- |||||||||| entecavir / Generic mfg., lamivudine HBV / Generic mfg.
Journal: Reactivation of Occult Hepatitis B Virus Infection During Long-Term Entecavir Antiviral Therapy. (Pubmed Central) - Apr 2, 2022
Drug resistance gene analysis found RtL229W mutant, resistant to lamivudine but sensitive to ETV and other nucleoside analogs...Secondly, identifying the risk factors and mechanisms associated with HBVr could help quantify the risk of HBVr and manage the clinical consequences. Thirdly, the OBI patients with hepatitis B e antigen-positive, HBV DNA > 1 × 10 IU/ml should be recommended regular and continuous antiviral therapy as soon as possible to prevent the occurrence of hepatocirrhosis and hepatocellular carcinoma (HCC).
- |||||||||| lamivudine HBV / Generic mfg., lamivudine / Generic mfg.
Clinical, Journal: Tenofovir versus lamivudine followed by tenofovir in severe exacerbation of hepatitis B: a randomized controlled study. (Pubmed Central) - Mar 23, 2022
P3
This study aimed to compare the short-term efficacy of tenofovir disoproxil fumarate (TDF) and LAM for 24 weeks followed by TDF in the treatment of CHB with severe acute exacerbation...The biochemical and virological responses at 12, 24 and 48 weeks were also similar between the two groups. TDF and LAM for 24 weeks followed by TDF achieved a similar clinical outcome in CHB patients with SAE.
- |||||||||| lamivudine HBV / Generic mfg.
Monitoring patients with anti HBs trough levels can minimise hepatitis B immune globulin therapy after liver transplant (Poster Area) - Mar 16, 2022 - Abstract #EASLILC2022EASL_ILC_1481;
All patients received a combined HBV prophylaxis with NUCs (tenofovir, entecavir, or lamivudine) and intramuscular HBIg therapy administered at individualised multiple-week intervals, aiming at obtaining anti-HBs trough levels of 50–100 UI/L... Our data support the use of a minimised HBIg for the prevention of HBV recurrence in LT recipients who should prudently continue combined prophylaxis (e. g. HDV coinfection).
- |||||||||| lamivudine HBV / Generic mfg.
Journal: Design and synthesis of novel quinazolinone derivatives as anti-HBV agents with TLR8 agonist effect. (Pubmed Central) - Mar 4, 2022
Among them, compound 5l exhibited potent inhibitory effect on HBV DNA replication in both wild type and drug resistant (lamivudine and entecavir) HBV strains with IC values of 0.15 and 0.10 μM, respectively...Dual-luciferase reporter gene assay further confirmed that compound 5l could dose-dependently activate TLR8, thus effectively inducing the activity of TLR8-dependent NF-κB. Collectively, compound 5l displayed potent anti-HBV activities and TLR8 agonist effect in vitro, and might be a potential immunomodulatory anti-HBV agent to warrant further investigation.
- |||||||||| Triumeq (dolutegravir/abacavir/lamivudine) / ViiV Healthcare, bictegravir (GS-9883) / Gilead, Tivicay (dolutegravir) / ViiV Healthcare
Journal: An up-to-date evaluation of dolutegravir/abacavir/lamivudine for the treatment of HIV. (Pubmed Central) - Feb 26, 2022
Bictegravir with tenofovir alafenamide and emtricitabine offers the benefit of same day initiation and efficacy in hepatitis B co-infection, while new two-drug regimens enhance the simplicity of HIV treatment. Continued study is required into the mechanisms and optimal management strategies for weight gain for many regimens, including DTG/ABC/3TC.
- |||||||||| Besivo (besifovir) / Gilead, LG Chem, Ildong
Journal: Identification and Characterization of Besifovir-Resistant Hepatitis B Virus Isolated from a Chronic Hepatitis B Patient. (Pubmed Central) - Feb 26, 2022
Besifovir dipivoxil maleate (BSV) is a newly developed NA against HBV in the form of acyclic nucleotide phosphonate that is available for oral administration similar to adefovir and tenofovir...To further identify the responsible mutations for BSV resistance, we performed in vitro drug susceptibility assay on several artificial clones. As a result, our study revealed that rtL180M (M) and rtM204V (V) mutations, already known as lamivudine-resistant mutations, confer resistance to BSV in the CHB patient.
- |||||||||| Besivo (besifovir) / Gilead, LG Chem, Ildong
PK/PD data, Journal: Influence of renal function on the single-dose pharmacokinetics of besifovir, a novel antiviral agent for the treatment of hepatitis B virus infection. (Pubmed Central) - Feb 22, 2022
Per the well-known resistance of hepatitis B virus to nucleoside/nucleotide analogs, alternative treatment options with higher resistance barriers have been approved for use in both treatment-naïve and lamivudine-resistant hepatitis B virus infections...The ratios of LB80331 renal clearance and the average estimated glomerular filtration rate of each renal impairment group with respect to the normal group were similar. The increase in plasma exposure and decrease in renal clearance suggest the need to adjust dosage regimens in patients with moderate-to-severe renal impairment.
- |||||||||| Undisclosed HBV therapeutic / Kainos Medicine, Institut Pasteur Korea
Journal: Determination of infectious hepatitis B virus particles by an end-point dilution assay identifies a novel class of inhibitors. (Pubmed Central) - Feb 19, 2022
Furthermore, the assay was validated using serially diluted lamivudine, an HBV replication inhibitor, inhibiting HBV DNA secretion and infectious viral progeny by approx...Interestingly, we identified dexmedetomidine (DMM), an alpha-2 adrenergic agonist, inhibiting the secretion of infectious viral progeny by approx...We identified DMM as a novel inhibitor that exclusively interferes with the secretion of infectious HBV particles without affecting the secretion of HBV genomes. This end-point dilution assay enables the precise determination of the number of infectious HBV particles, assessment of the specific infectivity and stability of HBV particles, and identification of novel classes of HBV inhibitors.
- |||||||||| Biktarvy (bictegravir/emtricitabine/tenofovir alafenamide) / Gilead
HIV-1 RNA DECAY IN SEMEN AND RECTUM WITH DTG PLUS 3TC VERSUS BIC/FTC/TAF ([VIRTUAL]) - Feb 7, 2022 - Abstract #CROI2022CROI_643;
HIV decay in semen and rectum have not yet been described for the dual combination dolutegravir (DTG) plus lamivudine (3TC)...At week 12 and week 24 most subjects had HIV-1 RNA <20 copies per mL (or swab) in BP, SP and RF (Table 1). Both DTG+3TC and BIC/F/TAF achieved rapid HIV-1 RNA suppression in SP and RF and no significant differences were observed between treatment groups in all study timepoints from BL through week 24.
- |||||||||| ribavirin / Generic mfg., lamivudine HBV / Generic mfg.
Journal: Mean HBsAg decline at week 24 of PEG-IFN based treatment predicts subsequent rate of HBsAg clearance - suggesting a valuable endpoint for early development HBV trials. (Pubmed Central) - Feb 3, 2022
We used individual patient data from the studies HBV 9901 (peginterferon [PEG-IFN] versus PEG-IFN+lamivudine for HBeAg-positive CHB), PARC (PEG-IFN±ribavirin for HBeAg-negative CHB) and published data from 0149 (PEG-IFN±tenofovir for HBeAg-positive and HBeAg-negative CHB) and LIRA-B (PEG-IFN for HBeAg-positive CHB) to define the relationship between mean week HBsAg decline and HBsAg loss at 6 months post-treatment...Observations were similar for week 12 data, but the relationship was less strong. Mean week 24 HBsAg decline predicts subsequent HBsAg loss and could be a valuable and useful early endpoint in HBV-treatment trials.
- |||||||||| lamivudine HBV / Generic mfg., lamivudine / Generic mfg.
Journal, HEOR: Uptake Success and Cost Savings from Switching to a Two-Drug Antiretroviral Regimen. (Pubmed Central) - Feb 3, 2022
Between January 1, 2020 and January 1, 2021 eligible patients (i.e., virally suppressed, no active hepatitis B infection, no documented nucleoside reverse transcriptase inhibitors/integrase strand transfer inhibitor resistance) were offered, on a convenience basis and as part of routine care, the opportunity to adjust their current three-drug STF to a two-drug STF (dolutegarvair/lamivudine)...It provided significant and immediate cost savings within the first year. Our results bring clarity to discussions on whether using two-drug regimens would be practical and acceptable in nonclinical trial settings.
- |||||||||| Tyzeka (telbivudine) / Novartis
Clinical, Journal: Developmental consequences of children born from mothers with telbivudine treatment during late pregnancy: A prospective study with 3-year follow-up. (Pubmed Central) - Jan 27, 2022
Multivariate regression analyses showed that exposure to LdT during pregnancy was independently associated with infant's development in gross motor (OR 6.49, 95% CI 1.37-30.20, P = 0.02) and adaptive (OR 0.18, 95% CI 0.05-0.71, P = 0.01) at 36 months. These results suggest that prenatal LdT exposure might affect neurological development in long-term observation.Abbreviations: LdT: telbivudine; HBV: hepatitis B virus; HBsAg: hepatitis B surface antigen; HBeAg: hepatitis Be antigen; HbsAb: hepatitis B surface antibody; ALT: alanine aminotransferase; NA: nucleoside/nucleotide analog; LAM: lamivudine; MTCT: mother-to-child transmission; GDS: Gesell Developmental Schedule; OR: odds ratio; CI: confidence interval; DQ: developmental quotient; RMB: renminbi; BMI: body mass Index; HBIG: hepatitis B immunoglobulin.
- |||||||||| entecavir / Generic mfg., adefovir dipivoxil / Generic mfg.
Clinical, Journal, Adverse events, Real-world evidence: Adverse Events During Pregnancy Associated With Entecavir and Adefovir: New Insights From a Real-World Analysis of Cases Reported to FDA Adverse Event Reporting System. (Pubmed Central) - Jan 21, 2022
We found a moderate or strong signal for increased risk of spontaneous abortion when comparing ETV with tenofovir disoproxil fumarate (TDF) and telbivudine (LdT), with RORs equal to 1.58 (95% CI, 1.09-2.30) and 2.13 (95% CI, 1.04-4.36), respectively...Futhermore, a strong signal for increased risk of spontaneous abortion was identified in patients with HBV infection when comparing ETV or ADV with lamivudine (LAM), with RORs of 3.55 (95% CI, 1.54-8.18) and 2.85 (95% CI, 1.15-7.08), respectively...Moreover, no obvious signal association of human teratogenicity with exposure to ETV or ADV was identified in fetuses during pregnancy. Nevertheless, owing to the limitations of a spontaneous reporting database, which inevitably contains potential biases, there is a pressing need for well-designed comparative safety studies to validate these results in clinical practice.
- |||||||||| lamivudine HBV / Generic mfg.
Journal: Design, synthesis and evaluation of heteroaryldihydropyrimidine analogues bearing spiro ring as hepatitis B virus capsid protein inhibitors. (Pubmed Central) - Jan 14, 2022
Potent in vitroanti-HBV activity and low cytotoxicity were observed for compound 4r (EC = 0.20 ± 0.00 μM, CC > 87.03 μM), which was more potent than the positive control lamivudine (EC = 0.37 ± 0.04 μM, CC > 100.00 μM) in this assay and was about a quarter as effective as GLS4 (EC = 0.045 ± 0.01 μM, CC > 99.20 μM)...In terms of the physicochemical properties, 4r was predicted to be consistent with the rule-of-five, which means 4r may have favourable absorption and permeation. Finally, ADMET and PK characteristics of 4r and GLS4 were predicted to be comparable in most aspects, implying that the two compounds may have similar profiles in vivo.
- |||||||||| lamivudine HBV / Generic mfg.
Clinical, Journal: Efficacy of antiviral therapy in patients with hepatitis B-related primary liver cancer. (Pubmed Central) - Dec 21, 2021
For the treatment naïve group, a clinical choice could be performed, knowing that reactivation could seldomly occur and be detected in time to promptly treat the pts, but prophylaxis is not mandatory for a favourable clinical course. Combined antiviral therapy on the basis of conventional treatment can significantly improve the liver function, reduce the viral load and prolong the survival time of patients with hepatitis B-related hepatocellular carcinoma associated.
- |||||||||| lamivudine HBV / Generic mfg., lamivudine / Generic mfg.
Journal: Formulation and optimisation of lamivudine-loaded Eudragit S 100 polymer-coated pectin microspheres for colon-specific delivery. (Pubmed Central) - Nov 29, 2021
The obtained microspheres were then subjected to different characterisation studies, including scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and X-ray diffraction (XRD). The results of this study clearly indicate that Eudragit-coated pectin microspheres could be the promising controlled release carriers for colon-specific delivery of lamivudine in the presence of rat cecal content.
- |||||||||| lamivudine HBV / Generic mfg.
Journal: Novel Anti-Hepatitis B Virus Activity of Euphorbia schimperi and Its Quercetin and Kaempferol Derivatives. (Pubmed Central) - Nov 10, 2021
The observed in vitro anti-HBV potential was strongly supported by in silico analysis, which suggested their structure-based activity via interfering with viral Pol/RT and core proteins. In conclusion, this is the first report on the anti-HBV activity of E. schimperi-derived quercitrin-3-O-glucuronide, quercitrin-3-O-rhamnoside, and kaempferol-3-O-glucuronide, most likely through interfering with HBV proteins.
- |||||||||| lamivudine HBV / Generic mfg.
Clinical, Journal: Bone loss in hepatitis B virus-infected patients can be associated with greater osteoclastic activity independently of the retroviral use. (Pubmed Central) - Nov 4, 2021
Participants, both gender, were divided according to the use of antiretrovirals: Group1: 27 inactive virus carriers without medication; Group2: 27 patients using tenofovir; and Group3: 27 patients using lamivudine or entecavir...Increased levels in the bone resorption markers indicated a high resorptive activity of bone tissue. These data suggested high resorption activity of bone tissue in hepatitis B virus-infected patients independent of the use of antiretrovirals.
- |||||||||| lamivudine HBV / Generic mfg.
Clinical, Journal: Fast and sensitive real-time PCR detection of major antiviral drug-resistance mutations in chronic hepatitis B patients using a predesigned panel of Locked-Nucleic-Acid TaqMan probes. (Pubmed Central) - Oct 27, 2021
We developed a novel real-time PCR assay that simultaneously evaluates 11 major nucleos(t)ide antiviral (NA) drug resistance mutations (mt) in chronic hepatitis B patients (CHB), including L180M, M204I/V, and V207M (lamivudine [LMV] resistance), N/H238A/T (adefovir [ADF] resistance), which are circulating in Vietnam; and T184G/L, S202I, and M250V (entecavir [ETV] resistance) and A194T (tenofovir resistance), which have been recently reported in several studies across the globe...In conclusion, this assay accurately identified the mt profile of children (98.4%) and adults (91.2%) with CHB, which is comparable to established methods. This fast and sensitive screening method can be used for the detection of major NA-resistant mt circulating in developing countries, as well as providing a model for the development of similar mt-detection assays, especially for use in non-hospitalised patients who need their results within half a day before starting treatment.
- |||||||||| lamivudine HBV / Generic mfg.
[VIRTUAL] CHRONIC HEPATITIS B PATIENTS REFERRED FOR LIVER TRANSPLANTATION AFTER NUCLEOS(T)IDE ANALOGUE DISCONTINUATION () - Oct 21, 2021 - Abstract #AASLD2021AASLD_1764;
In this study, among patients who were referred for liver transplantation after NA cessation, most experienced the decompensating event soon after cessation . Our data reinforce that patients should not discontinue NA themselves and that physicians should very carefully select non-cirrhotic patients for NA withdrawal after which close monitoring and timely retreatment is crucial .
- |||||||||| Vemlidy (tenofovir alafenamide) / Gilead
[VIRTUAL] TENOFOVIR ALAFENAMIDE FOR MULTIPLE DRUG-RESISTANT CHRONIC HEPATITIS B: A 3-YEAR CLINICAL TRIAL () - Oct 21, 2021 - Abstract #AASLD2021AASLD_1044;
174 patients with hepatitis B virus (HBV) resistant to multiple drugs (lamivudine, entecavir, and/or adefovir) under TDF monotherapy for 96 weeks were randomized 1:1 to switch to TAF (n=87) or continue TDF (n=87) for 48 weeks... TAF monotherapy was efficacious and safe for up to 144 weeks, providing sustained virological response in heavily pre-treated patients with multidrug-resistant HBV.
- |||||||||| tenofovir disoproxil fumarate / Generic mfg., lamivudine HBV / Generic mfg.
[VIRTUAL] RELATIVELY DECREASED RISK OF HEPATOCELLULAR CARCINOMA RECURRENCE DURING TENOFOVIR TREATMENT IN CHRONIC HEPATITIS B PATIENTS () - Oct 21, 2021 - Abstract #AASLD2021AASLD_1033;
NAs prescribed after initial treatment were lamivudine plus adefovir (LAM/ ADV; n = 27, recurrence; n = 19), entecavir (ETV; n = 70, recurrence; n = 44), and tenofovir disoproxil fumarate or tenofovir alafenamide (TDF/TAF; n = 25, recurrence; n = 5)... The non- recurrence of HBV-related HCC after initial treatment is associated with antiviral effects in addition to the degree of liver fibrosis.
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