adefovir dipivoxil / Generic mfg. - LARVOL DELTA

Protective Effects of Adefovir Dipivoxil in Pancreatic β Cell Lines (ENDO 2025) - "These data show that ADV can protect against fatty acid toxicity and increase insulin secretion in pancreatic β cells, potentially through mitohormesis. This drug can elucidate the role of mitochondria in the pathogenesis of type 2 diabetes mellitus, which may lead to new understandings and therapeutic approaches."

Preclinical • Diabetes • Genetic Disorders • Metabolic Disorders • Obesity • Type 2 Diabetes Mellitus

Structural insights into human polyspecific organic anion transporters OAT1 and OAT4. (PubMed, Cell Rep) - "Here, we resolved the cryo-electron microscopy structures of human OAT1 in its apo form and bound to probenecid, adefovir, cefazolin, and para-aminohippuric acid (PAH), as well as human OAT4 in its apo form and in complex with dehydroepiandrosterone sulfate (DHEAS). DHEAS in OAT4 exhibits a different binding mode, illustrating the multispecific ligand-binding characteristics of OATs. Our findings provide a framework for drug design and management of drug-drug interactions involving OAT1."

Journal

Molecular Mechanism of Tenofovir Nephrotoxicity When Combined with an ABCC Inhibitor (ASM Microbe 2025) - "However, it is still unclear as to how PIs such as ritonavir (RTV) and Lopinavir (LPV) increase the risk for nephrotoxicity...Additional data will be further presented for other ANPs such as adefovir combined with escalating PIs or cobicistat on cytotoxicity... These findings suggest that overexpression of MRP4 and MRP5 could render resistance toward TFV-mediated toxicities, while MRP2 is most efficient in transporting TFV out of the cells. These findings affirmed that intracellular levels of ANPs such as TFV may be regulated by MRP2-mediated activity."

Human Immunodeficiency Virus • Infectious Disease • Nephrology • ABCB1 • ABCC2 • ABCC4

Transcriptomic insights into the mechanism of action of telomere-related biomarkers in rheumatoid arthritis. (PubMed, Front Immunol) - "Five drugs-methotrexate, adefovir, furosemide, azathioprine, and cefmetazole-were also identified as targeted biomarkers. The results of the in vitro experiments were consistent with those obtained from the bioinformatics analysis. This study identified five biomarkers-ABCC4, S100A8, VAMP2, PIM2, and ISG20-and offered new insights into potential therapeutic strategies for RA."

Biomarker • Journal • Immunology • Inflammation • Inflammatory Arthritis • Rheumatoid Arthritis • Rheumatology • Transplant Rejection • CD4 • S100A8 • VAMP2

QuEChERS and UPLC-MS/MS-Based Quantification of Human Plasma of Eight Nucleoside Reverse Transcriptase Inhibitors and Platinum Anticancer Drugs for Hepatocellular Carcinoma. (PubMed, Molecules) - "The target analytes-lamivudine, telbivudine, emtricitabine, entecavir, tenofovir, nedaplatin, oxaliplatin, and adefovir dipivoxil-exhibited strong linearity within the 10-1000 ng/mL and 1-100 ng/mL ranges, showing correlations (r2) ≥ 0.9962. Overall, this analytical approach can be used to detect the combination of eight NRTIs and platinum-based drugs in human plasma. This method enables plasma drug-level monitoring in real time, with applications for individualized treatment approaches."

Journal • Hepatocellular Cancer • Oncology • Solid Tumor

A global comparison of hepatitis B & C drug pricing. (PubMed, Ann Hepatol) - "HBV and HCV originator medications cost significantly more in the US compared to seven other major industrial countries. However, the introduction of HBV generic medications has lowered the cost of treatment for patients in the US. Future adoption of international reference pricing may help bridge remaining pricing disparities."

Journal • Pricing • Hepatitis B • Hepatitis C • Infectious Disease • Inflammation

EFFICACY AND SAFETY OF TREATMENTS FOR CHRONIC HEPATITIS D: A SYSTEMATIC REVIEW AND META-ANALYSIS OF 19 RANDOMIZED CONTROLLED TRIALS (DDW 2025) - "Objective: This meta-analysis evaluates the efficacy and safety of pharmacological treatments for chronic HDV, including Lamivudine, Peg-IFN, Ribavirin, IFN alfa-2a, Adefovir, Bulevirtide, Lonafarnib, TDF, and Entecavir... Bulevirtide with Peg-IFN is the most effective and safest treatment for chronic HDV, particularly in cirrhotic patients. TDF shows potential but requires further study in larger, long-term trials. Adverse effects from therapies like Peg-IFN and Lonafarnib emphasize the need for careful monitoring."

Retrospective data • Review • Anemia • Fatigue • Gastrointestinal Disorder • Hematological Disorders • Hepatitis B • Hepatology • Infectious Disease • Inflammation • Liver Cirrhosis • Pain

FDA-approved drug repurposing screen identifies inhibitors of SARS-CoV-2 pseudovirus entry. (PubMed, Front Pharmacol) - "Pyridoxal 5'-phosphate, Dovitinib, Adefovir dipivoxil, and Biapenem potently inhibit ACE2-dependent viral entry with inhibitory concentration 50% (IC50) values of 57nM, 74 nM, 130 nM, and 183 nM, respectively. We identified four novel FDA-approved candidate drugs for anti-SARS-CoV-2 combination therapy. Our findings contribute to the growing body of evidence supporting drug repurposing as a viable strategy for rapidly developing COVID-19 treatments."

FDA event • Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Use of Sodium-Glucose Co-Transporter-2 Inhibitors and Risk of Hepatocellular Carcinoma in Patients with Chronic Hepatitis B, Type 2 Diabetes, and Varying Fibrosis Status (APASL 2025) - "Patients with T2D and CHB who received SGLT-2i (empagliflozin, dapagliflozin, canagliflozin or ertugliflozin) or sulfonylureas between 2015 and 2021 were enrolled from Hong Kong and all patients were followed from the first prescription of study medication till 2022. In this population-based cohort study, use of SGLT-2i, compared with sulfonylureas, decreased the risk of HCC among individuals with T2D and CHB especially in more severe liver fibrosis, suggesting a potential chemopreventive role of SGLT-2i in patients with both chronic diseases. Table and Figure:Figure 1.Table. Association between SGLT-2i use and the risk of hepatocellular carcinoma in patients with type 2 diabetes and chronic hepatitis B. *adjusted for demographic data (age and sex), lifestyle factors (alcohol, smoking, and body mass index), comorbidities (hypertension, hyperlipidemia, heart failure, coronary heart disease, stroke, atrial fibrillation, and chronic kidney disease), HBV medications..."

Clinical • Atrial Fibrillation • Cardiovascular • Chronic Kidney Disease • Congestive Heart Failure • Coronary Artery Disease • Diabetes • Diabetic Nephropathy • Dyslipidemia • Fibrosis • Heart Failure • Hepatitis B • Hepatitis C • Hepatocellular Cancer • Hepatology • Hypertension • Immunology • Infectious Disease • Liver Cirrhosis • Metabolic Disorders • Nephrology • Oncology • Renal Disease • Solid Tumor • Type 2 Diabetes Mellitus

96-week treatment of Pradefovir vs. Tenofovir Disoproxil Fumarate in chronic hepatitis B patients (APASL 2025) - "Background: Pradefovir (PDF) is a liver-targeted prodrug of adefovir, a nucleoside/nucleotide analogue developed to treat the patients with hepatitis B virus (HBV) infection. After 96-week treatment of the patients with HBV infection, PDF remained its viral suppression rate as good as TDF with a significant reduction of the serum HBsAg level; a continued better safety profiles and a better bone and renal safety suggesting that PDF maybe a better choice of NUCs in hepatitis cure regimen. Table and Figure:Figure 1.Proportion of patients with virological suppression (LLOQ=29IU/mL) at week 48w and 96w in HBeAg-positive patients (A) and HBeAg-negative patients (B). Proportion of patients whose serum HBsAg level declined more than 1log10 IU/mL in HBeAg-positive patients (C)."

Clinical • Hepatitis B • Hepatitis C • Hepatology • Infectious Disease • Inflammation

Tenofovir-based antiviral therapy reduces long-term incidence of hepatocellular carcinoma in chronic hepatitis B patients (APASL 2025) - "Studies 102 and 103 randomized patients 2:1 to double-blind (DB) treatment with tenofovir disoproxil fumarate (TDF) or adefovir dipivoxil (ADV) for 48 weeks, then open-label (OL) TDF, whereas Studies 108 and 110 randomized patients 2:1 to DB treatment with tenofovir alafenamide (TAF) or TDF for up to 144 weeks, then OL TAF. In this large dataset of prospectively followed CHB patients, HCC risk was significantly impacted with long-term TFV-based treatment in CHB patients with and without cirrhosis."

Clinical • Fibrosis • Hepatitis B • Hepatitis C • Hepatocellular Cancer • Hepatology • Immunology • Infectious Disease • Oncology • Solid Tumor

Comprehensive study of clinical features and laboratory findings of chronic viral hepatitis (APASL 2025) - "A history of HBV antiviral therapy was reported by 112 (44.4%) patients, of whom 72.5% used tenofovir, 27.1% entecavir, and 0.4% adefovir. Two patients began receiving bulevirtide injections against HDV in 2023... Young adults in their prime are affected by chronic HDV infection, with 21.8% diagnosed with liver cirrhosis. Laboratory tests revealed elevated transaminase activity above normal levels, and 44.9% of HDV-RNA levels exceeded 106."

Clinical • Fibrosis • Hepatitis B • Hepatitis C • Hepatocellular Cancer • Hepatology • Infectious Disease • Inflammation • Liver Cirrhosis • Oncology • Solid Tumor

Effect of emitinofovir combined with thymidin a 1 treatment on surface antigen in patients with compensatory stage of hepatitis B cirrhosis (APASL 2025) - "In HBeAg-negative patients with compensated hepatitis B cirrhosis, regardless of whether HBV DNA is low-positive (<1.0E+04) or negative, the combination effectively reduces hepatitis B surface antigen levels."

Clinical • Fibrosis • Hepatitis B • Hepatitis C • Hepatology • Immunology • Infectious Disease • Inflammation

Adefovir anticancer potential: Network pharmacology, anti-proliferative & apoptotic effects in HeLa cells. (PubMed, Biomol Biomed) - "In vitro, adefovir significantly suppressed HeLa cell viability, with an Inhibitory Concentration 50 (IC50) of 7.8 μM, outperforming 5-Fluorouracil (5-FU). These integrated computational and experimental findings suggest that adefovir exerts multi-targeted effects against cervical cancer. Its promising preclinical efficacy warrants further investigation as a potential alternative therapy."

Journal • Cervical Cancer • Oncology • Solid Tumor • MAPK3

Evaluation of Adefovir PBPK Model to Assess Biomarker-Informed OAT1 Drug-Drug Interaction and Effect of Chronic Kidney Disease. (PubMed, CPT Pharmacometrics Syst Pharmacol) - "A previously verified probenecid model, incorporating in vivo OAT1/3 inhibitory constant estimated using OAT1/3 endogenous biomarker (4-pyridoxic acid) clinical data, was utilized. The model successfully predicted 3-fold higher adefovir Cmax and 6-fold higher AUC in patients with severe CKD relative to healthy individuals. This study reinforces the role of PBPK modeling to predict transporter-mediated DDI (coupled with biomarker-informed approach to optimize in vivo inhibitory constant) and the effect of renal impairment on OAT1/3 drugs in lieu of clinical studies."

Biomarker • Journal • Chronic Kidney Disease • Nephrology • Renal Disease

Successful treatment of a hepatitis B-related acute-on-chronic liver failure patient with adefovir dipivoxil combined with artificial liver and human umbilical mesenchymal stem cells (PubMed, Zhonghua Gan Zang Bing Za Zhi) - No abstract available

Journal • Hepatitis B • Hepatology • Infectious Disease • Inflammation • Liver Failure

Targeting hepatitis B virus-associated nephropathy: efficacy and challenges of current antiviral treatments. (PubMed, Clin Exp Med) - "Antiviral therapy, particularly with nucleos(t)ide analogs like entecavir and tenofovir (including TAF and TMF), demonstrates superior efficacy and safety compared to older agents such as lamivudine and adefovir...Additionally, individualized treatment strategies for specific populations, including pregnant women and HIV co-infected patients, are crucial. Addressing HBV-associated nephropathy requires enhanced surveillance, timely antiviral intervention, and tailored therapeutic approaches to improve patient outcomes."

Journal • Review • Acute Kidney Injury • Chronic Kidney Disease • Glomerulonephritis • Hepatitis B • Hepatology • Human Immunodeficiency Virus • Infectious Disease • Inflammation • Lupus Nephritis • Nephrology • Renal Disease • Transplantation

Glycoconjugates of adefovir and tenofovir as asialoglycoprotein-mediated Anti-HBV prodrugs with enhanced liver targeting. (PubMed, Eur J Med Chem) - "Notably, the tris-GalNAc conjugates A2 and T2 demonstrated superior liver targeting, showing a threefold higher concentration in the liver compared to the kidneys, thus minimizing renal exposure. These findings suggest that GalNAc and tris-GalNAc conjugation is a promising strategy for enhancing the therapeutic efficacy and safety of adefovir and tenofovir, with potential for further optimization as liver-targeted anti-HBV prodrugs."

Journal • Fibrosis • Hepatitis B • Hepatology • Immunology • Infectious Disease • Oncology • ASGR • MUC4

Clinical management of hypophosphatemic osteomalacia induced by adefovir and tenofovir: Insights from a case report. (PubMed, Medicine (Baltimore)) - "Accurate diagnosis requires a combination of clinical presentation, medical history, biochemical and radiological findings, and, if available, measurement of fibroblast growth factor 23 (FGF 23). The role of national, provincial, or regional centers for rare diseases is crucial for conducting unconventional tests and providing access to rare medications."

Journal • Fatigue • Hepatitis B • Hepatology • Infectious Disease • Musculoskeletal Diseases • Oncology • Orthopedics • Pain • Rare Diseases • FGF23

A Global Comparison of Hepatitis B Drug Pricing: US vs the Other G7 Countries and Australia (ACG 2024) - "Similarly, adefovir costs $37.89 in the US, compared to $15.79-23.37 globally, TDF $50.14 vs. $1.20-$14.76, tenofovir alafenamide fumarate $57.66 vs. $6.72-17.81, entecavir $54.90 vs. $1.83-$17.12, peginterferon alfa-2a $1336.10 vs. $116.76-$336.65, emtricitabine/TDF $73.69 vs. $0.90-$30.11... US prices for HBV originator medications were on average 4.71x the prices in the non-US G7 countries and Australia. Lamivudine costs $16.09 per dosage unit in the US, whereas it ranges between $1.67 and $4.13 among comparison countries. Similarly, adefovir costs $37.89 in the US, compared to $15.79-23.37 globally, TDF $50.14 vs."

Clinical • Pricing • Hepatitis B • Hepatology • Infectious Disease • Inflammation

7-Hydroxycoumarin and its conjugated metabolites interact with organic anion transporters 1 and 3 in vitro and in vivo. (PubMed, Chem Biol Interact) - "After co-administration of 100 mg/kg of 7-HC to mice, systemic exposure and clearance of furosemide (a clinical substrate of OATs) were significantly increased and decreased, respectively. In addition, 7-HC decreased OAT-mediated cytotoxicity and reduced the renal distribution of adefovir in mice. Together, these findings will provide support for OAT-mediated drug interactions and the renal protection of 7-HC."

Journal • Preclinical • Nephrology • Renal Disease

ESTIMATING THE PREVALENCE OF CHRONIC HEPATITIS B IN THE UNITED STATES BY STATE USING MEDICARE DATA (AASLD 2024) - " The 2021 Medicare Part D database was accessed and the number of recipients receiving any NA specific to CHB [lamivudine, adefovir, entecavir, tenofovir disoproxil fumarate (TDF) and tenofovir alafenamide (TAF)] were extracted by state... There is a significant burden of CHB in the US and this study highlights geographic variations by state seen beyond differences in population. Further study into factors affecting these differences would be important for further understanding of the epidemiology of this disease."

Medicare • Reimbursement • US reimbursement • Hepatitis B • Hepatology • Infectious Disease • Inflammation

VARIATION IN NULEOS(T)IDE ANALOGUE USE IN MEDICARE PART D THROUGHOUT THE UNITED STATES (AASLD 2024) - "The analysis included types of NA used [lamivudine, adefovir, entecavir, tenofovir disoproxil fumarate (TDF), and tenofovir alafenamide (TAF)], stratified into originator (n=6) and generic (n=5) forms, as well as access to highly potent NA (entecavir, TDF and TAF). There is considerable variation in NA utilization throughout the US although notably all states/regions provide access to highly potent NA. Formulary adjustment to a preferred generic CHB treatment strategy in the Medicare Part D program could offer cost-savings."

Medicare • Reimbursement • US reimbursement • Fibrosis • Gastrointestinal Cancer • Hepatitis B • Hepatology • Immunology • Infectious Disease • Liver Cancer • Oncology • Solid Tumor

AFFORDABLE HEPATOLOGY: EXPLORING THE POTENTIAL BENEFITS OF THE MARK CUBAN COST PLUS DRUG COMPANY MODEL FOR LIVER DISEASE TREATMENTS (AASLD 2024) - "The impact of pharmacy and shipping fees varied widely; for instance, Furosemide's fees accounted for 83% of its 30-day price, while Adefovir's fees were only 2%. Notable savings were identified for Tenofovir and Entecavir, each offering over $17 million in potential 30-day savings. In contrast, Prednisolone and Lactulose showed potential cost increases over 90 days, leading to negative savings. The total Medicare Part D spending for these drugs in 2022 was roughly $637.99 million, with significant expenses on drugs like Spironolactone and Ursodiol... The U.S. generic hepatology drug market offers significant potential for cost savings through increased competition, reduced administrative costs, and patient advocacy for price comparison. MCCPDC provides a cost-effective option, particularly for 90-day supplies, demonstrating potential savings for liver patients. This study highlights the impact of pharmacy and shipping fees on Medicare expenditures and..."

Hepatology

Albumin-Mediated Drug Uptake by Organic Anion Transporter 1/3 Is Real: Implications for the Prediction of Active Renal Secretion Clearance. (PubMed, Mol Pharm) - "The albumin-mediated uptake effect (fold increase in CLint,u,active) was more pronounced with highly bound substrates compared to no effect seen for weakly protein-bound substrates adefovir (OAT1-specific) and oseltamivir carboxylate (OAT3-specific)...For the first time, this study confirmed the presence of the albumin-mediated uptake effect with renal OAT1/3 transporters; the extent of the effect was more pronounced for highly protein-bound substrates. We recommend the inclusion of HSA in routine in vitro OAT1/3 assays due to considerable improvements in the IVIVE of CLsec and CLr."

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