ArticleAntimicrobial agents and chemotherapy2015
Implications of efficient hepatic delivery by tenofovir alafenamide (GS-7340) for hepatitis B virus therapy.
Article in Antimicrobial agents and chemotherapy, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 82 papers, 3 of them syntheses that pooled it.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
82 citing papers in PubMed, 3 syntheses or guidelines pooled it, 173 citations in OpenAlex.
- Efficacy and safety of tenofovir alafenamide versus tenofovir disoproxil in chronic hepatitis b: a systematic review and meta-analysis of randomized controlled trials.BMC infectious diseases · 2026Pooled it
- Tenofovir disoproxil fumarate versus entecavir on the prognosis of hepatitis B virus-related hepatocellular carcinoma after surgical resection: a systematic review and meta-analysis.Frontiers in oncology · 2025Pooled it
- Bayesian Network Meta-Analysis for Assessing Adverse Effects of Anti-hepatitis B Drugs.Clinical drug investigation · 2019Pooled it
- Efficacy and Safety of Tenofovir Alafenamide (TAF) and Tenofovir Disoproxil Fumarate (TDF) Followed by TAF in Chronic Hepatitis B Patients of East Asian Ethnicity Following 5 Years of Treatment.Alimentary pharmacology & therapeutics · 2026Trial
- Eight-year efficacy and safety of tenofovir alafenamide for treatment of chronic hepatitis B virus infection: Final results from two randomised phase 3 trials.Alimentary pharmacology & therapeutics · 2024Trial
- 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.BMC infectious diseases · 2021Trial
- Trial
- Bioequivalence Evaluation of Two Formulations of Tenofovir Alafenamide Tablets in Healthy Subjects Under Fasting and Fed Conditions.Drug design, development and therapy · 2021Trial
- Sofosbuvir and Ribavirin Liver Pharmacokinetics in Patients Infected with Hepatitis C Virus.Antimicrobial agents and chemotherapy · 2018Trial
- Brief Report: Efficacy and Safety of Switching to a Single-Tablet Regimen of Elvitegravir/Cobicistat/Emtricitabine/Tenofovir Alafenamide in HIV-1/Hepatitis B-Coinfected Adults.Journal of acquired immune deficiency syndromes (1999) · 2016Trial
- Antiviral Therapy and Post-Resection Outcomes in Patients With Hepatitis B Virus-Related Hepatocellular Carcinoma.Alimentary pharmacology & therapeutics · 2026Article
- Differential Hepatitis B Surface Antigen Glycan Isomer Kinetics Between Tenofovir Alafenamide and Entecavir: Hepatocellular Carcinoma Risk Stratification in Hepatitis B e Antigen-Positive Patients.Journal of viral hepatitis · 2026Article
- Tenofovir Alafenamide Versus Entecavir as Switch Therapy After Tenofovir Disoproxil Fumarate in Patients with Chronic Hepatitis B.Journal of clinical medicine · 2026Article
- Superior Efficacy of Tenofovir Alafenamide Compared With Entecavir in Reducing Hepatitis B Surface Antigen: A Multicentre Propensity Score-Matched Study Using Linear Mixed-Effects Models.Alimentary pharmacology & therapeutics · 2026Article
- Contemporary antiretroviral pharmacology in the male genital tract: implications for HIV treatment and prevention.Antimicrobial agents and chemotherapy · 2026Review
- Hepatocyte-Targeted Drug Delivery Strategies for Chronic Hepatitis B: Overcoming Delivery Barriers Toward Functional Cure.Pharmaceutics · 2026Review
- HBV status modulates transaminase decrease after switching from tenofovir disoproxil fumarate to tenofovir alafenamide in people with HIV.The Journal of antimicrobial chemotherapy · 2026Observational
- Prodrug strategies in developing antiviral nucleoside analogs.RSC medicinal chemistry · 2026Review
- Evaluation of the Efficacy of Tenofovir Alafenamide in Patients with Low-Level Viremia Under Chronic Hepatitis B Treatment.Viruses · 2025Article
- The use of phosphotriesterase in the synthesis of enantiomerically pure ProTide prodrugs.Chemico-biological interactions · 2025Review
22 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
7 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Tenofovir alafenamide (TAF) is a prodrug of tenofovir (TFV) currently in clinical evaluation for treatment for HIV and hepatitis B virus (HBV) infections. Since the target tissue for HBV is the liver, the hepatic delivery and metabolism of TAF in primary human hepatocytes in vitro and in dogs in vivo were evaluated here. Incubation of primary human hepatocytes with TAF resulted in high levels of the pharmacologically active metabolite tenofovir diphosphate (TFV-DP), which persisted in the cell with a half-life of >24 h. In addition to passive permeability, studies of transfected cell lines suggest that the hepatic uptake of TAF is also facilitated by the organic anion-transporting polypeptides 1B1 and 1B3 (OATP1B1 and OATP1B3, respectively). In order to inhibit HBV reverse transcriptase, TAF must be converted to the pharmacologically active form, TFV-DP. While cathepsin A is known to be the major enzyme hydrolyzing TAF in cells targeted by HIV, including lymphocytes and macrophages, TAF was primarily hydrolyzed by carboxylesterase 1 (CES1) in primary human hepatocytes, with cathepsin A making a small contribution. Following oral administration of TAF to dogs for 7 days, TAF was rapidly absorbed. The appearance of the major metabolite TFV in plasma was accompanied by a rapid decline in circulating TAF. Consistent with the in vitro data, high and persistent levels of TFV-DP were observed in dog livers. Notably, higher liver TFV-DP levels were observed after administration of TAF than those given TDF. These results support the clinical testing of once-daily low-dose TAF for the treatment of HBV infection.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.