Prezista (darunavir) / J&J 
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 32 Diseases   11 Trials   11 Trials   1696 News 


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  • ||||||||||  remdesivir / Generic mfg.
    Drug-drug interactions between antiretrovirals and remdesivir () -  May 12, 2022 - Abstract #AIDS2022AIDS_775;    
    Other treatments for COVID-19 studied here did not demonstrate significant DDIs with ARVs. As new COVID-19 therapeutics emerge, and given the prevalence of HIV worldwide, DDIs with ARVs must continue to be assessed.
  • ||||||||||  Advanced HIV infection in the US: immune response to ART initiation () -  May 12, 2022 - Abstract #AIDS2022AIDS_745;    
    In the OPERA cohort, all ART-naïve, adults with advanced HIV (CD4200 cells/µL). No difference was observed in CD4:CD8 ratio changes over time across groups; CD4:CD8 ratio normalization was rare with all regimens.
  • ||||||||||  Prezista (darunavir) / J&J, Tivicay (dolutegravir) / ViiV Healthcare
    Journal:  Switching to a NRTI-free 2 drug regimen (2DR) -a sub-analysis of the 48 weeks DUALIS study on metabolic and renal changes. (Pubmed Central) -  May 6, 2022   
    The LDL-fraction increased by + 13.3 (-3.0 to +31.3) mg/dL on 2DRs and was stable (-14.0 to +18.0 mg/dL) on 3DRs (p < 0.0010).PLWH gained +2.0 (-0.2 to +4.0) kg and +0.2 (-1.9 to +2.1) kg in body weight on 2DRs and 3DRs, respectively 3 (p = 0.0006).The MDRD eGFR decreased by -7,8 (-17.4 to -0.3) mL/min/1.73m and 0.4 (-8.8 to +5.7) mL/min/1.73m on 2DRs and 3DRs, respectively (p = 0.0002), while serum levels of cystatin C were stable in both arms (2DR: -0.1 to +0.1 mg/L; 3DR: 0.0 to +0.1 mg/L). While being non-inferior in terms of viral suppression, sparing the NRTI backbone showed a non-favorable profile in metabolic or renal parameters over 48 weeks.
  • ||||||||||  ivermectin oral / Generic mfg.
    Journal:  A VSV-based assay quantifies coronavirus Mpro/3CLpro/Nsp5 main protease activity and chemical inhibition. (Pubmed Central) -  May 5, 2022   
    Moreover, we show that the system can be adapted to report both the function and the chemical inhibition of proteases from different coronavirus species as well as from distantly related viruses. Together with the fact that live cell assays also reflect compound permeability and toxicity, we anticipate that this system will be useful for both identification and optimization of additional coronavirus protease inhibitors.
  • ||||||||||  Prezista (darunavir) / J&J
    Journal:  Multiple Molecular Dynamics Simulations and Energy Analysis Unravel the Dynamic Properties and Binding Mechanism of Mutants HIV-1 Protease with DRV and CA-p2. (Pubmed Central) -  Apr 30, 2022   
    To describe the effects of these mutated residues on the dynamic properties and the binding mechanism of PR with substrate and inhibitor, focused on six systems (two complexes of WT PR and PR with inhibitor Darunavir (DRV), two complexes of WT PR and PR with substrate analogue CA-p2, two unligand WT PR and PR), we performed multiple molecular dynamics (MD) simulations combined with MM-PBSA and solvated interaction energy (SIE) methods...Compared with the experiments, MD simulations along with energy calculations help reduce the time and cost of designing new inhibitors. Based on our simulation results, we propose two factors that may help design effective inhibitors against HIV-1 PR: (i) importance of hydrophobic cavity, and (ii) introduction of polar groups similar to the guanidine group.
  • ||||||||||  Prezista (darunavir) / J&J
    Journal:  In silico study of natural compounds from sesame against COVID-19 by targeting M, PL and RdRp. (Pubmed Central) -  Apr 29, 2022   
    This activity continued to include the RdRp as it displayed a comparable docking score with remdesivir...All the compounds were investigated for their ADME and drug likeness properties, which showed acceptable ADME properties and obeying Lipinski's rule of five parameters. It can be concluded that the isolated compounds from sesame lignans could be an alternative source for the development of new natural leads against COVID-19.
  • ||||||||||  Prezista (darunavir) / J&J, Isentress (raltegravir) / Merck (MSD)
    Journal:  From Undetectable Equals Untransmittable (U=U) to Breastfeeding: Is the Jump Short? (Pubmed Central) -  Apr 22, 2022   
    Our experience, gathered in the setting of freedom of choice on the patient's side, while insufficient to address the eventual safety of breastfeeding in HIV-infected mothers since the represented cohort is numerically irrelevant, supports the extension of the U=U (Undetectable Equals Untransmittable) paradigm to this setting. Since breastfeeding is often requested by women with HIV planning pregnancy, more extensive comparative studies should be performed.
  • ||||||||||  Prezista (darunavir) / J&J
    Journal:  Trends in antiretroviral use in pregnancy in the UK and Ireland, 2008-2018. (Pubmed Central) -  Mar 15, 2022   
    These national surveillance data enable investigation of the 'real-world' use of antiretrovirals in pregnancy on a population level. Findings demonstrate mixed responsiveness of antiretroviral prescription to changes in pregnancy guideline recommendations and may also reflect changes in commissioning and in the characteristics of pregnant women living with HIV.
  • ||||||||||  Prezista (darunavir) / J&J
    Journal:  Potential of Ficus microcarpa metabolites against SARS-CoV-2 main protease supported by docking studies. (Pubmed Central) -  Mar 3, 2022   
    Docking studies concerning these compounds against SARS-CoV-2 main protease showed that quercetin 3,7-O-α-L-dirhamnoside (1) and rutin (3) possessed significant binding stability at the N3 binding site in different activity degrees, which is comparable with COVID-19 main protease inhibitor, darunavir. Our study suggests that compounds quercetin 3,7-O-α-L-dirhamnoside and rutin might be potential candidates for the development of therapies against SARS-CoV-2.
  • ||||||||||  Journal:  Advanced HIV Infection in Treatment-Naïve Individuals: Effectiveness and Persistence of Recommended 3-Drug Regimens. (Pubmed Central) -  Feb 17, 2022   
    Compared with B/F/TAF, bDRV initiators were statistically less likely to suppress to <50 copies/mL (aHR, 0.72; 95% CI, 0.52-0.99) and <200 copies/mL (aHR, 0.55; 95% CI, 0.43-0.70); no statistically significant difference was detected with DTG or EVG/c. Among people with advanced HIV infection, those initiating B/F/TAF were less likely to discontinue/modify their regimen than those on any other regimen, and more likely to achieve viral suppression compared with those on bDRV but not compared with those on other integrase inhibitors.
  • ||||||||||  ribavirin / Generic mfg.
    Journal:  Multiple Computational Approaches for Predicting Drug Interactions with Human Equilibrative Nucleoside Transporter 1. (Pubmed Central) -  Feb 16, 2022   
    Mizoribine and ribavirin mapped to the ENT1 substrate pharmacophore and proved to be substrates of the ENTs...Darunavir mapped to the ENT1 inhibitor pharmacophore and NBMPR did not significantly influence darunavir accumulation in either ENT1 or ENT2 cells (ENT1: P = 0.28; ENT2: P = 0.53), indicating that darunavir's interaction with the ENTs is limited to inhibition...These computational and in vitro models can inform compound selection in the drug discovery and development process, thereby reducing time and expense of identification and optimization of ENT interacting compounds. Significance Statement This study developed computational models of human equilibrative nucleoside transporters (ENTs) to predict drug interactions and validated these models with two compounds in vitro Identification and prediction of ENT1 and ENT2 substrates allows for the determination of drugs that can penetrate tissues expressing these transporters.
  • ||||||||||  Roctavian (valoctocogene roxaparvovec) / BioMarin
    Valoctocogene roxaparvovec gene transfer in participants with HIV (hall 1; hall 2; hall 3; hall 4; hall 5) -  Feb 16, 2022 - Abstract #GTH2022GTH_302;    
    P3
    P2 received darunavir, dolutegravir, and ritonavir...Prednisone 60 mg/d was initiated on d109; AEs resolved...Following discussion between P3, a hepatologist, and the investigator on d65, his HIV treatment was replaced with raltegravir and emtricitabine/tenofovir alafenamide... Of 3 HIV+ participants, 2 had reduced bleeding and no or G1 LFT AEs; 1 had hepatic enzyme elevation unresponsive to corticosteroids, likely due to an interaction between gene therapy and efavirenz, a known hepatotoxic agent.
  • ||||||||||  Prezista (darunavir) / J&J
    Journal:  Combinatorial approach of vitamin C derivative and anti-HIV drug-darunavir against SARS-CoV-2. (Pubmed Central) -  Feb 8, 2022   
    As HIV-1 protease drug resistance remains a concern, our results open a new avenue to help establish a direct quantitative link between protein vibrational dynamics and drug resistance. Overall, the present work suggests that bioinformatics tools are suitable for recognizing potential candidates in an emergency, and herein the selected 'anti-HIV-drug-vitamin c derivatives' cocktails may potential-cum-fewer toxic regimens against COVID-19 treatment.
  • ||||||||||  Prezista (darunavir) / J&J, Tivicay (dolutegravir) / ViiV Healthcare
    GENERIC DARUNAVIR AND DOLUTEGRAVIR ARE COST-EFFECTIVE IN SECOND-LINE ART ([VIRTUAL]) -  Feb 7, 2022 - Abstract #CROI2022CROI_778;    
    In most settings It is highly cost-effective to replace LPV/r and ATV/r with DRV/r with a less than 1x GDP threshold. The most optimal strategy is to maximize use of DTG in 2L, which was the most effective and cheapest scenario across all comparisons.
  • ||||||||||  Prezista (darunavir) / J&J, Tivicay (dolutegravir) / ViiV Healthcare
    METABOLIC PERTURBATIONS BY INTEGRASE INHIBITORS IN DIFFERENTIATED HUMAN ADIPOCYTES ([VIRTUAL]) -  Feb 7, 2022 - Abstract #CROI2022CROI_667;    
    The observed increases in lactate production and decreased oxygen consumption in preadipocytes and adipocytes treated with DTG indicate impairments in mitochondrial function. These alterations in metabolism combined with suppression of key regulatory adipokines may help explain the increased weight gain observed in individuals taking INSTIs.
  • ||||||||||  Prezista (darunavir) / J&J, Tivicay (dolutegravir) / ViiV Healthcare
    SWITCHING TO A NRTI-FREE 2 DRUG REGIMEN (2DR) – A SUB-ANALYSIS OF THE DUALIS STUDY ([VIRTUAL]) -  Feb 7, 2022 - Abstract #CROI2022CROI_628;    
    Switching from a three-drug regimen (3DR: boosted darunavir [bDRV] and two nucleoside reverse transcriptase inhibitors [NRTIs]) to a two-drug regimen (2DR: bDRV and dolutegravir) demonstrated non-inferiority with regard to viral suppression in people living with HIV (PLWH) in the DUALIS study...In the 3DR arm, a switch to the tenofovir alafenamid-backbone during the study period resulted in an increase in body weight by +0.5 (-0.8 to +4.0) kg and in BMI by +0.2 (-0.3 to +1.2) kg/m2...The LDL-fraction changed by + 8.0 (-3.0 to +27.0) mg/dL on TAF versus -1.0 (-14.0 to +16.0) mg/dL on TDF (p=0.1043). While being non-inferior in terms of viral suppression, sparing the NRTI backbone showed no advantages in metabolic or renal parameters over 48 weeks.
  • ||||||||||  bictegravir (GS-9883) / Gilead
    REVERSIBILITY OF CENTRAL NERVOUS SYSTEM ADVERSE EVENTS IN COURSE OF ART ([VIRTUAL]) -  Feb 7, 2022 - Abstract #CROI2022CROI_613;    
    Central nervous system (CNS) adverse events (AE) can occur during various antiretroviral therapies (ART), as well as being a major cause of treatment discontinuation during dolutegravir-containing ART (DTG)...Sixty SNC-AE leading to ART discontinuation were reported, 26/3613 (0.7%) in non DTG-cohorts (2/731 lopinavir, 1/616 atazanavir, 2/721 darunavir, 8/421 rilpivirine, 5/514 raltegravir, 3/339 elvitegravir and 5/211 bictegravir), and 34/1138 (3.1%) in DTG-cohort...AE leading to ART discontinuation were more frequent in DTG than non-DTG treated PLWH. However, most AE resolved after ART switch, with similar frequency in DTG and non-DTG cohorts.
  • ||||||||||  Vemlidy (tenofovir alafenamide) / Gilead
    TENOFOVIR ALAFENAMIDE IS ASSOCIATED WITH SHORTER TELOMERE LENGTH IN PEOPLE WITH HIV ([VIRTUAL]) -  Feb 7, 2022 - Abstract #CROI2022CROI_599;    
    The inconsistent findings between TAF and TDF may be because intracellular TFV concentrations are higher with TAF than with TDF. A limitation is that TAF was not used at the first visit since it was not yet approved for clinical use so the findings should be confirmed in controlled trials.
  • ||||||||||  Prezista (darunavir) / J&J, Tivicay (dolutegravir) / ViiV Healthcare
    NUCLEOSIDES AND DARUNAVIR/DOLUTEGRAVIR IN AFRICA (NADIA) TRIAL: OUTCOMES AT 96 WEEKS ([VIRTUAL]) -  Feb 7, 2022 - Abstract #CROI2022CROI_392;    
    Tenofovir is superior to zidovudine and may protect against dolutegravir resistance. Guidelines that recommend switch from tenofovir to zidovudine for second-line therapy in the public health approach should be reconsidered.