 , 29White Blood Cells-OTWhite Blood Cells-OF; n=26 , 29Neutrophils -OTNeutrophils-OF; n=26 , 26Platelets-OTPlatelets-OF; n=26 , 29International Normalized Ratio-OTInternational Normalized Ratio-OF; n=26 , 29
Black / African American1015713440184
Total2018813440234

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Number of Participants With HCC Malignant Neoplasm

The number of participants with HCC malignant neoplasm, as adjudicated by Events Adjudication Committee (EAC) (NCT00388674)
Timeframe: 10 years

InterventionParticipants (Number)
Entecavir (ETV)240
Other Anti-HBV Medication (Non-ETV)263

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Number of Participants With Adjudicated Overall Malignant Neoplasms

The number of participants with Overall Malignant Neoplasm, as adjudicated by Events Adjudication Committee (EAC) (NCT00388674)
Timeframe: 10 years

InterventionParticipants (Number)
Entecavir (ETV)331
Other Anti-HBV Medication (Non-ETV)337

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Number of Participants With Non-HCC Malignant Neoplasm

The number of participants with non-HCC malignant neoplasm, as adjudicated by Events Adjudication Committee (EAC) (NCT00388674)
Timeframe: 10 years

InterventionParticipants (Number)
Entecavir (ETV)95
Other Anti-HBV Medication (Non-ETV)81

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Number of Deaths

The number of deaths, as adjudicated by Events Adjudication Committee (EAC) (NCT00388674)
Timeframe: 10 years

InterventionParticipants (Number)
Entecavir (ETV)238
Other Anti-HBV Medication (Non-ETV)264

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Number of Participants With Grade 3 or 4 Abnormalities in Laboratory Test Results by World Health Organization (WHO) Criteria at Week 96

ULN=upper limit of normal; ALT=alanine transaminase. WHO criteria: Grade 3=Severe (inability to carry out usual activity); Grade 4=Very severe (debilitating or significantly incapacitating patient despite symptomatic treatment). (NCT00393484)
Timeframe: Start of dosing (Day 1) until Week 96

,
InterventionParticipants (Number)
PlateletsProthrombin timeNeutrophilsASTALTTotal bilirubiinCreatinineLipasePotassiumGlucose, fasting
Entecavir, 0.5 mg + Placebo1100012203
Lamivudine, 100 mg + Placebo1013630412

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Number of Participants With Hepatitis B Virus (HBV) DNA <10^3, <10^4, or < 10^5 Copies/mL by Polymerase Chain Reaction (PCR) Assy at Weeks 24, 48, and 96

The number and percentage of participants achieving the following endpoints will be tabulated at each visit through Week 240 by treatment group: HBV DNA <300 copies/mL by PCR assay; HBV DNA <10^3, <10^4, or < 10^5 copies/mL by PCR assay. Treatment comparisons will be assessed using the same method as the primary endpoint. (NCT00393484)
Timeframe: At Weeks 24, 48, and 96

,
InterventionParticipants (Number)
Week 24: HBV DNA <10^3Week 24: HBV DNA <10^4Week 24: HBV DNA <10^5Week 48: HBV DNA <10^3Week 48: HBV DNA <10^4Week 48: HBV DNA <10^5Week 96: HBV DNA <10^3Week 96: HBV DNA <10^4Week 96: HBV DNA <10^5
Entecavir, 0.5 mg + Placebo545454545555535353
Lamivudine, 100 mg + Placebo465359455052384245

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Number of Participants With Normalization of Serum Alanine Aminotransferase (ALT) Levels at Weeks 24, 48, and 96

Normalization of serum ALT= ≤*institutional upper limit of normal. (NCT00393484)
Timeframe: At Weeks 24, 48, and 96

,
InterventionParticipants (Number)
At 24 WeeksAt 48 WeeksAt 96 Weeks
Entecavir, 0.5 mg + Placebo434849
Lamivudine, 100 mg + Placebo373833

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Number of Participants With Viral Rebound and Drug-resistant Hepatitis B Virus (HBV) DNA Mutations at Week 96

Virologic rebound was defined as a confirmed ≥1 log10 increase in HBV DNA from nadir on blinded treatment (as determined by 2 sequential HBV DNA values or last on-treatment measurement). (NCT00393484)
Timeframe: At 96 weeks

,
InterventionParticipants (Number)
Viral reboundDrug-resistant mutations
Entecavir, 0.5 mg + Placebo10
Lamivudine, 100 mg + Placebo2613

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Percentage of Participants With a Virologic Response as Defined by Undetectable Hepatitis B Virus DNA at Weeks 48, 96, 144, 192, and 240

Undetectable HBV DNA= <300 copies/mL by polymerase chain reaction assay (NCT00393484)
Timeframe: At Weeks 48, 96, 144, 192, and 240

,
InterventionPercetage of participants (Number)
At 48 WeeksAt 96 WeeksAt 144 WeeksAt 192 WeeksAt 240 Weeks
Entecavir, 0.5 mg + Placebo94.6494.6467.8669.6467.86
Lamivudine, 100 mg + Placebo60.9448.4434.3825.0015.63

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Number of Participants With Death as Outcome, Serious Adverse Events (SAEs), Discontinuations Due to Adverse Events (AEs), Most Common AEs, and Grade 3/4 AEs at Week 240

AE=any new unfavorable symptom, sign, or disease or worsening of a preexisting condition that may not have a causal relationship with treatment. SAE=a medical event that at any dose results in death, persistent or significant disability/incapacity, or drug dependency/abuse; is life-threatening, an important medical event, or a congenital anomaly/birth defect; or requires or prolongs hospitalization. (NCT00393484)
Timeframe: Start of dosing (Day 1) until end of treatment (Week 240) + 5 days

,
InterventionParticipants (Number)
SAEsDiscontinuations due to AEsAny nonserious AEsNonserious AEs related to study conditionsSAEs related to study conditions
Entecavir, 0.5 mg + Placebo704810
Lamivudine, 100 mg + Placebo1714960

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Mean Laboratory Test Values for Alanine Aminotransferase (ALT) at Week 24

Mean ALT values from baseline by laboratory test. . (NCT00393484)
Timeframe: At Week 24

InterventionU/L (Mean)
Entecavir, 0.5 mg + Placebo31.5
Lamivudine, 100 mg + Placebo43.26

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Number of Participants With Clinically or Statistically Significant Changes in Vital Sign Measurements at Week 24

Vital signs assessed included blood pressure, heart rate, body temperature, and respiration rate. (NCT00393484)
Timeframe: Start of dosing (Day 1) until end of treatment (Week 24) + 5 days and to end of 24-week follow-up period

InterventionParticipants (Number)
Entecavir, 0.5 mg + Placebo0
Lamivudine, 100 mg + Placebo0

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Number of Participants With Virologic Rebound at Week 24

Virologic rebound was defined as a confirmed ≥1 log10 increase in hepatitis B virus (HBV) DNA from nadir on blinded treatment (as determined by 2 sequential HBV DNA measurements or last on-treatment measurement). (NCT00393484)
Timeframe: At Week 24

InterventionParticipants (Number)
Entecavir, 0.5 mg + Placebo0
Lamivudine, 100 mg3

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Percentage of Participants Who Achieved a Virologic Response at Week 24

Virologic response=Hepatitis B virus DNA <300 copies/mL by polymerase chain reaction assay. (NCT00393484)
Timeframe: At Week 24

InterventionPercentage of participants (Number)
Entecavir, 0.5 mg + Placebo92.86
Lamivudine, 100 mg + Placebo67.19

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Mean Log10 Reduction From Baseline in Hepatitis B Virus (HBV) DNA at Weeks 24, 48, 96, 144, 192, and 240

Mean log10 reduction from Baseline in HBV DNA virus by the Roche Comprehensive Bio-Analytical System Amplicor polymerase chain reaction (PCR) assay at Week 24. The extent of the decrease was estimated by comparing HBV DNA levels of all participants in each group with a linear regression model with covariates of treatment and baseline HBV DNA by PCR assay. (NCT00393484)
Timeframe: At Weeks 24, 48, 96, 144, 192, and 240

,
Interventionlog10 copies/mL (Mean)
At 24 WeeksAt 48 WeeksAt 96 WeeksAt 144 WeeksAt 192 WeeksAt 240 Weeks
Entecavir, 0.5 mg + Placebo3.583.563.59-3.60-3.60-3.53
Lamivudine, 100 mg+ Placebo2.952.652.42-2.74-2.75-2.69

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Number of Participants With Death as Outcome, Serious Adverse Events (SAEs), Discontinuations Due to Adverse Events (AEs), Most Common AEs, and Grade 3/4 AEs at Week 24

AE=any new unfavorable symptom, sign, or disease or worsening of a preexisting condition that may not have a causal relationship with treatment. SAE=a medical event that at any dose results in death, persistent or significant disability/incapacity, or drug dependency/abuse; is life-threatening, an important medical event, or a congenital anomaly/birth defect; or requires or prolongs hospitalization. Most common AEs=AEs affecting ≥3 participants. Grade 3 (Severe)/Grade 4 (Very Severe)AEs per World Health Organization (WHO) criteria.Serious adverse events/deaths reported for enrolled patients regardless of treatment status. (NCT00393484)
Timeframe: Start of dosing (Day 1) until end of treatment (Week 24) + 5 days and to end of 24-week follow-up period

,
InterventionParticipants (Number)
DeathsSAEsDiscontinuations Due to AEsAny AEsMost common AEs: Upper Respiratory InfectionMost common AEs: NasopharyngitisMost common AEs: UrticariaWHO Grade 3/4 AEs
Entecavir, 0.5 mg + Placebo000143100
Lamivudine, 100 mg + Placebo031237430

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Number of Participants With Elevations in Alanine Transaminase (ALT) and Aspartate Aminoaminase (AST) Levels, Elevations in ALT and AST Levels,Simultaneous Elevations in ALT and Total Bilirubin Levels, and ALT Flares at Week 24

ALT flares=ALT>2*Baseline and 10*upper limit of normal. Serious adverse events/deaths reported for enrolled patients regardless of treatment status. (NCT00393484)
Timeframe: Start of dosing (Day 1) until end of treatment (24 weeks) + 5 days and to end of 24-week follow-up period

,
InterventionParticipants (Number)
ALT elevations >2*Baseline (BL)AST elevations >2*BLALT elevations >3*BL & AST elevations >2*BLSimultaneous ALT & Total bilirubin elevationALT flares
Entecavir, 0.5 mg + Placebo00000
Lamivudine, 100 mg + Placebo11100

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Number of Participants With Grade 3 or 4 Abnormalities in Laboratory Test Results by World Health Organization (WHO) Criteria at Week 24

ULN=upper limit of normal; ALT=alanine transaminase. WHO criteria: Grade 3=Severe (inability to carry out usual activity); Grade 4=Very severe (debilitating or significantly incapacitating patient despite symptomatic treatment). (NCT00393484)
Timeframe: Start of dosing (Day 1) until end of treatment (Week 24) + 5 days and to the end of the 24-week follow-up period

,
InterventionParticipants (Number)
Gr 4 Prothrombin time (>3*ULN)Gr 3 Glucose (251-500 mg/dL)Gr 3 ALT (5.1-10*ULN)Gr 3 Lipase (2.0-5.0*ULN)
Entecavir, 0.5 mg + Placebo1100
Lamivudine, 100 mg + Placebo0211

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Percentage of Participants With HBeAg Loss at Week 72 (for HBeAg-positive Participants)

HBeAg is a hepatitis B viral protein. HBeAg loss = HBeAg-negative at the specified analysis week. (NCT00395018)
Timeframe: At week 72

Interventionpercentage of participants (Number)
Entecavir (ETV)100

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Percentage of Participants With HBeAg Seroconversion at Week 72 (for HBeAg-positive Participants)

HBeAg is a hepatitis B viral protein. HBeAg Seroconversion = HBeAg Loss and Presence of Hepatitis B e Antibody (HBeAb). (NCT00395018)
Timeframe: At week 72

Interventionpercentage of participants (Number)
Entecavir (ETV)0

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Percentage of Participants With HBsAg Loss at Week 72

HBsAg = a part of the hepatitis B virus that, when in the blood, is an early marker of infection. HBsAg loss = HBsAg-negative at the specified analysis week. (NCT00395018)
Timeframe: At week 72

Interventionpercentage of participants (Number)
Entecavir (ETV)96.7

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Percentage of Participants With HBsAg Recurrence At Week 72

HBsAg = a part of the hepatitis B virus that, when in the blood, is an early marker of infection. HBsAg recurrence is defined as having detectable HBsAg among participants who have already experienced loss of HBsAg on-treatment. HBsAg recurrence = HBsAg-positive at the specified analysis week. (NCT00395018)
Timeframe: At week 72

Interventionpercentage of participants (Number)
Entecavir (ETV)3.3

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Percentage of Participants With HBV Deoxyribonucleic Acid (DNA) => 50 IU/mL by Polymerase Chain Reaction (PCR) at Week 72

HBV DNA assessments were performed using the Roche COBAS® TaqMan High+Pure system (HPS) assay. HBV DNA => 50 IU/mL = approximately => 300 copies/mL. (NCT00395018)
Timeframe: At 72 weeks

Interventionpercentage of participants (Number)
Entecavir (ETV)0

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Percentage of Participants With HBsAg Seroconversion at Week 72

HBsAg = a part of the hepatitis B virus that, when in the blood, is an early marker of infection. HBs seroconversion is defined as HBsAg loss with positive HBsAb. (NCT00395018)
Timeframe: At week 72

Interventionpercentage of participants (Number)
Entecavir (ETV)80.3

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Number of Participants With HBV DNA by PCR >= 50 IU/mL Through Week 72

HBV DNA assessments were performed using the Roche COBAS® TaqMan High+Pure system (HPS) assay. HBV DNA => 50 IU/mL = approximately => 300 copies/mL. (NCT00395018)
Timeframe: At baseline (day 1), week 12, 24, 36, 48, 60, and 72

Interventionparticipants (Number)
BaselineWeek 12 (n = 54)Week 24 (n = 58)Week 36 (n = 10)Week 48 (n = 49)Week 60 (n = 48)Week 72 (n = 49)
Entecavir (ETV)3000000

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Distribution of ALT Levels Through 72 Weeks: Overall

ALT is an enzyme present in serum and various tissues of the body, associated commonly with the liver. Elevated levels of ALT often suggests existence of medical problems which includes viral hepatitis. Normal range varies from laboratory to laboratory. Values of 5-60 U/L is usually considered normal. ALT abnormality = >1.25 x ULN (upper limit of normal). (NCT00395018)
Timeframe: On Day 1 (baseline) and at week 4, 12, 24, 36, 48, 60, 72

InterventionU/L (Mean)
BaselineWeek 4Week 12Week 24 (n=59)Week 36 (n=58)Week 48 (n=57)Week 60 (n=53)Week 72 (n=54)
Entecavir (ETV)158.761.228.428.441.224.930.626.9

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Number of Participants With Liver Rejection Through Week 72

(NCT00395018)
Timeframe: Through week 72

Interventionparticipants (Number)
Entecavir (ETV)18

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Number of Participants With Laboratory Abnormalities On-treatment (OT) and Off-Treatment (OF) Follow-up: Serum Chemistry (All Grades)

Normal ranges are local lab data and vary according to the site. Criteria for laboratory abnormalities:ALT:>1.25xULN;AST:>1.25xULN;ALP:>1.25xULN;Total Bilirubin:>1.1xULN;Serum Lipase:>1.10xULN;Creatinine:>1.1xULN;Blood Urea Nitrogen:>1.25xULN;Hyperglycemia:>116mg/dL;Hypoglycemia:<64mg/dL;Hyponatremia:<132meq/L;Hypernatremia:>148meq/L;Hypokalemia:<3.4meq/L;hyperkalemia:>5.6meq/L;Hypochloremia:<93meq/L;Hyperchloremia:>113meq/L;Albumin: Decrease >= 1g/dL from baseline and < 3 g/dL. HYPER=value>ULN(upper limit of normal). HYPO=valueNCT00395018)
Timeframe: OT:From start of dosing through Week 72 + 5 days; OF:End of OT through 24-weeks follow-up

Interventionparticipants (Number)
ALANINE AMINOTRANSFERASE (ALT)-OTALT-OF (n=4)ASPARTATE AMINOTRANSFERASE (AST)-OTAST-OF (n=4)ALKALINE PHOSPHATASE (ALP)-OTALP-OF (n=4)ALBUMIN-OT (n=64)ALBUMIN-OF (n=3)TOTAL BILIRUBIN-OTTOTAL BILIRUBIN-OF (n=4)SERUM LIPASE-OT (n=64)SERUM LIPASE-OF (n=3)CREATININE-OTCREATININE-OF (n=4)BLOOD UREA NITROGEN-OTBLOOD UREA NITROGEN-OF (n=4)HYPERGLYCEMIA-OT (n=64)HYPERGLYCEMIA-OF (n=3)HYPOGLYCEMIA-OT (n=64)HYPOGLYCEMIA-OF (n=3)HYPERNATREMIA-OTHYPERNATREMIA-OF (n=4)HYPONATREMIA-OTHYPONATREMIA-OF (n=4)HYPERKALEMIA-OTHYPERKALEMIA-OF (n=4)HYPOKALEMIA-OTHYPOKALEMIA-OF (n=4)HYPERCHLOREMIA-OTHYPERCHLOREMIA-OF (n=4)HYPOCHLOREMIA-OTHYPOCHLOREMIA-OF (n=4)
Entecavir (ETV)5405603415105703714304305201507014015022011070

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Number of Participants With Laboratory Abnormalities On-treatment (OT) and Off-Treatment Follow-up(OF): Hematology (All Grades)

Criteria for hematology abnormalities were: Hemoglobin : <11.0 g/dL; White Blood Cells : <4000/mm^3; Neutrophils : <1500/mm^3; Platelets : < 99,000/mm^3; International Normalized Ratio (INR) : increase >= 0.5 from baseline. (NCT00395018)
Timeframe: OT:From start of dosing through Week 72 + 5 days; OF:End of OT through 24-weeks follow-up

Interventionparticipants (Number)
HEMOGLOBIN-OTHEMOGLOBIN-OF (n=5)WHITE BLOOD CELLS-OTWHITE BLOOD CELLS-OF (n=5)NEUTROPHILS (Includes absolute bands)-OTNEUTROPHILS (Includes absolute bands)-OF (n=5)PLATELETS-OTPLATELETS-OF (n=5)INR-OT (n=63)INR-OF (n=4)
Entecavir (ETV)561502241402300

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Participants With Adverse Events (AE), Serious Adverse Events (SAE), and Discontinuations From Study Drug Due to AEs (On-treatment [OT] and Off-treatment Follow-up [OF])

AE: any new untoward medical occurrence/worsening of pre-existing medical condition, whether or not related to study drug. SAE: any AE that resulted in death; was life threatening; resulted in persistent/significant disability/incapacity; resulted in/prolonged an existing in-patient hospitalization; was a congenital anomaly/birth defect; or an overdose. Toxicity grading by modified WHO grade system. Grade (GR) 2=moderate; GR3=severe; GR4=very severe. OT=from start of dosing to end of dosing+5 days; OF=from end of dosing+6 days to start of other anti-HBV therapy or end of follow-up. (NCT00395018)
Timeframe: OT:From start of dosing through Week 72 + 5 days; OF:End of OT through 24-weeks follow-up

Interventionparticipants (Number)
Death-OTSAEs-OTSAEs-OF (n=5)Discontinuation due to AEs-OTAny AE-OTAny AE-OF (n=5)Related AEs-OTGrade 2 - 4 related AEs-OTGrade 3 - 4 AEs-OT
Entecavir (ETV)4360062011830

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Number of Participants With Re-transplantation Through Week 72

(NCT00395018)
Timeframe: Through week 72

Interventionparticipants (Number)
Entecavir (ETV)3

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Total Bilirubin at Week 72

Bilirubin measures are used to diagnose or monitor liver functioning or diseases that include hepatitis. Viral hepatitis is one of the condition in which bilirubin levels are elevated. Normal range varies from laboratory to laboratory. Bilirubin abnormality : => 1.1 x ULN mg/dL. (NCT00395018)
Timeframe: At week 72

Interventionmg/dL (Mean)
Entecavir (ETV)0.79

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Prothrombin Time (PT) at Week 72

Prothrombin, a liver protein, plays an important role in the extrinsic pathway of clotting. Increased prothrombin time indicates abnormal liver functioning. Normal prothrombin time varies from laboratory to laboratory. Generally, normal prothrombin time varies between 10 to 13.2 seconds. Abnormal PT: > 1.01 x ULN. (NCT00395018)
Timeframe: At week 72

Interventionseconds (Mean)
Entecavir (ETV)13.32

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Percentage of Participants With HBeAg Seroconversion [( at Weeks 48 and 96

HBeAg seroconversion=HBeAg loss and presence of hepatitis B e antibody (HBeAb). HBeAg is a hepatitis B viral protein and is an indicator of active viral replication. (NCT00410072)
Timeframe: At Weeks 48 and 96

,
InterventionPercentage of participants (Number)
Week 48Week 96
ETV 0.5 mg22.232.5
ETV 0.5 mg +TDF 300 mg18.121.7

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Percentage of Participants With Alanine Aminotransferase (ALT) Normalization at Weeks 48 and 96

ALT normalization= ≤1*upper limit of normal (ULN). Analyses of binary efficacy endpoint during on-treatment period focused on participants who received treatment and used the analysis of noncompleter=failure (NC=F). All participants who received treatment were included in the denominator, and participants with missing measurements were counted as nonresponders for the specific endpoints. (NCT00410072)
Timeframe: At Weeks 48 and 96

,
InterventionPercentage of participants (Number)
Overall at Week 48Overall at Week 96
ETV 0.5 mg83.081.9
ETV 0.5 mg +TDF 300 mg72.668.0

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Percentage of Participants Who Achieved HBV DNA Levels

LOQ=lower limit of quantitation. LOQ=29 IU/mL, or approximately 169 copies/mL. LOQ is the level above which quantitative results may be obtained with a specified degree of confidence. The LOQ is mathematically defined as equal to 10 times the standard deviation of the results for a series of replicates used to determine a justifiable limit of detection. Limits of quantitation are matrix-, method-, and analyte-specific.Analyses of binary efficacy endpoint during on-treatment period focused on participants who received treatment and used the analysis of noncompleter=failure (NC=F). All participants who received treatment were included in the denominator, and participants with missing measurements were counted as nonresponders for the specific endpoints. (NCT00410072)
Timeframe: At Weeks 48 and 96

,
InterventionPercentage of participants (Number)
Overall at Week 48Overall at Week 96
ETV 0.5 mg67.674.7
ETV 0.5 mg +TDF 300 mg74.681.7

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Percentage of Participants Who Achieved HBV DNA Levels

LOD=Lower limit of detection. LOD) LOD=10 IU/mL, or approximately 58 copies/mL. LOD is the lowest concentration level that can be determined to be statistically different from a blank (99% confidence). The LOD is typically determined to be in the region where the signal to noise ratio is greater than 5. Limits of detection are matrix-, method-, and analyte-specific.Analyses of binary efficacy endpoint during on-treatment period focused on participants who received treatment and used the analysis of noncompleter=failure (NC=F). All participants who received treatment were included in the denominator, and participants with missing measurements were counted as nonresponders for the specific endpoints. (NCT00410072)
Timeframe: At Weeks 48 and 96

,
InterventionPercentage of participants (Number)
Overall at Week 48Overall at Week 96
ETV 0.5 mg58.268.1
ETV 0.5 mg +TDF 300 mg66.076.6

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Percentage of Participants Who Achieved HBV DNA Levels <50 IU/mL by PCR at Week 48 and Week 96 by Hepatitis B e Antigen (HBeAg) Status

HBV DNA levels <50 IU/mL=approximately 300 copies/mL. Analyses of binary efficacy endpoint during on-treatment period focused on participants who received treatment and used the analysis of noncompleter=failure (NC=F). All participants who received treatment were included in the denominator, and participants with missing measurements were counted as nonresponders for the specific endpoints. (NCT00410072)
Timeframe: At Weeks 48 and 96

,
InterventionPercentage of participants (Number)
HBeAg+ at Week 48 (n=126, n=138)HBeAg- at Week 48 (n=56, n=59)HBeAg+ at Week 96 (n=126, n=138)HBeAg- at Week 96 (n=56, n=59)
ETV 0.5 mg61.191.169.891.1
ETV 0.5 mg +TDF 300 mg74.693.280.489.8

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Number of Participants With Virologic Breakthrough at Week 48

ETVr=entecavir resistance; TFDr=tenofovir resistance. Virologic breakthrough= confirmed >= 1 log10 increase in HBV DNA from the on-treatment nadir (NCT00410072)
Timeframe: Week 48

,
InterventionParticipants (Number)
ETVrTDFr
ETV 0.5 mg00
ETV 0.5 mg +TDF 300 mg00

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Number of Participants With HBV Resistance Through Week 48

ETVr=entecavir resistance; TDFr=tenofovir resistance. HBV polymerase using the Trugene® HBV Genotyping Kit. HBV resistance: genotyping of HBV polymerase will be performed on stored viral samples at any timepoint when considered appropriate based on virologic response, including any specimen with detectable HBV DNA. When appropriate, phenotyping will also be used. (NCT00410072)
Timeframe: Week 48

,
InterventionParticipants (Number)
ETVrTDFr
ETV 0.5 mg00
ETV 0.5 mg +TDF 300 mg00

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Number of Participants With HBV Resistance at Week 96

ETVr=entecavir resistance; TFDr=tenofovir resistance. HBV polymerase using the Trugene® HBV Genotyping Kit. HBV resistance: genotyping of HBV polymerase will be performed on stored viral samples at any timepoint when considered appropriate based on virologic response, including any specimen with detectable HBV DNA. When appropriate, phenotyping will also be used. (NCT00410072)
Timeframe: Week 96

,
InterventionParticipants (Number)
ETVrTDFr
ETV 0.5 mg00
ETV 0.5 mg +TDF 300 mg00

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Number of Participants With HBV DNA in Relevant Categories at Weeks 48 and 96

Using the Roche COBAS TaqMan - HPS assay. Lower limit of Quantitation (LOQ) is the level above which quantitative results may be obtained with a specified degree of confidence. The LOQ is mathematically defined as equal to 10 times the standard deviation of the results for a series of replicates used to determine a justifiable limit of detection. Limits of quantitation are matrix-, method-, and analyte-specific. (NCT00410072)
Timeframe: At Weeks 48 and 96

,
InterventionPercentage of participants (Number)
< LOQ (29 IU/mL) at Week 48LOQ - <50 IU/mL at Week 4850 - <172 IU/mL at Week 48172 - <1720 IU/mL at Week 481720 - <17,200 IU/mL at Week 4817,200 - <172,000 IU/mL at Week 48≥172,000 IU/mL at Week 48Missing at Week 48< LOQ (29 IU/mL) at Week 96LOQ - <50 IU/mL at Week 9650 - <172 IU/mL at Week 96172 - <1720 IU/mL at Week 961720 - <17,200 IU/mL at Week 9617,200 - <172,000 IU/mL at Week 96≥172,000 IU/mL at Week 96Missing at Week 96
ETV 0.5 mg67.62.77.17.79.31.60.53.374.71.63.35.54.90.509.3
ETV 0.5 mg +TDF 300 mg74.65.66.64.10.5008.681.71.51.01.5000.513.7

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Number of Participants With Adverse Events, Serious Adverse Events, and Discontinuations From Study Drug Due to Adverse Events or Laboratory Abnormalities

AE: any new untoward medical occurrence/worsening of pre-existing medical condition, whether or not related to study drug. SAE: any AE that resulted in death; was life threatening; resulted in persistent/significant disability/incapacity; resulted in/prolonged an existing in-patient hospitalization; was a congenital anomaly/birth defect; or was an overdose. Participants who discontinued the study due to any AEs were recorded. (NCT00410072)
Timeframe: From enrollment through Week 100 + 24-week follow-up

,
InterventionParticipants (Number)
DeathsSAEsAdverse eventsDiscontinuations due to AEsRelated AEs
ETV 0.5 mg012132239
ETV 0.5 mg +TDF 300 mg314131549

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Mean Log 10 HBV DNA at Weeks 48 and 96

HBV DNA was analyzed by PCR, using the Roche COBAS®TaqMan - HPS assay. Reduction in Log 10 HBV count=reduced viral load. (NCT00410072)
Timeframe: Baseline, Weeks 48 and 96

,
Interventionlog10 copies/mL (Mean)
Baseline (n=182, 197)Overall at Week 48 (n=176, 180)Overall at Week 96 (n=165, 170)
ETV 0.5 mg7.481.881.68
ETV 0.5 mg +TDF 300 mg7.531.561.51

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Percentage of Participants Who Achieved Hepatitis B Virus DNA (HBV DNA) Levels <50 IU/mL by Polymerase Chain Reaction (PCR) at Week 96

HBV DNA levels <50 IU/mL=approximately 300 copies/mL. Analyses of binary efficacy endpoint during on-treatment period focused on participants who received treatment and used the analysis of noncompleter=failure (NC=F). All participants who received treatment were included in the denominator, and participants with missing measurements were counted as nonresponders for the specific endpoints. (NCT00410072)
Timeframe: At Week 96

InterventionPercentage of participants (Number)
ETV 0.5 mg76.4
ETV 0.5 mg +TDF 300 mg83.2

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Number of Participants With Virologic Breakthrough at Week 96

ETVr=entecavir resistance; TFDr=tenofovir resistance. Virologic breakthrough=confirmed >=1 log10 increase in HBV DNA from moving nadir (NCT00410072)
Timeframe: Week 96

,
InterventionParticipants (Number)
ETVrTDFr
ETV 0.5 mg00
ETV 0.5 mg +TDF 300 mg00

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Percentage of Participants With Hepatitis B Surface Antigen (HBsAg) Loss at Weeks 48 and 96

HBsAg = A part of the hepatitis B virus. When found in the blood, HBsAg is an early marker of infection. Analyses of binary efficacy endpoint during on-treatment period focused on participants who received treatment and used the analysis of noncompleter=failure (NC=F). All participants who received treatment were included in the denominator, and participants with missing measurements were counted as nonresponders for the specific endpoints. (NCT00410072)
Timeframe: At Weeks 48 and 96

,
InterventionPercent of participants (Number)
Week 48Week 96
ETV 0.5 mg3.24.0
ETV 0.5 mg +TDF 300 mg1.45.1

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Percentage of Participants With Hepatitis B e Antigen (HBeAg) Loss at Weeks 48 and 96

HBeAg is a hepatitis B viral protein and is an indicator of active viral replication. Analyses of binary efficacy endpoint during on-treatment period focused on participants who received treatment and used the analysis of noncompleter=failure (NC=F). All participants who received treatment were included in the denominator, and participants with missing measurements were counted as nonresponders for the specific endpoints. (NCT00410072)
Timeframe: At Weeks 48 and 96

,
InterventionPercentage of participants (Number)
Week 48Week 96
ETV 0.5 mg25.43.97
ETV 0.5 mg +TDF 300 mg19.629.7

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Percentage of Participants With HBsAg Seroconversion at Weeks 48 and 96

HBsAg = a part of the hepatitis B virus that, when in the blood, is an early marker of infection. (NCT00410072)
Timeframe: At Weeks 48 and 96

,
InterventionPercentage of participants (Number)
Week 48Week 96
ETV 0.5 mg0.81.6
ETV 0.5 mg +TDF 300 mg0.72.9

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Percentage of Participants With Alanine Aminotransferase (ALT) > 1 x Upper Limit of Normal (ULN) at Baseline Who Achieve ALT Normalization at Week 96

ALT normalization=ALT level being less than or equal to 1 times the upper limit of normal (ULN). ULN for ALT is 37 U/L. (NCT00410202)
Timeframe: Baseline, Week 96

Interventionpercentage of participants (Number)
ETV+ADV Combination Therapy76.9
ETV Monotherapy74.4
ADV+LVD Combination Therapy79.7

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Percentage of Participants With Alanine Aminotransferase (ALT) > 1 x Upper Limit of Normal (ULN) at Baseline Who Achieve ALT Normalization at Week 48

ALT normalization=ALT level being less than or equal to 1 times the upper limit of normal (ULN). ULN for ALT is 37 or 48 U/L. (NCT00410202)
Timeframe: Week 48

Interventionpercentage of participants (Number)
ETV+ADV Combination Therapy75.6
ETV Monotherapy78.0
ADV+LVD Combination Therapy76.8

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Percentage of Participants Who Achieve HBV DNA < Lower Limit of Quantitation (LOQ = 29 IU/mL [Approximately 169 Copies/mL]) at Week 96

HBV DNA assessments were performed using the Roche COBAS® TaqMan HPS assay. LOQ is the level above which quantitative results may be obtained with a specified degree of confidence. The LOQ is mathematically defined as equal to 10 times the standard deviation of the results for a series of replicates used to determine a justifiable limit of detection. Percentage n/N: n= number of participants with outcome result; N = number of participants analyzed. (NCT00410202)
Timeframe: Week 96

InterventionPercentage of participants (Number)
ETV+ADV Combination Therapy38.4
ETV Monotherapy36.4
ADV+LVD Combination Therapy25.5

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Percentage of Participants Who Achieve HBV DNA < Lower Limit of Quantitation (LOQ = 29 IU/mL [Approximately 169 Copies/mL]) at Week 48

HBV DNA assessments were performed using the Roche COBAS® TaqMan HPS assay. LOQ is the level above which quantitative results may be obtained with a specified degree of confidence. The LOQ is mathematically defined as equal to 10 times the standard deviation of the results for a series of replicates used to determine a justifiable limit of detection. Percentage n/N: n= number of participants with outcome result; N = number of participants analyzed. (NCT00410202)
Timeframe: Week 48

Interventionpercentage of participants (Number)
ETV+ADV Combination Therapy25.4
ETV Monotherapy13.6
ADV+LVD Combination Therapy16.8

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Percentage of Participants Who Achieve HBV DNA < Lower Limit of Detection (LOD = 10 IU/mL [Approximately 58 Copies/mL]) at Week 96

HBV DNA assessments were performed using the Roche COBAS® TaqMan HPS assay. LOD is the lowest amount or concentration of analyte in a sample, which can be reliably detected, but not necessarily quantified. (NCT00410202)
Timeframe: Week 96

Interventionpercentage of participants (Number)
ETV+ADV Combination Therapy33.3
ETV Monotherapy27.1
ADV+LVD Combination Therapy20.4

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Percentage of Participants Who Achieve HBV DNA < Lower Limit of Detection (LOD = 10 IU/mL [Approximately 58 Copies/mL]) at Week 48

HBV DNA assessments were performed using the Roche COBAS® TaqMan HPS assay. LOD is the lowest concentration level that can be determined to be statistically different from a blank (99% confidence). The LOD is typically determined to be in the region where the signal to noise ratio is greater than 5. Limits of detection are matrix-, method-, and analyte-specific. (NCT00410202)
Timeframe: Week 48

Interventionpercentage of participants (Number)
ETV+ADV Combination Therapy20.3
ETV Monotherapy11.4
ADV+LVD Combination Therapy11.7

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Change in Mean log10 From Baseline in HBV DNA at Week 96

HBV DNA was analyzed by PCR, using the Roche COBAS® TaqMan HPS assay. Reduction in log10 HBV count=reduced viral load. (NCT00410202)
Timeframe: Baseline, Week 96

Interventionparticipants (Mean)
ETV+ADV Combination Therapy-5.06
ETV Monotherapy-4.17
ADV+LVD Combination Therapy-4.49

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Percentage of Participants With HBV DNA < 50 IU/mL (Approximately 300 Copies/mL) by PCR at Week 96

HBV DNA assessments were performed using the Roche COBAS® TaqMan HPS assay. HBV DNA < 50 IU/mL = approximately 300 copies/mL. Percentage n/N: n= number of participants with HBV DNA <50 IU/mL; N = number of participants analyzed. (NCT00410202)
Timeframe: Week 96

InterventionPercentage of participants (Number)
ETV+ADV Combination Therapy43.5
ETV Monotherapy39.3
ADV+LVD Combination Therapy28.5

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Percentage of Participants With Hepatitis B Surface Antigen (HBsAg) Loss at Week 48

HBsAg = a part of the hepatitis B virus that, when in the blood, is an early marker of infection. HBsAg loss = HBsAg-negative at the specified analysis week. (NCT00410202)
Timeframe: Week 48

Interventionpercentage of participants (Number)
ETV+ADV Combination Therapy0.7
ETV Monotherapy0
ADV+LVD Combination Therapy0.7

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Percentage of Participants With HBsAg Seroconversion at Week 96

HBsAg = a part of the hepatitis B virus that, when in the blood, is an early marker of infection. HBs seroconversion is defined as HBsAg loss with positive HBsAb. (NCT00410202)
Timeframe: Week 96

Interventionpercentage of participants (Number)
ETV+ADV Combination Therapy0
ETV Monotherapy0
ADV+LVD Combination Therapy0

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Percentage of Participants With Hepatitis B Surface Antigen (HBsAg) Loss at Week 96

HBsAg = a part of the hepatitis B virus that, when in the blood, is an early marker of infection. HBsAg loss = HBsAg-negative at the specified analysis week. (NCT00410202)
Timeframe: Week 96

Interventionpercentage of participants (Number)
ETV+ADV Combination Therapy0
ETV Monotherapy0
ADV+LVD Combination Therapy0

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Percentage of Participants With Hepatitis B Virus (HBV) Deoxyribonucleic Acid (DNA) < 50 IU/mL (Approximately 300 Copies/mL) by Polymerase Chain Reaction (PCR) at Week 48

HBV DNA assessments were performed using the Roche COBAS® TaqMan High Pure System (HPS) assay. HBV DNA less than (<)50 International units per milliliter (IU/mL) = approximately 300 copies/mL. Percentage of participants calculated n/N; n= number of participants with HBV DNA <50 IU/mL; N = number of participants analyzed. (NCT00410202)
Timeframe: Week 48

Interventionpercentage of participants (Number)
ETV+ADV Combination Therapy25.4
ETV Monotherapy16.4
ADV+LVD Combination Therapy19.7

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Change in Mean log10 From Baseline in HBV DNA at Week 48

HBV DNA was analyzed by PCR, using the Roche COBAS®TaqMan TaqMan HPS assay. Reduction in log10 HBV count=reduced viral load, negative values means reduction. (NCT00410202)
Timeframe: Baseline, Week 48

,,
Interventionlog10 (IU/mL (Mean)
HBV DNA at Week 48Change from baseline
ADV+LVD Combination Therapy3.36-4.11
ETV Monotherapy4.01-3.35
ETV+ADV Combination Therapy2.79-4.65

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Cumulative Probability of Emergent Genotypic Resistance at Year 1

"yr=year. Cumulative probability (CP): Ptotal=1-(1-Pyr1)*(1-Pyr2) where Pyear(i)= number of participants with events at Year i divided by number of participants at risk at Year i for i = 1,2. An event is defined as resistance or resistance with virologic breakthrough in a yearly interval. Participants 'at risk' are those who were treated during Year i and did not develop that resistance or resistance with virologic breakthrough prior to Year i. CP were calculated separately for ETV, ADV and TDF resistance. Participants who discontinue from study drug in Year i were assumed to be in follow up for the entire year. (VBT; a ≥ 1 log10 increase in HBV DNA from the on-treatment nadir, confirmed by 2 sequential HBV DNA results or observed at the last on-treatment HBV DNA). ETVr = ETV resistance (rtM204V/I/S plus any substitution at rtT184, rtS202, or rtM250); ADVr/TDFr = ADV/TDF resistance (rtA181T/V or rtN236T = ADVr and TDFr, rtA194T = TDFr only)." (NCT00410202)
Timeframe: Year 1

,,
Interventionpercentage of participants (Number)
ETVr : n=134, 134, 134ADVr /TDFr : n=137, 137, 135ETVr or TDFr/ADVr : n=133, 132, 132ETVr and TDFr/ADVr : n=138, 139, 137ETVr with VBT: n=134, 134, 134ADVr /TDFr with VBT: n=137, 137, 135ETVr or ADVr/TDFr with VBT: n=133, 132, 132ETVr and ADVr/TDFr with VBT: n=138, 139, 137
ADV+LVD Combination Therapy0.71.52.300000
ETV Monotherapy30.73.800.700.80
ETV+ADV Combination Therapy00.70.800000

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Cumulative Probability of Emergent Genotypic Resistance at Year 2

"Cumulative probability (CP): Ptotal=1-(1-Pyr1)*(1-Pyr2) where Pyear(i)= number of participants with events at Year i divided by number of participants at risk at Year i for i = 1,2. An event is defined as resistance or resistance with virologic breakthrough in a yearly interval. Participants 'at risk' are those who were treated during Year i and did not develop that resistance or resistance with virologic breakthrough prior to Year i. CP were calculated separately for ETV, ADV and TDF resistance. Participants who discontinue from study drug in Year i were assumed to be in follow up for the entire year. (VBT; a ≥ 1 log10 increase in HBV DNA from the on-treatment nadir, confirmed by 2 sequential HBV DNA results or observed at the last on-treatment HBV DNA). ETVr = ETV resistance (rtM204V/I/S plus any substitution at rtT184, rtS202, or rtM250); ADVr/TDFr = ADV/TDF resistance (rtA181T/V or rtN236T = ADVr and TDFr, rtA194T = TDFr only)." (NCT00410202)
Timeframe: Year 2

,,
Interventionpercentage of participants (Number)
ETVr : n=130, 128, 131ADVr/TDFr : n=132, 134, 131ETVr or ADVr/TDFr : n=128, 125, 127ETVr and ADVr/TDFr : n=134, 137, 135ETVr with VBT: n=130, 128, 131ADVr/TDFr with VBT: n=132, 134, 131ETVr or ADVr/TDFr with VBT: n=128, 125, 127ETVr and ADVr/TDFr with VBT: n=134, 137, 135
ADV+LVD Combination Therapy1.52.23.800000
ETV Monotherapy9.81.510.70.76.20.76.30.7
ETV+ADV Combination Therapy0.80.71.500000

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Number of Participants With Laboratory Abnormalities: Hematology

Criteria for hematology abnormalities were: Hemoglobin: <=11.0 g/dL; White Blood Cells: <4000/mm^3; Absolute Neutrophils (includes absolute bands): <1500/mm^3; Platelets: <=99,000/mm^3; International Normalized Ratio: ≥ 1.5 and ≥ 0.5 from baseline. (NCT00410202)
Timeframe: From start of study through Week 100 + 5 days

,,
Interventionparticipants (Number)
HemoglobinWhite Blood CellsNeutrophilsPlateletsInternational Normalized Ratio
ADV+LVD Combination Therapy113815129
ETV Monotherapy94817147
ETV+ADV Combination Therapy85314138

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Number of Participants With Laboratory Abnormalities: Serum Chemistry

ULN=upper limit of normal (Normal ranges are Central lab data and vary according to the site). ALT:>1.25*ULN, AST:>1.25*ULN, ALP:>1.25*ULN, Total Bilirubin:>1.1*ULN, Serum Lipase:>1.10*ULN, Creatinine:>1.1*ULN, Blood Urea Nitrogen:1.25*ULN, Hyperglycemia:>116 mg/dL, Hypoglycemia:<64 mg/dL, Hyponatremia:<132meq/L, Hypokalemia:<3.4 meq/L, Albumin:≥1g/dL decrease from baseline, <3 g/dL; Hypernatremia:>148 meq/L, Hyperkalemia:>5.6 meq/L, Hypokalemia:<3.4 meq/L, Hyperchloremia:>113 meq/L, Hypochloremia:<93 meq/L; ALT flare: on treatment (OT), >2*Baseline and >10*ULN; off treatment (OF), 2*end of dosing value and >10*ULN (NCT00410202)
Timeframe: On treatment : Day 1 through Week 100 + 5 days; Offtreatment = End of OT period through 24 weeks

,,
Interventionparticipants (Number)
Alanine aminotransferase (ALT)Aspartate aminotransferase (AST)Alkaline Phosphatase (ALP)AlbuminSerum LipaseCreatinineBlood Urea NitrogenHyperglycemiaHypoglycemiaHypernatremiaHyponatremiaHyperkalemiaHypokalemiaHyperchloremiaHypochloremiaALT flare - OntreatmentALT flare - Offtreatment
ADV+LVD Combination Therapy7453612442379100521020
ETV Monotherapy8362413321465100421020
ETV+ADV Combination Therapy7660812420399100341130

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Participants With Adverse Events (AE), Serious Adverse Events (SAE), and Discontinuations Due to Adverse Events or Laboratory Abnormalities During Treatment

AE: any new untoward medical occurrence/worsening of pre-existing medical condition, whether or not related to study drug. SAE: any AE that resulted in death; was life threatening; resulted in persistent/significant disability/incapacity; resulted in/prolonged an existing in-patient hospitalization; was a congenital anomaly/birth defect; or was an overdose. Participants who discontinued the study due to any AEs were recorded. Grade 1 = mild, Grade 2= moderate, Grade 3 = severe, Grade 4 = life threatening/disabling, Grade 5 = death. (NCT00410202)
Timeframe: From start of study therapy through Week 100 + 5 days

,,
Interventionparticipants (Number)
DeathsSAEsDiscontinuations due to AEsAEsGrade 2-4 Related AEsGrade 3-4 Related AEs
ADV+LVD Combination Therapy11229219
ETV Monotherapy0172109127
ETV+ADV Combination Therapy011110125

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Percentage of Participants With HBV DNA by PCR Category at Week 48

HBV DNA assessments were performed using the Roche COBAS® TaqMan High Pure System (HPS) assay. (NCT00410202)
Timeframe: Week 48

,,
Interventionpercentage of participants (Number)
< LOQ (29 IU/mL)LOQ to < 5050 to < 172172 to < 1,7201,720 to < 17,20017,200 to < 172,000>= 172,000Missing
ADV+LVD Combination Therapy16.82.95.812.431.424.84.41.5
ETV Monotherapy13.62.92.97.922.125.723.61.4
ETV+ADV Combination Therapy25.408.026.128.38.00.73.6

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Percentage of Participants With HBV DNA by PCR Category at Week 96

HBV DNA assessments were performed using the Roche COBAS® TaqMan HPS assay. (NCT00410202)
Timeframe: Week 96

,,
Interventionpercentage of participants (Number)
< LOQ (29 IU/mL)LOQ to < 5050 to < 172172 to < 1,7201,720 to < 17,20017,200 to < 172,000>= 172,000Missing
ADV+LVD Combination Therapy25.52.95.818.224.813.92.95.8
ETV Monotherapy36.42.93.66.410.015.716.48.6
ETV+ADV Combination Therapy38.45.110.115.220.35.805.1

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Percentage of Participants With Confirmed HBeAg Loss at Week 48 (Treated HBeAg Positive Participants Only)

HBeAg is a hepatitis B viral protein. HBeAg loss = HBeAg-negative at the specified analysis week (NCT00410202)
Timeframe: Week 48

Interventionpercentage of participants (Number)
ETV+ADV Combination Therapy7.2
ETV Monotherapy6.5
ADV+LVD Combination Therapy5.9

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Percentage of Participants With Confirmed HBeAg Loss at Week 96 (Treated HBeAg Positive Participants Only)

HBeAg is a hepatitis B viral protein. HBeAg loss = HBeAg-negative at the specified analysis week (NCT00410202)
Timeframe: Week 96

Interventionpercentage of participants (Number)
ETV+ADV Combination Therapy12.3
ETV Monotherapy10.7
ADV+LVD Combination Therapy13.9

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Percentage of Participants With HBsAg Seroconversion at Week 48

HBsAg = a part of the hepatitis B virus that, when in the blood, is an early marker of infection. HBs seroconversion is defined as HBsAg loss with positive HBsAb. (NCT00410202)
Timeframe: Week 48

Interventionpercentage of participants (Number)
ETV+ADV Combination Therapy0.7
ETV Monotherapy0
ADV+LVD Combination Therapy0

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Percentage of Participants With HBeAg Seroconversion at Week 48 (Treated HBeAg-positive Participants Only)

HBeAg is a hepatitis B viral protein. It is an indicator of active viral replication. HBeAg Seroconversion = HBeAg Loss and Presence of Hepatitis B e Antibody (HBeAb). (NCT00410202)
Timeframe: Week 48

Interventionpercentage of participants (Number)
ETV+ADV Combination Therapy5.1
ETV Monotherapy2.9
ADV+LVD Combination Therapy3.7

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Percentage of Participants With HBeAg Seroconversion at Week 96 (Treated HBeAg-positive Participants Only)

HBeAg is a hepatitis B viral protein. It is an indicator of active viral replication. HBeAg Seroconversion = HBeAg Loss and Presence of Hepatitis B e Antibody (HBeAb). (NCT00410202)
Timeframe: Week 96

Interventionpercentage of participants (Number)
ETV+ADV Combination Therapy7.2
ETV Monotherapy3.6
ADV+LVD Combination Therapy5.1

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The Area Under the Curve (AUC) of HBV DNA Change.

In AUC efficacy analyses, all the visits from baseline to Week 12 visit (including the planned and the repeated) with a non-missing HBV DNA level were included. (NCT00412529)
Timeframe: From Baseline to Week 12

Intervention(log10 copies/mL) * days (Mean)
Telbivudine-453.5
Entecavir-442.6

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Characterization of Very Early Viral Kinetics: Estimation of Viral Clearance

"Viral kinetic parameters were estimated with a bi-phasic mathematical model:~V(t) = (1-ε)pI(t) - cV(t)~I(t) = (1- η)TV(t) - δI(t)~V serum viral load, I productively infected cells, ε efficiency factor of blocking virus production, p viral production rate, c viral clearance rate, η efficiency factor of blocking de novo infection, β de novo infection rate, T uninfected target cells, δ rate of infected cell loss. Maximum-likelihood estimation for the viral kinetic parameters entailed fitting a nonlinear differential equation system via the least-squares approach from serum HBV DNA data." (NCT00412529)
Timeframe: Baseline to 12 weeks

Interventionclearance per day (Mean)
Telbivudine0.809
Entecavir1.002

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Characterization of Very Early Viral Kinetics: Estimation of the Rate of Infected Cell Loss

"Viral kinetic parameters were estimated with a bi-phasic mathematical model:~V(t) = (1-ε)pI(t) - cV(t)~I(t) = (1- η)TV(t) - δI(t)~V serum viral load, I productively infected cells, ε efficiency factor of blocking virus production, p viral production rate, c viral clearance rate, η efficiency factor of blocking de novo infection, β de novo infection rate, T uninfected target cells, δ rate of infected cell loss. Maximum-likelihood estimation for the viral kinetic parameters entailed fitting a nonlinear differential equation system via the least-squares approach from serum HBV DNA data." (NCT00412529)
Timeframe: Baseline to 12 weeks

Interventioninfected cell loss per day (Mean)
Telbivudine0.075
Entecavir0.071

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Characterization of Very Early Viral Kinetics: Estimation of the Efficiency Factor of Blocking Virus Production

Viral kinetic parameters were estimated with a bi-phasic mathematical model of HBV DNA by using compartments of free virus, infected cells, and uninfected target cells. The model parameter of interest was the effectiveness of the drug in blocking virus production from infected cells (efficacy, ε). Blocking efficiency was within the range between 0 and 1. (NCT00412529)
Timeframe: Baseline to 12 weeks

Interventionpercentage of blocking efficiency (Mean)
Telbivudine0.991
Entecavir0.992

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Change in Alanine Aminotransferase (ALT) Levels

(NCT00412529)
Timeframe: From Baseline to Week 12

,
InterventionIU/L (Mean)
BaselineAt Week 12Change from Baseline to Week 12
Entecavir170.254.0-116.3
Telbivudine163.155.1-108.0

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Number of Patients Who Are Polymerase Chain Reaction (PCR) Negative

PCR negative was considered <300 copies/mL. PCR positive was considered =>300 copies/mL. (NCT00412529)
Timeframe: At Week 12

,
InterventionParticipants (Number)
<300 copies/mL>= 300 copies/mL
Entecavir615
Telbivudine221

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Change in Mean Hepatitis B Virus (HBV) DNA Levels

Baseline HBV DNA is defined as the last pre-dose assessment of HBV DNA. (NCT00412529)
Timeframe: Baseline (day 1) to Week 12 (day 85)

,
Interventionlog10 copies/mL (Mean)
Baseline (day 1)At Week 12Change from Baseline to week 12
Entecavir9.7213.194-6.527
Telbivudine10.2903.669-6.621

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Change in Mean HBV DNA Level

Baseline HBV DNA is defined as the last pre-dose assessment of HBV DNA.HBV DNA reductions, considered as the repeated measures, from baseline to Weeks 2, 4, 8. (NCT00412529)
Timeframe: Baseline (day 1) to Weeks 2, 4, 8

,
Interventionlog10 copies/mL (Mean)
Change from Baseline to week 2 :(N=20, 21)Change from Baseline to week 4 : (N= 23, 21)Change from Baseline to week 8 : (N= 23, 21)
Entecavir-3.974-4.875-5.976
Telbivudine-3.999-5.273-6.161

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Number of Participants With HBV DNA Less Than 50 IU/mL Through Week 96 in Treated Participants

Hepatitis B virus DNA by polymerase chain reaction (PCR) was measured using the Roche COBAS TaqMan - high pure system (HPS) assay and was reported in international units per milliliter (IU/mL). Baseline was the last value measured prior to or on the date of the first dose of study therapy. (NCT00423891)
Timeframe: Baseline to Week 96

,,
Interventionparticipants (Number)
BaselineWeek 12Week 24Week 36Week 48Week 96
Lamivudine (LVD)-Experienced (Group B)0036911
Lamivudine (LVD)-Naive (Group A)011011148
Nucleoside/Tide Analog (NA) - Experienced (Group C)000002

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Number of Participants With HBV DNA Less Than Lower Limit of Quantification (LLQ) for the Roche COBAS TaqMan - HPS Assay Through Week 96 in Treated Participants

Hepatitis B virus DNA by PCR was measured using the Roche COBAS TaqMan - HPS assay and was reported in IU/mL. LLQ = 29 IU/mL. Baseline was the last value measured prior to or on the date of the first dose of study therapy. (NCT00423891)
Timeframe: Baseline through Week 96

,,
Interventionparticipants (Number)
BaselineWeek 12Week 24Week 36Week 48Week 96
Lamivudine (LVD)-Experienced (Group B)002578
Lamivudine (LVD)-Naive (Group A)01910148
Nucleoside/Tide Analog (NA) - Experienced (Group C)000002

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Number of Participants With HBV DNA Less Than Lower Limit of Detection (LLD) for the Roche COBAS TaqMan - HPS Assay at Week 96 in Treated Participants

Hepatitis B virus DNA by PCR was measured using the Roche COBAS TaqMan - HPS assay and was reported in IU/mL. LLD = 6 IU/mL). Baseline was the last value measured prior to or on the date of the first dose of study therapy. (NCT00423891)
Timeframe: Baseline to Week 96

,,
Interventionparticipants (Number)
BaselineWeek 12Week 24Week 36Week 48Week 96
Lamivudine (LVD)-Experienced (Group B)001568
Lamivudine (LVD)-Naive (Group A)0167138
Nucleoside/Tide Analog (NA) - Experienced (Group C)000001

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Number of Participants Who Had a Protocol Defined Response (PDR) Through Week 96 in Treated Participants

PDR was defined as confirmed HBV DNA < 50 IU/mL plus confirmed HBeAg seroconversion on 2 sequential measurements at least 14 days apart. Baseline was the last value measured prior to or on the date of the first dose of study therapy. (NCT00423891)
Timeframe: Baseline to Week 96

,,
Interventionparticipants (Number)
Week 12Week 24Week 36Week 48Week 96
Lamivudine (LVD)-Experienced (Group B)00131
Lamivudine (LVD)-Naive (Group A)04473
Nucleoside/Tide Analog (NA) - Experienced (Group C)00000

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Number of Participants With a Combination of ALT Normalization and HBV DNA Less Than 50 IU/mL Through Week 96 in Treated Participants

Hepatitis B virus DNA by PCR was measured using the Roche COBAS TaqMan - HPS assay and was reported in IU/mL. Baseline was the last value measured prior to or on the date of the first dose of study therapy. Normalization in ALT= ALT ≤ 1.0*ULN. (NCT00423891)
Timeframe: Baseline to Week 96

,,
Interventionparticipants (Number)
BaselineWeek 12Week 24Week 36Week 48Week 96
Lamivudine (LVD)-Experienced (Group B)0034911
Lamivudine (LVD)-Naive (Group A)001011137
Nucleoside/Tide Analog (NA) - Experienced (Group C)000002

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Number of Participants With a Combination of ALT Normalization and HBV DNA Less Than 50 IU/mL, Plus HBeAg Seroconversion Through Week 96 in Treated Participants

Hepatitis B virus DNA by PCR was measured using the Roche COBAS TaqMan - HPS assay and was reported in IU/mL. Baseline was the last value measured prior to or on the date of the first dose of study therapy. Normalization in ALT= ALT ≤ 1.0*ULN. HBe seroconversion was determination of presence of HBeAb and loss of HBeAg. The method used for the detection of HBeAg seroconversion was the DiaSorin - Anti HBe enzyme immunoassay kit. (NCT00423891)
Timeframe: Baseline to Week 96

,,
Interventionparticipants (Number)
BaselineWeek 12Week 24Week 36Week 48Week 96
Lamivudine (LVD)-Experienced (Group B)000131
Lamivudine (LVD)-Naive (Group A)004483
Nucleoside/Tide Analog (NA) - Experienced (Group C)000000

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Number of Participants With Chemistry Laboratory Abnormalities (Grades 1 - 4) - On Treatment - Treated Participants

Toxicity Scale: DAIDS Version 1.0 and modified World Health Organization (WHO). Grade (Gr). ALT: Gr1:1.25-<2.5*ULN; Gr2: 2.6-<5.0 *ULN; Gr3: 5.1-10.0*ULN; Gr4:>10.0*ULN. Aspartate aminotransferase (AST): Gr1: 1.25-<2.5*ULN; Gr2:2.6-<5.0*ULN; Gr 3: 5.1-10.0*ULN; Gr4>10.0*ULN. Alkaline phosphatase: Gr1:1.25-<2.5*ULN; Gr2: 2.6-<5.0*ULN; Gr3: 5.1-10.0*ULN; Gr4: >10.0*ULN. Lipase: Gr1:1.1-<1.5*ULN;Gr2:1.6-<3.0*ULN; Gr3: 3.1-5.0*ULN; Gr4: >5.0*ULN. Creatinine: Gr1: 1.1-1.3*ULN; Gr2: 1.4-<1.8*ULN; Gr3: 1.9 - <3.4*ULN; Gr4: >=3.5*ULN. Glucose mg/dL (high): Gr1:110-<125 (Fasting)/116-<160;Gr2:126-<250 (F)/161-<250; Gr3: 251-500; Gr4: >500.Glucose (low): Gr1: 55-64; Gr2: 40 - <54; Gr3: 30-39; Gr4: <30 mg/dL. (NCT00423891)
Timeframe: Day 1 to Week 120

,,
Interventionparticipants (Number)
ALTASTAlkaline PhosphataseLipaseCreatinineGlucose, highGlucose, low
Lamivudine (LVD)-Experienced (Group B)179312144
Lamivudine (LVD)-Naive (Group A)231435133
Nucleoside/Tide Analog (NA) - Experienced (Group C)4103011

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Number of Participants With Electrolyte Laboratory Abnormalities (Grades 1 - 4) - On Treatment - Treated Participants

Toxicity Scale: DAIDS Version 1.0 and modified World Health Organization (WHO) for chloride. Milliequivalents per liter (mEq/L); Grade (Gr). Chloride high (mEq/L): Gr1: 113-<117; Gr2: 117-<121; Gr3: 121-125; Gr4: >125. Potassium low (mEq/L): Gr1: 3.0-3.4; Gr2: 2.5-2.9; Gr3:2.0-<2.4; Gr4: <2.0. Potassium high: Gr1; 5.6- <6.0; Gr2: 6.1-<6.5; Gr3: 6.6-7.0; Gr4: >7.0. Sodium high (mEq/L): Gr1; 146-<150; Gr2: 151-<154; Gr3: 155-<159; Gr4: >=160. (NCT00423891)
Timeframe: Day 1 Week 120

,,
Interventionparticipants (Number)
Chloride, highPotassium, lowPotassium, highSodium, high
Lamivudine (LVD)-Experienced (Group B)0013
Lamivudine (LVD)-Naive (Group A)3114
Nucleoside/Tide Analog (NA) - Experienced (Group C)0000

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Number of Participants With HB s Antigen (HBsAg) Seroconversion Through Week 96 in Treated Participants

HB s Ag seroconversion: loss of HBsAg (HBsAg negative) and presence of HB s antibodies (HBsAb). The method used for the detection of HBsAg seroconversion was the ADVIA Centaur iImmunoassay system. Baseline was the last value measured prior to or on the date of the first dose of study therapy. (NCT00423891)
Timeframe: Baseline through Week 96

,,
Interventionparticipants (Number)
BaselineWeek 12Week 24Week 36Week 48Week 96
Lamivudine (LVD)-Experienced (Group B)000000
Lamivudine (LVD)-Naive (Group A)000000
Nucleoside/Tide Analog (NA) - Experienced (Group C)000000

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Number of Participants With HBV DNA by PCR Categories at Weeks 48 and 96 in Treated Participants

Hepatitis B virus DNA by PCR was measured using the Roche COBAS TaqMan - HPS assay and was reported in IU/mL. LLQ = 29 IU/mL. Baseline was the last value measured prior to or on the date of the first dose of study therapy. (NCT00423891)
Timeframe: Baseline, Week 48, Week 96

,,
Interventionparticipants (Number)
Baseline >=17,200 IU/mLWeek 48: < 50 IU/mLWeek 48: 50 - < 172 IU/mLWeek 48: 172 - < 1720 IU/mLWeek 48: 1720 - < 17,200 IU/mLWeek 48: > = 17,200 IU/mLWeek 96: < 50 IU/mLWeek 96: 50 - < 172 IU/mLWeek 96: 172 - < 1720 IU/mLWeek 96: 1720 - < 17,200 IU/mLWeek 96: > = 17,200 IU/mL
Lamivudine (LVD)-Experienced (Group B)1992313111010
Lamivudine (LVD)-Naive (Group A)2414133181300
Nucleoside/Tide Analog (NA) - Experienced (Group C)50013120110

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Alanine Aminotransferase (ALT) Normalization From Baseline Through Week 96 in Treated Participants

Normalization in ALT= ALT ≤ 1.0*upper limit of normal (ULN). Baseline was the last value measured prior to or on the date of the first dose of study therapy. (NCT00423891)
Timeframe: Baseline to Week 96

,,
Interventionparticipants (Number)
BaselineWeek 4Week 8Week 12Week 18Week 24Week 30Week 36Week 42Week 48Week 96
Lamivudine (LVD)-Experienced (Group B)112710121316151813
Lamivudine (LVD)-Naive (Group A)013515151616162010
Nucleoside/Tide Analog (NA) - Experienced (Group C)22235555543

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Mean Apparent Total Body Clearance (CLT/F) of Entecavir in LVD-naive and LVD-experienced Participants, by Age Cohort

CLT/F was calculated by dividing the dose of ETV by AUC(TAU) of ETV and was measured in liters per hour (L/h). Blood samples were obtained before study drug administration and at 0.5, 1, 2, 4, 8, and 24 hours after study drug administration on Day 14 (+/- 4 days) for the PK assessment. Plasma samples were analyzed for ETV with a validated method using liquid chromatography-tandem mass spectrometry detection. PK assessment was optional for Group C participants (NA-experienced participants who were included with the September 2011 country-specific protocol amendment). No Group C participants chose to participate in the PK assessment. (NCT00423891)
Timeframe: At 2 weeks

,
InterventionL/h (Mean)
CLT/F of ETV (≥ 2 yrs to ≤ 6 yrs), (n=7, 3)CLT/F of ETV (> 6 yrs to ≤ 12 yrs), (n=9, 7)CLT/F of ETV (> 12 yrs to ≤ 18 yrs), (n=8,9)
Lamivudine (LVD)-Experienced (Group B)12.3121.6728.95
Lamivudine (LVD)-Naive (Group A)11.4022.6631.92

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Mean Area Under the Concentration-Time Curve in One Dosing Interval [AUC(TAU)] of Entecavir in LVD-naive and LVD-experienced Participants, by Age Cohort

Area under the Curve (AUC) was derived from plasma concentration of ETV versus time. AUC(TAU) was calculated by log- and linear trapezoidal summations, TAU = 24 hours, and was measured in nanograms*hours per milliliter (ng*h/mL). Blood samples were obtained before study drug administration and at 0.5, 1, 2, 4, 8, and 24 hours after study drug administration on Day 14 (+/- 4 days) for the PK assessment. Plasma samples were analyzed for ETV with a validated method using liquid chromatography-tandem mass spectrometry detection. PK assessment was optional for Group C participants (NA-experienced participants who were included with the September 2011 country-specific protocol amendment). No Group C participants chose to participate in the PK assessment. (NCT00423891)
Timeframe: Day 14

,
Interventionng*h/mL (Geometric Mean)
AUC(TAU) of ETV (≥ 2 yrs to ≤ 6 yrs), (n=7, 3)AUC(TAU) of ETV (> 6 yrs to ≤ 12 yrs), (n=9, 7)AUC(TAU) of ETV (> 12 yrs to ≤ 18 yrs), (n=8,9)
Lamivudine (LVD)-Experienced (Group B)42.2641.5035.36
Lamivudine (LVD)-Naive (Group A)18.6920.4215.96

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Mean Log10 Change From Baseline in HBV DNA Using Roche COBAS TaqMan - HPS Through Week 96 in Treated Participants

Hepatitis B virus DNA by PCR was measured using the Roche COBAS TaqMan - HPS assay and was reported in IU/mL. HBV DNA log10 changes from baseline were summarized over time. (NCT00423891)
Timeframe: Baseline to Week 96

,,
InterventionIU/mL (Mean)
Week 12Week 24Week 36Week 48Week 96
Lamivudine (LVD)-Experienced (Group B)-3.89-4.85-5.14-5.36-5.86
Lamivudine (LVD)-Naive (Group A)-4.45-5.30-5.61-5.86-6.30
Nucleoside/Tide Analog (NA) - Experienced (Group C)-3.80-3.89-3.90-4.32-5.79

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Mean Maximum Observed Plasma Concentration (Cmax) and Mean Trough Observed Plasma Concentration (Cmin) of Entecavir in LVD-naive and LVD-experienced Participants, by Age Cohort

Cmax and Cmin were derived from plasma concentration of ETV versus time and measured in nanograms per milliliters (ng/mL). Blood samples were obtained before study drug administration and at 0.5, 1, 2, 4, 8, and 24 hours after study drug administration on Day 14 (+/- 4 days) for the PK assessment. Plasma samples were analyzed for ETV with a validated method using liquid chromatography-tandem mass spectrometry detection. Note: PK parameters were summarized for only Groups A and B. PK assessment was optional for Group C participants (NA-experienced participants who were included with the September 2011 country-specific protocol amendment). No Group C participants chose to participate in the PK assessment. (NCT00423891)
Timeframe: Day 14

,
Interventionng/mL (Geometric Mean)
Cmax of ETV (≥ 2 yrs to ≤ 6 yrs), (n=7, 3)Cmax of ETV (> 6 yrs to ≤ 12 yrs), (n=9, 7)Cmax of ETV (> 12 yrs to ≤ 18 yrs), (n=8,9)Cmin of ETV (≥ 2 yrs to ≤ 6 yrs), (n=7, 3)Cmin of ETV (> 6 yrs to ≤ 12 yrs), (n=9, 7)Cmin of ETV (> 12 yrs to ≤ 18 yrs), (n=8,9)
Lamivudine (LVD)-Experienced (Group B)16.0319.0111.320.4680.4970.455
Lamivudine (LVD)-Naive (Group A)8.076.295.110.2440.3200.271

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Median Time of Maximum Observed Plasma Concentration (Tmax) in LVD-naive and LVD-experienced Participants, by Age Cohort

Tmax was derived from plasma concentration of ETV versus time and measured in hours (h). Blood samples were obtained before study drug administration and at 0.5, 1, 2, 4, 8, and 24 hours after study drug administration on Day 14 (+/- 4 days) for the PK assessment. Plasma samples were analyzed for ETV with a validated method using liquid chromatography-tandem mass spectrometry detection. Age categories presented below: participants age as of first day of dosing. PK assessment was optional for Group C participants (NA-experienced participants who were included with the September 2011 country-specific protocol amendment). No Group C participants chose to participate in the PK assessment. (NCT00423891)
Timeframe: Day 14

,
Interventionh (Median)
Tmax of ETV (≥ 2 yrs to ≤ 6 yrs), (n=7, 3)Tmax of ETV (> 6 yrs to ≤ 12 yrs), (n=9, 7)Tmax of ETV (> 12 yrs to ≤ 18 yrs), (n=8,9)
Lamivudine (LVD)-Experienced (Group B)1.000.720.52
Lamivudine (LVD)-Naive (Group A)0.500.570.78

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Number of Participants With a Combination of ALT Normalization and HBV DNA Less Than 50 IU/mL, Without HBeAg Seroconversion, Through Week 96 in Treated Participants

Hepatitis B virus DNA by PCR was measured using the Roche COBAS TaqMan - HPS assay and was reported in IU/mL. Baseline was the last value measured prior to or on the date of the first dose of study therapy. Normalization in ALT= ALT ≤ 1.0*ULN. HBe seroconversion: loss of HBeAg (HBeAg negative) with positive HBeAb. The method used for the detection of HBeAg/Ab serologies was the DiaSorin enzyme immunoassay kit. (NCT00423891)
Timeframe: Baseline to Week 96

,,
Interventionparticipants (Number)
BaselineWeek 12Week 24Week 36Week 48Week 96
Lamivudine (LVD)-Experienced (Group B)0033610
Lamivudine (LVD)-Naive (Group A)006754
Nucleoside/Tide Analog (NA) - Experienced (Group C)000002

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Number of Participants With Serious Adverse Events (SAE) and Discontinuations Due to Adverse Events (AEs) - On Treatment

AE=any new unfavorable symptom, sign, or disease or worsening of a preexisting condition that may not have a causal relationship with treatment. SAE=a medical event that at any dose results in death, persistent or significant disability/incapacity, or drug dependency/abuse; is life-threatening, an important medical event, or a congenital anomaly/birth defect; or requires or prolongs hospitalization. Medical Dictionary for Regulatory Activities (MedDRA) version 16.0 was used. (NCT00423891)
Timeframe: Day 1 to Week 120

,,
Interventionparticipants (Number)
Serious Adverse Events (n=24, 19, 5)Discontinuations Due to AEs (n=24,19,5)
Lamivudine (LVD)-Experienced (Group B)00
Lamivudine (LVD)-Naive (Group A)20
Nucleoside/Tide Analog (NA) - Experienced (Group C)00

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Number of Participants With Hepatitis B s Antigen (HBsAg) Loss Through Week 96 in Treated Participants

HBsAg loss: HBsAg negative. The method used for detection of HBsAg was the ADVIA Centaur iImmunoassay system. Baseline was the last value measured prior to or on the date of the first dose of study therapy. (NCT00423891)
Timeframe: Baseline to Week 96

,,
Interventionparticipants (Number)
BaselineWeek 12Week 24Week 36Week 48Week 96
Lamivudine (LVD)-Experienced (Group B)000000
Lamivudine (LVD)-Naive (Group A)000110
Nucleoside/Tide Analog (NA) - Experienced (Group C)000000

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Number of Participants With Hepatitis B e Antigen Seroconversion Through Week 96 in Treated Participants

HBe seroconversion: loss of HBeAg (HBeAg negative) with positive HB e antibodies (HBeAb), ie both the presence of HBeAb and the absence of HBeAg. The method used for the detection HBeAg seroconversion was the DiaSorin - Anti HBe enzyme immunoassay kit. Baseline was the last value measured prior to or on the date of the first dose of study therapy. (NCT00423891)
Timeframe: Baseline through Week 96

,,
Interventionparticipants (Number)
BaselineWeek 12Week 24Week 36Week 48Week 96
Lamivudine (LVD)-Experienced (Group B)001131
Lamivudine (LVD)-Naive (Group A)0345105
Nucleoside/Tide Analog (NA) - Experienced (Group C)000000

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Number of Participants With Hepatitis B e Antigen (HBeAg) Loss Through Week 96 in Treated Participants

HBeAg loss: HBeAg negative. The method used for the detection of HBe Ag was the DiaSorin - Anti HBe enzyme immunoassay kit. Baseline was the last value measured prior to or on the date of the first dose of study therapy. (NCT00423891)
Timeframe: Baseline to Week 96

,,
Interventionparticipants (Number)
BaselineWeek 12Week 24Week 36Week 48Week 96
Lamivudine (LVD)-Experienced (Group B)001132
Lamivudine (LVD)-Naive (Group A)0345105
Nucleoside/Tide Analog (NA) - Experienced (Group C)000000

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Number of Participants With Hematology Laboratory Abnormalities (Grades 1 - 4) - On Treatment - Treated Participants

Toxicity Scale: Division of AIDs (DAIDS) grades Version 1.0. Upper limit of normal (ULN); lower limit of normal (LLN); Cells per Liter (c/L); cells per microliter (c/µL); grams per deciliter (g/dL); milliequivalents per liter (mEq/L); cells per microliter (c/µL): Grade (Gr). Hemoglobin g/dL: Gr1:10.0-10.9;Gr2: 9.0-9.9; Gr3:7.0-8.9; Gr4: <7.0. International normalization ratio (INR): Gr1:1.1-<1.5*ULN; Gr2: 1.6-<2.0*ULN; Gr3: 2.1-3.0*ULN;Gr4: >3.0*ULN. Neutrophils/bands c/µL: Gr1;1.0-1.3*10^3; Gr2: 0.75-0.99*10^3; Gr 3: 0.50-0.749*10^3; Gr4: <0.5*10^3. (NCT00423891)
Timeframe: Day 1 to Week 120

,,
Interventionparticipants (Number)
HemoglobinInternational normalization ratioNeutrophils (absolute) + bands
Lamivudine (LVD)-Experienced (Group B)033
Lamivudine (LVD)-Naive (Group A)143
Nucleoside/Tide Analog (NA) - Experienced (Group C)100

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Number of Participants With Adverse Events (AEs), Serious Adverse Events (SAEs), and Discontinuations Due to AEs or Laboratory Abnormalities

AE=any new untoward medical occurrence or worsening of a pre-existing medical condition which does not necessarily have a causal relationship with this treatment. Related AE=relationship of certain, probable, possible, or missing. SAE=any untoward medical occurrence that at any dose: results in death, is life-threatening, requires inpatient hospitalization or causes prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect, and/or is an important medical event. (NCT00605384)
Timeframe: Day 1 through end of treatment (Week 100 +/- 5 days)

,
Interventionparticipants (Number)
AEsSAEsDeathsDiscontinuations due to AEsDiscontinuations due to Laboratory Abnormalities
Adefovir + Continuing Lamivudine10000
Entecavir + Tenofovir10000

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Incidence of Permanent Discontinuation Due to Toxicity

(NCT00662545)
Timeframe: 24 weeks

Interventionparticipants (Number)
Entecavir Intensification0
Standard of Care0

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Incidence of New Hepatic Decompensation( Ascites, Variceal Hemorrhage, Encephalopathy)

(NCT00662545)
Timeframe: every 4 weeks for 24 weeks

Interventionparticipants (Number)
Entecavir Intensification0
Standard of Care0

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Incidence of ALT Flares

ALT flare: sudden increase in blood level of alanine transaminase (ALT) (NCT00662545)
Timeframe: every 4 weeks for 24 weeks

Interventionparticipants (Number)
Entecavir Intensification0
Standard of Care0

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HIV RNA < 75 Copies/ml

(NCT00662545)
Timeframe: entry, week 12, and week 24

Interventionparticipants (Number)
Entecavir Intensification5
Standard of Care5

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Hepatitis B Virus (HBV) DNA

"HBV DNA carries the genetic blueprint of the virus. How many HBV DNA particles or copies are found in the blood indicates how rapidly the virus is reproducing in the liver." (NCT00662545)
Timeframe: week 24

Interventionlog 10 IU/ml (Median)
Entecavir Intensification2.4
Standard of Care0.8

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Mean log10 Reduction From Baseline in Serum HBV DNA Level by Polymerase Chain Reaction Testing

HBV=hepatitis B virus (NCT00718887)
Timeframe: At Weeks 12 and 48 from Day 1

,
Interventionlog10 IU/mL (Mean)
Week 12 (n=88, 77)Week 48 (n=87, 71)
Adefovir, 10 mg QD/Entecavir, 0.5 mg QD-0.2-3.2
Entecavir, 0.5 mg QD-2.5-3.3

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Percentage of Participants With Loss of Hepatitis B e Antigen (HBeAg) and Hepatitis B e (HBe) Seroconversion

(NCT00718887)
Timeframe: At Weeks 12 and 48 from Day 1

,
InterventionPercentage of participants (Number)
HBeAG loss Week 12 (n=79, 72)HBeAG loss Week 48 (n=79, 72)HBe seroconversion Week 12 (n=79, 72)HBe seroconversion Week 48 (n=79, 72)
Adefovir, 10 mg QD/Entecavir, 10 mg QD6.96.91.452.8
Entecavir, 0.5 mg QD3.87.62.53.8

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Percentage of Participants With Grade 3 or 4 Abnormalities in Laboratory Test Results

Hematology testing assessed levels of hemoglobin, white blood cells, platelets, neutrophils, international normalized ration, red blood cells, lymphocytes, and monocytes. (NCT00718887)
Timeframe: Day 1 through Week 48

,
InterventionPercentage of participants (Number)
Alanine aminotransferaseAspartate aminotransferaseHyperkalemiaHematology
Adefovir, 10 mg QD5.2010
Entecavir, 0.5 mg QD92.200

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Percentage of Participants Who Achieved Normalization of Alanine Aminotransferase (ALT)

ULN=upper limit of normal. ALT normalization= ≤1*ULN, among participants with baseline ALT >1*ULN (NCT00718887)
Timeframe: At Weeks 12 and 48 from Day 1

,
InterventionPercentage of participants (Number)
Week 12 (n=51, 36)Week 48 (n=51, 36)
Adeforvi, 10 mg QD/Entecavir, 0.5 mg QD22.247.2
Entecavir, 0.5 mg QD31.460.8

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Number of Participants With Hepatitis B s Surface Antibody (HBsAG) Loss and HBsAG Seroconversion

(NCT00718887)
Timeframe: At Weeks 12 and 48 from Day 1

,
InterventionParticipants (Number)
Week 12 HBsAg lossWeek 48 HBsAg lossWeek 12 HBsAg seroconversionWeek 48 HBsAg seroconversion
Adefovir, 10 mg QD/Entecavir, 0.5 mg QD0000
Entecavir, 0.5 mg QD0000

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Number of Participants With Genotypic Resistance to Entecavir

(NCT00718887)
Timeframe: At Week 48 from Day 1

,
InterventionParticipants (Number)
At baselineWeek 48
Adefovir, 10 mg QD/Entecavir, 0.5 mg QD00
Entecavir, 0.5 mg QD00

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Percentage of Participants Who Achieved an HBV DNA Level <50 IU/mL at Week 48 by Polymerase Chain Reaction Testing

HBV=hepatitis B virus. HBV DNA Level <50 IU/mL=approximately 300 copies/mL. (NCT00718887)
Timeframe: At Week 48 from Day 1

InterventionPercentage of participants (Number)
Entecavir, 0.5 mg QD31.5
Adefovir, 10 mg QD/Entecavir, 0.5 mg QD28.6

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Percentage of Participants Who Achieved a Hepatitis B Virus (HBV) DNA Level <50 IU/mL at Week 12 by Polymerase Chain Reaction Testing

HBV DNA Level <50 IU/mL=approximately 300 copies/mL. (NCT00718887)
Timeframe: At Week 12 from Day 1

InterventionPercentage of participants (Number)
Entecavir, 0.5 mg QD5.6
Adefovir, 10 mg QD0.0

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Percentage of Participants Who Were HBeAg Negative

(NCT00922207)
Timeframe: Baseline, Weeks 4, 8, 16, 28, 40, 52, 64, 76, 88, and 100

,,
Interventionpercentage of participants (Number)
Baseline (n=91,95,94)Week 4 (n=90,94,92)Week 8 (n=90,94,92)Week 16 (n=90,94,92)Week 28 (n=90,94,92)Week 40 (n=90,94,92)Week 52 (n=90,94,92)Week 64 (n=90,92,92)Week 76 (n=88,88,92)Week 88 (n=86,87,90)Week 100 (n=84,87,91)
Peg-IFN-Alfa-2a + Adefovir3.35.66.76.711.118.922.224.425.027.928.6
Peg-IFN-Alfa-2a + Entecavir2.14.36.48.510.618.122.325.028.427.632.2
Peg-IFN-Alfa-2a + Placebo0.01.14.310.916.322.829.331.537.034.437.4

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Percentage of Participants With Combined Response

Combined response was defined as having negative HBeAg, HBV DNA less than (<) 100,000 copies/mL, and normal ALT level (10-40 IU/L). (NCT00922207)
Timeframe: Baseline, Weeks 4, 8, 16, 28, 40, 52, 64, 76, 88, and 100

,,
Interventionpercentage of participants (Number)
Baseline (n=91,95,94)Week 16 (n=90,93,92)Week 28 (n=90,93,92)Week 40 (n=90,93,92)Week 52 (n=90,93,92)Week 64 (n=90,92,92)Week 76 (n=88,89,92)Week 88 (n=86,88,91)Week 100 (n=84,88,91)
Peg-IFN-Alfa-2a + Adefovir0.00.00.00.00.02.23.43.52.4
Peg-IFN-Alfa-2a + Entecavir0.00.01.10.00.00.00.00.00.0
Peg-IFN-Alfa-2a + Placebo0.00.00.00.00.00.00.00.00.0

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Percentage of Participant Who Were Both Hepatitis B Surface Antigen (HBsAg) Negative and Hepatitis B Surface Antibody (Anti-HBs/HBsAb) Positive

(NCT00922207)
Timeframe: Baseline, Weeks 4, 8, 16, 28, 40, 52, 64, 76, 88, and 100

,,
Interventionpercentage of participants (Number)
Baseline (n=91,95,94)Week 4 (n=90,94,92)Week 8 (n=90,94,92)Week 16 (n=90,94,92)Week 28 (n=90,94,92)Week 40 (n=90,94,92)Week 52 (n=90,94,92)Week 64 (n=90,92,92)Week 76 (n=88,88,92)Week 88 (n=86,87,90)Week 100 (n=84,87,91)
Peg-IFN-Alfa-2a + Adefovir0.00.00.00.00.00.00.00.00.01.20.0
Peg-IFN-Alfa-2a + Entecavir0.00.00.00.00.00.00.00.00.00.00.0
Peg-IFN-Alfa-2a + Placebo0.00.00.00.00.00.00.00.00.03.40.0

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Percentage of Participant With Normal Alanine Aminotransferase (ALT) Levels

The normal range for ALT is 10 to 40 international units per liter (IU/L). (NCT00922207)
Timeframe: Baseline, Weeks 6, 12, 16, 22, 28, 34, 40, 46, 52, 64, 76, 88, and 100

,,
Interventionpercentage of participants (Number)
Baseline (n=91,95,94)Week 6 (n=90,93,92)Week 12 (n=90,93,92)Week 16 (n=90,93,92)Week 22 (n=90,93,92)Week 28 (n=90,93,92)Week 34 (n=90,93,92)Week 40 (n=90,93,92)Week 46 (n=90,93,92)Week 52 (n=90,93,92)Week 64 (n=90,92,92)Week 76 (n=89,89,92)Week 88 (n=86,88,91)Week 100 (n=84,88,91)
Peg-IFN-Alfa-2a + Adefovir4.44.415.621.125.626.726.730.030.033.332.243.832.636.9
Peg-IFN-Alfa-2a + Entecavir3.25.417.224.734.430.134.439.841.934.437.038.233.040.9
Peg-IFN-Alfa-2a + Placebo2.16.513.020.722.823.932.632.633.732.642.446.748.449.5

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Change From Baseline in Hepatitis B Virus Deoxyribonucleic Acid (HBV DNA) Levels at Weeks 4, 8, 16, 28, 40, 52, 64, 76, 88, and 100

HBV DNA (copies per milliliter [copies/mL]) represented the viral load for Hepatitis B Virus (HBV), and was considered an indicator of viral replication. (NCT00922207)
Timeframe: Baseline, Weeks 4, 8, 16, 28, 40, 52, 64, 76, 88, and 100

,,
Interventioncopies/mL (Mean)
Baseline (n=91,95,94)Change at Week 4 (n=90,94,92)Change at Week 8 (n=90,94,92)Change at Week 16 (n=90,94,92)Change at Week 28 (n=90,94,92)Change at Week 40 (n=90,94,92)Change at Week 52 (n=90,94,92)Change at Week 64 (n=90,94,92)Change at Week 76 (n=90,94,92)Change at Week 88 (n=90,94,92)Change at Week 100 (n=90,94,92)
Peg-IFN-Alfa-2a + Adefovir8.65-2.15-1.87-2.14-2.34-2.61-2.75-1.87-1.91-1.78-2.00
Peg-IFN-Alfa-2a + Entecavir8.30-2.76-3.58-3.77-3.07-2.97-2.81-1.37-1.39-1.39-1.78
Peg-IFN-Alfa-2a + Placebo8.41-0.23-1.32-2.13-2.84-3.27-3.32-2.11-2.20-2.30-2.17

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Percentage of Participants With Hepatitis B e-Antigen (HBeAg) Seroconversion at 100 Weeks After Start of Treatment

HBeAg seroconversion was defined as the absence of HBeAg (a negative result for HBeAg) and the presence of hepatitis B e-antibody (anti-HBe/HBeAb) (a positive result for anti-HBe). (NCT00922207)
Timeframe: Week 100

Interventionpercentage of participants (Number)
Peg-IFN-Alfa-2a + Adefovir27.4
Peg-IFN-Alfa-2a + Entecavir29.5
Peg-IFN-Alfa-2a + Placebo36.3

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Change From Baseline in HBsAg Levels at Weeks 4, 8, 16, 28, 40, 52, 64, 76, 88, and 100

(NCT00922207)
Timeframe: Baseline, Weeks 4, 8, 16, 28, 40, 52, 64, 76, 88, and 100

,,
InterventionInternational Units/milliliter (IU/mL) (Mean)
Baseline (n=91,95,94)Change at Week 4 (n=90,94,92)Change at Week 8 (n=90,94,92)Change at Week 16 (n=90,94,92)Change at Week 28 (n=90,94,92)Change at Week 40 (n=90,94,92)Change at Week 52 (n=90,94,92)Change at Week 64 (n=90,94,92)Change at Week 76 (n=90,94,92)Change at Week 88 (n=90,94,92)Change at Week 100 (n=90,94,92)
Peg-IFN-Alfa-2a + Adefovir3.97-0.26-0.33-0.40-0.61-0.71-0.78-0.67-0.58-0.50-0.41
Peg-IFN-Alfa-2a + Entecavir3.76-0.18-0.31-0.49-0.68-0.67-0.69-0.54-0.45-0.44-0.60
Peg-IFN-Alfa-2a + Placebo3.84-0.02-0.25-0.48-0.70-0.82-0.88-0.67-0.53-0.62-0.56

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Percentage of Participants With Hepatitis B Virus - Deoxyribonucleic Acid <1000 Copies/ Millilitre at Week 48

Blood was collected for Hepatitis B Virus - Deoxyribonucleic Acid (HBV -DNA) and was analysed at the central laboratories using the Roche approved polymerase chain reaction (PCR) methodology at Week 48. Percentage of participants with HBV-DNA < 1000 copies/mL was reported. (NCT00940485)
Timeframe: At Week 48

InterventionPercentage of participants (Number)
Peginterferon Alfa-2a + Entecavir62.77
Entecavir91.84

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Percentage of Participants With Loss of Hepatitis B Envelope Antigen at Week 48

Loss of Hepatitis B Envelope Antigen (HBeAg) is defined as the absence of HBeAg. (NCT00940485)
Timeframe: At Week 48

InterventionPercentage of participants (Number)
Peginterferon Alfa-2a + Entecavir62.77
Entecavir60.20

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Quantitative Change in Mean Hepatitis B Envelope Antigen Over Time

Quantitative hepatitis B envelope antigen (HBeAg) results were analyzed in central lab. Values that were less than lower limit of quantification (LLOQ) had been replaced by LLOQ when analyzed, e.g. <1000 was replaced by 1000 and <0.2 was replaced by 0.2. Quantitative HBeAg value unit was calculated using 'Paul Ehrlich Institute units per millilitre' (PEIU/ml). Change in HBeAg was analysed at Weeks 0, 8, 12, 24, 36, and 48. (NCT00940485)
Timeframe: Up to Week 48

,
InterventionPEIU/ml) (Mean)
At Week 0; n= 93, 95At Week 8; n= 93, 97At Week 12; n= 94, 97At Week 24; n= 91, 97At Week 36; n= 88, 94At Week 48; n= 85, 92
Entecavir5.665.855.004.764.524.07
Peginterferon Alfa-2a + Entecavir8.334.763.832.283.5813.23

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Quantitative Change in Mean Hepatitis B Surface Antigen Change Over Time

Quantitative Hepatitis B Surface Antigen (HBsAg) results were analyzed in central lab. Values that were less than LLOQ had been replaced by LLOQ when analyzed, e.g. <1000 was replaced by 1000 and <0.2 was replaced by 0.2. Quantitative HBsAg calculated using 'International Units Per Millilitre' (IU/mL). Change in HBsAg was analysed at Weeks 0, 8, 12, 24, 36, and 48. (NCT00940485)
Timeframe: Up to Week 48

,
InterventionIU/ml (Mean)
At Week 0; n= 93, 95At Week 8; n= 93, 97At Week 12; n= 94, 97At Week 24; n= 91, 97At Week 36; n= 88, 94At Week 48; n= 85, 92
Entecavir3241.063050.793037.822895.252699.182672.71
Peginterferon Alfa-2a + Entecavir3737.843603.563041.862280.602097.891886.02

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Number of Participants With Laboratory Abnormalities Which Were Captured as an Adverse Event

Participants with clinically significant laboratory abnormalities which were captured as an AE (at the >=5% threshold) were presented. (NCT00940485)
Timeframe: Up to Week 48

,
InterventionParticipants (Number)
Haemoglobin decreasedAspartate aminotransferase increasedAlanine aminotransferase increasedPlatelet count decreasedNeutrophil count decreasedWhite blood cell count decreased
Entecavir000000
Peginterferon Alfa-2a + Entecavir689425359

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Percentage of Participants With Normalized Alanine Aminotransferase at Week 48

Normalized Alanine Aminotransferase (ALT) is defined as having a baseline ALT value > upper limit of normal (ULN), and a decrease in ALT value to ≤ ULN at the given time point. (NCT00940485)
Timeframe: At Week 48

InterventionPercentage of participants (Number)
Peginterferon Alfa-2a + Entecavir51.06
Entecavir85.71

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Number of Participants With Incidence of Adverse Events and Serious Adverse Events

An adverse event (AE) was defined as any untoward medical occurrence that occurred during the course of the trial after study treatment had started. An adverse event was therefore any unfavourable and unintended sign, symptom, or disease temporally associated with the use of study drug, whether or not considered related to the study drug. A Serious Adverse Events (SAE) is any untoward medical occurrence that at any dose results in death, are life threatening, requires hospitalization or prolongation of hospitalization or results in disability/incapacity, and congenital anomaly/birth defect. (NCT00940485)
Timeframe: Up to Week 48

,
InterventionParticipants (Number)
Non serious AESerious AEAE
Entecavir505
Peginterferon Alfa-2a + Entecavir65667

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Percentage of Participants With Hepatitis B Envelope Antigen Seroconversion at Week 48

Hepatitis B envelope Antigen (HBeAg) seroconversion was defined as the absence of HBeAg and the presence of antibody to Hepatitis B envelope antigen (anti-HBe). (NCT00940485)
Timeframe: At Week 48

InterventionPercentage of participants (Number)
Peginterferon Alfa-2a + Entecavir14.89
Entecavir6.12

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Percentage of Participants With Hepatitis B Surface Antigen Loss at Week 48

Loss of Hepatitis B Surface Antigen (HBsAg) was defined as change of detectable HBsAg from positive to negative. (NCT00940485)
Timeframe: At Week 48

InterventionPercentage of participants (Number)
Peginterferon Alfa-2a + Entecavir8.51
Entecavir0

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Percentage of Participants With Hepatitis B Surface Antigen Seroconversion at Week 48

Hepatitis B Surface Antigen (HBsAg) seroconversion was defined as loss of HBsAg and presence of anti-HBs .(antibody to Hepatitis B surface antigen) (NCT00940485)
Timeframe: At Week 48

InterventionPercentage of participants (Number)
Peginterferon Alfa-2a + Entecavir4.26
Entecavir0

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Complete Virologic Response (CVR, Serum HBV DNA Undetectable by PCR or Less Than 60 IU/mL)

(NCT01023217)
Timeframe: at week 52 from randomization

Interventionparticipants (Number)
Adefovir Plus Entecavir13
Adefovir Plus Lamivudine2

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Percentage of Participants With Hepatitis B Surface Antigen (HBsAg) Seroconversion at Weeks 24, 48, and 96 - Treated Population Who Were HBsAg-Positive at Baseline

HBsAg seroconversion was defined as being both HBsAg-negative and HBsAb-positive at Weeks 24, 48, and 96 in those participants who had been HBsAg-positive at baseline. Percentage was calculated as number of participants with HBs seroconversion at Weeks 24 and 48 divided by the number of treated participants who were HBsAg-positive at baseline. Positive result for HBsAg was one of the inclusion criteria. Treated participants (HBsAg positive at baseline) were evaluated using NC=F. The method used was an Immunoassay testing - ADVIA CENTAUR from SIEMENS: in vitro diagnostic immunoassay for the qualitative and quantitative determination of HBsAg in human serum and plasma [potassium ethylenediaminetetraacetic acid (EDTA), lithium or sodium heparinized]. Baseline was Day 1, before start of study drug. (NCT01063036)
Timeframe: Baseline, Weeks 24, 48, and 96

Interventionpercentage of participants (Number)
Week 24 (n=92)Week 48 (n=92)Week 96 (n=92)
Entecavir + Tenofovir1.101.1

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Percentage of Participants With Hepatitis B Surface Antigen (HBsAg) Loss at Weeks 24, 48, 96 - Treated Population Who Were HBsAg-Positive at Baseline

Loss of HBsAg was defined as being HBsAg-negative at Weeks 24, 48, 96 in those participants who had been HBsAg-positive at baseline. The method used: Immunoassay - ADVIA CENTAUR from SIEMENS: in vitro diagnostic immunoassay for the qualitative and quantitative determination of HBsAg in human serum and plasma (potassium ethylene diamine tetraacetic acid, lithium or sodium heparinized). Percentage calculated as number of participants with a HBsAg loss at Weeks 24, 48, and 96 divided by the number of treated participants who were HBsAg-positive at baseline (participants were not enrolled into the study unless they were positive for HBsAg). Treated participants (HBsAg-positive at baseline) were evaluated using NC=F. Baseline was Day 1, before start of study drug. (NCT01063036)
Timeframe: Baseline, Weeks 24, 48, 96

Interventionpercentage of participants (Number)
Week 24 (n=92)Week 48 (n=92)Week 96 (n=92)
Entecavir + Tenofovir1.102.2

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Percentage of Participants With Hepatitis B e Antigen (HBeAg) Loss at Weeks 24, 48, and 96 - Treated Population Who Were HBeAg Positive at Baseline

Loss of HBeAg was defined as being HBeAg-negative at Weeks 24, 48, and 96 in those participants who had been HBeAg-positive at baseline. Method used for HBeAg was DiaSorin - Anti HBe enzyme immunoassay kit - procedure for qualitative determination of antibodies to HBeAg in human serum or plasma samples. Percentage was calculated as number of participants with HBeAg loss at Weeks 24 and 48 divided by the number of treated participants who were HBeAg-positive at baseline. Treated participants (HBeAg-positive at baseline) were evaluated using NC = F. Baseline was Day 1, before start of study drug. (NCT01063036)
Timeframe: Baseline to Weeks 24, 48, and 96

Interventionpercentage of participants (Number)
Week 24 (n=56)Week 48 (n=56)Week 96 (n=56)
Entecavir + Tenofovir3.65.48.9

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Percentage of Participants With HBV DNA Less Than the Lower Limit of Detection (LLD) at Weeks 24, 48, and 96 - Treated Population

HBV DNA less than (<) LLD (6 IU/mL) was defined/measured by the COBAS(REGISTERED) TaqMan HPS assay at Weeks 24, 48, and 96. Percentage was calculated as number of participants with HBV DNA < LLD at Weeks 24, 48, 96 divided by the number of treated participants. Treated participants were evaluated using non-completer (NC) = failure (F). (NCT01063036)
Timeframe: Weeks 24, 48, 96

Interventionpercentage of participants (Number)
Week 24 (n=92)Week 48 (n=92)Week 96 (n=92)
Entecavir + Tenofovir12.018.516.3

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Percentage of Participants With a Virologic Response at Week 24 and at Week 96 - Treated Population

Virologic response was defined as Hepatitis B virus (HBV) Deoxyribonucleic acid (DNA) less than 50 international units per milliliter (IU/mL); approximately 300 copies/mL. Percentage was calculated as number of participants with virologic response at Week 24, Week 96 divided by the number of treated participants. Treated participants were evaluated using non-completer (NC) = failure (F). The HBV DNA by polymerase chain reaction (PCR) was measured using the Roche COBAS(REGISTERED) TaqMan - High Pure System (HPS) assay. The results were reported in IU/mL, with the limit of quantification (LOQ) = 29 IU/mL and lower limit of detection (LLD) = 6 IU/mL. HBV DNA measurements were transformed by the log10 scale when analyzed as a continuous variable, using log10(LOQ-1) for values below LOQ. (NCT01063036)
Timeframe: Week 24, Week 96

Interventionpercentage of participants (Number)
Week 24 (n=92)Week 96 (n=92)
Entecavir + Tenofovir64.184.8

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Number of Participants With Treatment Emergent Serious Adverse Events (SAEs) on Treatment, and Discontinuation of Study Drug Due to Adverse Events (AE) - Treated Population

AE=any new unfavorable symptom, sign, or disease or worsening of a preexisting condition that may not have a causal relationship with treatment. SAE=a medical event that at any dose results in death, persistent or significant disability/incapacity, or drug dependency/abuse; is life-threatening, an important medical event, or a congenital anomaly/birth defect; or requires or prolongs hospitalization. Treatment-related=having certain, probable, possible, or missing relationship to study drug. Grade (Gr) 1=Mild, Gr 2=Moderate, Gr 3=Severe, Gr 4=Life-threatening or disabling, Gr 5=Death. On-treatment = on Day 1 through last dose of study therapy + 5 days. (NCT01063036)
Timeframe: Day 1 to last dose of study drug plus 5 days; up to Week 96

Interventionparticipants (Number)
Treatment emergent SAEDiscontinuation of treatment due to AE
Entecavir + Tenofovir61

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Number of Participants With Emergence of Genotypic Resistance to Study Drugs at Weeks 48 and 96- Treated Population

Testing of HBV genotype was performed at baseline for all treated patients and for participants at Weeks 48 and 96 with primary non-response or virologic breakthrough. Emergent genotypic resistance to study drugs was defined as follows: Emergent = not detected at baseline; entecavir (ETV) resistance (ETVr): participant's sample was to have rtM204V/I/S and any substitution at rtT184, rtS202, or rtM250; tenofovir (TDF) resistance (TDFr) which was based on adefovir (ADV)-mutations: participant's sample was to have rtA181T/V, rtN236T, or (rtA194T and rtM204V/I/S). Primary non-response was defined as < 1 log10 decrease in HBV DNA from baseline on treatment at or after Week 12. Virologic breakthrough was defined as ≥ 1 log10 increase in HBV DNA over nadir on treatment, either confirmed or last on-treatment followed by discontinuation of study therapy. (NCT01063036)
Timeframe: Baseline to Weeks 48, 96

Interventionparticipants (Number)
Week 48 (n=5)Week 96 (n=7)
Entecavir + Tenofovir00

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Percentage of Participants With HBe Seroconversion at Weeks 24, 48, and 96 - Treated Population Who Were HBeAg-positive at Baseline

HBe seroconversion was defined as being both HBeAg-negative and HBeAb-positive at Weeks 24, 48, and 96 in those participants who had been HBeAg-positive at baseline. Method used was DiaSorin - Anti HBe enzyme immunoassay kit - procedure for qualitative determination of antibodies to HBeAg in human serum or plasma samples. Percentage was calculated as number of participants with HBe seroconversion at Weeks 24, 48, and 96 divided by the number of treated participants who were HBeAg-positive at baseline. Treated participants (HBeAg-positive at baseline) were evaluated using NC = F. Baseline was Day 1, before start of study drug. (NCT01063036)
Timeframe: Baseline, Weeks 24, 48, and 96

Interventionpercentage of participants (Number)
Week 24 (n=56)Week 48 (n=56)Week 96 (n=56)
Entecavir + Tenofovir3.63.61.8

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Percentage of Participants With a Virologic Response at Week 48 - Treated Population

Virologic response was defined as Hepatitis B virus (HBV) Deoxyribonucleic acid (DNA) less than 50 international units per milliliter (IU/mL); approximately 300 copies/mL. Percentage was calculated as number of participants with virologic response at Week 48 divided by the number of treated participants. Treated participants were evaluated using non-completer (NC) = failure (F). The HBV DNA by polymerase chain reaction (PCR) was measured using the Roche COBAS(REGISTERED) TaqMan - High Pure System (HPS) assay, in a central laboratory. The results were reported in IU/mL, with the limit of quantification (LOQ) = 29 IU/mL and lower limit of detection (LLD) = 6 IU/mL. HBV DNA measurements were transformed by the log10 scale when analyzed as a continuous variable, using log10(LOQ-1) for values below LOQ. (NCT01063036)
Timeframe: Week 48

Interventionpercentage of participants (Number)
Entecavir + Tenofovir76.1

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Change From Baseline in Mean log10 HBV DNA at Weeks 12, 24, 48, and 96 - Treated Evaluable Population

HBV DNA by polymerase chain reaction (PCR) was measured using the Roche COBAS(REGISTERED) TaqMan - High Pure System (HPS) assay. The results were reported in log 10 IU/mL, with the limit of quantification (LOQ) = 29 IU/mL and lower limit of detection (LLD) = 6 IU/mL. HBV DNA measurements were transformed by the log10 scale when analyzed as a continuous variable, using log10(LOQ-1) for values below LOQ. Baseline was Day 1, prior to study drug administration. (NCT01063036)
Timeframe: Baseline to Weeks 12, 24, 48, 96

Interventionlog10 IU/mL (Mean)
Week 12 (n=89)Week 24 (n=89)Week 48 (n=88)Week 96 (n=84)
Entecavir + Tenofovir-2.230-2.581-2.829-2.965

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Number of Participants on Treatment With Study Drug With Laboratory Test Abnormalities Meeting Selected Criteria on Treatment - Treated Population

Selected criteria presented in each category. Upper limit of normal among all laboratory ranges (ULN); Baseline (BL); alanine transaminase (ALT); milligram per deciliter (mg/dL); milliliters per minute (mL/min); greater than (>);greater than, equal to (>=); less than (<). Creatinine data presented below were confirmed, ie, at least 2 consecutive values. On-treatment = after Day 1 through last dose of study therapy + 5 days. (NCT01063036)
Timeframe: Day 1 to last dose of study drug plus 5 days; up to Week 96

Interventionparticipants (Number)
ALT > 2*Baseline(N=90)ALT > 3*Baseline(N=90)Total bilirubin >2*Baseline (N=90)Total bilirubin >3*Baseline (N=90)Lipase > 3*Baseline (N=90)Creatinine increase from BL >= 20%(N=91)Creatinine >1.5 mg/dL (N=91)Creatinine clearance < 50 mL/min (N=91)Phosphate < 2.0 mg/dL (N=90)Phosphate < 2.3 mg/dL (N=90)
Entecavir + Tenofovir92113442128

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Percentage of Participants Who Achieved a Combination of Hepatitis B Virus (HBV) DNA Suppression and Hepatitis B e Antigen (HBeAg) Seroconversion at Week 48

Suppression=HBV DNA<50 IU/mL (approximately 300 copies/mL) using the Roche COBAS TaqMan HBV Test for use with the High Pure System assay; seroconversion=undetectable HBeAg and detectable anti-hepatitis B e antibodies. While the analysis of the primary endpoint was based on a randomized sample size of 123 participants (the Primary Cohort), the size of the overall study population was augmented to 180 randomized participants to meet global regulatory requirements. (NCT01079806)
Timeframe: At Week 48

InterventionPercentage of participants (Number)
Entecavir24.4
Placebo2.4

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Histological Analysis (Percentage) Among Participants With Available Liver Biopsy Data

Liver function test elevations and abnormalities on blinded and open-label ETV (the All ETV Safety Cohort). Participants who experienced elevation of alanine aminotransferase (ALT) greater than three times ETV (entecavir) baseline measure (Participants who displayed liver biopsy with ALT value greater than three times baseline.) (NCT01079806)
Timeframe: Between weeks 48 and 96

InterventionPercentage of participants (Number)
Blinded and Open-Label (All ETV)5.9

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Percentage of Participants With HBeAg Seroconversion (Undetectable HBeAg and Presence of Anti-HBeAb) up to Week 96

On Treatment through week 96 - 2 year cohort NC = F: (The numerator was based on participants meeting the response criteria. The denominator was based on treated participants. Participants who had missing data at the analysis week were considered failures.) (NCT01079806)
Timeframe: up to week 96

InterventionPercentage of participants (Number)
Entecavir40.8

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Percentage of Participants With HBeAg Seroconversion on ETV Over-time at Week 96 (All ETV Cohort)

HBe seroconversion=undetectable HBe antigen and detectable anti-HBe antibodies. While the analysis of the primary endpoint was based on a randomized sample size of 123 participants (the Primary Cohort), the size of the overall study population was augmented to 180 randomized participants to meet global regulatory requirements. (NCT01079806)
Timeframe: At Week 96

InterventionPercentage of participants (Number)
Blinded and Open-Label (All ETV)38.6

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Percentage of Participants With Hepatitis B e Antigen (HBeAg) Seroconversion at Week 48 (Undetectable HBeAg and Presence of Anti-HBeAb)

Percentage of participants in the primary cohort with HBeAg seroconversion (undetectable HBeAg and presence of anti-HBe antibodies) at week 48 (NCT01079806)
Timeframe: At Week 48

InterventionPercentage of participants (Number)
Entecavir24.4
Placebo12.2

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Percentage of Participants With Hepatitis B Virus (HBV) DNA <50 IU/mL at Week 48

While the analysis of the primary endpoint was based on a randomized sample size of 123 participants (the Primary Cohort), the size of the overall study population was augmented to 180 randomized participants to meet global regulatory requirements. (NCT01079806)
Timeframe: At Week 48

InterventionPercentage of participants (Number)
Entecavir46.3
Placebo2.4

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Percentage of Participants With Hepatitis B Virus DNA

LOQ=29 IU/mL. While the analysis of the primary endpoint was based on a randomized sample size of 123 participants (the Primary Cohort), the size of the overall study population was augmented to 180 randomized participants to meet global regulatory requirements. (NCT01079806)
Timeframe: At Week 48

InterventionPercentage of participants (Number)
Entecavir42.7
Placebo2.4

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Percentage of Participants With Serum Alanine Aminotransferase ≤1*Upper Limit of Normal at Week 48

While the analysis of the primary endpoint was based on a randomized sample size of 123 participants (the Primary Cohort), the size of the overall study population was augmented to 180 randomized participants to meet global regulatory requirements. (NCT01079806)
Timeframe: At Week 48

InterventionPercentage of participants (Number)
Entecavir67.1
Placebo22.0

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Number of Participants With Adverse Events (Including Palatability Issues), SAEs, Discontinuous Due to Adverse Events, and HBV Disease Progression Through Week 48

AE=any new unfavorable symptom, sign, or disease or worsening of a preexisting condition that may not have a causal relationship with treatment. SAE=a medical event that at any dose results in death, persistent or significant disability/incapacity, or drug dependency/abuse; is life-threatening, an important medical event, or a congenital anomaly/birth defect; or requires or prolongs hospitalization. Related=having certain, probable, possible, or unknown relationship to study drug. Grade 1=Mild, Grade 2=Moderate, Grade 3=Severe, Grade 4=Life-threatening or disabling, Grade 5=Death. ALT=alanine aminotransferase. (NCT01079806)
Timeframe: Day 1 through Week 48 on blinded therapy

,
Interventionparticipants (Number)
DeathsSerious Adverse EventsDiscontinuation due to Adverse Eventany adverse eventRelated Adverse EventsRelated Grade 2 - 4 Adverse EventsGrade 3 - 4 Adverse EventsALT FlaresHBV disease progressionMalignant neoplasms or pre-malignant lesions
Entecavir040781144200
Placebo07246623500

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Number of Participants With Laboratory Test Results Meeting the Criteria for Abnormality (Grades 1-4)

Toxicities graded per Division of AIDS criteria, Version 1.0, and modified World Health Organization criteria. INR=international normalization ratio of prothrombin time; ULN=upper limit of normal. Hemoglobin (g/dL): Grade 1=10-10.9; Grade 2=9-9.9; Grade 3=7-8.9; Grade 4= <7. Platelets (/mm^3): Grade 1=100,000-124,999; Grade 2=50,000-99,999; Grade 3=25,000-49,999; Grade 4= <25,000. INR (*ULN): Grade 1=1.1-1.5; Grade 2=1.6-2; Grade 3=2.1-3; Grade 4= >3. WBC (/mm^3): Grade 1=2000-2500; Grade 2=1500-1999; Grade 3=1000-1499; Grade 4= <1000. Neutrophils (/mm^3): Grade 1=1000-1300; Grade 2=750-999; Grade 3=500-749; Grade 4= <500. (NCT01079806)
Timeframe: Day 1 through Week 48 on blinded therapy

,
InterventionParticipants (Number)
HemoglobinPlateletsINRWhite blood cells (WBC)Neutrophils + bands (absolute)
Entecavir532214
Placebo42612

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Number of Participants With Laboratory Test Results Meeting the Criteria for Abnormality (Grades 1-4) (Continued)

Toxicities graded per Division of AIDS criteria, Version 1.0, and modified World Health Organization criteria. ALT=alanine aminotransferase; AST=aspartate aminotransferase; BUN=blood urea nitrogen; ULN=upper limit of normal; LLN=lower limit of normal. ALT, AST (*ULN): Grade 1=1.25-2; Grade 2=2.6-5; Grade 3=5.1-10; Grade 4 => 10. Bilirubin (*ULN): Grade 1 = 1.1-1.5; Grade 2=1.6-2.5; Grade 3 = 2.6-5; Grade 4= >5. Albumin (g/dL): Grade 1=3- 5. BUN/urea (*ULN): Grade 1=1.25-<2.6; Grade 2=2.6-<5.1; Grade 3=5.1-10; Grade 4= >10. Chloride, high (mEq/L): Grade 1=113-<117; Grade 2=117-<121; Grade 3=121-125; Grade 4= >125. Potassium, low (mEq/L): Grade 1=3-3.4; Grade 2=2.5-<3; Grade 3=2-<2.5; Grade 4=<2. Potassium, high (mEq/L): : Grade 1= 5.6-<6.1; Grade 2=6.1-<6.6; Grade 3=6.6-7; Grade 4= >7. Sodium, high (mEq/L): Grade 1=146<151; Grade 2=151-<155; Grade 3=155-<160; Grade 4= >=160. (NCT01079806)
Timeframe: Day 1 through Week 48 on blinded therapy

,
Interventionparticipants (Number)
ALTASTTotal bilirubinAlbuminLipaseBUN/UreaChloride, highPotassium, lowPotassium, highSodium, high
Entecavir113875038102118
Placebo5951612021104

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Percentage of Participants Who Achieved Sustained HBeAg Seroconversion During Off-treatment Follow up Among Participants Who Achieved HBeAg Seroconversion at End of Dosing (EOD).

Participants who demonstrated HBeAg seroconversion at EOD were followed and assessed for presence of sustained HBeAg seroconversion during entire study. The study reached the end of dosing (EOD) on 22 Feb-2016. (NCT01079806)
Timeframe: Week 48, EOD (2 years)

,
InterventionPercentage of participants (Number)
EOD (end of dosing)Week 48
Entecavir100.074.4
Placebo100.059.1

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Percentage of Participants Who Maintained HBeAg Seroconversion at Week 96 (End of Blinded Therapy) Among Participants With HBeAg Seroconversion at Week 48

Participants who achieved HBeAg seroconversion by Week 48 and maintained seroconversion to week 96 (NCT01079806)
Timeframe: At Week 96

,
InterventionPercentage of participants (Number)
Week 48Week 96
Entecavir24.236.7
Placebo10.020.0

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Percentage of Participants With HbeAg Loss at Weeks 48 and 96

HBeAg Loss (NC = F and NC = M) - On Treatment through Week 96 - Year 2 Efficacy Cohort Non-Completer - Failure (NC=F): The numerator was based on participants meeting the response criteria. The denominator was based on treated participants. Participants who had missing data at the analysis week were considered failures. Non-Completer - Missing (NC=M): The numerator was based on participants meeting the response criteria. The denominator was based on participants with data at the analysis week. Participants who had missing data at the analysis week were excluded. (NCT01079806)
Timeframe: At 48 and 96 weeks

InterventionPercentage of participants (Number)
48 weeks
Placebo10.0

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Percentage of Participants With HbeAg Loss at Weeks 48 and 96

HBeAg Loss (NC = F and NC = M) - On Treatment through Week 96 - Year 2 Efficacy Cohort Non-Completer - Failure (NC=F): The numerator was based on participants meeting the response criteria. The denominator was based on treated participants. Participants who had missing data at the analysis week were considered failures. Non-Completer - Missing (NC=M): The numerator was based on participants meeting the response criteria. The denominator was based on participants with data at the analysis week. Participants who had missing data at the analysis week were excluded. (NCT01079806)
Timeframe: At 48 and 96 weeks

InterventionPercentage of participants (Number)
48 weeks96 Weeks
Entecavir25.040.8

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Percentage of Participants With HBeAg Seroconversion at Week 48

"Primary endpoint data were summarised under End of Study,using the last available post-baseline observation(Last Observation Carried Forward,LOCF)" (NCT01326546)
Timeframe: 48 weeks

InterventionParticipants (Count of Participants)
Therapeutic HBV Vaccine+Entecavir21
Placebo+Entecavir23

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Overall OLT-free Survival

Overall OLT-free survival until development of OLT and death and participants will be followed for the duration of hospital stay or outpatients visit, an expected average of 12 months (NCT01354652)
Timeframe: Participants will be followed for the duration of hospital stay or outpatients visit, an expected average of 12 months

Interventionday (Mean)
Entecavir411
Lamivudine175

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Incidence of Elevated Venous Lactate Levels More Than 2 mmol/L of Any Etiology

incidence of elevated venous lactate levels more than 2 mmol/L of any etiology until development of lactic acidosis, orthotropic liver transplantation (OLT), death, or improvement of hepatic or renal function to MELD score less than 18 and and participants will be followed for the duration of hospital stay, an expected average of 8 weeks. (NCT01354652)
Timeframe: participants will be followed for the duration of hospital stay, an expected average of 8 weeks

Interventionparticipants (Number)
Entecavir3
Lamivudine2

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Proportion of Participants With Hepatitis B Surface Antigen (HBsAg) Loss

(NCT01368497)
Timeframe: End of treatment (up to 48 weeks)

InterventionProportion of participants (Number)
Entecavir and Peginterferon.050

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Proportion of Participants With Hepatitis B Surface Antigen (HBsAg) Loss

(NCT01368497)
Timeframe: End of follow-up (up to 96 weeks)

InterventionProportion of participants (Number)
Entecavir and Peginterferon.033

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Proportion of Participants With Hepatitis B e Antigen (HBeAg) Loss & Hepatitis B Virus (HBV) Deoxyribonucleic Acid (DNA) Levels ≤1,000 International Units (IU) Per Milliliter (mL)

(NCT01368497)
Timeframe: End of follow-up (up to 96 weeks)

InterventionProportion of participants (Number)
Entecavir and Peginterferon.033

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Proportion of Participants With Hepatitis B e Antigen (HBeAg) Loss

(NCT01368497)
Timeframe: End of treatment (up to 48 weeks)

InterventionProportion of participants (Number)
Entecavir and Peginterferon.033

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Proportion of Participants With Hepatitis B e Antigen (HBeAg) Loss

(NCT01368497)
Timeframe: End of follow-up (up to 96 weeks)

InterventionProportion of participants (Number)
Entecavir and Peginterferon.033

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Proportion of Participants With HBV DNA ≤1000 IU/mL

(NCT01368497)
Timeframe: End of treatment (up to 48 weeks)

InterventionProportion of participants (Number)
Entecavir and Peginterferon.750

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Proportion of Participants With HBV DNA ≤1000 IU/mL

(NCT01368497)
Timeframe: End of follow-up (up to 96 weeks)

InterventionProportion of participants (Number)
Entecavir and Peginterferon.033

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Proportion of Participants With HBV DNA < 20 IU/mL

(NCT01368497)
Timeframe: End of treatment (up to 48 weeks)

InterventionProportion of participants (Number)
Entecavir and Peginterferon.233

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Proportion of Participants With HBV DNA < 20 IU/mL

(NCT01368497)
Timeframe: End of follow-up (up to 96 weeks)

InterventionProportion of participants (Number)
Entecavir and Peginterferon.033

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Proportion of Participants With HBsAg Seroconversion

(NCT01368497)
Timeframe: End of treatment (up to 48 weeks)

InterventionProportion of participants (Number)
Entecavir and Peginterferon.033

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Proportion of Participants With HBsAg Seroconversion

(NCT01368497)
Timeframe: End of follow-up (up to 96 weeks)

InterventionProportion of participants (Number)
Entecavir and Peginterferon.033

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Proportion of Participants With HBeAg Seroconversion

(NCT01368497)
Timeframe: End of treatment (up to 48 weeks)

InterventionProportion of participants (Number)
Entecavir and Peginterferon.033

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Proportion of Participants With HBeAg Seroconversion

(NCT01368497)
Timeframe: End of follow-up (up to 96 weeks)

InterventionProportion of participants (Number)
Entecavir and Peginterferon.033

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Proportion of Participants With ALT ≤ 40 U/L for Males, ≤ 35 U/L for Females

(NCT01368497)
Timeframe: End of follow-up (up to 96 weeks)

InterventionProportion of participants (Number)
Entecavir and Peginterferon.650

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Proportion of Participants With Alanine Aminotransferase (ALT) ≤ 40 Units (U) Per Liter (L) for Males, ≤ 35 U/L for Females

(NCT01368497)
Timeframe: End of treatment (up to 48 weeks)

InterventionProportion of participants (Number)
Entecavir and Peginterferon.350

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Tanner Stages of Pubic Hair Growth

"The Tanner Stage questionnaire is only completed by participants 8 years of age and older. The copyrighted form includes pictures and descriptions. Participants selected the picture closest to their self-perceived pubic hair growth.~Boys and girls: I-prepubertal (no pubic hair at all); II-sparse growth of long, slightly pigmented hair, straight or curled, at base of penis or along labia; III: darker, coarser and more curled hair, spreading sparsely over junction of pubes; IV- hair adult in type, but covering smaller area than in adult; V-adult in type and quantity.~There is no better or worse outcome. They are self-assessed descriptive measures of physical growth." (NCT01368497)
Timeframe: End of follow-up (up to 96 weeks)

InterventionParticipants (Count of Participants)
IIIIIIIVVMissing
Entecavir and Peginterferon166591212

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Proportion Without Detectable Antiviral Drug-resistance HBV Mutations

HBV drug resistance variant testing was performed at the CDC laboratory. The sequences of the HBV polymerase spanning nucleotide positions 311-1021 were determined by Sanger sequencing. Drug resistance mutations that were tested in this study included L80VI, L82M, T128N, W153Q, F166L, I169T, V173L, L180M, A181TV, T184ACFGILMS, V191T, A194T, A200V, S202ETV, M204IV, V207I, N236T, M250ILV, and G145R. (NCT01368497)
Timeframe: End of treatment (up to 48 weeks)

InterventionProportion of participants (Number)
Entecavir and Peginterferon.733

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Tanner Stages of Pubic Hair Growth

"The Tanner Stage questionnaire is only completed by participants 8 years of age and older. The copyrighted form includes pictures and descriptions. Participants selected the picture closest to their self-perceived pubic hair growth.~Boys and girls: I-prepubertal (no pubic hair at all); II-sparse growth of long, slightly pigmented hair, straight or curled, at base of penis or along labia; III: darker, coarser and more curled hair, spreading sparsely over junction of pubes; IV- hair adult in type, but covering smaller area than in adult; V-adult in type and quantity.~There is no better or worse outcome. They are self-assessed descriptive measures of physical growth." (NCT01368497)
Timeframe: End of treatment (up to 48 weeks)

InterventionParticipants (Count of Participants)
IIIIIIIVVMissing
Entecavir and Peginterferon154412718

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Growth Measures: Z-scores Weight, Height, and Body Mass Index

A child's Z-score is the number of standard deviations that the child is from the average of children of the same sex and age from a reference population. The reference population is provided in the 2000 Centers for Disease Control and Prevention (CDC) growth charts. Positive Z scores mean the growth measure (weight, height, or body mass index) is above the average, negative Z scores mean the growth measure is below the average. (NCT01368497)
Timeframe: End of follow-up (up to 96 weeks)

InterventionZ-score (Mean)
Z-score weightZ-score heightZ-score BMI
Entecavir and Peginterferon-0.34-0.45-0.14

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Growth Measures: Z-scores Weight, Height, and Body Mass Index

A child's Z-score is the number of standard deviations that the child is from the average of children of the same sex and age from a reference population. The reference population is provided in the 2000 Centers for Disease Control and Prevention (CDC) growth charts. Positive Z scores mean the growth measure (weight, height, or body mass index) is above the average, negative Z scores mean the growth measure is below the average. (NCT01368497)
Timeframe: End of treatment (up to 48 weeks)

InterventionZ-score (Mean)
Z-score weightZ-score heightZ-score BMI
Entecavir and Peginterferon-0.48-0.41-0.37

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Incidence of Adverse Events (AEs) Per Person-Year

The number of AEs includes both AEs and Serious Adverse Events (SAEs). The incidence is calculated as the number of AEs divided by the number of person-years of observation, which is the sum, across all participants, of the number of years between the start of treatment and the end of treatment, or the end of follow-up, respectively. (NCT01368497)
Timeframe: From first treatment to the end of treatment (up to 48 weeks) and the end of follow-up (up to 96 weeks)

InterventionAEs per person-year of observation (Number)
End of treatment (Up to 48 weeks)End of follow-up (Up to 96 weeks)
Entecavir and Peginterferon1.130.70

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Incidence of Serious Adverse Events (SAEs) Per Person-Year

The incidence is calculated as the number of SAEs divided by the number of person-years of observation, which is the sum, across all participants, of the number of years between the start of treatment and the end of treatment, or the end of follow-up, respectively. (NCT01368497)
Timeframe: From first treatment to the end of treatment (up to 48 weeks) and the end of follow-up (up to 96 weeks)

InterventionSAEs per person-year of observation (Number)
End of treatment (Up to 48 weeks)End of follow-up (Up to 96 weeks)
Entecavir and Peginterferon00.01

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Tanner Stages of Physical Growth

"The Tanner Stage questionnaire is only completed by participants 8 years of age and older. The copyrighted form includes pictures and descriptions. Girls selected the picture closest to their self-perceived breast growth from among 5 stages of breast growth and boys did the same for testes, scrotum, and penis growth.~Boys: I-prepubertal; II-enlargement of scrotum and testes; III-enlargement of the penis and further growth of testes; IV- increased size of penis with growth in breadth and development of glans, testes, and scrotum larger, scrotum skin darker; V- adult genitalia.~Girls: I-prepubertal; II-breast bud stage with the elevation of breast and papilla and enlargement of the areola; III-further enlargement of breast and areola, no separation of their contour; IV-areola and papilla form a secondary mound above the level of the breast; V: mature adult stage.~There is no better or worse outcome. They are self-assessed descriptive measures of physical growth." (NCT01368497)
Timeframe: End of follow-up (up to 96 weeks)

InterventionParticipants (Count of Participants)
IIIIIIIVVMissing
Entecavir and Peginterferon145981212

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Tanner Stages of Physical Growth

"The Tanner Stage questionnaire is only completed by participants 8 years of age and older. The copyrighted form includes pictures and descriptions. Girls selected the picture closest to their self-perceived breast growth from among 5 stages of breast growth and boys did the same for testes, scrotum, and penis growth.~Boys: I-prepubertal; II-enlargement of scrotum and testes; III-enlargement of the penis and further growth of testes; IV- increased size of penis with growth in breadth and development of glans, testes, and scrotum larger, scrotum skin darker; V- adult genitalia.~Girls: I-prepubertal; II-breast bud stage with the elevation of breast and papilla and enlargement of the areola; III-further enlargement of breast and areola, no separation of their contour; IV-areola and papilla form a secondary mound above the level of the breast; V: mature adult stage.~There is no better or worse outcome. They are self-assessed descriptive measures of physical growth." (NCT01368497)
Timeframe: End of treatment (up to 48 weeks)

InterventionParticipants (Count of Participants)
IIIIIIIVVMissing
Entecavir and Peginterferon123128718

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Proportion of Participants With HBV DNA <20 IU/mL

(NCT01369199)
Timeframe: End of follow-up (up to 96 weeks)

InterventionProportion of participants (Number)
Peginterferon and Entecavir0

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Proportion of Participants With HBsAg Seroconversion

(NCT01369199)
Timeframe: End of treatment (up to 48 weeks)

InterventionProportion of participants (Number)
Peginterferon and Entecavir0

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Proportion of Participants With HBsAg Seroconversion

(NCT01369199)
Timeframe: End of follow-up (up to 96 weeks)

InterventionProportion of participants (Number)
Peginterferon and Entecavir0

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Proportion of Participants With HBeAg Loss

(NCT01369199)
Timeframe: End of treatment (up to 48 weeks)

InterventionProportion of participants (Number)
Peginterferon and Entecavir.036

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Proportion of Participants With HBeAg Loss

(NCT01369199)
Timeframe: End of follow-up (up to 96 weeks)

InterventionProportion of participants (Number)
Peginterferon and Entecavir.036

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Proportion of Participants With ALT Normalization (Men <30 U/L, Women <20 U/L)

(NCT01369199)
Timeframe: End of treatment (up to 48 weeks)

InterventionProportion of participants (Number)
Peginterferon and Entecavir.393

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Proportion of Participants With ALT Normalization (Men <30 U/L, Women <20 U/L)

(NCT01369199)
Timeframe: End of follow-up (up to 96 weeks)

InterventionProportion of participants (Number)
Peginterferon and Entecavir.464

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Proportion of Participants With ALT <45 U/L for Men, <30 U/L for Women

(NCT01369199)
Timeframe: End of follow-up (up to 96 weeks)

InterventionProportion of participants (Number)
Peginterferon and Entecavir.750

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Proportion of Participants With Alanine Aminotransferase (ALT) <45 U/L for Men, <30 U/L for Women

(NCT01369199)
Timeframe: End of treatment (up to 48 weeks)

InterventionProportion of participants (Number)
Peginterferon and Entecavir.571

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Absence of Detectable Antiviral Drug-resistance HBV Mutations

HBV drug resistance variant testing was performed at the CDC laboratory. The sequences of the HBV polymerase spanning nucleotide positions 311-1021 were determined by Sanger sequencing. Drug resistance mutations that were tested in this study included L80VI, L82M, T128N, W153Q, F166L, I169T, V173L, L180M, A181TV, T184ACFGILMS, V191T, A194T, A200V, S202ETV, M204IV, V207I, N236T, M250ILV, and G145R. (NCT01369199)
Timeframe: End of treatment (up to 48 weeks)

InterventionProportion of participants (Number)
Peginterferon and Entecavir.893

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Proportion of Participants With HBsAg Loss

(NCT01369199)
Timeframe: End of treatment (up to 48 weeks)

InterventionProportion of participants (Number)
Peginterferon and Entecavir0

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Proportion of Participants With HBsAg Loss

(NCT01369199)
Timeframe: End of follow-up (up to 96 weeks)

InterventionProportion of participants (Number)
Peginterferon and Entecavir0

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Proportion of Participants With HBeAg Seroconversion

(NCT01369199)
Timeframe: End of treatment (up to 48 weeks)

InterventionProportion of participants (Number)
Peginterferon and Entecavir.036

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Proportion of Participants With HBeAg Seroconversion

(NCT01369199)
Timeframe: End of follow-up (up to 96 weeks)

InterventionProportion of participants (Number)
Peginterferon and Entecavir.036

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Proportion of Participants With HBeAg Loss (Lack of Detectable HBeAg) AND HBV DNA ≤1,000 IU/mL

Lack of data was considered to be treatment failure. (NCT01369199)
Timeframe: End of follow-up (up to 96 weeks)

InterventionProportion of participants (Number)
Peginterferon and Entecavir0

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Incidence of Serious Adverse Events (SAEs) Per Person-Year

The incidence is calculated as the number of SAEs divided by the number of person-years of observation, which is the sum, across all participants, of the number of years between the start of treatment and the end of treatment, or the end of follow-up, respectively. (NCT01369199)
Timeframe: From first treatment to the end of treatment (up to 48 weeks) and the end of follow-up (up to 96 weeks)

InterventionSAEs per person-year of observation (Number)
End of treatment (Up to 48 weeks)End of follow-up (Up to 96 weeks)
Peginterferon and Entecavir0.021

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Incidence of Adverse Events (AEs) Per Person-Year of Observation

The number of AEs includes both AEs and Serious Adverse Events (SAEs). The incidence is calculated as the number of AEs divided by the number of person-years of observation, which is the sum, across all participants, of the number of years between the start of treatment and the end of treatment, or the end of follow-up, respectively. (NCT01369199)
Timeframe: From first treatment to the end of treatment (up to 48 weeks) and the end of follow-up (up to 96 weeks)

InterventionEvents per person-year of observation (Number)
End of treatment (Up to 48 weeks)End of follow-up (Up to 96) weeks
Peginterferon and Entecavir1.600.86

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Proportion of Participants With HBV DNA ≤1000 IU/mL

(NCT01369199)
Timeframe: End of treatment (up to 48 weeks)

InterventionProportion of participants (Number)
Peginterferon and Entecavir.929

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Proportion of Participants With HBV DNA ≤1000 IU/mL

(NCT01369199)
Timeframe: End of follow-up (up to 96 weeks)

InterventionProportion of participants (Number)
Peginterferon and Entecavir0

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Proportion of Participants With HBV DNA <20 IU/mL

(NCT01369199)
Timeframe: End of treatment (up to 48 weeks)

InterventionProportion of participants (Number)
Peginterferon and Entecavir.179

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Overall Study: Percentage of Participants With Sustained HBV DNA <10^4 Copies/mL by PCR Assay

(NCT01438424)
Timeframe: Study entry to Week 192

InterventionPercentage of participants (Number)
At study entry (n=1051)Week 48 (n=905)Week 96 (n=691)Week 144 (n=597)Week 192 (n=485)
Entecavir, 0.5 or 1.0 mg, With or Without Lamivudine2876778185

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Overall Study: Percentage of Participants With HBeAg Seroconversion

Observed values. Seroconversion=negative HBeAg with detectable anti-HBe antibody. (NCT01438424)
Timeframe: Study entry to Week 216

InterventionPercentage of participants (Number)
At study entry (n=1051)Week 12 (n=931)Week 24 (n=934)Week 48 (n=862)Week 72 (n=755)Week 96 (n=678)Week 120 (n=607)Week 144 (n=587)Week 168 (n=517)Week 192 (n=491)Week 216 (n=434)
Entecavir, 1.0 mg, With or Without Lamivudine3033343632343637394240

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Overall Study: Percentage of Participants Who Achieved ALT Normalization

ULN=upper limit of normal. ALT normalization=ALT levels ≤1.0*ULN. (NCT01438424)
Timeframe: Study entry to Week 216

InterventionPercentage of participants (Number)
At study entry (n=1019)Week 48 (n=942)Week 144 (n=627)Week 216 (n=482)
Entecavir, 0.5 or 1.0 mg, With or Without Lamivudine40757478

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Overall Study: Percentage of Participants Who Achieved a Loss of Hepatitis B e Antigen (HBeAg)

Observed values. (NCT01438424)
Timeframe: Study entry to Week 216

InterventionPercentage of participants (Number)
At study entry (n=1051)Week 12 (n=935)Week 24 (n=939)Week 48 (n=864)Week 72 (n=752)Week 96 (n=679)Week 120 (n=609)Week 144 (n=587)Week 168 (n=518)Week 192 (n=491)Week 216 (n=436)
Entecavir, 1.0 mg, With or Without Lamivudine3440424645505153586059

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Overall Study: Percentage of Participants by HBV DNA Category by PCR Assay

Observed values. (NCT01438424)
Timeframe: Baseline to Week 192

InterventionPercentage of participants (Number)
Baseline: <300 copies/mL (n=1051)Baseline: 300 - <1.0E3 copies/mL (n=1051)Baseline: 1.0E3 - <1.0E4 copies/mL (n=1051)Baseline: 1.0E4 - <1.0E5 copies/mL (n=1051)Baseline: 1.0E5 - <1.0E6 copies/mL (n=1051)Baseline: 1.0E6 - <1.0E7 copies/mL (n=1051)Baseline: 1.0E7 - <1.0E8 copies/mL (n=1051)Baseline: 1.0E8 - <1.0E9 copies/mL (n=1051)Baseline: 1.0E9 - <1.0E10 copies/mL (n=1051)Baseline: >= 1.0E10 copies/mL (n=1051)Week 192: < 300 copies/mL (n=485)Week 192: 300 - <1.0E3 copies/mL (n=485)Week 192: 1.0E3 - <1.0E4 copies/mL (n=485)Week 192: 1.0E4 - <1.0E5 copies/mL (n=485)Week 192: 1.0E5 - <1.0E6 copies/mL (n=485)Week 192: 1.0E6 - <1.0E7 copies/mL (n=485)Week 192: 1.0E7 - <1.0E8 copies/mL (n=485)Week 192: 1.0E8 - <1.0E9 copies/mL (n=485)Week 192: 1.0E9 - <1.0E10 copies/mL (n=485)Week 192: >= 1.0E10 copies/mL (n=485)
Entecavir, 1.0 mg, With or Without Lamivudine17488121381113678334221520

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Overall Study: Number of Participants With Normal Pancreatic Enzyme and Renal Function Values at Baseline and Abnormalities in Pancreatic Enzyme and Renal Function Laboratory Test Results at End of Dosing

Amylase: Grade 1=1.10-<1.40*ULN; Grade 2=1.40-< 2.10*ULN; Grade 3=2.10-5.00*ULN; Grade 4=>5.00*ULN. Lipase: Grade 1.1-<1.4*ULN; Grade 2=1.4-<2.1*ULN; Grade 3=2.1-5.0*ULN; Grade 4=>5.0*ULN. Creatinine: Grade 1=1.10-< 1.60*ULN; Grade 2=1.60-<3.10*ULN; Grade 3=3.10-6.00*ULN; Grade 4=>6.00*ULN. Blood urea nitrogen (BUN): Grade 1=1.25-<2.60*ULN; Grade 2=2.60-<5.10*ULN; Grade 3=5.10-10*ULN; Grade 4=>10*ULN. ULN=upper limit of normal. (NCT01438424)
Timeframe: Day 1 of treatment through Week 240

InterventionParticipants (Number)
Amylase (All grades) (n=875)Lipase (All grades) (n=390)Amylase (Grades 3-4) (n=875)Lipase (Grades 3-4) (n=390)BUN/Urea (All grades) (n=998)Creatinine (All grades) (n=1000)BUN/Urea (Grades 3-4) (n=998)Creatinine (Grades 3-4) (n=1000)
Entecavir, 0.5 or 1.0 mg, With or Without Lamivudine1791261338576102

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Overall Study: Number of Participants With Normal Hematology Values at Baseline and Abnormalities in Hematology Laboratory Test Results Through Week 240

Hemoglobin (g/dL): Grade (Gr) 1=9.5-11.0; Gr 2=8.0-<9.5; Gr 3=6.5-<8.0; Gr 4=<6.5 White blood cells (cells/mm^3): Gr 1=2,500-<4,000; Gr 2=1,000-<2,500; Gr 3=800-<1,000; Gr 4=<800. Neutrophils (cells/mm^3): Gr 1=1000-<1500; Gr 2=750-<1000; Gr 3=500-<750; Gr 4=<500. Platelets (cells/mm^3): Gr 1=75,000-99,000; Gr 2=50,000-<75,000; Gr 3=20,000-<50,000; Gr 4=<20,000. Prothrombin time (seconds): Gr 1=1.01-<1.26*ULN; Gr 2=1.26-<1.51 *ULN; Gr 3=1.51-3*ULN; Gr 4=>3*ULN. INR: Gr 1=1.24-1.5; Gr 2=1.5-2; Gr 3=2-3; Gr 4=>3. INR=international normalized ratio; ULN=upper limit of normal. . (NCT01438424)
Timeframe: Day 1 of treatment through Week 240

InterventionParticipants (Number)
Hemoglobin (All grades) (n=1007)White blood cells (All grades) (n=950)Neutrophils (All grades) (n=1002)Platelets (All grades) (n=979)Protrombin time (All grades) (n=746)INR (All grades)(n=746)Hemoglobin (Grades 3-4) (n=1007)White blood cells (Grades 3-4) (n=950)Neutrophils (Grades 3-4) (n=1002)Platelets (Grades 3-4) (n=979)Prothrombin time (Grades 3-4) (n=746)INR (Grades 3-4) (n=746)
Entecavir, 0.5 or 1.0 mg, With or Without Lamivudine4922610951226214212112112

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Overall Study: Number of Participants With Normal Electrolyte and Fasting Glucose Values at Baseline and Abnormalities in Electrolyte and Fasting Glucose Laboratory Test Results at End of Dosing

Hypochloremia: Grade (Gr) 1=90-93; Gr 2=85-<90; Gr 3=80-<85; Gr 4=40-<80. Hyperchloremia: Gr 1=113-<117; Gr 2=117-<121; Gr 3=121-125; Gr 4>125. Hypocarbia: Gr 1=19-21; Gr 2=15-<19; Gr 3=41-45; Gr 4=>45. Hypercarbia: Gr 1=31-36; Gr 2=37-40; Gr 3=41-45; Gr 4=>45. Hyponatremia: Gr 1=130-132; Gr 2=123-<130; Gr 3=116-<123; Gr 4<116. Hypernatremia: Gr 1=148-<151; Gr 2=151-<158; Gr 3=158-165; Gr 4=>165. Hypokalemia: Gr 1=3-3.4; Gr 2=2.5-<3; Gr 3=2-<2.5; Gr 4=<2. Hyperkalemia: Gr 1=5.6-<6.1; G2=6.1-<6.6; Gr 3=6.6-7; Gr 4=>7. Hypoglycemia: Gr 1=55-64; Gr 2=40-<55; Gr 3=30-< 40; G4=-<30. Hyperglycemia: Gr 1=116-<161; Gr 2=161-<251; Gr 3=251-500; Gr 4>500. (NCT01438424)
Timeframe: Day 1 of treatment through Week 240

InterventionParticipants (Number)
Hypochloremia (mEq/L) (All grades) (n=982)Hyperchloremia (mEq/L) (All grades) (n=982)Hypocarbia (mEq/L) (All grades) (n=831)Hypercarbia (mEq/L) (All grades) (n=831)Hyponatremia (mEq/L) (All grades) (n=1003)Hypernatremia (mEq/L) (All grades) (n=1003)Hypokalemia (mEq/L) (All grades) (n=993)Hyperkalemia (mEq/L) (All grades (n=993)Hypochloremia (mEq/L) (Grades 3-4) (n=982)Hyperchloremia (mEq/L) (Grades 3-4) (n=982)Hypocarbia (mEq/L) (Grades 3-4) (n=831)Hypercarbia (mEq/L) (Grades 3-4) (n=831)Hyponatremia (mEq/L)(Grades 3-4) (n=1003)Hypernatremia (mEq/L) (Grades 3-4) (n=1003)Hypokalemia (mEq/L) (Grades 3-4) (n=993)Hyperkalemia (mEq/L) (Grades 3-4) (n=993)Hypoglycemia (mg/dL) (All grades) (n=521)Hyperglycemia (mg/dL) (All grades) (n=521)Hypoglycemia (mg/dL) (Grades 3-4) (n=521)Hyperglycemia (mg/dL) (Grades 3-4) (n=521)
Entecavir, 0.5 or 1.0 mg, With or Without Lamivudine447628514868106135423714225164715034

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Overall Study: Number of Participants With Death As Outcome, Any Adverse Event (AE), Grade 3-4 AEs, Serious Adverse Events (SAEs), and Discontinuations Due to AEs

An AE is a new unfavorable symptom, sign, or disease or worsening of a preexisting condition that may not be causally related to treatment. An SAE is an unfavorable medical event that at any dose results in death, persistent or significant disability/incapacity, or drug dependency or abuse; is life-threatening, an important medical event, or a congenital anomaly/birth defect; or requires or prolongs hospitalization. Grade 1=mild; Grade 2=moderate; Grade 3=severe; Grade 4=life-threatening or disabling. ALT=alanine transaminase; ULN=upper limit of normal. (NCT01438424)
Timeframe: Continuously from Day 1 through Week 240

InterventionParticipants (Number)
Deaths on treatmentDeaths off treatmentSAEs on treatmentDiscontinuations due to AEs on treatmentAny AE on treatmentGrade 3 and 4 AEs on treatmentMalignancies on and off treatmentALT flares (ALT>2*entry and >10*ULN) on treatmentHepatic disease progression on and off treatment
Entecavir, 0.5 or 1.0 mg QD, With or Without Lamivudine18916914900203353233

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Overall Study: Mean HBV DNA Level by PCR Assay

(NCT01438424)
Timeframe: Study entry to Week 216

Interventionlog10 copies/mL (Mean)
At study entry (n=1051)Week 12 (n=1017)Week 24 (n=1010)Week 48 (n=905)Week 72 (n=769)Week 96 (n=691)Week 120 (n=629)Week 144 (n=597)Week 168 (n=514)Week 192 (n=485)Week 216 (n=455)
Entecavir, 0.5 or 1.0 mg, With or Without Lamivudine6.143.873.623.373.313.343.323.343.183.193.20

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Overall Study: Mean Alanine Transaminase (ALT) Levels

Observed values. (NCT01438424)
Timeframe: Study entry to Week 216

InterventionU/L (Mean)
At study entry (n=1051)Week 12 (n=1049)Week 24 (n=1029)Week 48 (n=942)Week 72 (n=835)Week 96 (n=740)Week 120 (n=675)Week 144 (n=627)Week 168 (n=563)Week 192 (n=528)Week 216 (n=482)
Entecavir, 1.0 mg, With or Without Lamivudine109.448.7742.1037.0638.1039.3037.4338.5136.8037.3638.43

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Off-treatment Follow-up: Percentage of Participants With Sustained Hepatitis B Virus (HBV) DNA <10,000 Copies by Polymerase Chain Reaction (PCR) Assay (Amendment 11 Cohort)

The Amendment 11 Cohort consisted of participants who were hepatitis B e antigen (HBeAg) negative and who had compensated liver disease, a minimum of 192 weeks (4 years) of treatment with entecavir, HBV DNA <300 copies/mL by PCR assay for ≥48 weeks before end of dosing and on the last observed result ≤24 weeks prior to end of dosing, and serum ALT levels ≤1.0*ULN at the end of study drug dosing.ALT=alanine aminotransferase; ULN=upper limit of normal. (NCT01438424)
Timeframe: End of dosing to Week 48 off-treatment follow-up

InterventionPercentage of participants (Number)
End of dosing current studyOff-treatment Week 48
Entecavir, 0.5 or 1.0 mg, With or Without Lamivudine10021

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Overall Study: Percentage of Participants With Sustained HBV DNA Level <300 Copies/mL by PCR Assay

(NCT01438424)
Timeframe: Study entry to Week 192

InterventionPercentage of participants (Number)
At study entry (n=1051)Week 48 (n=905)Week 96 (n=691)Week 144 (n=597)Week 192 (n=485)
Entecavir, 0.5 or 1.0 mg, With or Without Lamivudine1763677378

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Off-treatment Follow-up: Mean Change in HBV DNA (Amendment 11 Cohort)

The Amendment 11 Cohort consisted of participants who were HBeAg negative and who had compensated liver disease, a minimum of 192 weeks (4 years) of treatment with entecavir, HBV DNA <300 copies/mL by PCR assay for ≥48 weeks before end of dosing and on the last observed result ≤24 weeks prior to end of dosing, and serum ALT levels ≤1.0*ULN at the end of study drug dosing. (NCT01438424)
Timeframe: End of dosing to Weeks 48 and 96 off-treatment follow-up

InterventionLog10 copies/mL (Mean)
Off-treatment Week 48Off-treatment Week 96
Entecavir, 0.5 or 1.0 mg, With or Without Lamivudine1.541.18

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Overall Study: Percentage of Participants With a Confirmed ≥1 log10 Increase From Nadir in HBV DNA by PCR Assay

(NCT01438424)
Timeframe: Baseline to Week 144

InterventionPercentage of participants (Number)
Entecavir, 0.5 or 1.0 mg, With or Without Lamivudine18

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Week 144: Number of Participants With Death As Outcome, Any AE, Grade 3-4 AEs, SAEs, Discontinuations Due to AEs, and Abnormalities in Selected Laboratory Test Results

An AE is any new unfavorable symptom, sign, or disease or worsening of a preexisting condition that does not necessarily have a causal relationship with treatment. An SAE is any unfavorable medical event that at any dose results in death, persistent or significant disability/incapacity, or drug dependency or abuse; is life-threatening, an important medical event, or a congenital anomaly/birth defect; or requires or prolongs hospitalization. Grade 1=mild; Grade 2=moderate; Grade 3=severe; Grade 4=life-threatening or disabling. AST=aspartate aminotransferase; ULN=upper limit of normal. (NCT01438424)
Timeframe: Continuously from Day 1 through Week 144

InterventionParticipants (Number)
Deaths on studyMalignant neoplasmsSAEsDiscontinuations due to AEsAny AEGrade 3 and 4 AEsALT flares (ALT>2*entry and >10*ULN)ALT >5.0*ULNAST >5.0*ULNTotal bilirubin >2.5*ULNLipase >2.0*ULNCreatinine ≥0.5 mg/dL from baselineHypocarbia
Entecavir, 0.5 or 1.0 mg QD, With or Without Lamivudine131710713842156299353227164

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Week 96: Percentage of Participants Who Achieved HBV DNA <300 Copies/mL by PCR Assay, Loss of HBeAg, HBeAg Seroconversion, and ALT ≤1.0*ULN (Lamivudine Continuous Switch Cohort)

The Lamivudine Continuous Switch Cohort consisted of participants who were nucleoside-naive, HBeAg-positive and received lamivudine in BMS study AI463-022 (NCT00035633) and enrolled in the current study with ≤35 days off treatment between end of dosing in AI463-022 and the switch to entecavir in the current study. This cohort permitted assessment of entecavir, 1.0 mg, provided as switch therapy in the current study. (NCT01438424)
Timeframe: Baseline to Week 96

InterventionPercentage of participants (Number)
HBV DNA <300 copies/mL (n=147)Achieved loss of HbeAg (n=129)Achieved HBeAg seroconversion (n=129)Achieved ALT ≤1.0*ULN (n=154)
Entecavir, 0.5 or 1.0 mg, With or Without Lamivudine5825876

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Week 96: Percentage of Participants Who Achieved HBV DNA <300 Copies/mL by PCR Assay and ALT ≤1.0*ULN (Lamivudine Retreatment Switch Cohort)

The Lamivudine Retreatment Switch Cohort consisted of participants who were nucleoside-naive HBeAg negative and enrolled from BMS study AI463-027 (NCT00035789) with >60 days between end of dosing in AI463-027 and the switch to entecavir in the current study. This cohort permitted assessment of entecavir, 1.0 mg, provided as switch therapy in the current study. (NCT01438424)
Timeframe: Baseline to Week 96

InterventionPercentage of participants (Number)
HBV DNA <300 copies/mL (n=69)ALT ≤1.0*ULN (n=81)
Entecavir, 0.5 or 1.0 mg, With or Without Lamivudine9781

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Week 192: Percentage of Participants With Improvement in Fibrosis (Efficacy Evaluable Cohort)

The Ishak Modification for Hepatic Activity Index (HAI) scores necroinflammatory activity in chronic hepatitis. 0=no fibrosis, 1=fibrosis expansion of some portal areas, 2=fibrosis expansion of most portal areas, 3=fibrosis expansion of most portal areas with occasional bridging, 4=fibrosis expansion of portal areas with marked bridging, 5=incomplete cirrhosis, 6=probable or definite cirrhosis. Higher score=more severe necrosis. Improvement in fibrosis=≥1-point reduction in HAI score. Cohort participants had to have adequate baseline and long-term biopsy samples and baseline Knodell scores ≥2. (NCT01438424)
Timeframe: Baseline to Week 192

InterventionPercentage of participants (Number)
Improvement in fibrosis (n=56) (Week 48)Improvement in fibrosis (n=57) (Long-term biopsy)
Entecavir, 0.5 or 1.0 mg, With or Without Lamivudine3288

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Week 192: Percentage of Participants With Histologic Improvement (Efficacy Evaluable Cohort)

The Knodell Histologic Activity Index scores stage of necrosis and grade of inflammation in liver biopsies. Components are necrosis near the portal vein, intralobular degeneration and focal necrosis, portal inflammation, and fibrosis. The 4 components are scored from 1 to 4 and 1 to 10 (necrosis near the portal vein) and combined for a total score, with 22 being the highest possible score. Higher the score for each component=greater liver damage. Histologic improvement=a ≥2-point reduction in total Knodell score and no worsening in fibrosis. Cohort participants had to have adequate baseline and long-term biopsy samples and baseline Knodell necroinflammatory scores ≥2. (NCT01438424)
Timeframe: Baseline to Week 192

InterventionPercentage of participants (Number)
Histologic improvement (n=56) (Week 48)Histologic improvement (n=57) (Long-term biopsy)
Entecavir, 0.5 or 1.0 mg, With or Without Lamivudine7396

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Week 192: Number of Participants With Death As Outcome, Any AE, Grade 3-4 AEs, SAEs, Discontinuations Due to AEs, and Abnormalities in Selected Laboratory Test Results

An AE is any new unfavorable symptom, sign, or disease or worsening of a preexisting condition that does not necessarily have a causal relationship with treatment. An SAE is any unfavorable medical event that at any dose results in death, persistent or significant disability/incapacity, or drug dependency or abuse; is life-threatening, an important medical event, or a congenital anomaly/birth defect; or requires or prolongs hospitalization. CTC Grade 1=mild; Grade 2=moderate; Grade 3=severe; Grade 4=life-threatening or disabling. ALT=alanine aminotransferase; ULN=upper limit of normal. (NCT01438424)
Timeframe: Continuously from Day 1 through Week 192

InterventionParticipants (Number)
Deaths on studyMalignant neoplasmsSAEsDiscontinuations due to AEsAny AEGrade 3 and 4 AEsALT flares (ALT>2*entry and >10*ULN)ALT >5.0*ULNTotal bilirubin >2.5*ULNLipase >2.0*ULNCreatinine ≥0.3 mg/dL from baselineHypocarbia Grades 3-4
Entecavir, 0.5 or 1.0 mg QD, With or Without Lamivudine182713511862174301753281805

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Off-treatment Follow-up: Percentage of Participants With Sustained HBV DNA <1,000, <300, and <10,000 Copies/mL by PCR Assay and With ALT ≤1*ULN (Amendment 11 Cohort)

The Amendment 11 Cohort consisted of participants who were HBeAg negative and who had compensated liver disease, a minimum of 192 weeks (4 years) of treatment with entecavir, HBV DNA <300 copies/mL by PCR Assay for ≥48 weeks before end of dosing and on the last observed result ≤24 weeks prior to end of dosing, and serum ALT levels ≤1.0*ULN at the end of study drug dosing. ULN=upper limit of normal. (NCT01438424)
Timeframe: End of dosing to Weeks 48 and 96 off-treatment follow-up

InterventionPercentage of participants (Number)
Off-treatment Week 48 <1000 copies/mLOff-treatment Week 96 <1000 copies/mLOff-treatment Week 48 <300 copies/mLOff-treatment Week 96 <300 copies/mLOff treatment Week 96 <10,000 copies/mLOff treatment Week 48: ALT ≤1*ULNOff treatment Week 96: ALT ≤1*ULN
Entecavir, 0.5 or 1.0 mg, With or Without Lamivudine101073143124

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Percentage of Participants Who Achieved HBV DNA <300 and <10^4 Copies/mL by PCR Assay and ALT ≤1.0*Upper Limit of Normal (ULN) (Entecavir Retreatment Cohort)

The Entecavir Retreatment Cohort consisted of participants who were nucleoside-naive, HBeAg-negative and enrolled from BMS study AI463-027 with >60 days off treatment between the last dose in AI463-027 and the first dose in the current study. This cohort permitted assessment of entecavir, 1.0 mg, provided as retreatment in the current study. (NCT01438424)
Timeframe: Baseline to Weeks 48, 96, and 144

InterventionPercentage of participants (Number)
Week 48: HBV DNA <300 copies/mL (n=119)Week 48: HBV DNA <10^4 copies/mL (n=88)Week: 48: ALT ≤1.0*ULN (n=95)Week 96: HBV DNA <300 copies/mL (n=74)Week: 96: ALT ≤1.0*ULN (n=76)Week 144: HBV DNA <300 copies/mL (n=57)Week 144: ALT ≤1.0*ULN (n=66)
Entecavir, 0.5 or 1.0 mg, With or Without Lamivudine88878391799586

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Week 144: Percentage of Participants Who Achieved HBV DNA <300 Copies/mL by PCR Assay and ALT ≤1.0*ULN (Lamivudine Retreatment Switch Cohort)

The Lamivudine Retreatment Switch Cohort consisted of participants who were nucleoside-naive HBeAg negative and enrolled from BMS study AI463-027 (NCT00035789) with >60 days between end of dosing in AI463-027 and the switch to entecavir in the current study. This cohort permitted assessment of entecavir, 1.0 mg, provided as switch therapy in the current study. (NCT01438424)
Timeframe: Baseline to Week 144

InterventionPercentage of participants (Number)
HBV DNA <300 copies/mL (n=67)Achieved ALT ≤1.0*ULN (n=73)
Entecavir, 0.5 or 1.0 mg, With or Without Lamivudine9985

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Percentage of Participants Who Achieved HBV DNA <300 Copies/mL by PCR Assay, Loss of HBeAG, Seroconversion, and ALT ≤1.0*Upper Limit of Normal (ULN) (Entecavir Continuous Treatment Cohort)

The Entecavir Continuous Treatment Cohort consisted of participants from study AI463-022 (NCT00035633) who were nucleoside-naive HBeAg-positive and enrolled in the current study with ≤35 days off treatment between the last dose in AI463-022 and the first dose in the current. This cohort is considered to be on continuous entecavir treatment and permitted assessment of continuous administration of entecavir in AI463-022 and the current study. (NCT01438424)
Timeframe: Baseline to Weeks 48, 96, 144, 192, and 240

InterventionPercentage of participants (Number)
Week 48: HBV DNA <300 copies/mL (n=146)Week 96: HBV DNA <300 copies/mL (n=140)Week 144: HBV DNA <10^4 copies/mL (n=131)Week 192: HBV DNA < 10^4 copies/mL (n=108)Week 240: HBV DNA <300 copies/mL (n=94)Week 48: Loss of HBeAg (n=146)Week 96: Loss of HBeAg (n=140)Week 144: Loss of HBeAg (n=132)Week 192: Loss of HBeAg (n=111)Week 240: Loss of HBeAg (n=95)Week 48: Seroconversion (n=146)Week 96: Seroconversion (n=140)Week 144: Seroconversion (n=133)Week 192: Seroconversion (n=111)Week 240: Seroconversion (n=95)Week 48: ALT ≤1.0*ULN (n=146)Week 96: ALT ≤1.0*ULN (n=140)Week 144: ALT ≤1.0*ULN (n=134)Week 192: ALT ≤1.0*ULN (n=112)Week 240: ALT ≤1.0*ULN (n=98)
Entecavir, 0.5 or 1.0 mg, With or Without Lamivudine558389919414303941131716176578778680

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Week 144: Percentage of Participants Who Achieved HBV DNA <300 Copies/mL by PCR Assay and ALT ≤1.0*ULN (Lamivudine Continuous Switch Cohort)

The Lamivudine Continuous Switch Cohort consisted of participants who were nucleoside-naive, HBeAg-positive and received lamivudine in BMS study AI463-022 (NCT00035633) and enrolled in the current study with ≤35 days off treatment between end of dosing in AI463-022 and the switch to entecavir in the current study. This cohort permitted assessment of entecavir, 1.0 mg, provided as switch therapy in the current study. (NCT01438424)
Timeframe: Baseline to Week 144

InterventionPercentage of participants (Number)
HBV DNA <300 copies/mL (n=130)Achieved ALT ≤1.0*ULN (n=135)
Entecavir, 0.5 or 1.0 mg, With or Without Lamivudine6568

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Number of Participants With Treatment-Emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)

An adverse event (AE) is any untoward medical occurrence which does not necessarily have a causal relationship with this treatment. An SAE is any AE that: results in death; is life-threatening; requires inpatient hospitalization or prolongation of an existing hospitalization; results in persistent or significant disability/incapacity; is a congenital anomaly/birth defect; or is a medically important event or reaction.Events were categorized as mild, moderate or severe. TEAEs were defined as all AEs starting or worsening after commencement of treatment with investigational product. A treatment-related TEAE was one whose relationship to treatment was noted as unlikely, possibly, or probably related. (NCT02065336)
Timeframe: through Day 85 (Cohorts 1-7) and through 24 weeks post-last dose (last dose: Day 85 Cohort 9; Day 225 Cohort 10)

,,,,,,,,,
InterventionParticipants (Count of Participants)
Any TEAEAny mild TEAEAny moderate TEAEAny severe TEAEAny TEAE related to study drugAny TEAE leading to discontinuation of treatmentAny SAEAny SAE related to study drugAny life-threatening SAEAny SAE leading to death
ARC-520 Cohort 11100000000
ARC-520 Cohort 107700400000
ARC-520 Cohort 24310000000
ARC-520 Cohort 31100000000
ARC-520 Cohort 40000000000
ARC-520 Cohort 51100000000
ARC-520 Cohort 61100000000
ARC-520 Cohort 71100000000
ARC-520 Cohort 91100000000
Placebo Normal Saline Cohorts 1-50000000000

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Number of Participants With Negative Bee Venom Allergy Test Results at Baseline, Day 29, and Day 85

Bee venom allergy tests were used to assess immunoglobulin E (IgE) in Cohorts 1-7. Analysis values less than 0.35 kU/L were taken as negative. (NCT02065336)
Timeframe: Baseline, Day 29, Day 85

,,,,,,,
InterventionParticipants (Count of Participants)
BaselineDay 29Day 85
ARC-520 Cohort 1666
ARC-520 Cohort 2666
ARC-520 Cohort 3666
ARC-520 Cohort 4666
ARC-520 Cohort 5666
ARC-520 Cohort 6666
ARC-520 Cohort 7121111
Placebo Normal Saline Cohorts 1-5101010

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Change From Baseline Over Time in Quantitative Hepatitis B Surface Antigen (HBsAG)

(NCT02065336)
Timeframe: Baseline, through Day 85 (Cohorts 1-7) and through 24 weeks post-last dose (last dose: Day 85 Cohort 9; Day 253 Cohort 10)

,,,,,
InterventionIU/mL (Mean)
Day 3Day 8Day 15Day 22Day 29Day 43Day 57Day 85
ARC-520 Cohort 3-1003.6-884.3-470.8-204.393.3-1471.8-2330.1-2119.3
ARC-520 Cohort 4-1501.0-2591.2-3069.0-2978.8-2972.8-3219.8-2813.0-926.3
ARC-520 Cohort 5-1664.7-1789.8-1672.8-1951.7-1964.3-1939.7-1536.0-537.5
ARC-520 Cohort 2-1194.0-2179.2-2260.8-2266.2-1826.3-1288.8-1056.7-542.8
ARC-520 Cohort 7-12401.1-20123.8-22915.6-23872.7-24148.3-23932.0-22658.4-20827.2
Placebo Normal Saline Cohorts 1-543.342.2236.6115.1168.858.3156.1225.4

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Change From Baseline Over Time in Quantitative Hepatitis B Surface Antigen (HBsAG)

(NCT02065336)
Timeframe: Baseline, through Day 85 (Cohorts 1-7) and through 24 weeks post-last dose (last dose: Day 85 Cohort 9; Day 253 Cohort 10)

InterventionIU/mL (Mean)
Day 3Day 8Day 22Day 29Day 43Day 57Day 85
ARC-520 Cohort 6-948.0-1344.0-1553.7-1532.3-1566.8-1370.7-791.0

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Change From Baseline Over Time in Quantitative Hepatitis B Surface Antigen (HBsAG)

(NCT02065336)
Timeframe: Baseline, through Day 85 (Cohorts 1-7) and through 24 weeks post-last dose (last dose: Day 85 Cohort 9; Day 253 Cohort 10)

InterventionIU/mL (Mean)
Day 3Day 8Day 15Day 22Day 29Day 43Day 85
ARC-520 Cohort 1-554.8-928.1-1055.1-1225.4-579.1-1020.1-670.1

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Change From Baseline Over Time in Quantitative Hepatitis B Surface Antigen (HBsAG)

(NCT02065336)
Timeframe: Baseline, through Day 85 (Cohorts 1-7) and through 24 weeks post-last dose (last dose: Day 85 Cohort 9; Day 253 Cohort 10)

InterventionIU/mL (Mean)
Day 1Day 29Day 57Day 85Day 113Day 141Day 169Day 197Day 225Day 253
ARC-520 Cohort 10-19222-22617-22840-23305-23205-23182-26481-30234-1249-643

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Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Terminal Elimination Half-Life (t1/2), Cohorts 1-5

(NCT02065336)
Timeframe: Day 1 predose, immediately prior to the end of infusion, 0.5, 1, 3, 6, 24, and 48 hours postdose

,,,,
Interventionhours (Median)
AD0009AD0010
ARC-520 Cohort 14.385.29
ARC-520 Cohort 25.366.32
ARC-520 Cohort 34.645.48
ARC-520 Cohort 44.184.79
ARC-520 Cohort 54.325.36

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Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Area Under the Plasma Concentration-Time Curve From Time 0 Extrapolated to Infinity (AUCinf), Cohorts 1-5 Only

(NCT02065336)
Timeframe: Day 1 predose, immediately prior to the end of infusion, 0.5, 1, 3, 6, 24, and 48 hours postdose

,,,,
Interventionµg*hr/mL (Mean)
AD0009AD0010
ARC-520 Cohort 181.497.8
ARC-520 Cohort 2196207
ARC-520 Cohort 3218318
ARC-520 Cohort 4326386
ARC-520 Cohort 5356435

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Pharmacokinetics of ARC-520 of ARC-520 Product Constituents AD0009 and AD0010: Area Under the Plasma Concentration-Time Curve From Time 0 to the Last Quantifiable Plasma Concentration (AUClast), Cohorts 1-5

(NCT02065336)
Timeframe: Day 1 predose, immediately prior to the end of infusion, 0.5, 1, 3, 6, 24, and 48 hours postdose

,,,,
Interventionµg*hr/mL (Mean)
AD0009AD0010
ARC-520 Cohort 181.497.6
ARC-520 Cohort 2196205
ARC-520 Cohort 3218317
ARC-520 Cohort 4326385
ARC-520 Cohort 5356434

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Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Apparent Volume of Distribution During the Terminal Phase (Vz), Cohorts 1-5

(NCT02065336)
Timeframe: Day 1 predose, immediately prior to the end of infusion, 0.5, 1, 3, 6, 24, and 48 hours postdose

,,,,
InterventionmL/kg (Mean)
AD0009AD0010
ARC-520 Cohort 139.539.4
ARC-520 Cohort 243.246.1
ARC-520 Cohort 345.737.1
ARC-520 Cohort 439.037.9
ARC-520 Cohort 535.436.9

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Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Area Under the Plasma Concentration-Time Curve From Time 0 to 24 Hours (AUC0-24), Cohorts 1-5

(NCT02065336)
Timeframe: Day 1 predose, immediately prior to the end of infusion, 0.5, 1, 3, 6, 24, and 48 hours postdose

,,,,
Interventionµg*hr/mL (Mean)
AD0009AD0010
ARC-520 Cohort 179.193.0
ARC-520 Cohort 2185190
ARC-520 Cohort 3212301
ARC-520 Cohort 4318370
ARC-520 Cohort 5349412

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Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Clearance (CL), Cohorts 1-5

(NCT02065336)
Timeframe: Day 1 predose, immediately prior to the end of infusion, 0.5, 1, 3, 6, 24, and 48 hours postdose

,,,,
InterventionmL/hr/kg (Mean)
AD0009AD0010
ARC-520 Cohort 16.215.16
ARC-520 Cohort 25.585.08
ARC-520 Cohort 37.114.84
ARC-520 Cohort 46.475.41
ARC-520 Cohort 55.704.65

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Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Maximum Observed Plasma Concentration (Cmax), Cohorts 1-5

(NCT02065336)
Timeframe: Day 1 predose, immediately prior to the end of infusion, 0.5, 1, 3, 6, 24, and 48 hours postdose

,,,,
Interventionµg/mL (Mean)
AD0009AD0010
ARC-520 Cohort 113.712.7
ARC-520 Cohort 226.422.5
ARC-520 Cohort 333.539.7
ARC-520 Cohort 454.850.5
ARC-520 Cohort 558.252.4

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Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Terminal Elimination Rate Constant (Kel), Cohorts 1-5

(NCT02065336)
Timeframe: Day 1 predose, immediately prior to the end of infusion, 0.5, 1, 3, 6, 24, and 48 hours postdose

,,,,
Intervention1/hr (Mean)
AD0009AD0010
ARC-520 Cohort 10.1570.132
ARC-520 Cohort 20.1320.111
ARC-520 Cohort 30.1540.130
ARC-520 Cohort 40.1650.142
ARC-520 Cohort 50.1610.126

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Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Volume in Steady State (Vss), Cohorts 1-5

(NCT02065336)
Timeframe: Day 1 predose, immediately prior to the end of infusion, 0.5, 1, 3, 6, 24, and 48 hours postdose

,,,,
InterventionmL/kg (Mean)
AD0009AD0010
ARC-520 Cohort 139.640.7
ARC-520 Cohort 245.846.7
ARC-520 Cohort 345.338.1
ARC-520 Cohort 439.639.8
ARC-520 Cohort 535.338.5

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Change From Baseline in Entecavir Plasma Trough Concentration, Cohorts 1-7

(NCT02065336)
Timeframe: Baseline, Days 1, 2, 3, 8, 15, 22, 29

,,,,,,
Interventionng/mL (Mean)
Day 1Day 2Day 3Day 8Day 15Day 22Day 29
ARC-520 Cohort 100.06-0.02-0.010.010.040.00
ARC-520 Cohort 200.06-0.06-0.09-0.03-0.02-0.01
ARC-520 Cohort 300.13-0.06-0.09-0.03-0.030.01
ARC-520 Cohort 60-0.91-1.04-1.01-1.01-1.00-1.00
ARC-520 Cohort 700.160.150.450.320.330.36
ARC-520 Cohorts 4 and 500.120.12-0.030.000.000.00
Placebo Normal Saline Cohorts 1-50-0.31-0.29-0.30-0.10-0.30-0.30

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Serum Concentration of Peg-INF-Alfa-2A

The serum concentration of Peg-INF-Alfa-2A was measured in picogram/milliliter. (NCT02263079)
Timeframe: At Weeks 12, 16, 20, 32, 44, 56

Interventionpg/mL (Mean)
Week 12 PredoseWeek 16 PredoseWeek 20 PredoseWeek 32 PredoseWeek 32 24-48h Post-doseWeek 32 72-96h Post-doseWeek 32 168h Post-doseWeek 44 PredoseWeek 56 Predose
Peg-IFN-Alfa-2A + Lamivudine or Entecavir84301630013800149002270023000193002190025400

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Percentage of Participants With AEs Leading to Dose Modification or Interruption

This endpoint measures AEs and lab abnormalities leading to dose interruption or dose modification. Does modification included dose reduced, dose increased or drug interrupted. Adverse events included laboratory abnormalities reported as adverse events. (NCT02263079)
Timeframe: Baseline up to 24 weeks post-end of treatment

InterventionPercentage of Participants (Number)
Peg-IFN-Alfa-2A + Lamivudine or Entecavir23.0

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Percentage of Participants With Loss of HBsAg

This endpoint is defined as loss of HBsAg at 1 year post-treatment in the treated group. The 95% Confidence Interval of response rate is calculated by Clopper-Pearson method. (NCT02263079)
Timeframe: 1 year post-end of treatment (End of treatment = Week 56)

InterventionPercentage of Participants (Number)
Peg-IFN-Alfa-2A + Lamivudine or Entecavir3.8

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Percentage of Participants With Loss of Hepatitis B Surface Antigen (HBsAg) at 24 Weeks Post-End of Treatment/End of Untreated Observation

This endpoint is defined as loss of HBsAg at 24 weeks post-treatment (follow-up Week 24)/end of untreated observation (Week 80). The percentage of responders (response rate) and 95% CI (using the Clopper-Pearson method) for the response rate are presented for each group. (NCT02263079)
Timeframe: 24 weeks post-treatment/at the end of untreated observation (Week 80)

InterventionPercentage of Participants (Number)
Peg-IFN-Alfa-2A + Lamivudine or Entecavir3.8
Untreated Control Participants0

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Change From Baseline in HBV DNA Levels in the Peg-INF-Alfa-2A (Treated) Arm

This outcome measure presents HBV DNA levels measured at defined time points from baseline in the Peg-INF-Alfa-2A + Lamivudine or Entecavir arm. (NCT02263079)
Timeframe: Baseline, Week 8, 20, 32, 44, 56, Follow up Week 4 and 24

Interventionlog10 IU/mL (Mean)
BaselineWeek 8Week 20Week 32Week 44Week 56Fu Week 4Fu Week 24
Peg-IFN-Alfa-2A + Lamivudine or Entecavir8.024.743.542.562.152.214.347.31

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Change From Baseline in HBV DNA Levels in the Untreated Control Participants

This outcome measure presents HBV DNA levels measured at defined time points from baseline in the Untreated Control arm. (NCT02263079)
Timeframe: Baseline, Week 32, 56 and end of untreated observation (Week 80)

Interventionlog10 IU/mL (Mean)
BaselineWeek 32Week 56Week 80
Untreated Control Participants8.228.297.577.24

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Percentage of Participants With Adverse Events (AEs)

An adverse event is any untoward medical occurrence in a participant administered a pharmaceutical product and which does not necessarily have to have a causal relationship with the treatment. An adverse event can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding, for example), symptom, or disease temporally associated with the use of a pharmaceutical product, whether or not considered related to the pharmaceutical product. Preexisting conditions which worsen during a study are also considered as adverse events. (NCT02263079)
Timeframe: Baseline up to 24 weeks post-treatment/end of untreated observation (Week 80)

,
InterventionPercentage of Participants (Number)
With at least one Non-Serious AEWith at least one Serious Adverse Event (SAE)
Peg-IFN-Alfa-2A + Lamivudine or Entecavir92.30
Untreated Control Participants45.53.0

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Percentage of Participants With Combined Response for HBeAg Seroconversion (Defined as Loss of HBeAg and Presence of Anti-HBe) and HBV DNA Levels <20,000 IU/mL

This endpoint measures the combined response for HBeAg Seroconversion and HBV DNA Levels <20,000 IU/mL at 24 weeks post-treatment (follow-up Week 24)/end of untreated observation (Week 80) and at 1 year post-end of treatment in the treated group. The HBeAg is defined as loss of HBeAg and presence of anti-HBe. The 95% Confidence Interval of response rate is calculated by Clopper-Pearson method. (NCT02263079)
Timeframe: 24 weeks post-treatment /end of untreated observation (Week 80), and 1 year post-end of treatment (End of treatment = Week 56)

InterventionPercentage of Participants (Number)
24 Weeks post-treatment/Week 80
Untreated Control Participants9.1

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Percentage of Participants With Combined Response for HBeAg Seroconversion (Defined as Loss of HBeAg and Presence of Anti-HBe) and HBV DNA Levels <20,000 IU/mL

This endpoint measures the combined response for HBeAg Seroconversion and HBV DNA Levels <20,000 IU/mL at 24 weeks post-treatment (follow-up Week 24)/end of untreated observation (Week 80) and at 1 year post-end of treatment in the treated group. The HBeAg is defined as loss of HBeAg and presence of anti-HBe. The 95% Confidence Interval of response rate is calculated by Clopper-Pearson method. (NCT02263079)
Timeframe: 24 weeks post-treatment /end of untreated observation (Week 80), and 1 year post-end of treatment (End of treatment = Week 56)

InterventionPercentage of Participants (Number)
24 Weeks post-treatment/Week 801 year post-end of treatment
Peg-IFN-Alfa-2A + Lamivudine or Entecavir0.07.7

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Percentage of Participants With Combined Response for HBeAg Seroconversion (Defined as Loss of HBeAg and Presence of Anti-HBe) and HBV DNA Levels <2000 IU/mL

This endpoint measures the combined response for HBeAg Seroconversion and HBV DNA Levels <2000 IU/mL at 24 weeks post-treatment (follow-up Week 24)/end of untreated observation (Week 80) and at 1 year post-end of treatment in the treated group. The HBeAg is defined as loss of HBeAg and presence of anti-HBe. The 95% Confidence Interval of response rate is calculated by Clopper-Pearson method. (NCT02263079)
Timeframe: 24 weeks post-treatment /end of untreated observation (Week 80), and 1 year post-end of treatment (End of treatment = Week 56)

InterventionPercentage of Participants (Number)
24 Weeks post-treatment/Week 80
Untreated Control Participants9.1

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Percentage of Participants With Combined Response for HBeAg Seroconversion (Defined as Loss of HBeAg and Presence of Anti-HBe) and HBV DNA Levels <2000 IU/mL

This endpoint measures the combined response for HBeAg Seroconversion and HBV DNA Levels <2000 IU/mL at 24 weeks post-treatment (follow-up Week 24)/end of untreated observation (Week 80) and at 1 year post-end of treatment in the treated group. The HBeAg is defined as loss of HBeAg and presence of anti-HBe. The 95% Confidence Interval of response rate is calculated by Clopper-Pearson method. (NCT02263079)
Timeframe: 24 weeks post-treatment /end of untreated observation (Week 80), and 1 year post-end of treatment (End of treatment = Week 56)

InterventionPercentage of Participants (Number)
24 Weeks post-treatment/Week 801 year post-end of treatment
Peg-IFN-Alfa-2A + Lamivudine or Entecavir0.07.7

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Percentage of Participants With Different Hepatitis B Virus (HBV) Deoxyribonucleic Acid (DNA) Levels (Less Than [<] 20,000 International Units Per Milliliter [IU/mL], < 2000 IU/mL, or Undetectable HBV DNA)

This endpoint measures different HBV DNA levels (<20000 IU/mL, <2000 IU/mL and undetectable) measured by PCR or hybridization at 24 weeks post-treatment (follow-up Week 24)/end of untreated observation (Week 80) and at 1 year post-treatment in the treated group. HBV-DNA undetectable is defined as <29 IU/mL. The 95% Confidence Interval of response rate is calculated by Clopper-Pearson method. (NCT02263079)
Timeframe: 24 weeks post-treatment /end of untreated observation (Week 80), and 1 year post-end of treatment (End of treatment = Week 56)

InterventionPercentage of Participants (Number)
HBV-DNA <20000 IU/mL at follow up Week 24/Week 80HBV-DNA <2000 IU/mL at follow up Week 24/Week 80HBV-DNA Undetectable at follow up Week 24/Week 80
Untreated Control Participants12.112.16.1

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Percentage of Participants With Different Hepatitis B Virus (HBV) Deoxyribonucleic Acid (DNA) Levels (Less Than [<] 20,000 International Units Per Milliliter [IU/mL], < 2000 IU/mL, or Undetectable HBV DNA)

This endpoint measures different HBV DNA levels (<20000 IU/mL, <2000 IU/mL and undetectable) measured by PCR or hybridization at 24 weeks post-treatment (follow-up Week 24)/end of untreated observation (Week 80) and at 1 year post-treatment in the treated group. HBV-DNA undetectable is defined as <29 IU/mL. The 95% Confidence Interval of response rate is calculated by Clopper-Pearson method. (NCT02263079)
Timeframe: 24 weeks post-treatment /end of untreated observation (Week 80), and 1 year post-end of treatment (End of treatment = Week 56)

InterventionPercentage of Participants (Number)
HBV-DNA <20000 IU/mL at follow up Week 24/Week 80HBV-DNA <2000 IU/mL at follow up Week 24/Week 80HBV-DNA Undetectable at follow up Week 24/Week 80HBV-DNA <20000 IU/mL 1 year post-end of treatmentHBV-DNA <2000 IU/mL 1 year post-end of treatmentHBV-DNA Undetectable 1 year post-end of treatment
Peg-IFN-Alfa-2A + Lamivudine or Entecavir7.77.70.015.47.70.0

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Percentage of Participants With Loss of Hepatitis B Virus Envelope Antigen (HBeAg)

This endpoint is defined as loss of HBeAg at 24 weeks post-treatment (follow-up Week 24)/end of untreated observation (Week 80) and at 1 year post-end of treatment in the treated group. The 95% Confidence Interval of response rate is calculated by Clopper-Pearson method. (NCT02263079)
Timeframe: 24 weeks post-treatment /end of untreated observation (Week 80), and 1 year post-end of treatment (End of treatment = Week 56)

InterventionPercentage of Participants (Number)
24 Weeks post-treatment/Week 80
Untreated Control Participants12.1

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Percentage of Participants With Loss of Hepatitis B Virus Envelope Antigen (HBeAg)

This endpoint is defined as loss of HBeAg at 24 weeks post-treatment (follow-up Week 24)/end of untreated observation (Week 80) and at 1 year post-end of treatment in the treated group. The 95% Confidence Interval of response rate is calculated by Clopper-Pearson method. (NCT02263079)
Timeframe: 24 weeks post-treatment /end of untreated observation (Week 80), and 1 year post-end of treatment (End of treatment = Week 56)

InterventionPercentage of Participants (Number)
24 Weeks post-treatment/Week 801 year post-end of treatment
Peg-IFN-Alfa-2A + Lamivudine or Entecavir3.811.5

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Percentage of Participants With Seroconversion to Hepatitis B Envelope Antibody (Anti-HBe), Defined as Loss of HBeAg and Presence of Anti-HBe

This endpoint measures the seroconversion to anti-HBe defined as loss of HBeAg and presence of anti-HBe at 24 weeks post-treatment (follow-up Week 24)/end of untreated observation (Week 80) and at 1 year post-end of treatment in the treated group. The 95% Confidence Interval of response rate is calculated by Clopper-Pearson method. (NCT02263079)
Timeframe: 24 weeks post-treatment /end of untreated observation (Week 80), and 1 year post-end of treatment (End of treatment = Week 56)

InterventionPercentage of Participants (Number)
24 Weeks post-treatment/Week 80
Untreated Control Participants9.1

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Percentage of Participants With Seroconversion to Hepatitis B Envelope Antibody (Anti-HBe), Defined as Loss of HBeAg and Presence of Anti-HBe

This endpoint measures the seroconversion to anti-HBe defined as loss of HBeAg and presence of anti-HBe at 24 weeks post-treatment (follow-up Week 24)/end of untreated observation (Week 80) and at 1 year post-end of treatment in the treated group. The 95% Confidence Interval of response rate is calculated by Clopper-Pearson method. (NCT02263079)
Timeframe: 24 weeks post-treatment /end of untreated observation (Week 80), and 1 year post-end of treatment (End of treatment = Week 56)

InterventionPercentage of Participants (Number)
24 Weeks post-treatment/Week 801 year post-end of treatment
Peg-IFN-Alfa-2A + Lamivudine or Entecavir0.07.7

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Percentage of Participants With Seroconversion to Hepatitis B Surface Antibody (Anti-HBs), Defined as Loss of HBsAg and Presence of Anti-HBs

This endpoint measures the seroconversion to anti-HBs defined as loss of HBsAg and presence of anti-HBs at 24 weeks post-treatment (follow-up Week 24)/end of untreated observation (Week 80) and at 1 year post-end of treatment in the treated group. The 95% Confidence Interval of response rate is calculated by Clopper-Pearson method. (NCT02263079)
Timeframe: 24 weeks post-treatment /end of untreated observation (Week 80), and 1 year post-end of treatment (End of treatment = Week 56)

InterventionPercentage of Participants (Number)
24 Weeks post-treatment/Week 80
Untreated Control Participants0.0

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Percentage of Participants With Seroconversion to Hepatitis B Surface Antibody (Anti-HBs), Defined as Loss of HBsAg and Presence of Anti-HBs

This endpoint measures the seroconversion to anti-HBs defined as loss of HBsAg and presence of anti-HBs at 24 weeks post-treatment (follow-up Week 24)/end of untreated observation (Week 80) and at 1 year post-end of treatment in the treated group. The 95% Confidence Interval of response rate is calculated by Clopper-Pearson method. (NCT02263079)
Timeframe: 24 weeks post-treatment /end of untreated observation (Week 80), and 1 year post-end of treatment (End of treatment = Week 56)

InterventionPercentage of Participants (Number)
24 Weeks post-treatment/Week 801 year post-end of treatment
Peg-IFN-Alfa-2A + Lamivudine or Entecavir3.83.8

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Number of Participants With Treatment-Emergent Adverse Events (TEAEs), Serious Adverse Events (SAEs), Deaths, and Discontinuations Due to Adverse Events (AEs)

An AE was defined as any untoward medical occurrence in a participant which does not necessarily have to have a causal relationship with treatment. An SAE was defined as any untoward medical occurrence that, at any dose: results in death; is life-threatening; requires inpatient hospitalization or prolongation of an existing hospitalization; results in persistent or significant disability/incapacity; is a congenital anomaly/birth defect; or is a medically important event or reaction. An AE was classified as a TEAE if the AE was not present prior to the first study medication administration and started at or after the time of initiation of administration of study medication, or if the AE presented prior to initiation of administration of study medication, continued and increased in intensity after administration of study medication. (NCT02452528)
Timeframe: From time of informed consent through Day 147 ± 3 days

,
InterventionParticipants (Count of Participants)
TEAEsSAEsDeathsDiscontinuations due to AEs
ARC-5200000
Placebo1000

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Number of Participants With Adverse Events (AEs), Serious AEs (SAEs), Deaths and Discontinuations Due to AEs

An AE is any untoward medical occurrence which does not necessarily have a causal relationship with this treatment. An SAE is any AE that: results in death; is life-threatening; requires inpatient hospitalization or prolongation of an existing hospitalization; results in persistent or significant disability/incapacity; is a congenital anomaly/birth defect; or is a medically important event or reaction. A treatment emergent AE (TEAE) was defined as an AE that was not present prior to the first study medication administration and started at/after the time of initiation of administration of study medication, or an AE which was present prior to initiation of study medication administration, which increased in severity after study medication administration. (NCT02604199)
Timeframe: Through Day 169

,,,
InterventionParticipants (Count of Participants)
≥ 1 AE≥ 1 TEAE≥ 1 Serious TEAEDeaths≥ 1 TEAE Leading to Study Discontinuation≥ 1 TEAE Leading to Treatment Discontinuation
ARC-520 Injection 1 mg/kg662000
ARC-520 Injection 2 mg/kg12121000
PBO High Dose540000
PBO Low Dose440000

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Change From Baseline in Quantitative Hepatitis B Surface Antigen (Log qHBsAg) Over Time

Change From Baseline in log qHBsAg at Day 113 in response to multiple doses of ARC-520 versus placebo, using a a mixed effect model for repeated measures (MMRM). Includes parameter baseline as a continuous covariate, and treatment and visit as fixed factors, interaction of treatment and visit, and interaction of parameter baseline and visit. (NCT02604199)
Timeframe: Baseline, Day 15, 29, 43, 57, 71, 85, 99

,,
Interventionlog IU/mL (Least Squares Mean)
Day 15Day 29Day 43Day 57Day 71Day 85Day 99
ARC-520 Injection 1 mg/kg3.0843.0983.0163.0723.0512.9072.938
ARC-520 Injection 2 mg/kg2.5062.5032.5092.3292.3012.3662.360
Placebo3.2973.2913.1883.2913.2063.3093.302

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Change From Baseline in Quantitative Hepatitis B Surface Antigen (Log qHBsAg) at Day 113

Change From Baseline in log qHBsAg at Day 113 in response to multiple doses of ARC-520 versus placebo, using a a mixed effect model for repeated measures (MMRM). Includes parameter baseline as a continuous covariate, and treatment and visit as fixed factors, interaction of treatment and visit, and interaction of parameter baseline and visit. (NCT02604199)
Timeframe: Baseline, Day 113

Interventionlog IU/mL (Least Squares Mean)
Placebo-0.070
ARC-520 Injection 1 mg/kg-0.157
ARC-520 Injection 2 mg/kg-0.379

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Change From Baseline at Day 99 in Log qHBsAg, by Category

Change in log qHBsAg from baseline, categorized into the following groups: no decrease, decrease > 0 to < 0.5 log IU/mL; decrease 0.5 to 1.0 log IU/mL; decrease > 1.0 log IU/mL, tabulated by dose and treatment for each visit. (NCT02604212)
Timeframe: Baseline, Day 99

Interventionlog IU/mL (Mean)
1 participant analyDecrease > 0 to < 0.5 log IU/mLDecrease 0.5 to 1.0 log IU/mLDecrease > 1.0 log IU/mL
ARC-520 2.0 mg/kg-0.343-0.652-1.011

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Change From Baseline at Day 99 in Log qHBsAg, by Category

Change in log qHBsAg from baseline, categorized into the following groups: no decrease, decrease > 0 to < 0.5 log IU/mL; decrease 0.5 to 1.0 log IU/mL; decrease > 1.0 log IU/mL, tabulated by dose and treatment for each visit. (NCT02604212)
Timeframe: Baseline, Day 99

Interventionlog IU/mL (Mean)
No Decrease1 participant analyDecrease > 0 to < 0.5 log IU/mL
Placebo0.027-0.160

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Change From Baseline at Day 99 in Log qHBsAg, by Category

Change in log qHBsAg from baseline, categorized into the following groups: no decrease, decrease > 0 to < 0.5 log IU/mL; decrease 0.5 to 1.0 log IU/mL; decrease > 1.0 log IU/mL, tabulated by dose and treatment for each visit. (NCT02604212)
Timeframe: Baseline, Day 99

Interventionlog IU/mL (Mean)
1 participant analyDecrease > 0 to < 0.5 log IU/mL
ARC-520 1.0 mg/kg-0.210

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Change From Baseline at Day 85 in Log qHBsAg, by Category

Change in log qHBsAg from baseline, categorized into the following groups: no decrease, decrease > 0 to < 0.5 log IU/mL; decrease 0.5 to 1.0 log IU/mL; decrease > 1.0 log IU/mL, tabulated by dose and treatment for each visit. (NCT02604212)
Timeframe: Baseline, Day 85

Interventionlog IU/mL (Mean)
No Decrease1 participant analyDecrease > 0 to < 0.5 log IU/mL
Placebo0.009-0.112

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Change From Baseline at Day 85 in Log qHBsAg, by Category

Change in log qHBsAg from baseline, categorized into the following groups: no decrease, decrease > 0 to < 0.5 log IU/mL; decrease 0.5 to 1.0 log IU/mL; decrease > 1.0 log IU/mL, tabulated by dose and treatment for each visit. (NCT02604212)
Timeframe: Baseline, Day 85

Interventionlog IU/mL (Mean)
1 participant analyDecrease > 0 to < 0.5 log IU/mLDecrease 0.5 to 1.0 log IU/mL
ARC-520 2.0 mg/kg-0.293-0.684

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Change From Baseline at Day 85 in Log qHBsAg, by Category

Change in log qHBsAg from baseline, categorized into the following groups: no decrease, decrease > 0 to < 0.5 log IU/mL; decrease 0.5 to 1.0 log IU/mL; decrease > 1.0 log IU/mL, tabulated by dose and treatment for each visit. (NCT02604212)
Timeframe: Baseline, Day 85

Interventionlog IU/mL (Mean)
1 participant analyDecrease > 0 to < 0.5 log IU/mL
ARC-520 1.0 mg/kg-0.171

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Change From Baseline at Day 71 in Log qHBsAg, by Category

Change in log qHBsAg from baseline, categorized into the following groups: no decrease, decrease > 0 to < 0.5 log IU/mL; decrease 0.5 to 1.0 log IU/mL; decrease > 1.0 log IU/mL, tabulated by dose and treatment for each visit. (NCT02604212)
Timeframe: Baseline, Day 71

Interventionlog IU/mL (Mean)
No Decrease1 participant analyDecrease > 0 to < 0.5 log IU/mL
Placebo0.011-0.094

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Change From Baseline at Day 71 in Log qHBsAg, by Category

Change in log qHBsAg from baseline, categorized into the following groups: no decrease, decrease > 0 to < 0.5 log IU/mL; decrease 0.5 to 1.0 log IU/mL; decrease > 1.0 log IU/mL, tabulated by dose and treatment for each visit. (NCT02604212)
Timeframe: Baseline, Day 71

Interventionlog IU/mL (Mean)
1 participant analyDecrease > 0 to < 0.5 log IU/mLDecrease 0.5 to 1.0 log IU/mL
ARC-520 2.0 mg/kg-0.296-0.662

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Change From Baseline at Day 71 in Log qHBsAg, by Category

Change in log qHBsAg from baseline, categorized into the following groups: no decrease, decrease > 0 to < 0.5 log IU/mL; decrease 0.5 to 1.0 log IU/mL; decrease > 1.0 log IU/mL, tabulated by dose and treatment for each visit. (NCT02604212)
Timeframe: Baseline, Day 71

Interventionlog IU/mL (Mean)
1 participant analyDecrease > 0 to < 0.5 log IU/mL
ARC-520 1.0 mg/kg-0.235

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Change From Baseline at Day 57 in Log qHBsAg, by Category

Change in log qHBsAg from baseline, categorized into the following groups: no decrease, decrease > 0 to < 0.5 log IU/mL; decrease 0.5 to 1.0 log IU/mL; decrease > 1.0 log IU/mL, tabulated by dose and treatment for each visit. (NCT02604212)
Timeframe: Baseline, Day 57

Interventionlog IU/mL (Mean)
No Decrease1 participant analyDecrease > 0 to < 0.5 log IU/mL
Placebo0.027-0.067

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Change From Baseline at Day 57 in Log qHBsAg, by Category

Change in log qHBsAg from baseline, categorized into the following groups: no decrease, decrease > 0 to < 0.5 log IU/mL; decrease 0.5 to 1.0 log IU/mL; decrease > 1.0 log IU/mL, tabulated by dose and treatment for each visit. (NCT02604212)
Timeframe: Baseline, Day 57

Interventionlog IU/mL (Mean)
1 participant analyDecrease > 0 to < 0.5 log IU/mLDecrease 0.5 to 1.0 log IU/mL
ARC-520 2.0 mg/kg-0.276-0.571

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Change From Baseline at Day 43 in Log qHBsAg, by Category

Change in log qHBsAg from baseline, categorized into the following groups: no decrease, decrease > 0 to < 0.5 log IU/mL; decrease 0.5 to 1.0 log IU/mL; decrease > 1.0 log IU/mL, tabulated by dose and treatment for each visit. (NCT02604212)
Timeframe: Baseline, Day 43

Interventionlog IU/mL (Mean)
No Decrease1 participant analyDecrease > 0 to < 0.5 log IU/mLDecrease 0.5 to 1.0 log IU/mL
ARC-520 2.0 mg/kg0.017-0.275-0.633

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Change From Baseline at Day 43 in Log qHBsAg, by Category

Change in log qHBsAg from baseline, categorized into the following groups: no decrease, decrease > 0 to < 0.5 log IU/mL; decrease 0.5 to 1.0 log IU/mL; decrease > 1.0 log IU/mL, tabulated by dose and treatment for each visit. (NCT02604212)
Timeframe: Baseline, Day 43

Interventionlog IU/mL (Mean)
No Decrease1 participant analyDecrease > 0 to < 0.5 log IU/mL
Placebo0.022-0.050

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Change From Baseline at Day 43 in Log qHBsAg, by Category

Change in log qHBsAg from baseline, categorized into the following groups: no decrease, decrease > 0 to < 0.5 log IU/mL; decrease 0.5 to 1.0 log IU/mL; decrease > 1.0 log IU/mL, tabulated by dose and treatment for each visit. (NCT02604212)
Timeframe: Baseline, Day 43

Interventionlog IU/mL (Mean)
1 participant analyDecrease > 0 to < 0.5 log IU/mL
ARC-520 1.0 mg/kg-0.226

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Change From Baseline at Day 29 in Log qHBsAg, by Category

Change in log qHBsAg from baseline, categorized into the following groups: no decrease, decrease > 0 to < 0.5 log IU/mL; decrease 0.5 to 1.0 log IU/mL; decrease > 1.0 log IU/mL, tabulated by dose and treatment for each visit. (NCT02604212)
Timeframe: Baseline, Day 29

,
Interventionlog IU/mL (Mean)
No DecreaseDecrease > 0 to < 0.5 log IU/mL
ARC-520 2.0 mg/kg0.064-0.251
Placebo0.048-0.084

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Change From Baseline at Day 29 in Log qHBsAg, by Category

Change in log qHBsAg from baseline, categorized into the following groups: no decrease, decrease > 0 to < 0.5 log IU/mL; decrease 0.5 to 1.0 log IU/mL; decrease > 1.0 log IU/mL, tabulated by dose and treatment for each visit. (NCT02604212)
Timeframe: Baseline, Day 29

Interventionlog IU/mL (Mean)
Decrease > 0 to < 0.5 log IU/mL
ARC-520 1.0 mg/kg-0.129

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Change From Baseline at Day 15 in Log qHBsAg, by Category

Change in log qHBsAg from baseline, categorized into the following groups: no decrease, decrease > 0 to < 0.5 log IU/mL; decrease 0.5 to 1.0 log IU/mL; decrease > 1.0 log IU/mL, tabulated by dose and treatment for each visit. (NCT02604212)
Timeframe: Baseline, Day 15

Interventionlog IU/mL (Mean)
No DecreaseDecrease > 0 to < 0.5 log IU/mLDecrease 0.5 to 1.0 log IU/mL
ARC-520 2.0 mg/kg0.032-0.266-0.666

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Change From Baseline at Day 15 in Log qHBsAg, by Category

Change in log qHBsAg from baseline, categorized into the following groups: no decrease, decrease > 0 to < 0.5 log IU/mL; decrease 0.5 to 1.0 log IU/mL; decrease > 1.0 log IU/mL, tabulated by dose and treatment for each visit. (NCT02604212)
Timeframe: Baseline, Day 15

Interventionlog IU/mL (Mean)
No DecreaseDecrease > 0 to < 0.5 log IU/mL
Placebo0.026-0.035

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Change From Baseline at Day 15 in Log qHBsAg, by Category

Change in log qHBsAg from baseline, categorized into the following groups: no decrease, decrease > 0 to < 0.5 log IU/mL; decrease 0.5 to 1.0 log IU/mL; decrease > 1.0 log IU/mL, tabulated by dose and treatment for each visit. (NCT02604212)
Timeframe: Baseline, Day 15

Interventionlog IU/mL (Mean)
Decrease > 0 to < 0.5 log IU/mLDecrease 0.5 to 1.0 log IU/mL
ARC-520 1.0 mg/kg-0.153-0.707

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Change From Baseline at Day 113 in Log qHBsAg, by Category

Change in log qHBsAg from baseline, categorized into the following groups: no decrease, decrease > 0 to < 0.5 log IU/mL; decrease 0.5 to 1.0 log IU/mL; decrease > 1.0 log IU/mL, tabulated by dose and treatment for each visit. (NCT02604212)
Timeframe: Baseline, Day 113

Interventionlog IU/mL (Mean)
No Decrease1 participant analyDecrease > 0 to < 0.5 log IU/mL
Placebo0.042-0.115

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Change From Baseline at Day 113 in Log qHBsAg, by Category

Change in log qHBsAg from baseline, categorized into the following groups: no decrease, decrease > 0 to < 0.5 log IU/mL; decrease 0.5 to 1.0 log IU/mL; decrease > 1.0 log IU/mL, tabulated by dose and treatment for each visit. (NCT02604212)
Timeframe: Baseline, Day 113

Interventionlog IU/mL (Mean)
1 participant analyDecrease > 0 to < 0.5 log IU/mLDecrease 0.5 to 1.0 log IU/mL
ARC-520 2.0 mg/kg-0.359-0.726

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Change From Baseline at Day 113 in Log qHBsAg, by Category

Change in log qHBsAg from baseline, categorized into the following groups: no decrease, decrease > 0 to < 0.5 log IU/mL; decrease 0.5 to 1.0 log IU/mL; decrease > 1.0 log IU/mL, tabulated by dose and treatment for each visit. (NCT02604212)
Timeframe: Baseline, Day 113

Interventionlog IU/mL (Mean)
1 participant analyDecrease > 0 to < 0.5 log IU/mL
ARC-520 1.0 mg/kg-0.142

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Change From Baseline in Quantitative Hepatitis B Surface Antigen (Log qHBsAg) at Day 113

Change From Baseline in log qHBsAg at Day 113 in response to multiple doses of ARC-520 versus placebo, using a a mixed effect model for repeated measures (MMRM). Includes parameter baseline as a continuous covariate, and treatment and visit as fixed factors, interaction of treatment and visit, and interaction of parameter baseline and visit. (NCT02604212)
Timeframe: Baseline, Day 113

Interventionlog IU/mL (Least Squares Mean)
Placebo-0.104
ARC-520 1.0 mg/kg-0.146
ARC-520 2.0 mg/kg-0.542

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Number of Participants With Adverse Events (AEs), Serious AEs (SAEs), Deaths, and Discontinuations Due to AEs

An AE is any untoward medical occurrence which does not necessarily have to have a causal relationship with this treatment. A treatment emergent AE (TEAE) was defined as an AE that was not present prior to the first study drug administration and started at/after the time of initiation of administration of study drug, or an AE which was present prior to initiation of study drug administration, which increased in severity after study drug administration. An SAE is any untoward medical occurrence that, at any dose: results in death; is life-threatening; requires inpatient hospitalization or prolongation of an existing hospitalization; results in persistent or significant disability/incapacity; is a congenital anomaly/birth defect; is a medically important event or reaction. (NCT02604212)
Timeframe: Through Day 169 (± 3 days)

,,,
Interventionparticipants (Number)
≥ 1 AE≥ 1 TEAE≥ 1 Serious TEAEDeaths≥ 1 TEAE Leading to Study Discontinuation≥ 1 TEAE Leading to Treatment Discontinuation
ARC-520 1.0 mg/kg650000
ARC-520 2.0 mg/kg330000
Placebo High Dose Comparator000000
Placebo Low Dose Comparator440000

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Change From Baseline at Day 57 in Log qHBsAg, by Category

Change in log qHBsAg from baseline, categorized into the following groups: no decrease, decrease > 0 to < 0.5 log IU/mL; decrease 0.5 to 1.0 log IU/mL; decrease > 1.0 log IU/mL, tabulated by dose and treatment for each visit. (NCT02604212)
Timeframe: Baseline, Day 57

Interventionlog IU/mL (Mean)
1 participant analyDecrease > 0 to < 0.5 log IU/mL
ARC-520 1.0 mg/kg-0.176

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Change From Baseline in Log qHBsAg Over Time

Change From Baseline in log qHBsAg up to Day 99 in response to multiple doses of ARC-520 versus placebo, using a a mixed effect model for repeated measures (MMRM). Includes parameter baseline as a continuous covariate, and treatment and visit as fixed factors, interaction of treatment and visit, and interaction of parameter baseline and visit. (NCT02604212)
Timeframe: Baseline, Days 15, 29, 43, 57, 71, 85, 99

,,
Interventionlog IU/mL (Mean)
Day 15Day 29Day 43Day 57Day 71Day 85Day 99
ARC-520 1.0 mg/kg3.0693.1483.0973.1483.0883.1983.048
ARC-520 2.0 mg/kg3.0003.0272.8932.8822.7142.6982.606
Placebo3.7343.6923.8123.7933.7563.7433.767

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Number of Patients Experiencing Reductions in Serum HBsAg

To assess antiviral activity of REP 2139-Ca when combined with pegylated interferon on serum HBsAg. (NCT02726789)
Timeframe: 48 weeks (treatment)

InterventionParticipants (Count of Participants)
Experimental5

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Number of Patients Experiencing Reductions in Serum HBV DNA

To assess antiviral activity of REP 2139-Ca when combined with pegylated interferon on serum HBV DNA. (NCT02726789)
Timeframe: 48 weeks (treatment)

InterventionParticipants (Count of Participants)
Experimental5

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Number of Patients Experiencing Serum Anti-HBs > 10 mIU / ml

To assess antiviral activity of REP 2139-Ca when combined with pegylated interferon on anti-HBsAg antibody titer. (NCT02726789)
Timeframe: 48 weeks (treatment)

InterventionParticipants (Count of Participants)
Experimental5

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Number of Patients Experiencing Treatment Emergent Laboratory Test Abnormalities or Adverse Events.

To record side effects, symptoms and adverse effects of exposure to REP 2139-Ca when combined pegylated interferon. (NCT02726789)
Timeframe: 48 weeks (treatment)

InterventionParticipants (Count of Participants)
Experimental5

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Number of Participants With Treatment Emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)

An adverse event (AE) is any untoward medical occurrence which does not necessarily have a causal relationship with this treatment. An SAE is any AE that: results in death; is life-threatening; requires inpatient hospitalization or prolongation of an existing hospitalization; results in persistent or significant disability/incapacity; is a congenital anomaly/birth defect; or is a medically important event or reaction. A TEAE was defined as an AE that was not present prior to the first study medication administration and started at/after the time of initiation of administration of study medication, or an AE which was present prior to initiation of study medication administration, which increased in severity after study medication administration. (NCT02738008)
Timeframe: From first dose of study drug up to 28 weeks of treatment, plus up to 24 weeks of follow-up

,,
InterventionParticipants (Count of Participants)
AEsSAEs
Heparc-2002: ARC-520 1.0 mg/kg10
Heparc-2002: ARC-520 2.0 mg/kg40
Heparc-2003: ARC-520 2.0 mg/kg40

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Number of Participants With TEAEs: CHB Participants

An AE is any untoward medical occurrence which does not necessarily have a causal relationship with this treatment. A serious AE is any AE that: results in death; is life-threatening; requires inpatient hospitalization or prolongation of an existing hospitalization; results in persistent or significant disability/incapacity; is a congenital anomaly/birth defect; or is a medically important event or reaction.Events were categorized as mild, moderate or severe. TEAEs were defined as all AEs starting or worsening after commencement of treatment with investigational product. A treatment-related TEAE was one whose relationship to treatment was noted as unlikely, possibly, or probably related. (NCT02797522)
Timeframe: From first dose of study drug through Day 142 (± 3 days)

,,,
InterventionParticipants (Count of Participants)
>/= 1 TEAE>/= 1 Serious TEAE>/= 1 Related TEAE>/= 1 Related Serious TEAE
CHB Participants: Cohort 3b2000
CHB Participants: Cohort 3c4020
CHB Participants: Cohort 4b1111
CHB Participants: Cohort 4c1000

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Number of Participants With Treatment-Emergent Adverse Events (TEAEs): Healthy Volunteers

An adverse event (AE) is any untoward medical occurrence which does not necessarily have a causal relationship with this treatment. A serious AE is any AE that: results in death; is life-threatening; requires inpatient hospitalization or prolongation of an existing hospitalization; results in persistent or significant disability/incapacity; is a congenital anomaly/birth defect; or is a medically important event or reaction.Events were categorized as mild, moderate or severe. TEAEs were defined as all AEs starting or worsening after commencement of treatment with investigational product. A treatment-related TEAE was one whose relationship to treatment was noted as unlikely, possibly, or probably related. (NCT02797522)
Timeframe: From first dose of study drug through Day 29 (± 1 day)

,,,,,,
InterventionParticipants (Count of Participants)
>/= 1 TEAE>/= 1 Serious TEAE>/= 1 Related TEAE>/= 1 Related Serious TEAE
NHV Participants: Cohort 11000
NHV Participants: Cohort 22000
NHV Participants: Cohort 33010
NHV Participants: Cohort 44020
NHV Participants: Cohort 53020
NHV Participants: Cohort 62010
NHV Participants: Placebo10030

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Proportion of Patients With HBsAg Response at 24 Week of Therapy

HBsAg response is defined as serum HBsAg decline of at least 0.5 logs IU/ml (or HBsAg negativation) at week 24 compared to baseline. (NCT02881008)
Timeframe: 24 weeks

InterventionParticipants (Count of Participants)
Arm D0
Arm F0

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Proportion of Patients With HBV DNA Response at Week 24 of Therapy

HBV DNA response is defined as persistent reduction of HBV DNA by >1 log IU/ml or negativation at week 24 compared to baseline. (NCT02881008)
Timeframe: 24 weeks

InterventionParticipants (Count of Participants)
Arm D7
Arm F6

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Proportion of Patients With HBV DNA Response at Week 12 of Therapy

HBV DNA response is defined as persistent reduction of HBV DNA by >1 log IU/ml or negativation at week 12 compared to baseline. (NCT02881008)
Timeframe: 12 weeks

InterventionParticipants (Count of Participants)
Arm A2
Arm B0
Arm C2
Arm D8
Arm E1
Arm F6

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Proportion of Patients With Biochemical Response at 24 Weeks of Therapy

Biochemical response is defined as normalization of ALT level at week 24 compared to baseline. (NCT02881008)
Timeframe: 24 weeks

InterventionParticipants (Count of Participants)
Arm D5
Arm F3

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Proportion of Patients With cccDNA Response at 24 Week of Therapy

Virological cccDNA response is defined as reduction of intrahepatic cccDNA by 0.5 logs in comparison to baseline at week 24. (NCT02881008)
Timeframe: 24 weeks

InterventionParticipants (Count of Participants)
Arm F0

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Proportion of Patients With HBsAg Response at 12 Week of Therapy

HBsAg response is defined as serum HBsAg decline of at least 0.5 logs IU/ml (or HBsAg negativation) at week 12 compared to baseline. (NCT02881008)
Timeframe: 12 week

InterventionParticipants (Count of Participants)
Arm A0
Arm B0
Arm C1
Arm D0
Arm E0
Arm F0

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Proportion of Patients With Biochemical Response at 12 Weeks of Therapy

Biochemical response is defined as normalization of ALT level at week 12 compared to baseline. (NCT02881008)
Timeframe: 12 weeks

InterventionParticipants (Count of Participants)
Arm A3
Arm B4
Arm C4
Arm D4
Arm E2
Arm F4

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Apparent Total Body Clearance (CLT/F)

CLT/F is defined as the apparent total body clearance (NCT03083821)
Timeframe: Up to 24 hours

InterventionmL/min (Mean)
Baraclude397

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Area Under the Concentration-time Curve in One Dosing Interval [AUC(TAU)]

AUC(TAU) is defined as the area under the concentration-time curve in one dosing interval (NCT03083821)
Timeframe: Up to 24 hours

Interventionh*ng/mL (Mean)
Baraclude21.8

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Maximum Observed Plasma Concentration (Cmax)

Cmax is defined as the peak plasma concentration (NCT03083821)
Timeframe: Up to 24 hours

Interventionng/mL (Mean)
Baraclude8.17

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Observed Plasma Concentration at 24 Hours Postdose (C24)

C24 is defined as the observed plasma concentration at 24 hours post-dose (NCT03083821)
Timeframe: 24 hours post-dose

Interventionng/mL (Mean)
Baraclude0.435

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Time of Maximum Observed Plasma Concentration (Tmax)

Tmax is defined as the time of maximum observed plasma concentration, measured in hours (NCT03083821)
Timeframe: Up to 24 hours

InterventionHours (Mean)
Baraclude0.667

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Trough Observed Plasma (Predose) Concentration (Ctrough)

Ctrough is defined as the trough in observed plasma (predose) concentrations (NCT03083821)
Timeframe: prior to administration of drug (predose)

Interventionng/mL (Mean)
Baraclude0

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Trough Levels of Tenofovir Alafenamide (TAF) on ABI-H0731 + SOC NUC Therapy as Compared With Placebo + SOC NUC Therapy

(NCT03576066)
Timeframe: Before dosing at Baseline (Day 1), Weeks 2, 4, 12, and 24

,
Interventionng/mL (Mean)
Baseline (Day 1)Week 2Week 4Week 12Week 24
ABI-H0731 + SOC NUC9.6713.121.318.418.9
Placebo + SOC NUC12.214.111.811.713.3

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Trough Levels of Tenofovir Disoproxil Fumarate (TDF) on ABI-H0731 + SOC NUC Therapy as Compared With Placebo + SOC NUC Therapy

(NCT03576066)
Timeframe: Before dosing at Baseline (Day 1), Weeks 2, 4, 12, and 24

,
Interventionng/mL (Mean)
Baseline (Day 1)Week 2Week 4Week 12Week 24
ABI-H0731 + SOC NUC77.585.586.879.379.3
Placebo + SOC NUC89.176.284.186.778.3

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Number of Participants With a Clinically-significant Change in Vital Signs

Vital signs assessed were body temperature, respiratory rate, and pulse rate (NCT03576066)
Timeframe: Baseline and up to Week 24

InterventionParticipants (Count of Participants)
ABI-H0731 + SOC NUC0
Placebo + SOC NUC0

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Number of Participants With Abnormal Alanine Aminotransferase (ALT) at Baseline Who Have Normal ALT at Week 24 on ABI-H0731 + NUC Therapy as Compared With Placebo + NUC Therapy

Abnormal ALT was defined as ≥1.25 x upper limit of normal (34 Units/L for female and 43 Units/L for male participants). (NCT03576066)
Timeframe: Baseline to Week 24

InterventionParticipants (Count of Participants)
ABI-H0731 + SOC NUC1
Placebo + SOC NUC0

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Number of Participants With One or More Abnormal Safety Laboratory Result

(NCT03576066)
Timeframe: Up to Week 36

InterventionParticipants (Count of Participants)
ABI-H0731 + SOC NUC27
Placebo + SOC NUC20

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Number of Participants With One or More Adverse Events

(NCT03576066)
Timeframe: Up to Follow-up (maximum up to Week 36)

InterventionParticipants (Count of Participants)
ABI-H0731 + SOC NUC24
Placebo + SOC NUC8

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Number of Participants With Premature Study Discontinuation

(NCT03576066)
Timeframe: Up to Follow-up (maximum up to Week 36)

InterventionParticipants (Count of Participants)
ABI-H0731 + SOC NUC0
Placebo + SOC NUC1

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Change in Mean log10 Serum HBeAg From Baseline (Day 1) to Week 24 on ABI-H0731 + SOC NUC as Compared to Placebo + SOC NUC

(NCT03576066)
Timeframe: Baseline to Week 24

,
InterventionLog10 International Units (IU)/mL (Mean)
BaselineChange from baseline
HBeAg-positive Participants: ABI-H0731 + SOC NUC0.55-0.05
HBeAg-positive Participants: Placebo + SOC NUC0.43-0.10

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Change in Mean log10 Serum HBsAg From Baseline (Day 1) to Week 24 on ABI-H0731 + SOC NUC as Compared to Placebo + SOC NUC

(NCT03576066)
Timeframe: Baseline to Week 24

,,,
InterventionLog10 International Units (IU)/mL (Mean)
BaselineChange from baseline
HBeAg-negative Participants: ABI-H0731 + SOC NUC2.990.09
HBeAg-negative Participants: Placebo + SOC NUC3.35-0.00
HBeAg-positive Participants: ABI-H0731 + SOC NUC3.480.03
HBeAg-positive Participants: Placebo + SOC NUC3.570.03

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Trough Levels of ABI-H0731 on ABI-H0731 + SOC NUC Therapy

(NCT03576066)
Timeframe: Before dosing at Baseline (Day 1), Weeks 2, 4, 12, and 24

Interventionng/mL (Mean)
Baseline (Day 1)Week 2Week 4Week 12Week 24
ABI-H0731 + SOC NUC0.4361390139013301330

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Trough Levels of Entecavir (ETV) on ABI-H0731 + SOC NUC Therapy as Compared With Placebo + SOC NUC Therapy

(NCT03576066)
Timeframe: Before dosing at Baseline (Day 1), Weeks 2, 4, 12, and 24

,
Interventionng/mL (Mean)
Baseline (Day 1)Week 2Week 4Week 12Week 24
ABI-H0731 + SOC NUC1.100.5540.8720.5831.04
Placebo + SOC NUC1.780.3460.6210.7040.739

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Number of Participants With a Clinically-significant Electrocardiogram Abnormality

(NCT03576066)
Timeframe: Up to Week 24

InterventionParticipants (Count of Participants)
ABI-H0731 + SOC NUC0
Placebo + SOC NUC0

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Change in Mean log10 HBV DNA From Baseline (Day 1) to Week 12 or Week 24 on ABI H0731 + SOC ETV as Compared to Placebo + SOC ETV

Hepatitis B virus (HBV) DNA was measured using COBAS TaqMan Version 2.0. The lower limit of quantitation (LLOQ) was 20 IU/mL and the limit of detection (LOD) was 10 IU/mL. (NCT03577171)
Timeframe: Baseline, Week 12, and Week 24

,
InterventionLog10 International Units (IU)/mL (Mean)
BaselineChange from Baseline at Week 12Change from Baseline at Week 24
ABI-H0731 + SOC ETV7.91-4.45-5.33
Placebo + SOC ETV8.03-3.30-4.20

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Number of Participants With a Decline in Viral DNA to Below Limit of Quantitation on ABI-H0731 + SOC ETV as Compared to Placebo + SOC ETV

HBV DNA was measured using COBAS TaqMan Version 2.0. The LLOQ was 20 IU/mL and the LOD was 10 IU/mL. The number of participants with HBV DNA below the limit of quantitation (<20 IU/mL) and target detected (≥10 IU/mL) was assessed. (NCT03577171)
Timeframe: Baseline, Weeks 2, 4, 8, 12, 16, 20, and 24

,
InterventionParticipants (Count of Participants)
BaselineWeek 2Week 4Week 8Week 12Week 16Week 20Week 24
ABI-H0731 + SOC ETV00011213
Placebo + SOC ETV00000011

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Number of Participants With One or More Abnormal Safety Laboratory Result

(NCT03577171)
Timeframe: Up to Week 36

InterventionParticipants (Count of Participants)
ABI-H0731 + SOC ETV8
Placebo + SOC ETV10

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Trough Levels of ABI-H0731 on ABI-H0731 + SOC ETV Therapy

(NCT03577171)
Timeframe: Before dosing at Baseline (Day 1), Weeks 2, 4, 12, and 24

Interventionng/mL (Mean)
Baseline (Day 1)Week 2Week 4Week 12Week 24
ABI-H0731 + SOC ETVNA1480129012701470

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Number of Participants One or More Adverse Events

(NCT03577171)
Timeframe: Up to Follow-up (maximum up to Week 36)

InterventionParticipants (Count of Participants)
ABI-H0731 + SOC ETV7
Placebo + SOC ETV5

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Number of Participants With a Clinically-significant Change in Vital Signs

Vital signs assessed were body temperature, respiratory rate, and pulse rate (NCT03577171)
Timeframe: Baseline and up to Week 24

InterventionParticipants (Count of Participants)
ABI-H0731 + SOC ETV0
Placebo + SOC ETV0

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Number of Participants With a Clinically-significant Electrocardiogram Abnormality

(NCT03577171)
Timeframe: Up to Week 24

InterventionParticipants (Count of Participants)
ABI-H0731 + SOC ETV0
Placebo + SOC ETV0

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Number of Participants With Abnormal Alanine Aminotransferase (ALT) at Baseline Who Have Normal ALT at Week 24 on ABI-H0731 + SOC ETV as Compared to Placebo + SOC ETV

(NCT03577171)
Timeframe: Baseline to Week 24

InterventionParticipants (Count of Participants)
ABI-H0731 + SOC ETV4
Placebo + SOC ETV2

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Number of Participants With Premature Study Discontinuation

(NCT03577171)
Timeframe: Up to Follow-up (maximum up to Week 36)

InterventionParticipants (Count of Participants)
ABI-H0731 + SOC ETV0
Placebo + SOC ETV0

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Trough Levels of ETV on ABI-H0731 + ETV Therapy as Compared With Placebo + ETV Therapy

(NCT03577171)
Timeframe: Before dosing at Baseline (Day 1), Weeks 2, 4, 12, and 24

,
Interventionng/mL (Mean)
Baseline (Day 1)Week 2Week 4Week 12Week 24
ABI-H0731 + SOC ETV0.003250.4320.4190.3780.411
Placebo + SOC ETV00.4970.6180.6660.408

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Number of Subjects With Adverse Events

Incidence of treatment emergent adverse events (AEs) (NCT03780543)
Timeframe: Up to Week 148

,,
InterventionParticipants (Count of Participants)
Number of subjects with AEsNumber of subjects with discontinuation due to an AENumber of subjects with significant abnormal ECGs
Treatment-naïve Subjects With HBeAg Positive cHBV1220
Virologically-suppressed HBeAg Negative Participants From Parent Study ABI-H0731-2011610
Virologically-suppressed HBeAg Positive Participants From Parent Study ABI-H0731-2012601

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Number of Subjects With Abnormal Alanine Aminotransferase (ALT) at Baseline Who Have Normal ALT at End of Treatment (EOT) and End of Study (EOS)

"To measure the number and proportion of subjects with abnormal ALT at baseline who have normal ALT at end of treatment (EOT) and end of study (EOS)~To measure the number and proportion of subjects regardless of levels of ALT at baseline at EOT and EOS" (NCT03780543)
Timeframe: EOT: up to Week 52 or 148; EOS: up to 3 years off treatment

,,
InterventionParticipants (Count of Participants)
Numbers with normal ALT levels at EOTNumber with normal ALT levels at EOS
Treatment-naïve Subjects With HBeAg Positive cHBV55
Virologically-suppressed HBeAg Negative Participants From Parent Study ABI-H0731-20121
Virologically-suppressed HBeAg Positive Participants From Parent Study ABI-H0731-20100

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Sustained Viral Response (SVR) at 24 Weeks Off Treatment

"To evaluate the potential for combination therapy with ABI-H0731+ NrtI to increase SVR rates in subjects who have chronic hepatitis B (CHB). To evaluate the proportion of subjects who meet the definition of SVR at 24 weeks off treatment, the SVR rate and corresponding 95% confidence interval will be presented for the overall population while on combination therapy.~SVR is defined as sustained viral response with HBV DNA , LOQ (20 IU/mL) through off-treatment Week 24." (NCT03780543)
Timeframe: Completing from week 52 until week 76

InterventionParticipants (Count of Participants)
Virologically-suppressed HBeAg Negative Participants From Parent Study ABI-H0731-2010
Virologically-suppressed HBeAg Positive Participants From Parent Study ABI-H0731-2010
Treatment-naïve Subjects With HBeAg Positive cHBV0

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Number of Subjects With Suppression/Loss of Viral HBeAg Antigen/DNA on Combination Treatment Whose Viral Antigens Rebound Off Therapy

"Incidence of subjects with suppression/loss of viral Hepatitis B e antigen (HBeAg) antigen/DNA on combination treatment whose viral antigens rebound off therapy" (NCT03780543)
Timeframe: upto Week 148

InterventionParticipants (Count of Participants)
Virologically-suppressed HBeAg Negative Participants From Parent Study ABI-H0731-2014
Virologically-suppressed HBeAg Positive Participants From Parent Study ABI-H0731-2014

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Percentage of Participants With Premature Treatment Discontinuation

Describes the number of participants who discontinued treatment with ABI-H2158/placebo prematurely. (NCT04398134)
Timeframe: Up to 72 weeks

InterventionParticipants (Count of Participants)
ABI-H2158 Plus ETV (HBeAg Positive Population)2
Placebo Plus ETV (HBeAg Positive Population)0
ABI-H2158 Plus ETV (HBeAg Negative Population)2
Placebo Plus ETV (HBeAg Negative Population)0

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Percentage of Participants With Adverse Events

Describes the number of participants with One or More Adverse Events while they were on treatment with the study drug. (NCT04398134)
Timeframe: Up to 72 weeks

InterventionParticipants (Count of Participants)
ABI-H2158 Plus ETV (HBeAg Positive Population)18
Placebo Plus ETV (HBeAg Positive Population)6
ABI-H2158 Plus ETV (HBeAg Negative Population)19
Placebo Plus ETV (HBeAg Negative Population)6

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Change From Baseline in Mean log10 HBV DNA

HBV DNA was measured by Cobas AmpliPrep/ Cobas TaqMan HBV Test v2.0 (LOD 10 IU/mL). The analysis of data was descriptive only. (NCT04398134)
Timeframe: Baseline and Week 24

Interventionlog10 IU/mL (Mean)
ABI-H2158 Plus ETV (HBeAg Positive Population)-6.2
Placebo Plus ETV (HBeAg Positive Population)-4.8

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Percentage of Participants With Abnormal Laboratory Results

Severity grades were defined by Grading Scale for Severity of Adverse Events and Laboratory Abnormalities [The DAIDS Version 2.1]. For maximum postbaseline toxicity grade, the most severe graded abnormality from all tests was counted for each participant. For each individual laboratory test, the most severe graded abnormality for that test was counted for a participant. A treatment-emergent laboratory abnormality was defined as an increase of at least 1 toxicity grade from baseline at any time postbaseline up to and including the date of last dose of ABI-H2158/Placebo plus 28 days. (NCT04398134)
Timeframe: Up to 72 weeks

InterventionParticipants (Count of Participants)
ABI-H2158 Plus ETV (HBeAg Positive Population)29
Placebo Plus ETV (HBeAg Positive Population)8
ABI-H2158 Plus ETV (HBeAg Negative Population)19
Placebo Plus ETV (HBeAg Negative Population)9

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HBsAg Change (Δ log10) From Day 1 to Week 16 of Treatment

Efficacy of Vonafexor on top of NA assessed as HBsAg decline (Δ log10) from Day 1 to Week 16 of treatment (NCT04465916)
Timeframe: LS mean at week 16 (Day 1, Week 2, Week 4, Week 6, Week 8, Week 10, Week 12, Week 14, and Week 16)

Interventionlog10 IU/mL (Least Squares Mean)
Experimental Arm-0.029
Control Arm-0.066

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Virologic Failure Rate

Virologic failure rate (breakthrough)2 of HBV-DNA (% patients with a confirmed quantifiable HBV DNA increase of ≥ 1log10 HBV DNA copies/mL above LLOQ3) assessed at Week 16 of treatment period and Weeks 20, 28 and 40 during follow-up period (NCT04465916)
Timeframe: 40 weeks

,
Interventionparticipants (Number)
Week 16Week 20Week 28Week 40
Control Arm0000
Experimental Arm0000

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Number of Participants With an Adverse Event

(NCT04781647)
Timeframe: Up to 60 weeks

InterventionParticipants (Count of Participants)
ABI-H0731 + ETV14
ABI-H0731 + ETV + Peg-IFNα17
ETV + Peg-IFNα17

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Number of Participants With a Laboratory Abnormality

(NCT04781647)
Timeframe: Up to 60 weeks

InterventionParticipants (Count of Participants)
ABI-H0731 + ETV19
ABI-H0731 + ETV + Peg-IFNα16
ETV + Peg-IFNα17

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Number of Participants With Premature Discontinuation of Treatment

(NCT04781647)
Timeframe: Up to 60 weeks

InterventionParticipants (Count of Participants)
ABI-H0731 + ETV18
ABI-H0731 + ETV + Peg-IFNα17
ETV + Peg-IFNα11

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Mean Change From Baseline in HBsAg

(NCT04781647)
Timeframe: Baseline and at pre-specified time points up to 60 weeks

,,
Interventionlog10 IU/mL (Mean)
Week 4Week 8Week 12Week 16Week 20Week 24Week 28Week 32Week 36Week 40Week 44Week 48
ABI-H0731 + ETV-.2-.4-.5-.6-.6-.6-.7-.6-.6-.7-1.0-1.1
ABI-H0731 + ETV + Peg-IFNα-.1-.4-.2-.2-.5-.5-.5-.4-.2-.1-.1-.1
ETV + Peg-IFNα-.2-.5-.5-.6-.7-.7-.7-.8-.9-.9-1.0-1.1

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Plasma Concentration of ABI-H0731

(NCT04781647)
Timeframe: Predose on Day 1, Week 4, and Week 24 and at pre-specified time points postdose up to Week 24

Interventionng/mL (Mean)
Week 24, predoseWeek 24, 30 min to 2 hours postdose
ETV + Peg-IFNα0374

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Mean Change From Baseline in HBV pgRNA

(NCT04781647)
Timeframe: Baseline and at pre-specified time points up to 60 weeks

,,
Interventionlog10 U/mL (Mean)
Week 1Week 2Week 4Week 6Week 8Week 12Week 16Week 20Week 24Week 28Week 32Week 36Week 40Week 44Week 48
ABI-H0731 + ETV-1.3-1.6-2.0-2.3-2.5-2.7-2.8-2.8-2.7-2.9-3.1-3.3-3.1-4.0-4.2
ABI-H0731 + ETV + Peg-IFNα-1.5-1.9-2.2-2.6-2.7-3.0-2.9-3.0-3.3-3.0-3.0-2.9-2.5-3.3-2.4
ETV + Peg-IFNα-.5-.6-.9-1.6-2.0-2.4-2.7-2.5-2.7-3.8-3.2-3.8-3.3-3.0-2.9

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Plasma Concentration of ABI-H0731

(NCT04781647)
Timeframe: Predose on Day 1, Week 4, and Week 24 and at pre-specified time points postdose up to Week 24

,
Interventionng/mL (Mean)
Day 1, PredoseDay 1, 2 to 4 hours postdoseWeek 2, 30 min to 2 hours postdoseWeek 4, predoseWeek 8, 30 min to 2 hours postdoseWeek 12, 30 min to 2 hours postdoseWeek 16, 4 to 6 hours postdoseWeek 20, 4 to 6 hours postdoseWeek 24, predoseWeek 24, 30 min to 2 hours postdose
ABI-H0731 + ETV085221302070200019202030221020202070
ABI-H0731 + ETV + Peg-IFNα0124017001390156016502200209017301580

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Mean Change From Baseline in HBeAg

(NCT04781647)
Timeframe: Baseline and at pre-specified time points up to 60 weeks

,,
Interventionlog10 IU/mL (Mean)
Week 8Week 12Week 16Week 20Week 24Week 28Week 32Week 36Week 40Week 44Week 48
ABI-H0731 + ETV-.6-.8-1.0-1.1-1.1-1.2-1.4-1.5-1.5-1.8-1.9
ABI-H0731 + ETV + Peg-IFNα-.8-.8-.9-1.1-1.2-1.2-1.2-1.1-1.2-1.1-1.1
ETV + Peg-IFNα-.9-1.1-1.2-1.3-1.3-1.4-1.5-1.7-1.8-1.9-2.1

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Mean Change From Baseline in HBcrAg

(NCT04781647)
Timeframe: Baseline and at pre-specified time points up to 60 weeks

,,
Interventionlog10 kU/mL (Mean)
Week 4Week 8Week 12Week 16Week 20Week 24Week 28Week 32Week 36Week 40Week 44Week 48
ABI-H0731 + ETV-.4-.6-.9-1.0-1.1-1.2-1.2-1.3-1.5-1.6-2.0-2.0
ABI-H0731 + ETV + Peg-IFNα-.4-.8-.9-1.0-1.2-1.3-1.3-1.2-1.2-1.3-1.3-1.2
ETV + Peg-IFNα-.3-.8-1.1-1.2-1.3-1.4-1.5-1.7-1.9-1.9-2.0-2.0

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Mean Change From Baseline HBV DNA

(NCT04781647)
Timeframe: Baseline and at pre-specified time points up to 60 weeks

,,
Interventionlog10 IU/mL (Mean)
Week 1Week 2Week 4Week 6Week 8Week 12Week 16Week 20Week 24Week 28Week 32Week 36Week 40Week 44Week 48
ABI-H0731 + ETV-2.1-2.5-3.2-3.6-4.2-4.9-5.5-5.8-6.0-6.2-6.2-6.2-6.2-6.5-6.7
ABI-H0731 + ETV + Peg-IFNα-2.1-2.6-2.9-3.6-4.1-4.4-5.2-5.6-6.0-6.3-6.2-6.2-6.0-5.8-5.9
ETV + Peg-IFNα-2.2-2.7-3.4-4.0-4.5-5.1-5.6-6.1-6.5-6.7-6.7-6.9-6.7-6.6-6.8

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Number of Participants With One or More Abnormal Laboratory Result

(NCT04820686)
Timeframe: Laboratory results were collected from the time of signing the informed consent until the study was early terminated, up to 96 weeks.

InterventionParticipants (Count of Participants)
VBR + AB-729 + SOC NrtI30
VBR + SOC NrtI16
AB-729 + SOC NrtI16

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Change From Baseline in Mean log10 HBV RNA Off-Treatment

(NCT04820686)
Timeframe: Weeks 52, 56, 60, 64, 68, 72, 76, 80, 84, 88, 92 and 96.

Interventionlog10 U/mL (Mean)
Off-Treatment Week 4Off-Treatment Week 8Off-Treatment Week 12Off-Treatment Week 16Off-Treatment Week 20Off-Treatment Week 24Off-Treatment Week 28Off-Treatment Week 32Off-Treatment Week 36Off-Treatment Week 40
AB-729 + SOC NrtI (Discontinued All)-1.1-0.8-0.8-0.8-0.6-0.5-0.6-0.1.5-0.4

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Change From Baseline in Mean log10 Serum Hepatitis B Surface Antigen (HBsAg) Off-Treatment

(NCT04820686)
Timeframe: Weeks 52, 56, 60, 64, 68, 72, 76, 80, 84, 88, 92 and 96.

Interventionlog10 IU/mL (Mean)
Off-Treatment Week 4Off-Treatment Week 8Off-Treatment Week 12Off-Treatment Week 16Off-Treatment Week 20Off-Treatment Week 24Off-Treatment Week 28Off-Treatment Week 32Off-Treatment Week 36Off-Treatment Week 40
AB-729 + SOC NrtI (Discontinued All)-1.8-1.8-1.7-1.4-1.2-1.3-1.6-1.5-1.2-1.2

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Number of Participants With Premature Treatment Discontinuation Due to AEs

(NCT04820686)
Timeframe: AEs were collected from the time of signing the informed consent until the final follow-up visit, up to 96 weeks.

InterventionParticipants (Count of Participants)
VBR discontinuation due to AEAB-729 discontinuation due to AE
VBR + AB-729 + SOC NrtI31

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Number of Participants With Premature Treatment Discontinuation Due to AEs

(NCT04820686)
Timeframe: AEs were collected from the time of signing the informed consent until the final follow-up visit, up to 96 weeks.

InterventionParticipants (Count of Participants)
VBR discontinuation due to AE
VBR + SOC NrtI1

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Number of Participants With One or More Adverse Events (AEs)

(NCT04820686)
Timeframe: AEs were collected from the time of signing the informed consent until the final follow-up visit, up to 96 weeks.

InterventionParticipants (Count of Participants)
VBR + AB-729 + SOC NrtI26
VBR + SOC NrtI12
AB-729 + SOC NrtI12

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Change From Baseline in Mean log10 HBV RNA Off-Treatment

(NCT04820686)
Timeframe: Weeks 52, 56, 60, 64, 68, 72, 76, 80, 84, 88, 92 and 96.

Interventionlog10 U/mL (Mean)
Off-Treatment Week 4Off-Treatment Week 8Off-Treatment Week 12Off-Treatment Week 16Off-Treatment Week 20Off-Treatment Week 24Off-Treatment Week 28Off-Treatment Week 32Off-Treatment Week 36Off-Treatment Week 40Off-Treatment Week 44Off-Treatment Week 48
VBR + AB-720 + SOC NrtI (Continued NrtI Only)-0.8-0.5-0.6-0.5-0.3-0.4-0.8-1.0-1.0-0.9-1.0-1.2

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Number of Participants With Premature Treatment Discontinuation Due to AEs

(NCT04820686)
Timeframe: AEs were collected from the time of signing the informed consent until the final follow-up visit, up to 96 weeks.

InterventionParticipants (Count of Participants)
AB-729 discontinuation due to AE
AB-729 + SOC NrtI0

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Change From Baseline in Mean log10 Serum Hepatitis B Surface Antigen (HBsAg) On-Treatment

Subjects remained on their assigned oral agents (ie, VBR+NrtI for Groups 1 and 2; NrtI for Group 3) until Week 48 laboratory results required for Treatment Stopping Criteria assessment were available so there are some results past Week 48. (NCT04820686)
Timeframe: Baseline and Weeks 2, 4, 8, 12, 16, 20, 24, 28, 32, 36, 40, 44, 48, 52 and 56.

,
Interventionlog10 IU/mL (Mean)
Week 2Week 4Week 8Week 12Week 16Week 20Week 24Week 28Week 32Week 36Week 40Week 44Week 48Week 52Week 56
VBR + AB-729 + SOC NrtI-0.3-.3-0.7-1.2-1.5-1.7-1.7-1.7-1.8-1.9-1.8-1.9-1.9-1.8-1.5
VBR + SOC Nrtl00000000000000-0.1

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Change From Baseline in Mean log10 Serum Hepatitis B Surface Antigen (HBsAg) On-Treatment

Subjects remained on their assigned oral agents (ie, VBR+NrtI for Groups 1 and 2; NrtI for Group 3) until Week 48 laboratory results required for Treatment Stopping Criteria assessment were available so there are some results past Week 48. (NCT04820686)
Timeframe: Baseline and Weeks 2, 4, 8, 12, 16, 20, 24, 28, 32, 36, 40, 44, 48, 52 and 56.

Interventionlog10 IU/mL (Mean)
Week 2Week 4Week 8Week 12Week 16Week 20Week 24Week 28Week 32Week 36Week 40Week 44Week 48
AB-729 + SOC NrtI-0.2-0.3-0.6-1.1-1.3-1.6-1.6-1.7-1.7-1.9-1.8-1.9-1.9

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Change From Baseline in Mean log10 HBV RNA Off-Treatment

(NCT04820686)
Timeframe: Weeks 52, 56, 60, 64, 68, 72, 76, 80, 84, 88, 92 and 96.

,
Interventionlog10 U/mL (Mean)
Off-Treatment Week 4Off-Treatment Week 8Off-Treatment Week 12Off-Treatment Week 16Off-Treatment Week 20Off-Treatment Week 24Off-Treatment Week 28Off-Treatment Week 32Off-Treatment Week 36
VBR + AB-729 + SOC NrtI (Discontinued All)-0.6-0.5-0.70.7.50.20
VBR + SOC Nrtl (Continued NrtI Only)-0.10-0.20.3-0.2-0.4-0.7-0.20

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Change From Baseline in Mean log10 Serum Hepatitis B Surface Antigen (HBsAg) Off-Treatment

(NCT04820686)
Timeframe: Weeks 52, 56, 60, 64, 68, 72, 76, 80, 84, 88, 92 and 96.

,
Interventionlog10 IU/mL (Mean)
Off-Treatment Week 4Off-Treatment Week 8Off-Treatment Week 12Off-Treatment Week 16Off-Treatment Week 20Off-Treatment Week 24Off-Treatment Week 28Off-Treatment Week 32Off-Treatment Week 36
VBR + AB-729 + SOC NrtI (Discontinued All)-1.9-1.9-1.8-1.7-1.8-1.7-1.8-1.7-1.6
VBR + SOC Nrtl (Continued NrtI Only)00-0.1-0.10000.00

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Change From Baseline in Mean log10 Serum Hepatitis B Surface Antigen (HBsAg) Off-Treatment

(NCT04820686)
Timeframe: Weeks 52, 56, 60, 64, 68, 72, 76, 80, 84, 88, 92 and 96.

Interventionlog10 IU/mL (Mean)
Off-Treatment Week 4Off-Treatment Week 8Off-Treatment Week 12Off-Treatment Week 16Off-Treatment Week 20Off-Treatment Week 24Off-Treatment Week 28Off-Treatment Week 32Off-Treatment Week 36Off-Treatment Week 40Off-Treatment Week 44Off-Treatment Week 48
VBR + AB-720 + SOC NrtI (Continued NrtI Only)-1.6-1.4-1.4-1.5-1.7-2.0-2.0-1.9-1.8-1.7-1.6-2.2

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Change From Baseline in Mean log10 HBV RNA On-Treatment

Subjects remained on their assigned oral agents (ie, VBR+NrtI for Groups 1 and 2; NrtI for Group 3) until Week 48 laboratory results required for Treatment Stopping Criteria assessment were available so there are some results past Week 48. (NCT04820686)
Timeframe: Baseline and Weeks 2, 4, 8, 12, 16, 20, 24, 28, 32, 36, 40, 44, 48, 52, and 56.

Interventionlog10 U/mL (Mean)
Week 2Week 4Week 8Week 12Week 16Week 20Week 24Week 28Week 32Week 36Week 40Week 44Week 48
AB-729 + SOC NrtI-.4-.6-0.5-0.7-0.8-0.8-0.7-0.8-0.7-0.7-0.6-0.8-0.7

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Change From Baseline in Mean log10 HBV RNA Off-Treatment

(NCT04820686)
Timeframe: Weeks 52, 56, 60, 64, 68, 72, 76, 80, 84, 88, 92 and 96.

Interventionlog10 U/mL (Mean)
Off-Treatment Week 4Off-Treatment Week 8Off-Treatment Week 12Off-Treatment Week 16Off-Treatment Week 20Off-Treatment Week 24Off-Treatment Week 28Off-Treatment Week 32Off-Treatment Week 36Off-Treatment Week 40Off-Treatment Week 44
AB-729 + SOC NrtI (Continued NrtI Only)-0.9-0.9-1.0-0.9-0.70.7-0.6-0.3-0.1-0.6.1

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Change From Baseline in Mean log10 HBV RNA On-Treatment

Subjects remained on their assigned oral agents (ie, VBR+NrtI for Groups 1 and 2; NrtI for Group 3) until Week 48 laboratory results required for Treatment Stopping Criteria assessment were available so there are some results past Week 48. (NCT04820686)
Timeframe: Baseline and Weeks 2, 4, 8, 12, 16, 20, 24, 28, 32, 36, 40, 44, 48, 52, and 56.

,
Interventionlog10 U/mL (Mean)
Week 2Week 4Week 8Week 12Week 16Week 20Week 24Week 28Week 32Week 36Week 40Week 44Week 48Week 52Week 56
VBR + AB-729 + SOC NrtI-.6-.7-.7-.6-0.6-0.7-0.5-0.9-0.7-0.7-0.6-0.6-0.7-0.7-1.0
VBR + SOC NrtI-.20.2000.1.2.2.1.1.10-0.1-0.1.2

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Change From Baseline in Mean log10 Serum Hepatitis B Surface Antigen (HBsAg) Off-Treatment

(NCT04820686)
Timeframe: Weeks 52, 56, 60, 64, 68, 72, 76, 80, 84, 88, 92 and 96.

Interventionlog10 IU/mL (Mean)
Off-Treatment Week 4Off-Treatment Week 8Off-Treatment Week 12Off-Treatment Week 16Off-Treatment Week 20Off-Treatment Week 24Off-Treatment Week 28Off-Treatment Week 32Off-Treatment Week 36Off-Treatment Week 40Off-Treatment Week 44
AB-729 + SOC NrtI (Continued NrtI Only)-1.8-1.8-2.0-1.6-2.1-2.9-3.0-3.2-3.0-2.9-2.8

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