- |||||||||| adefovir dipivoxil / Generic mfg.
Journal: Renal histology of Fanconi syndrome associated with adefovir dipivoxil: A (Pubmed Central) - Nov 30, 2023
Following discontinuation of ADV and supplementation with oral phosphate, hypophosphatemia, glucosuria, and proteinuria were resolved. These findings support the previous hypothesis that ADV-induced nephrotoxicity may involve mitochondrial injury.
- |||||||||| lamivudine HBV / Generic mfg.
Journal: High Frequency of Antiviral Resistance Mutations in HBV Genotypes A2 and H: Multidrug Resistance Strains in Mexico. (Pubmed Central) - Aug 14, 2023
Lamivudine (3TC), telbivudine (LdT), entecavir (ETV), adefovir (ADF), and tenofovir (TFV) are drugs used to treat hepatitis B virus (HBV) infection, but specific mutations allow some viruses to become resistant to antiviral drugs or to acquire immune escape capacities...Resistance mutations were found in genotypes A2 (11.8%, 2/17), and H (10.2%, 11/108), and escape mutations were detected in HBV genotypes A2 (11.8%, 2/17), H (10.2%, 11/108), F1b (9.1%, 1/11) and G (5.6%, 1/18). The highest prevalence of antiviral resistance mutations or escape mutations was detected in HBV genotypes A2 and H. The earliest cases of HBV multidrug resistance were detected in Mexico.
- |||||||||| lamivudine HBV / Generic mfg.
Journal: Inhibition of hepatitis B virus activities by Rhazya (Pubmed Central) - Jun 22, 2023
Although direct-acting nucleoside analogs, such as lamivudine (LAM), adefovir and famciclovir, are available, emergence of drug-resistance due to mutations in HBV polymerase (POL) restricts their further use...In conclusion, to the best of our knowledge, the present study demonstrates anti-HBV efficacies of ACT and ABC in vitro for the first time, endorsed by in silico data. However, further molecular and pharmacological studies are required to validate their pre-clinical therapeutic potential.
- |||||||||| Vistide (cidofovir) / Gilead, Sovaldi (sofosbuvir) / Gilead, valnivudine (FV-100) / Hepion Pharma
Journal: Hydrogen Bonding (Base Pairing) in Antiviral Activity. (Pubmed Central) - May 31, 2023
Hydrogen bonding (base pairing) may also explain the broad-spectrum antiviral effects of ribavirin and favipiravir. This may lead to lethal mutagenesis (error catastrophe), as has been demonstrated with molnutegravir in its activity against SARS-CoV-2.
- |||||||||| Livalo (pitavastatin) / Kowa, Eli Lilly
Preclinical, Journal: In vitro validation of an in vivo phenotyping drug cocktail for major drug transporters in humans. (Pubmed Central) - May 29, 2023
This may lead to lethal mutagenesis (error catastrophe), as has been demonstrated with molnutegravir in its activity against SARS-CoV-2. The inhibition of hOCT2 in vitro by sitagliptin is in agreement with the borderline inhibition of renal metformin elimination observed clinically, supporting a dose reduction of sitagliptin in the cocktail.
- |||||||||| Vemlidy (tenofovir alafenamide) / Gilead, Tyzeka (telbivudine) / Novartis
Hepatitis delta treatment utilization in the United States: an analysis of commercially insured adults with hepatitis delta virus infection (Poster Area) - Apr 12, 2023 - Abstract #EASLILC2023EASL_ILC_330;
In a large US national, primarily commercial, healthcare claims database, fewer than 40% of patients with HDV were treated with HBV-specific antiviral therapies, and very few patients (1.1%) were treated with Peg-IFN, the current off label standard of care for HDV infection. Greater awareness of the importance of timely initiation of antiviral therapy for patients with combined HBV/HDV infection is urgently needed.
- |||||||||| adefovir dipivoxil / Generic mfg.
Journal: Substrate binding and lipid-mediated allostery in the human organic anion transporter 1 at the atomic-scale. (Pubmed Central) - Mar 2, 2023
?s-long molecular dynamics simulation of hOAT1 were carried out suggesting two plausible binding sites for a typical substrate, adefovir, in line with experimental observations...Investigations regarding allosteric communications along hOAT1 also suggest that substrate binding event might modulate the dynamics of intracellular charge relay system, assisted by surrounding lipids as active partners. We here proposed a structural rationalisation of transport impairments observed for two single nucleotide polymorphisms, p.Arg50His and p.Arg454Gln suggesting that the present model may be used to transport dysfunctions arising from hOAT1 mutations.
- |||||||||| tenofovir disoproxil fumarate / Generic mfg., adefovir dipivoxil / Generic mfg.
Analytical methods development for the measurement of physico-chemical parameters of a new antiviral in pre-clinical stage (Hall F-H (Indiana Convention Center)) - Feb 14, 2023 - Abstract #ACSSp2023ACS_SP_12294;
We here proposed a structural rationalisation of transport impairments observed for two single nucleotide polymorphisms, p.Arg50His and p.Arg454Gln suggesting that the present model may be used to transport dysfunctions arising from hOAT1 mutations. Today, several active drugs against HBV are commercially available, such as Hepser
- |||||||||| Vistide (cidofovir) / Gilead
Review, Journal: Altered Serum Uric Acid Levels in Kidney Disorders. (Pubmed Central) - Nov 27, 2022
Finally, serum uric acid and the fractional excretion of uric acid are indicative of plasma volume status; hyperuricemia caused by the enhanced uric acid reabsorption can be induced by volume depletion, and hypouricemia caused by an increased fractional excretion of uric acid is the characteristic finding in syndromes of inappropriate anti-diuresis, cerebral/renal salt wasting, and thiazide-induced hyponatremia. Molecular mechanisms by which uric acid transport is dysregulated in volume or water balance disorders need to be investigated.
- |||||||||| adefovir dipivoxil / Generic mfg.
Journal: Adefovir dipivoxil inhibits APL progression through degradation of the oncoprotein PML-RARA. (Pubmed Central) - Nov 22, 2022
Most importantly, our study uncovered a novel mechanism of ADV prohibiting APL progression, which was mediated, at least in part, by inhibition of TRIB3 and degradation of the oncoprotein PML-RARA, therefore leading to APL cell differentiation and apoptosis. Taken together, our study demonstrated that ADV, an anti-HBV drug, had significantly inhibitory effects on APL, and provided a novel therapeutic strategy for APL patients with RA resistance.
- |||||||||| adefovir dipivoxil / Generic mfg.
Journal: Virtual Cocrystal Screening of Adefovir Dipivoxyl: Identification of New Solid Forms with Improved Dissolution and Permeation Profiles. (Pubmed Central) - Nov 15, 2022
They show improved dissolution profiles with respect to the single solid form, particularly the cocrystals of orcinol and resorcinol, which have 3.2- and 2-fold faster dissolution rates at stomach conditions (pH 1.5). Moreover, dynamic dissolution experiments that simultaneously mimic both the pH variation along the gastrointestinal tract and the partition into biological membranes show that, in addition to the faster initial dissolution, Adefovir Dipivoxyl also penetrates faster into the organic membranes in the form of resorcinol and orcinol cocrystals.
- |||||||||| entecavir / Generic mfg., adefovir dipivoxil / Generic mfg.
Trial completion, Enrollment change: ADVPR: Hepatitis B Virus (HBV) Viral Suppression by Entecavir in Adefovir Partial Responders (clinicaltrials.gov) - Nov 14, 2022
P=N/A, N=60, Completed,
Moreover, dynamic dissolution experiments that simultaneously mimic both the pH variation along the gastrointestinal tract and the partition into biological membranes show that, in addition to the faster initial dissolution, Adefovir Dipivoxyl also penetrates faster into the organic membranes in the form of resorcinol and orcinol cocrystals. Unknown status --> Completed | N=120 --> 60
- |||||||||| lamivudine HBV / Generic mfg., adefovir dipivoxil / Generic mfg.
Retrospective data, Review, Journal: Comparing the efficacy and safety of tenofovir and adefovir or combined drug treatment for the treatment of chronic hepatitis B infection: a systematic review and meta-analysis. (Pubmed Central) - Oct 22, 2022
To explore this issue, we performed a current literature review and meta-analysis to compare the efficacy and safety of ADV vs. TDF, TDF vs. ADV + lamivudine (LAM); TDF vs. ADV + entecavir (ETV)...However, when ADV was combined with LAM or ETV, they often showed the same therapeutic effect as TDF in parameters such as ALT level and Tbil level and combined therapy can effectively reduce the occurrence of adverse reactions. In this study, because the sample source countries were limited, a greater number of global studies are needed in the future to verify the current findings.
- |||||||||| Vistide (cidofovir) / Gilead, Descovy (emtricitabine/tenofovir alafenamide) / Gilead
Journal: The Elegance of the Acyclic Nucleoside Phosphonates (ANPs), Honorary Tribute to Antonín Holý, Who Passed Away on 16 July 2012, at the 10th Anniversary of His Death. (Pubmed Central) - Sep 30, 2022
The latter was further converted to two orally bioavailable prodrug forms, TDF and TAF, and both TDF and TAF were further combined with other antiviral drugs, thus giving rise to a broad array of antiviral drug combinations for the treatment of HIV infections. TDF and TAF are both available for the treatment of hepatitis B virus (HBV) infections, and, in combination with emtricitabine, also applicable as Truvada and Descovy, respectively, for the prophylaxis of HIV infections.
- |||||||||| cyclosporin A microemulsion / Generic mfg., adefovir dipivoxil / Generic mfg.
Retrospective data, Journal: Drug-induced Fanconi syndrome in patients with kidney allograft transplantation. (Pubmed Central) - Sep 14, 2022
These results confirmed that the long-term use of ADV or tacrolimus after kidney transplantation may have serious consequences, some of which are irreversible. Greater understanding of Fanconi syndrome after kidney transplantation is necessary in order to avoid incorrect and missed diagnosis.
- |||||||||| lopinavir/ritonavir / Generic mfg., adefovir dipivoxil / Generic mfg.
Review, Journal: Safety and Efficacy of Antiviral Drugs for the Treatment of COVID-19: A Systematic Review. (Pubmed Central) - Aug 21, 2022
The evaluated drugs included Ridzevir, Lopinavir/Ritonavir, Jingluwa, Fapiravi, Abidor, Danorivir, and interferon α...For critically ill patients, adefovir or more than two antiviral drugs can be used early...In view of the safety of the drug, it is necessary to consider the increase of serum uric acid caused by fapravi, the increase of bilirubin caused by abidol, and the gastrointestinal reactions of pitavir. In addition, other adverse reactions should also be noted.
- |||||||||| Besivo (besifovir) / Gilead, LG Chem, Ildong
Journal: Susceptibility of Drug Resistant Hepatitis B Virus Mutants to Besifovir. (Pubmed Central) - Jul 29, 2022
Several NAs, including lamivudine (LMV), adefovir (ADV), entecavir (ETV) and tenofovir (TDF or TAF) have been approved and administered to chronic hepatitis B (CHB) patients...In case of tenofovir-resistant mutations, the HBV mutants harboring primary mutations to tenofovir resistance were susceptible to BFV. Therefore, our study revealed that BSV may serve as an alternative drug for patients with ADV-, ETV-, TDF- or TAF-resistance.
- |||||||||| adefovir dipivoxil / Generic mfg.
Journal: Evidence that C/EBP-β LAP Increases Fat Metabolism and Protects Against Diet-Induced Obesity in Response to mTOR Inhibition. (Pubmed Central) - Jul 14, 2022
Independent activation of C/EBP-β LAP with the antiretroviral drug adefovir dipivoxil recapitulates the anti-obesogenic effects of rapamycin without reducing signaling through mTORC1 and increases markers of fat catabolism in the liver. Our findings support a model that C/EBP-β LAP acts downstream of mTORC1 signaling to regulate fat metabolism and identifies a novel drug that may be exploited to treat obesity and decrease the incidence of age-related disease.
- |||||||||| Journal: Impact of National Volume-Based Procurement on the Procurement Volumes and Spending for Antiviral Medications of Hepatitis B Virus. (Pubmed Central) - Jun 24, 2022
We employed an interrupted time series design to examine changes in cost per defined daily dose (DDD), procurement volumes, and spending for NVBP bid-winning antiviral medications (tenofovir disoproxil fumarate and entecavir) in 11 pilot cities from 2017 to 2020...In the secondary analysis, the control group comprised two non-NVBP drugs (adefovir and lamivudine) procured in 11 cities not exposed to the NVBP...In the secondary ITS analysis with a control group, the average cost per DDD of the NVBP bid-winning antivirals declined by CNY4.537 (p < 0.001), monthly procurement volumes increased by 7.209 million DDDs (p = 0.002), and monthly spending dropped by CNY138.83 million (p < 0.001). Volume-based procurement piloted in China may be effective for reducing price and total expenditures and improving drug utilization, which is especially important for HBV patients who need constant access to antiviral therapies.
- |||||||||| adefovir dipivoxil / Generic mfg.
Journal: Quantified integrated hepatitis B virus is related to viral activity in chronic hepatitis B patients. (Pubmed Central) - Jun 22, 2022
Integrated HBV levels are strongly correlated with surrogate markers for virological activity but not to cccDNA levels and are predictive for HBsAg loss. Our data suggest that integrated HBV is closely related to HBV replication and may therefore be an important tool in the evaluation and development of treatment modalities aiming to cure CHB.
- |||||||||| Vistide (cidofovir) / Gilead
Review, Journal: Phosphonates and Phosphonate Prodrugs in Medicinal Chemistry: Past Successes and Future Prospects. (Pubmed Central) - Jun 8, 2022
To overcome this problem, various prodrug strategies have been used to mask carboxylates and/or phosphonate functionalities with pivaloyloxymethyl, POC, ODOL and alkyl esters. Chemistry and biological characterization led to identification of prodrugs with 44-80 fold greater oral bioavailability (tetra-ODOL-2-PMPA).
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