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1

Ng, Hanna H., Howard Stock, Linda Rausch, et al. "Tenofovir Disoproxil Fumarate." International Journal of Toxicology 34, no. 1 (2015): 4–10. http://dx.doi.org/10.1177/1091581814565669.

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Tenofovir disoproxil fumarate (TDF) is a prodrug of tenofovir that exhibits activity against HIV and hepatitis B. The goals of this study were to evaluate the molecular mechanism of TDF-induced toxicity in mice after 13 weeks of daily oral administration (50-1000 mg/kg) by correlating transcriptional changes with plasma drug levels and traditional toxicology end points. Plasma levels and systemic exposure of tenofovir increased less than dose proportionally and were similar on days 1 and 91. No overt toxicity was observed following the completion of TDF administration. The kidneys of TDF-treat
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2

Dewi, Putu Itta Sandi Lesmana, Kadek Mercu Narapati Pamungkas, and I. Ketut Mariadi. "Renal Safety of Tenofovir Alafenamide versus Tenofovir Disoproxil Fumarate for the Treatment of Chronic Hepatitis B Patients: An Evidence-based Case Report." Indonesian Journal of Gastroenterology, Hepatology, and Digestive Endoscopy 25, no. 2 (2024): 187–93. https://doi.org/10.24871/2522024368.

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ABSTRACTBackground: Treatment modalities for chronic hepatitis B infection (CHB) are interferon and antiviral. The most commonly used antiviral is tenofovir disoproxil fumarate (TDF), however it is known to have nephrotoxicity. Recently, a new antiviral tenofovir alafenamide (TAF) has been developed, which also inhibits hepatitis B virus (HBV). This study aimed to compare the renal safety of TAF and TDF.Method: Literature searching was conducted in PubMed/Medline and Cochrane databases, with modified keywords as “chronic hepatitis B”, “tenofovir alafenamide”, “tenofovir disoproxil fumarate”, “
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3

Dickson, Sean, and Katelyn James. "Trends in HIV preexposure prophylaxis utilization and spending among individuals with commercial insurance." AIDS 38, no. 4 (2024): 610–12. http://dx.doi.org/10.1097/qad.0000000000003809.

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In a cross-sectional analysis of HIV preexposure prophylaxis (PrEP) utilization by commercially insured patients from 2019 to 2021, most prescriptions were for branded formulations of PrEP despite the availability of a generic version. Accounting for the modest relative clinical benefit of branded TAF/FTC (tenofovir alafenamide fumarate/emtricitabine) PrEP over generic TDF/FTC (tenofovir disoproxil fumarate/emtricitabine) PrEP, use of generic TDF/FTC PrEP would have reduced commercial insurers’ spending by 33%.
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4

Lee, William A., and Andrew K. Cheng. "Tenofovir alafenamide fumarate." Antiviral Therapy 27, no. 1 (2022): 135965352110676. http://dx.doi.org/10.1177/13596535211067600.

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Tenofovir alafenamide fumarate is a lipophilic prodrug of tenofovir which is preferentially metabolized in lymphatic tissue resulting in high concentrations of tenofovir (TFV) and its active diphosphate metabolite inside the cells that replicate HIV. Due to its selectivity for these tissues, lower total doses of TAF can be administered relative to tenofovir disoproxil fumarate (TDF) which results in improved bone and renal biomarkers. Tenofovir alafenamide fumarate has become the “backbone” of multiple combination products for the treatment of HIV, combined with emtricitabine for PreP and as a
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5

Wassner, Chanie, Nicole Bradley, and Yuman Lee. "A Review and Clinical Understanding of Tenofovir: Tenofovir Disoproxil Fumarate versus Tenofovir Alafenamide." Journal of the International Association of Providers of AIDS Care (JIAPAC) 19 (January 1, 2020): 232595822091923. http://dx.doi.org/10.1177/2325958220919231.

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HIV is a serious chronic medical condition. Significant improvements in antiretroviral therapy have led to a transformation in its management. No curative treatment is available for HIV, and lifelong therapy is required with a combination of agents to control viral replication and prevent complications. Some of the older agents are notorious for many side effects, making patient compliance difficult, which is critical to preventing HIV resistance. Tenofovir is one of the newer, more tolerable, nucleotide reverse transcriptase inhibitors on the market; is a mainstay of many antiretroviral thera
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6

Brooks, Kristina M., Jose R. Castillo-Mancilla, Joshua Blum, et al. "Increased tenofovir monoester concentrations in patients receiving tenofovir disoproxil fumarate with ledipasvir/sofosbuvir." Journal of Antimicrobial Chemotherapy 74, no. 8 (2019): 2360–64. http://dx.doi.org/10.1093/jac/dkz184.

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AbstractBackgroundIntracellular tenofovir diphosphate concentrations are markedly increased in HIV/HCV coinfected individuals receiving tenofovir disoproxil fumarate (TDF) with sofosbuvir-containing treatment. Sofosbuvir may inhibit the hydrolysis of TDF to tenofovir, resulting in increased concentrations of the disoproxil or monoester forms, which may augment cell loading. We sought to quantify tenofovir disoproxil and monoester concentrations in individuals receiving TDF with and without ledipasvir/sofosbuvir.MethodsHIV/HCV coinfected participants receiving TDF-based therapy were sampled pre
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7

Huynh, Tung, Delana MyAn Bui, Tina Xiwen Zhou, and Ke-Qin Hu. "Improvement of hepatic fibrosis after tenofovir disoproxil fumarate switching to tenofovir alafenamide for three years." World Journal of Hepatology 16, no. 7 (2024): 1009–17. http://dx.doi.org/10.4254/wjh.v16.i7.1009.

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BACKGROUND Both tenofovir alafenamide (TAF) and tenofovir disoproxil fumarate (TDF) are the first-line treatments for chronic hepatitis B (CHB). We have showed switching from TDF to TAF for 96 weeks resulted in further alanine aminotransferase (ALT) improvement, but data remain lacking on the long-term benefits of TDF switching to TAF on hepatic fibrosis. AIM To assess the benefits of TDF switching to TAF for 3 years on ALT, aspartate aminotransferase (AST), and hepatic fibrosis improvement in patients with CHB. METHODS A single center retrospective study on 53 patients with CHB who were initi
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8

De Clercq, Erik. "Tenofovir alafenamide (TAF) as the successor of tenofovir disoproxil fumarate (TDF)." Biochemical Pharmacology 119 (November 2016): 1–7. http://dx.doi.org/10.1016/j.bcp.2016.04.015.

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9

Agbaji, Oche O., Isaac O. Abah, Augustine O. Ebonyi, et al. "Long Term Exposure to Tenofovir Disoproxil Fumarate-Containing Antiretroviral Therapy Is Associated with Renal Impairment in an African Cohort of HIV-Infected Adults." Journal of the International Association of Providers of AIDS Care (JIAPAC) 18 (January 1, 2019): 232595821882196. http://dx.doi.org/10.1177/2325958218821963.

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Objectives and Method: There are growing concerns of tenofovir disoproxil fumarate (TDF)–associated renal toxicity. We evaluated the effect of long-term TDF exposure on renal function in a cohort of HIV-1-infected Nigerians between 2006 and 2015. Multivariate logistic regression was used to identify predictors of renal impairment at different time over 144 weeks of antiretroviral therapy (ART). Results: Data of 4897 patients, median age 42 years (interquartile range: 36-49), and 61% females were analyzed. The prevalence of renal impairment increased from 10% at week 24 to 45% at 144 weeks in T
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10

Liu, Rui, Jin Qiao, Lin Zhang, and Zhihua Dou. "Therapeutic effectiveness analysis of tenofovir alafenamide and tenofovir disoproxil fumarate on the treatment for chronic hepatitis B." Medicine 103, no. 20 (2024): e37953. http://dx.doi.org/10.1097/md.0000000000037953.

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To explore the therapeutic effectiveness of tenofovir alafenamide (TAF) and tenofovir disoproxil fumarate (TDF) on the treatment for chronic hepatitis B (CHB). Retrospectively analyzing 241 cases of chronic hepatitis B patients admitted to our hospital from January 2020 to December 2021, they were divided into a TAF group of 180 cases and a TDF group of 61 cases. The liver function, serum virus markers, clinical efficacy, adverse reactions and cost-effectiveness ratio (CER) analysis of 2 groups were compared. Two groups of patients had no statistically significant difference in the levels of a
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11

Suzuki, Kazuharu, Goki Suda, Yoshiya Yamamoto, et al. "Effect of switching from tenofovir disoproxil fumarate to tenofovir alafenamide on lipid profiles in patients with hepatitis B." PLOS ONE 17, no. 1 (2022): e0261760. http://dx.doi.org/10.1371/journal.pone.0261760.

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For long-term treatment of hepatitis B virus (HBV) infection, switching from tenofovir-disoproxil-fumarate (TDF) to tenofovir-alafenamide (TAF) may prevent renal dysfunction and bone loss. However, the precise effects of this switch on the blood lipid profile remain to be clarified. This is an important issue as TDF is known to have effects on both low- and high-density lipids. Therefore, our retrospective multi-center study aimed to evaluate the effects of switching from TDF to TAF on the lipid profile of patients with HBV infection. Samples were obtained prior to the switch from TDF to TAF a
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12

Noh, You Ran, and Hae Sun Suh. "Association of Osteoporosis-related Healthcare Costs with the Use of Tenofovir Disoproxil Fumarate and Tenofovir Alafenamide in Chronic Hepatitis B Patients: a Population-based National Cohort Study in Korea." Yakhak Hoeji 68, no. 1 (2024): 26–35. http://dx.doi.org/10.17480/psk.2024.68.1.26.

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Long-term administration of tenofovir disoproxil fumarate (TDF) for chronic hepatitis B (CHB) may lead to bone mineral density loss. Tenofovir alafenamide (TAF) developed to address these concerns. This study aimed to investigate whether there is a significant difference in osteoporosis-related healthcare costs between CHB patients treated with TDF and TAF. This study is a retrospective cohort study using claims data from the Health Insurance Review and Assessment Service (HIRA) covering the entire population in Korea. The cohort included CHB patients treated with TDF or TAF from November 2017
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13

Sepuri, Vijayalaxmi and N. Umasri. "FORMULATION DEVELOPMENT AND IN VITRO EVALUATION OF TENOFOVIR DISOPROXIL FUMARATE (TDF) IMMEDIATE RELEASE TABLETS." Indo Am. J. P. Sci, 2017 04, no. 05 (2017): 1229–41. https://doi.org/10.5281/zenodo.583712.

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In the present work, an attempt has been made to develop immediate release tablets of Tenofovir Disoproxil Fumarate (TDF). In the present work Sodium starch glycollate and Cross carmellose sodium were employed as super disintegrating agents for the selected drug molecule.. All the formulations were prepared by wet granulation method. The blend of all the formulations showed god flow properties such as angle of repose, bulk density, tapped density. The prepared tablets were shown good post compression parameters and they passed all the quality control evaluation parameters as per I.P limits. Am
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14

Callebaut, Christian, George Stepan, Yang Tian, and Michael D. Miller. "In VitroVirology Profile of Tenofovir Alafenamide, a Novel Oral Prodrug of Tenofovir with Improved Antiviral Activity Compared to That of Tenofovir Disoproxil Fumarate." Antimicrobial Agents and Chemotherapy 59, no. 10 (2015): 5909–16. http://dx.doi.org/10.1128/aac.01152-15.

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ABSTRACTTenofovir alafenamide (TAF) is an investigational oral prodrug of the HIV-1 nucleotide reverse transcriptase inhibitor tenofovir (TFV). Tenofovir disoproxil fumarate (TDF) is another TFV prodrug, widely used for the treatment of HIV-1 infection. TAF is converted mostly intracellularly to TFV and, in comparison to TDF, achieves higher tenofovir diphosphate (TFV-DP) levels in peripheral blood mononuclear cells. As a result, TAF has demonstrated potent anti-HIV-1 activity at lower doses than TDF in monotherapy studies. Here, thein vitrovirology profile of TAF was evaluated and compared to
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15

Lioufas, Nicole, Alan Street, Paul Champion De Crespigny, and Stephen G. Holt. "Monitoring the Effects of Tenofovir Disoproxil Fumarate to Tenofovir Alafenamide Switch for Tubulotoxicity in Highly Treatment-Experienced or in Very Sick Individuals Infected with HIV." Journal of Renal and Hepatic Disorders 2, no. 2 (2018): 1–5. http://dx.doi.org/10.15586/jrenhep.2018.33.

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Tenofovir disoproxil fumarate (TDF) is a common antiretroviral utilised in the treatment of human immunodeficiency virus (HIV) and hepatitis B infections. It is associated with the development of tubulotoxicity and tubulopathies, and is not recommended in the treatment of patients with baseline chronic kidney disease. Until now, guidelines have suggested frequent monitoring of serum biochemistry to detect the development of such complications. In recent trials, a new prodrug formulation of tenofovir alafenamide (TAF) has been shown to exhibit less tubular toxicity than its counterpart due to a
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16

Calcagno, Andrea, Ivano Dal Conte, Dario Cattaneo, et al. "Low Tenofovir Plasma Exposure in HIV Oral Pre-exposure Prophylaxis Recipients with Gastrointestinal Disorders." Antimicrobial Agents and Chemotherapy 65, no. 1 (2020): e01902-20. http://dx.doi.org/10.1128/aac.01902-20.

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ABSTRACTFour pre-exposure prophylaxis (PrEP) users with gastrointestinal disorders (sleeve gastrectomy, terminal ileitis, celiac disease, or chronic diarrhea) and receiving oral tenofovir disoproxil fumarate/emtricitabine (TDF/FTC) were included. Despite self-reported high adherence, trough plasma tenofovir concentrations (after supervised intake) were significantly lower in these patients than in PrEP recipients without gastrointestinal disorders (21 ± 9.1 versus 138 ± 85 ng/ml). PrEP users with gastrointestinal disorders may need increased TDF doses or alternative prophylactic measures.
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17

Venkatesan, S., and N. Kannappan. "Simultaneous Spectrophotometric Method for Determination of Emtricitabine and Tenofovir Disoproxil Fumarate in Three-Component Tablet Formulation Containing Rilpivirine Hydrochloride." International Scholarly Research Notices 2014 (November 16, 2014): 1–8. http://dx.doi.org/10.1155/2014/541727.

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Developing a single analytical method for estimation of individual drug from a multidrug composition is a very challenging task. A complexation, derivatization, extraction, evaporation, and sensitive-free direct UV spectrophotometric method is developed and validated for the simultaneous estimation of some antiviral drugs such as emtricitabine (EMT), tenofovir disoproxil fumarate (TDF), and rilpivirine HCl (RPV) in tablet dosage form by Vierordt’s method. The solutions of standard and sample were prepared in methanol. The λmax⁡ for emtricitabine, tenofovir disoproxil fumarate, and rilpivirine
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18

Cattaneo, Dario, Davide Minisci, Sara Baldelli, et al. "Effect of Cobicistat on Tenofovir Disoproxil Fumarate (TDF)." JAIDS Journal of Acquired Immune Deficiency Syndromes 77, no. 1 (2018): 86–92. http://dx.doi.org/10.1097/qai.0000000000001558.

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19

Silva, Sandra Regina, Gabriel Souza-Silva, Carolina Paula de Souza Moreira, et al. "Biodegradation of the Antiretroviral Tenofovir Disoproxil by a Cyanobacteria/Bacterial Culture." Toxics 12, no. 10 (2024): 729. http://dx.doi.org/10.3390/toxics12100729.

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Tenofovir disoproxil fumarate (TDF) is an antiretroviral drug extensively used by people living with HIV. The TDF molecule is hydrolysed in vivo and liberates tenofovir, the active part of the molecule. Tenofovir is a very stable drug and the discharge of its residues into the environment can potentially lead to risk for aquatic species. This study evaluated the TDF biodegradation and removal by cultures of Microcystis novacekii with the bacteria Pseudomonas pseudoalcaligenes. Concentrations of TDF of 12.5, 25.0, and 50.0 mg/L were used in this study. The process occurred in two stages. In the
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20

Łomiak, Michał, Jan Stępnicki, Tomasz Mikuła, and Alicja Wiercińska-Drapało. "Weight and body mass index increase after switch from tenofovir disoproxil fumarate to tenofovir alafenamide fumarate-containing treatment in an antiretroviral therapy-experienced group." International Journal of STD & AIDS 32, no. 6 (2021): 570–77. http://dx.doi.org/10.1177/0956462420983699.

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Tenofovir alafenamide fumarate (TAF) is an alternative to tenofovir disoproxil fumarate (TDF). Currently, TAF is increasingly being used because of its non-inferior antiviral properties, lower risk of nephrotoxicity, and lower decrease in bone mineral density than TDF. There is growing evidence of unfavorable effects of TAF on weight and body mass index (BMI) in antiretroviral therapy (ART)-experienced patients treated with TAF-based ART. The aim of this study was to evaluate whether switching from TDF-containing to TAF-containing ART is associated with an increase in BMI and body weight in AR
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21

Byrne, Ruth, Ivana Carey, and Kosh Agarwal. "Tenofovir alafenamide in the treatment of chronic hepatitis B virus infection: rationale and clinical trial evidence." Therapeutic Advances in Gastroenterology 11 (January 1, 2018): 175628481878610. http://dx.doi.org/10.1177/1756284818786108.

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Tenofovir alafenamide (TAF), a novel prodrug of tenofovir was developed to deliver enhanced antiviral potency and reduced systemic toxicities by more efficient intracellular delivery of the active metabolite tenofovir disphosphate than tenofovir disoproxil fumarate (TDF). In two randomized, double-blind, multinational phase III trials in patients with hepatitis B e antigen (HBeAg)-positive or -negative infection, TAF 25 mg was non-inferior to TDF 300 mg in achieving the primary efficacy outcome of a hepatitis B virus (HBV) DNA level < 29 IU/ml at week 48 and was associated with higher rates
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22

Lee, I.-Cheng, Keng-Hsin Lan, Chien-Wei Su, et al. "Efficacy and Renal Safety of Prophylactic Tenofovir Alafenamide for HBV-Infected Cancer Patients Undergoing Chemotherapy." International Journal of Molecular Sciences 23, no. 19 (2022): 11335. http://dx.doi.org/10.3390/ijms231911335.

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There are no data comparing the efficacy and safety of prophylactic entecavir (ETV), tenofovir disoproxil fumarate (TDF) and tenofovir alafenamide (TAF) for HBV-infected cancer patients undergoing chemotherapy. This study aimed to compare the efficacy and renal safety of ETV, TDF and TAF in this setting. HBsAg-positive cancer patients treated with ETV (n = 582), TDF (n = 200) and TAF (n = 188) during chemotherapy were retrospectively enrolled. Antiviral efficacy and risk of renal events were evaluated. The rate of complete viral suppression at 1 year was 94.7%, 94.7% and 96.1% in ETV, TDF and
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23

Hikasa, Shinichi, Shota Shimabukuro, Kyoko Hideta, et al. "Decreased levels of urinary liver-type fatty acid-binding protein after switching from tenofovir disoproxil fumarate to tenofovir alafenamide: a prospective observational study." International Journal of STD & AIDS 30, no. 13 (2019): 1311–17. http://dx.doi.org/10.1177/0956462419873772.

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A single-center, prospective, observational study was conducted between September 2016 and August 2018 in 33 HIV-positive Japanese patients who switched antiretroviral drug regimens from tenofovir disoproxil fumarate (TDF) to tenofovir alafenamide (TAF). The study assessed changes in urinary levels of liver-type fatty acid-binding protein (L-FABP) after switching from TDF to TAF and determined the potential of renal parameters to predict improvement in estimated glomerular filtration rate (eGFR). Median urinary levels of L-FABP were found to be 2.0, 1.4, and 1.3 µg/g creatinine before, at 6 mo
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24

Su, Pei-Yuan, Wei-Wen Su, Yu-Chun Hsu, Siou-Ping Huang, and Hsu-Heng Yen. "Real-world experience of switching from tenofovir disoproxil fumarate to tenofovir alafenamide in patients with chronic hepatitis B: a retrospective study." PeerJ 9 (November 19, 2021): e12527. http://dx.doi.org/10.7717/peerj.12527.

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Background Tenofovir alafenamide (TAF) has good viral suppression efficacy and less adverse effect than tenofovir disoproxil fumarate (TDF). Real-world studies on the antiviral efficacy and safety of switching from TDF to TAF in patients with chronic hepatitis B (CHB) are limited. Methods This retrospective study included 167 nucleos(t)ide analogue (NA)-naive patients with CHB. All the patients received TDF at least 12 months before switching and TAF at least 12 months after switching at a single medical center. The Friedman test with Dunn–Bonferroni post hoc tests and repeated-measures analys
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25

Sabrina, Lissa, and Sidharta Salim. "Fanconi Syndrome and Osteomalacia Induced by Tenofovir." Cermin Dunia Kedokteran 51, no. 4 (2024): 207–9. http://dx.doi.org/10.55175/cdk.v51i4.875.

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Introduction: Tenofovir disoproxil fumarate (TDF), an antiviral nucleoside analog reverse transcriptase inhibitor, has been used for the treatment of HIV and HBV in the past decades. TDF nephrotoxicity has been reported and could lead to renal failure and Fanconi Syndrome (FS). Case: A 58-year-old female HBsAg carrier with TDF treatment since 2013 presented with osteomalacia. She had glucosuria, albuminuria, vitamin D insufficiency, hypophosphatemia, and occasional hypokalemia episodes. Laboratory results showed amino aciduria, which indicates renal tubulopathy. The diagnosis of Fanconi syndro
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Samad, Sameer, Aparna Balachandran, Rahul Nalayadam, and Sajith Narayanan. "Tenofovir disoproxil fumarate-related toxicity: A case of Fanconi syndrome." Journal of Microbiology and Infectious Diseases 13, no. 4 (2023): 196. http://dx.doi.org/10.5455/jmid.2023.v13.i4.5.

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Background: Tenofovir-based regimens remain the first choice for the treatment of human immunodeficiency virus infection and hepatitis B infection. Despite its virologic efficacy and ease of administration, it can lead to significant nephrotoxicity which may not be fully reversible. Case Description: An elderly gentleman on Tenofovir disoproxil fumarate (TDF)-based antiretroviral therapy for 10 years presented with vague symptoms of fatigue, poor oral intake and constipation. He was found to have hypokalemia and a volume depleted status. Detailed evaluation revealed hyperchloremic metabolic ac
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27

Van Slyke, Loraine, and Mia Scott. "Acute Trigeminal Neuralgia Associated with Initiation of Emtricitabine/Tenofovir for HIV Pre-Exposure Prophylaxis." Journal of the International Association of Providers of AIDS Care (JIAPAC) 17 (January 1, 2018): 232595821876084. http://dx.doi.org/10.1177/2325958218760846.

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HIV pre-exposure prophylaxis (PrEP) with emtricitabine (FTC) and tenofovir disoproxil fumarate (TDF) fixed-dose combination (FTC/TDF) is undergoing rapid scale-up in the United States. While FTC/TDF is typically well tolerated, to our knowledge, cranial nerve pathology associated with FTC/TDF has not been previously described. We report the case of a 35-year-old patient who began FTC/TDF PrEP and developed acute trigeminal neuralgia. The neurologic symptoms resolved after treatment discontinuation and recurred upon rechallenge, resulting in permanent discontinuation of PrEP treatment.
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G.Al-Rakhat, Iman, and Nada N.Al-Shawi. "Effects of Hydrochlorothiazide on Tenofovir Disoproxil Fumarate-Induced Nephrotoxicity in Rats." Iraqi Journal of Pharmaceutical Sciences ( P-ISSN: 1683 - 3597 , E-ISSN : 2521 - 3512) 28, no. 2 (2019): 58–64. http://dx.doi.org/10.31351/vol28iss2pp58-64.

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Tenofovir disoproxil fumarate, a nucleotide reverse transcriptase inhibitor utilized for the treatment of hepatitis B virus and human immunodeficiency virus infections; and is now one of the most widely used antiretroviral drug. However, tenofovir disoproxil fumarate can induce nephrotoxicity, which may be attributed to the interaction between such drug and the organic anion transporters (hOAT1, and OAT3) with consequent changes in levels of some parameters that may have a role in nephrotoxicity. Thiazide diuretics have high to intermediate potency of inhibition of OAT1s and OAT3; thus, it may
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29

Man, Xie, and Rao Wei. "Advancements in the prevention of hepatitis B recurrence by nucleos(t)ide analogue monotherapies after liver transplantation." European Journal of Inflammation 20 (January 2022): 1721727X2211392. http://dx.doi.org/10.1177/1721727x221139254.

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Previous studies have shown that the recurrence rate of HBV (hepatitis B virus) after liver transplantation (LT) can be as high as 80% without any preventive measures. Therefore, prevention of HBV recurrence after LT is always an essential part of clinical work worldwide. The NAs that have been approved for HBV treatment include lamivudine, adefovir dipivoxil, entecavir (ETV), and telbivudine, tenofovir disoproxil fumarate (TDF), and tenofovir alafenamide (TAF). They are often combined with HBIG to prevent HBV recurrence after LT clinically. However, NAs with a higher genetic barrier, such as
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30

Abdool Karim, Salim S., Cheryl Baxter, and Quarraisha Abdool Karim. "Advancing HIV prevention using tenofovir-based pre-exposure prophylaxis." Antiviral Therapy 27, no. 1 (2022): 135965352110675. http://dx.doi.org/10.1177/13596535211067589.

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Tenofovir-based pre-exposure prophylaxis (PrEP) revolutionized the global HIV prevention landscape. Prior to the proof-of concept trial in 2010, which demonstrated that tenofovir (TFV) could prevent sexual transmission of HIV, prevention options were largely limited to behavior change, condoms, and circumcision. Several subsequent studies evaluating oral tenofovir disoproxil fumarate (TDF) or the TDF/emtricitabine (FTC) combination as PrEP for HIV prevention provided evidence for regulatory approval and inclusion in national and international guidelines. By 2021, 1.5 million people had initiat
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31

Salimi, Rozhin, Ishmath Begum, Danturulu Muralidhar Varma, B. Nandakrishna, Radhakrishnan Rajesh, and Sudha Vidyasagar. "Tenofovir disoproxil fumarate-induced distal renal tubular acidosis: A case report." International Journal of STD & AIDS 31, no. 3 (2020): 276–79. http://dx.doi.org/10.1177/0956462419887877.

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Tenofovir disoproxil fumarate (TDF) is an anti-retroviral drug that is known to cause nephrotoxicity including renal tubular acidosis (RTA). With increasing literature on proximal RTA caused by TDF, reports on distal RTA are scarce, with only one case reported so far. We report a case of distal RTA in patient living with human immunodeficiency virus, who presented with nausea and fatigue giving a history of TDF-based therapy for two years. Laboratory investigations revealed non-anion gap metabolic acidosis, positive urine anion gap, hyperchloremia, and hypokalemia. The patient improved after d
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32

Sinakos, E., P. Panas, N. Fragkou, et al. "Tenofovir alafenamide prophylaxis post-liver transplantation: a real-world study in patients with chronic kidney disease." Acta Gastro Enterologica Belgica 85, no. 2 (2022): 331–37. http://dx.doi.org/10.51821/85.2.9577.

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Background and aims: Tenofovir alafenamide fumarate (TAF) was shown equally efficacious in suppressing hepatitis B virus (HBV) but with less renal toxicity than tenofovir disoproxil fumarate (TDF). The aim of this real-world study was to evaluate renal function in post-liver transplantation (LT) patients that changed TDF with TAF. Methods: The TAF group (n=17) included patients who switched to TAF due to low (<60 ml/min/1.73m2) Glomerular Filtration Rate (GFR). The control group included patients that remained on TDF (n=30), although some (n= 14) had chronic kidney disease (CKD) (TDF-CKD gr
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Rombini, María F., Diego Cecchini, Sofía Diana Menendez, et al. "Tenofovir-Containing Antiretroviral Therapy and Clinical Outcomes of SARS-CoV-2 Infection in People Living with HIV." Viruses 15, no. 5 (2023): 1127. http://dx.doi.org/10.3390/v15051127.

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Tenofovir has been hypothesized to be effective against COVID-19 and is available as two prodrugs, tenofovir disoproxil fumarate (TDF) and tenofovir alafenamide (TAF), both part of antiretroviral therapy (ART) regimens. People living with human immunodeficiency virus (PLWH) might be at higher risk for COVID-19 progression; however, information about the impact of tenofovir on COVID-19 clinical outcomes remains controversial. The COVIDARE is a prospective observational multicentric study in Argentina. PLWH with COVID-19 were enrolled from September 2020 to mid-June 2022. Patients were stratifie
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Imaz, Arkaitz, Jordi Niubó, Mackenzie L. Cottrell, et al. "Seminal Tenofovir Concentrations, Viral Suppression, and Semen Quality With Tenofovir Alafenamide, Compared With Tenofovir Disoproxil Fumarate (Spanish HIV/AIDS Research Network, PreEC/RIS 40)." Clinical Infectious Diseases 69, no. 8 (2018): 1403–9. http://dx.doi.org/10.1093/cid/ciy1074.

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Abstract Background This study assessed the penetration and efficacy of tenofovir alafenamide (TAF) in the male genital tract (MGT) and the semen quality of individuals infected with human immunodeficiency virus (HIV)-1 who were treated with a TAF-containing regimen. Methods This was a prospective, open-label, single-arm study of 14 virologically-suppressed, HIV-1–infected men on stable antiretroviral therapy with elvitegravir, cobicistat, emtricitabine (E/C/F) and tenofovir disoproxil fumarate (TDF) who switched to E/C/F and TAF. At baseline (pre-switch) and at 12 weeks post-switch, we measur
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D, Debaje Priyanka, and Chavan Harishchandra H. "Force Degradation Study of Tenofovir Disoproxil Fumarate by UV-Spectrophotometric Method." Asian Journal of Pharmaceutical Research and Development 8, no. 2 (2020): 21–25. http://dx.doi.org/10.22270/ajprd.v8i2.679.

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Tenofovir disoproxil Fumarate (TDF), acyclic phosphonate nucleotide analogue, used as antiretroviral agents in the treatment of HIV-1 infection. A stability indicating UV -spectrophotometric method is simple, an accurate and economic, precise and reproducible method has been used for the estimation of Tenofovir disoproxil Fumarate in bulk and tablets dosage form in present work. The wavelength selected for the absorption correction method was 260 nm. The linearity range of 2-10μg/ml proved that it obeyed Beer’s Law and the correlation coefficient (r2) was found to be 0.999 at 260 nm. The drug
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Lee, Sung Won, Jonggi Choi, Seung Up Kim, and Young-Suk Lim. "Entecavir versus tenofovir in patients with chronic hepatitis B: Enemies or partners in the prevention of hepatocellular carcinoma." Clinical and Molecular Hepatology 27, no. 3 (2021): 402–12. http://dx.doi.org/10.3350/cmh.2021.0179.

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Over the past several decades, entecavir (ETV) and tenofovir disoproxil fumarate (TDF) have remained the first-line antiviral agents in several international guidelines. These two antiviral agents have shown similar short to intermediateterm efficacy, including virologic, biochemical, serologic, and histologic responses. However, huge controversies regarding the antiviral efficacy of ETV and TDF in preventing the development of hepatocellular carcinoma (HCC) still exist. In this review, we summarized recent studies that compared the treatment efficacy of ETV and TDF in terms of HCC development
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Taneva, Ekaterina, Kerry Crooker, Sung Hyun Park, et al. "Differential Mechanisms of Tenofovir and Tenofovir Disoproxil Fumarate Cellular Transport and Implications for Topical Preexposure Prophylaxis." Antimicrobial Agents and Chemotherapy 60, no. 3 (2015): 1667–75. http://dx.doi.org/10.1128/aac.02793-15.

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Intravaginal rings releasing tenofovir (TFV) or its prodrug, tenofovir disoproxil fumarate (TDF), are being evaluated for HIV and herpes simplex virus (HSV) prevention. The current studies were designed to determine the mechanisms of drug accumulation in human vaginal and immune cells. The exposure of vaginal epithelial or T cells to equimolar concentrations of radiolabeled TDF resulted in over 10-fold higher intracellular drug levels than exposure to TFV. Permeability studies demonstrated that TDF, but not TFV, entered cells by passive diffusion. TDF uptake was energy independent but its accu
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Lee, Hye Won. "Tenofovir disoproxil fumarate is not associated with a lower risk of hepatocellular carcinoma compared to entecavir in patients with chronic hepatitis B." Hepatoma Research 8 (2022): 13. http://dx.doi.org/10.20517/2394-5079.2021.114.

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A paper published several years ago suggested that tenofovir disoproxil fumarate (TDF) was superior to entecavir (ETV) for reducing the risk of hepatocellular carcinoma (HCC). Since then, many observational studies have been conducted comparing TDF and ETV. Many studies in Asia demonstrated similar HCC risks between ETV and TDF groups. Similarly, recent studies involving Caucasian and European did not observe any differences in HCC risk between these groups. In this article, we briefly review studies that compared the incidence rates of HCC between ETV and TDF and discuss potential reasons for
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De Clercq, Erik. "Tribute to John C. Martin at the Twentieth Anniversary of the Breakthrough of Tenofovir in the Treatment of HIV Infections." Viruses 13, no. 12 (2021): 2410. http://dx.doi.org/10.3390/v13122410.

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At Bristol-Myers (BM) (1985–1990), John C. Martin started his HIV career with directing the clinical development of didanosine (ddI) and stavudine (d4T). During this period, he became aware of the acyclic nucleoside phosphonates (ANPs), such as (S)-HPMPA and PMEA, as potential antiviral drugs. Under his impulse, BM got involved in the evaluation of these ANPs, but the merger of BM with Squibb (to become BMS) incited John to leave BM and join Gilead Sciences, and the portfolio of the ANPs followed the transition. At Gilead, John succeeded in obtaining the approval from the US FDA for the use of
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Surial, Bernard, Bruno Ledergerber, Alexandra Calmy, et al. "Changes in Renal Function After Switching From TDF to TAF in HIV-Infected Individuals: A Prospective Cohort Study." Journal of Infectious Diseases 222, no. 4 (2020): 637–45. http://dx.doi.org/10.1093/infdis/jiaa125.

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Abstract Background Replacing tenofovir disoproxil fumarate (TDF) with tenofovir alafenamide (TAF) improves renal tubular markers in HIV-infected individuals but the impact on estimated glomerular filtration rate (eGFR) remains unclear. Methods In all participants from the Swiss HIV Cohort Study who switched from TDF to TAF-containing antiretroviral regimen or continued TDF, we estimated changes in eGFR and urine protein-to-creatinine ratio (UPCR) after 18 months using mixed-effect models. Results Of 3520 participants (26.6% women, median age 50 years), 2404 (68.5%) switched to TAF. Overall, 1
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Huang, Xu-Sheng, Rong-Hua Luo, Xiong-Lin Hu, et al. "The New NNRTI ACC007 Combined with Lamivudine and Tenofovir Disoproxil Fumarate Show Synergy Anti-HIV Activity In Vitro." Current HIV Research 18, no. 5 (2020): 332–41. http://dx.doi.org/10.2174/1570162x18666200620211922.

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Background: Acquired immunodeficiency syndrome can hardly be cured currently and people with human immunodeficiency virus (HIV) need lifelong treatment that may result in the emergence of drug resistance which leads to failed treatment. Thus, the development of new anti- HIV drugs and new treatment regimens are necessary. Objective: The aim of this study is to analyze the combined anti-HIV activity of tenofovir disoproxil fumarate, lamivudine and ACC007, a new non-nucleoside reverse transcriptase inhibitor. Methods: The antiviral activity of tenofovir disoproxil fumarate, lamivudine and ACC007
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Harini, U., and AKM Pawar. "A validated stability indicating LC-MS compatible RP-HPLC assay and dissolution methods for marketed formulation Stribild." Journal of Drug Delivery and Therapeutics 8, no. 6 (2018): 159–70. http://dx.doi.org/10.22270/jddt.v8i6.2037.

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Objective: The prime objective of the current work is to develop a simple, rapid, efficient, economical and stability indicating LC-MS (liquid chromatography–mass spectroscopy) compatible RP - HPLC (reverse phase – high performance liquid chromatography) method for the analysis of emtricitabine (EMT), tenofovir disoproxil fumarate (TDF), cobicistat (COB) and elvitegravir (ELV) in bulk, marketed formulation (Stribild) and in In-vitro dissolution method.
 Method: The chromatography was achieved on Unisol C18 column (250 × 4.0 mm, 3 µ) with a mobile phase combination of acetate buffer (adjus
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Gérard, Laurence, Corine Chazallon, Anne-Marie Taburet, Pierre-Marie Girard, Jean-Pierre Aboulker, and Christophe Piketty. "Renal Function in Antiretroviral-Experienced Patients treated with Tenofovir Disoproxil Fumarate associated with Atazanavir/ritonavir." Antiviral Therapy 12, no. 1 (2007): 31–40. http://dx.doi.org/10.1177/135965350701200110.

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Objective To determine the evolution of renal function in highly treatment-experienced patients with normal renal function at baseline receiving tenofovir disoproxil fumarate (TDF) as part of a fixed combined antiretroviral regimen and to identify prognostic factors of change in renal function, including tenofovir concentrations. Methods A prospective 48-week open-label trial was carried out, evaluating the safety of TDF, associated with atazanavir/ritonavir, and optimized nucleoside reverse transcriptase inhibitors, in patients with documented failure in previous treatments. Statistical analy
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Wang, Xinzhu, Will Nutland, Michael Brady, Ian Green, Marta Boffito, and Myra McClure. "Quantification of tenofovir disoproxil fumarate and emtricitabine in generic pre-exposure prophylaxis tablets obtained from the internet." International Journal of STD & AIDS 30, no. 8 (2019): 765–68. http://dx.doi.org/10.1177/0956462419841144.

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In this study, we addressed the recent concerns over the authenticity of generic pre-exposure prophylaxis (PrEP) purchased online by sampling 14 generic PrEPs from different manufacturers and suppliers and measuring tenofovir disoproxil fumarate (TDF) and emtricitabine (FTC) content using high-performance liquid chromatography. We confirmed that all the PrEP tablets contained 94.3% to 104.9% of the 300 mg of TDF claimed on the label and 97.3% to 104.4% of the 200 mg FTC claimed on the label.
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Bosch, Bronwyn, Godspower Akpomiemie, Nomathemba Chandiwana, et al. "Weight and metabolic changes after switching from tenofovir alafenamide (TAF)/emtricitabine (FTC)+dolutegravir (DTG), tenofovir disoproxil fumarate (TDF)/FTC+DTG and TDF/FTC/efavirenz (EFV) to TDF/lamivudine (3TC)/DTG." Clinical Infectious Diseases, December 15, 2022. http://dx.doi.org/10.1093/cid/ciac949.

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Abstract Participants randomised to first-line tenofovir alafenamide (TAF)/emtricitabine (FTC)+dolutegravir (DTG), tenofovir disoproxil fumarate (TDF)/FTC+DTG or TDF/FTC/efavirenz (EFV) for 192 weeks were then switched to TDF/lamivudine (3TC)/DTG for 52 weeks. Participants switching either TAF/FTC+DTG or TDF/FTC/EFV to TDF/3TC/DTG showed statistically significant reductions in weight, low density lipoprotein, triglycerides, glucose and glycated haemoglobin.
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Odhiambo, Fredrick, Shallot Nareeba, Grace Mwangeka, Ann Njambi, and Vashti Nyakebati. "Tenofovir induced Fanconi syndrome in a middle age African female from Kenya, East Africa: Case report and brief literature review." Clinical Case Reports 12, no. 6 (2024). http://dx.doi.org/10.1002/ccr3.8889.

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Key Clinical MessageThis case presentation highlights the need to routinely monitor renal function in patients on Tenofovir Disoproxil Fumarate (TDF) due to its side effect of proximal tubule dysfunction.AbstractThis is a case presentation of a 50‐year‐old African female who had been on a Tenofovir based regimen for 12 years and developed Fanconi syndrome. She recovered after discontinuation of the Tenofovir Disoproxil Fumarate (TDF).
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Huhn, Gregory D., David J. Shamblaw, Jean-Guy Baril, et al. "Atherosclerotic Cardiovascular Disease Risk Profile of Tenofovir Alafenamide Versus Tenofovir Disoproxil Fumarate." Open Forum Infectious Diseases 7, no. 1 (2019). http://dx.doi.org/10.1093/ofid/ofz472.

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Abstract Background In human immunodeficiency virus (HIV) treatment, tenofovir alafenamide (TAF) is associated with greater increases in all fasting cholesterol subgroups compared with tenofovir disoproxil fumarate (TDF). Because lipid abnormalities may contribute to cardiovascular morbidity and mortality, cardiovascular risk assessment is integral to routine HIV care. This post hoc study evaluates the impact of lipid changes on predicted atherosclerotic cardiovascular disease (ASCVD) risk and statin eligibility in treatment-naive adults living with HIV treated with TAF or TDF. Methods Partici
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Hurchund, Rajendraparsad, Sinegugu E. Sibiya, Bernard O. Owaga, and Peter M. O. Owira. "Tenofovir alafenamide compared to tenofovir disoproxil fumarate, induces dysglycemia, and dyslipidemia in Wistar rats." AIDS, August 1, 2024. http://dx.doi.org/10.1097/qad.0000000000003987.

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Objectives: To determine the metabolic effects of tenofovir alafenamide (TAF) compared to tenofovir disoproxil fumarate (TDF) in vivo. Design and methods: Male Wistar rats (Rattus novergicus, 250–300 g body weight) were divided into 3 groups (n = 8) and orally treated daily with 1.0 ml distilled water (group 1), TAF (0.42 mg/kg) (group 2), or TDF (5.0 mg/kg) (group 3), respectively, for 56 days. Glucose tolerance tests were done before the animals were sacrificed by halothane overdose, and blood was collected by cardiac puncture for the analysis of plasma lipids, electrolytes, and insulin. The
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Johnson, Kelly A., Hideaki Okochi, Mireya Arreguin, et al. "Brief Report: Urine Tenofovir Levels Strongly Correlate with Virologic Suppression in Patients with HIV on Tenofovir Alafenamide-Based Antiretroviral Therapy." Clinical Infectious Diseases, October 18, 2022. http://dx.doi.org/10.1093/cid/ciac828.

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Abstract We found that urine tenofovir (TFV) levels >1500 ng/ml strongly predict virologic suppression among patients with HIV taking tenofovir alafenamide (TAF, OR 5.66; 95% CI 1.59-20.14; p = 0.007). This suggests an existing point-of-care assay developed for tenofovir disoproxil fumarate (TDF) will support adherence monitoring for patients on all TFV-based antiretrovirals.
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Rivera, Adovich S., Katherine Pak, Matthew T. Mefford, and Rulin C. Hechter. "Changes in Glomerular Filtration Rate after Switching from Tenofovir Disoproxil Fumarate to Tenofovir Alafenamide Fumarate for HIV Pre-exposure Prophylaxis." Open Forum Infectious Diseases, December 29, 2023. http://dx.doi.org/10.1093/ofid/ofad695.

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Abstract Background Tenofovir alafenamide fumarate (TAF) was promoted as a safer alternative to tenofovir disoproxil fumarate (TDF) for HIV oral pre-exposure prophylaxis (PrEP). It is unknown if switching from TDF to TAF translates to improved renal function. We used electronic health records (EHR) data to assess changes in creatinine-estimated glomerular filtration rate (eGFR) after switching from TDF to TAF. Methods We conducted a retrospective cohort study using EHR data from Kaiser Permanente Southern California. We identified individuals who switched from TDF to TAF between October 2019-M
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