- |||||||||| Roctavian (valoctocogene roxaparvovec) / BioMarin
VALOCTOCOGENE ROXAPARVOVEC GENE TRANSFER IN PARTICIPANTS WITH HIV ([VIRTUAL]) - Jan 28, 2022 - Abstract #EAHAD2022EAHAD_332; 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
Asymmetric glycolate aldol addition approach to the synthesis of the HIV protease inhibitor darunavir (In-Person Room (Virtual Room)) - Jan 28, 2022 - Abstract #ACSSp2022ACS_Sp_5592; This approach employs the asymmetric glycolate aldol addition reaction originally developed by Crimmins and coworkers. This reaction will be followed by a newly developed synthetic pathway to anti-configured beta-azido-alpha-p-methoxyphenoxycarboxylic acids that can be readily converted into the desired target.
- |||||||||| Prezista (darunavir) / J&J
ACUTE KIDNEY INJURY DUE TO CRYSTAL NEPHROPATHY SECONDARY TO DARUNAVIR (Poster Area (Virtual)) - Jan 21, 2022 - Abstract #ISNWCN2022ISN_WCN_562; Protease inhibitors cause kidney damage, which can manifest as crystalluria, leukocyturia, nephritis, nephrolithiasis, nephropathy and urolithiasis, secondary to the fact that they are poorly soluble in urine and tend to precipitate in the urine at physiological pH. In our case, the patient presented a significant improvement in renal function after withdrawal of Darunavir and initiation of prednisone.
- |||||||||| zidovudine / Generic mfg.
PK/PD data, Review, Journal: A Review on Pharmacokinetics properties of antiretroviral drugs to treat HIV-1 infections. (Pubmed Central) - Jan 18, 2022 These drugs are Fuzeon, Selzentry, Complera, Epivir, Retrovir, Emtriva, Ziagen, Edurant, Intelence, Pifeltro, Sustiva, Viramune, Isentress, Genvoya, Tivicay, Reyataz, Prezista, Lexiva, Invirase, Aptivus etc. classified into five major classes: fusion inhibitors, Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (NRTIs), Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs), Integrase Strand transfer inhibitors (INSTIs) and Protease inhibitors (PIs). This review may be helpful for the future development of potent antiretroviral drugs with improved pharmacokinetic properties.
- |||||||||| hydroxychloroquine / Generic mfg.
Review, Journal: Pharmacological strategies for COVID-19 - A review of the most promising repurposed antiviral drugs. (Pubmed Central) - Jan 18, 2022 Several drugs such as Hydroxychloroquine, Umifenovir, Remdesivir, Lopinavir/Ritonavir, interferon, Darunavir, Favipiravir, Nitazoxanide etc. are currently undergoing clinical studies to test the safety and efficacy of the drug against this pandemic. The present review gives a snapshot look of the current clinical experience with repurposed antiviral drugs.
- |||||||||| Prezista (darunavir) / J&J, Isentress (raltegravir) / Merck (MSD)
Journal, IO biomarker: Poorer Muscle Quality and Quantity with ART Initiation is Associated with Greater Inflammation and Immune Activation. (Pubmed Central) - Jan 18, 2022 The present review gives a snapshot look of the current clinical experience with repurposed antiviral drugs. Greater fat infiltration within the psoas muscle (lower density) and greater loss in lean psoas muscle area were associated with higher inflammation and immune activation, which may portend important effects on muscle function and cardiometabolic risk.
- |||||||||| Avastin (bevacizumab) / Roche
Clinical, Review, Journal: Drugs Associated With Ischemic Stroke: A Review for Clinicians. (Pubmed Central) - Jan 8, 2022 We identified a high level of association of IS with a limited number of drugs, a potential association with some, and a lack of data for others. The summarized information may help clinicians to estimate the contribution of a drug to an IS, to better assess drug benefit-risk ratios, and to support decisions about using specific drugs.
- |||||||||| ribavirin / Generic mfg., ritonavir / Generic mfg.
Journal: Computational Simulation of HIV Protease Inhibitors to the Main Protease (Mpro) of SARS-CoV-2: Implications for COVID-19 Drugs Design. (Pubmed Central) - Dec 21, 2021 Pharmacophore model analysis further revealed that the aromatic ring, hydrogen bond donor, and hydrophobic group are the essential infrastructure of Mpro inhibitors. Overall, this study applied computational simulation methods to study the interaction mechanism of HIV-1 protease inhibitors with SARS-CoV-2 Mpro, and the findings provide useful insights for the development of novel anti-SARS-CoV-2 agents for the treatment of COVID-19.
- |||||||||| hydroxychloroquine / Generic mfg., ivermectin oral / Generic mfg.
Journal: Potential Drugs for the Treatment of COVID-19: Synthesis, Brief History and Application. (Pubmed Central) - Dec 16, 2021 Scientists around the world are investigating few previously used clinical drugs for the treatment of COVID-19. This review provides synthesis and mode of action of recently investigated drugs like Chloroquine, Hydroxychloroquine, Ivermectin, Selamectin, Remdesivir, Baricitinib, Darunavir, Favipiravir, Lopinavir/ritonavir and Mefloquine hydrochloride that constitute an option for COVID-19 treatment.
- |||||||||| Sovaldi (sofosbuvir) / Gilead
Clinical, Journal: Access to medicines and South-South cooperation: a case study on joint drug price negotiations in South America (Pubmed Central) - Dec 16, 2021 In the case of darunavir, there was a reduction in the global price, including the price in the Global Fund to Fight AIDS, Tuberculosis, and Malaria. In conclusion, price negotiation was successful in the above-mentioned cases, and participation by the PAHO Strategic Fund in the drug purchases streamlined their procurement and their availability in the countries.
- |||||||||| Prezista (darunavir) / J&J
Journal: Potential of Marine Terpenoids against SARS-CoV-2: An In Silico Drug Development Approach. (Pubmed Central) - Nov 29, 2021 Similarly, marine terpenoids such as xiamycin (-9.3), thyrsiferol (-9.2), liouvilloside B (-8.9), liouvilloside A (-8.8), and stachyflin (-8.7) exhibited comparatively higher docking scores than the referral drug remdesivir (-7.4), and favipiravir (-5.7) against the target SARS-CoV-2-RdRp...Previously, stachyflin also exhibited potential activity against HSV-1 and CoV-A59 within IC, 0.16-0.82 µM. Therefore, some additional pharmacological studies are needed to develop 'stachyflin' as a drug against SARS-CoV-2.
- |||||||||| Prezista (darunavir) / J&J, Invirase (saquinavir) / Roche
Journal: Protease Inhibitors, Saquinavir and Darunavir, Inhibit Oligodendrocyte Maturation: Implications for Lysosomal Stress. (Pubmed Central) - Nov 24, 2021 Finally, we showed that acidifying endolysosomal pH via a mucolipin transient receptor potential channel 1 (TRPML1) agonist provides protection against saquinavir- or darunavir-induced inhibition of oligodendrocyte maturation. Our findings suggest, for the first time, a critical role of proper endolysosomal pH in regulating OL differentation, and that therapeutic targeting of endolysosomes may provide protection against antiretroviral-induced oligodendrocyte dysregulation.
- |||||||||| Prezista (darunavir) / J&J, Crixivan (indinavir sulfate) / Merck (MSD)
Retrospective data, Review, Journal: HIV Protease Inhibitors and Insulin Sensitivity: A Systematic Review and Meta-Analysis of Randomized Controlled Trials. (Pubmed Central) - Nov 21, 2021 Darunavir and indinavir did not demonstrate any significant changes in insulin sensitivity...Atazanavir, fosamprenavir, and darunavir did not demonstrate any significant changes in insulin sensitivity, compared to the rest of the group...All patients newly diagnosed with HIV should have DM investigations before the start of ARVs and routinely. RCTs should focus on sub-Saharan Africa as the region is worst affected by HIV, but limited studies have been documented.
- |||||||||| Prezista (darunavir) / J&J
Preclinical, Journal: Effect of four ABCB1 genetic polymorphisms on the accumulation of darunavir in HEK293 recombinant cell lines. (Pubmed Central) - Nov 12, 2021 In this work, we report on the intracellular accumulation of darunavir in recombinant HEK293 cell lines expressing wild-type ABCB1 or one of several variants: ABCB1 1199A, ABCB1 3435T, and ABCB1 1236T/2677T/3435T. We demonstrate that while ABCB1 expression limits intracellular accumulation of darunavir, there is no significant difference in efflux activity between cells expressing wild-type ABCB1 and those that express any of the studied variants.
- |||||||||| Prezista (darunavir) / J&J
Journal: Cardiovascular risks associated with protease inhibitors for the treatment of HIV. (Pubmed Central) - Nov 5, 2021 Ongoing studies registered on clinicaltrials.gov as well as conference abstracts from major HIV conferences from 2015-2020 were also searched.Expert opinion: Atazanavir and darunavir are no longer part of first-line HIV treatment, but continue to be recommended as alternative first line, second- and third-line regimens, as part of two drug regimens, and darunavir is used as salvage therapy. Although these drugs will likely remain in use globally for several years to come, baseline CVD risk should be considered when considering their use, especially as the population with HIV ages.
- |||||||||| Prezista (darunavir) / J&J, Vitekta (elvitegravir) / Japan Tobacco, Gilead
Journal: Brain-Accumulating Nanoparticles for Assisting Astrocytes to Reduce Human Immunodeficiency Virus and Drug Abuse-Induced Neuroinflammation and Oxidative Stress. (Pubmed Central) - Nov 4, 2021 Here, we report a strategy to deliver an optimized antiretroviral therapy combined with antioxidant and anti-inflammatory neuroprotectants using biodegradable brain-targeted polymeric nanoparticles to reduce the burden caused by viral reservoirs in the brain and tackle the oxidative stress and inflammation in astrocytes and microglia. Through in vitro coculture studies in human microglia and astrocytes as well as an in vivo efficacy study in an EcoHIV-infected, methamphetamine-exposed animal model, we established a nanoparticle-based therapeutic strategy with the ability to treat HIV infection in the central nervous system in conditions simulating drug use while providing enhanced protection to astrocytes, microglia, and neurons.
- |||||||||| zidovudine / Generic mfg.
Review, Journal, IO biomarker: Interactions of HIV and Antiretroviral Therapy With Neutrophils and Platelets. (Pubmed Central) - Sep 23, 2021 In this context, abacavir and ritonavir-boosted lopinavir and darunavir have all been linked to an increased risk of CVD. This narrative review is therefore focused primarily on the role of neutrophils and platelets in HIV transmission and disease, as well as on the effect of HIV and the most common ARVs on the numbers and functions of these cells, including neutrophil-platelet-endothelial interactions.
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