Clinical Features and Resistance to Entecavir Monotherapy of Patients with Hepatitis B

Takayama, Hideo; Komura, Takuya; Kagaya, Takashi; Sugimoto, Saiho; Orita, Noriaki; Asahina, Yasuhiko; Nishikawa, Masashi; Ohta, Hiroyuki; Kaneko, Shuichi; Unoura, Masashi

doi:10.1155/2021/3259833

Cited by 4 publications

(4 citation statements)

References 22 publications

(32 reference statements)

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“…Furthermore, it is known that people with a high initial hepatitis B virus viral load are more likely to develop resistance to ETV. Thus, it is important to emphasize the need to monitor the viral load in patients infected with the hepatitis B virus to better control the development of resistance [11].…”

Section: Antiviral Resistancementioning

confidence: 99%

Entecavir: A Review and Considerations for Its Application in Oncology

Lourenço,

Vale

2023

Pharmaceuticals

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Entecavir (ETV) is a drug used as a first-line treatment for chronic hepatitis B (CHB) virus infection because it is a guanosine nucleoside analogue with activity against the hepatitis B virus polymerase. The ETV dosage can range from 0.5 mg to 1 mg once a day and the most common side effects include headache, insomnia, fatigue, dizziness, somnolence, vomiting, diarrhea, nausea, dyspepsia, and increased liver enzyme levels. In addition to its conventional use, ETV acts as an inhibitor of lysine-specific demethylase 5B (KDM5B), an enzyme that is overexpressed in breast, lung, skin, liver, and prostate tumors and is involved in the hormonal response, stem cell regeneration, genomic stability, cell proliferation, and differentiation. The KDM5B enzyme acts as a transcriptional repressor in tumor suppressor genes, silencing them, and its overexpression leads to drug resistance in certain tumor types. Furthermore, the literature suggests that KDM5B activates the PI3K/AKT signaling pathway, while reducing KDM5B expression decreases AKT signaling, resulting in decreased tumor cell proliferation. In silico studies have demonstrated that ETV can inhibit tumor cell proliferation and induce apoptosis by reducing KDM5B expression. ETV also appears to inhibit PARP-1, has a high genetic barrier, reducing the chance of resistance development, and can also prevent the reactivation of the hepatitis B virus in cancer patients, which have proven to be significant advantages regarding its use as a repurposed drug in oncology. Therefore, ETV holds promise beyond its original therapeutic indication.

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Section: Antiviral Resistancementioning

confidence: 99%

Entecavir: A Review and Considerations for Its Application in Oncology

Lourenço,

Vale

2023

Pharmaceuticals

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“…However, antiviral drug resistance is an important determinant of the success of long‐term CHB therapy 13,14 . While the frequency of resistance to TDF and TAF is considered low, 15,16 the barrier to resistance for ETV is limited to patients who are naïve to NAs therapy 17–20 . Furthermore, lifelong treatment with TDF poses concerns regarding renal safety, particularly in older patients and those with pre‐existing renal insufficiency 21–23 .…”

Section: Introductionmentioning

confidence: 99%

“…13,14 While the frequency of resistance to TDF and TAF is considered low, 15,16 the barrier to resistance for ETV is limited to patients who are naïve to NAs therapy. [17][18][19][20] Furthermore, lifelong treatment with TDF poses concerns regarding renal safety, particularly in older patients and those with pre-existing renal insufficiency. [21][22][23] There are also reports of reduced bone mineral density (BMD) in patients treated with TDF.…”

mentioning

confidence: 99%

Real‐world safety and effectiveness of tenofovir alafenamide for 144 weeks in Japanese patients with chronic hepatitis B

Hige,

Aoki,

Nakamoto

et al. 2024

Journal of Viral Hepatitis

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Tenofovir alafenamide (TAF), a prodrug of tenofovir, delivers high levels of active drug to hepatocytes and is given in a lower dose than tenofovir disoproxil fumarate (TDF). TAF reduces viral replication in patients with chronic hepatitis B (CHB) similar to TDF and has shown a lower risk of the renal and bone toxicities associated with TDF use. This post‐marketing surveillance study examined the safety and effectiveness of TAF in treatment‐naïve and ‐experienced CHB patients who received TAF for 144 weeks at real‐world clinical sites in Japan. Safety assessments included the incidence of adverse drug reactions (ADRs), renal and bone events, and changes in selected laboratory parameters. Effectiveness was based on the proportion of patients with HBV DNA levels below the lower limit of quantitation or <29 IU/mL. This analysis included 580 patients; 18.4% of whom were treatment‐naïve. The cumulative incidence of ADRs was 0.21 per 100 person‐months, and the incidence of serious ADRs was 0.01 (95% CI, 0.00–0.04) per 100 person‐months. There were no ADRs of declines in estimated glomerular filtration rates, renal failure or proximal tubulopathy. The most common ADR was hypophosphataemia in seven (1.2%) patients. Two (0.4%) patients each had decreased blood phosphorus, bone mineral density decreased, dizziness and alopecia. Overall, the proportion of virologically suppressed patients increased from 68.8% at baseline to 97.5% at Week 144. These results confirm the real‐world safety and effectiveness of TAF in Japanese patients with CHB and are consistent with the findings of other evaluations of the safety and efficacy of TAF in CHB.

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“…However, currently, there is no consensus on which drugs are the most effective at preventing viral reactivation as some infections may develop resistance to the drug ( 8 ). Currently, LAM and ETV are the most commonly used NAs ( 9 , 10 ). The European Association for the Study of Liver Diseases guidelines recommended the use of TDF in 2017 ( 10 ).…”

Section: Introductionmentioning

confidence: 99%

Efficacy of nucleos(t)ide analogues(NAs) in preventing virus reactivation in oncology patients with HBV infection after chemotherapy or surgery: A network meta-analysis

et al. 2023

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ObjectiveIn this study, we aimed to perform a network meta-analysis to compare the effectiveness of NAs in decreasing the reactivation of HBV, reducing chemotherapy disruption, and improving survival in oncology patients.MethodsRelevant randomized controlled trials (RCT) evaluating the impact of NAs in HBV infected-related oncology patients were retrieved from electronic databases. The outcome indicators included reactivation rate, survival rate of 1 to 3 years after treatment, and chemotherapy disruption rate. The studies were evaluated for bias using the RCT risk of bias assessment tool recommended in the Cochrane Handbook. The risk ratio (RR) was used to compare the outcome indicators for the anti-viral treatment, and the surface under the cumulative ranking curves (SUCRA) was used to identify the optimal therapeutic regime.ResultsA total of 67 trials containing 5722 patients were included in this study. Regarding the reduction of reactivation rate, entecavir, lamivudine, adefovir alone were less effective than the combination of lamivudine and entecavir (94.9%), with RR values ranging from 3.16 to 3.73. However, based on SUCRA, the efficacy of telbivudine (80.3%) and the combination of lamivudine and adefovir dipivoxil (58.8%) were also acceptable. Entecavir (RR values ranging from 1.25 to 1.50) and lamivudine (RR values ranging from 1.27 to 1.35) can prolong the survival rate of patients at 1-3 years, and were better than adefovir dipivoxil in the comparison of 1-year survival rate. The RR values were 1.18 and 1.19, respectively. And entecavir ‘s ranking in SUCRA was more stable. Entecavir, lamivudine, and tenofovir all reduced chemotherapy interruption rates compared with no antiviral therapy, especially for tenofovir.ConclusionsCurrent evidence shows that lamivudine combined with entecavir, telbivudine, and lamivudine combined with adefovir dipivoxil were the most effective in preventing virus reactivation in HBV infected-related cancer patients treated with chemotherapy. Entecavir had the most stable effect on survival, while tenofovir had the best impact on reducing the chemotherapy disruption rate. Due to limited quality and quantity of the included studies, more high-quality studies are required to verify the above conclusions.Systematic review registrationPROSPEROI [https://www.crd.york.ac.uk/PROSPERO/index.php], identifier CRD4202250685.

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Clinical Features and Resistance to Entecavir Monotherapy of Patients with Hepatitis B

Cited by 4 publications

References 22 publications

Entecavir: A Review and Considerations for Its Application in Oncology

Entecavir: A Review and Considerations for Its Application in Oncology

Real‐world safety and effectiveness of tenofovir alafenamide for 144 weeks in Japanese patients with chronic hepatitis B

Efficacy of nucleos(t)ide analogues(NAs) in preventing virus reactivation in oncology patients with HBV infection after chemotherapy or surgery: A network meta-analysis

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