Crixivan (indinavir sulfate) / Merck (MSD) 
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  • ||||||||||  Prevymis (letermovir) / Merck (MSD), Zepatier (grazoprevir/elbasvir) / Merck (MSD), Crixivan (indinavir sulfate) / Merck (MSD)
    Discovery and development of MK-7845 as an investigational treatment for COVID-19 (Hybrid; Room 346 (Ernest N. Morial Convention Center)) -  Mar 12, 2024 - Abstract #ACSSp2024ACS_Sp_2199;    
    This commitment has remained strong, as evidenced by the introduction of Crixivan
  • ||||||||||  Rescriptor (delavirdine mesylate) / ViiV Healthcare, Crixivan (indinavir sulfate) / Merck (MSD)
    Journal:  Identification and characterization of domain-specific inhibitors of DENV NS3 and NS5 proteins by in silico screening methods. (Pubmed Central) -  Feb 9, 2024   
    Our comprehensive analysis identified tolcapone, cefprozil, delavirdine and indinavir as potential inhibitors of NS5 MTase, NS5 RdRp, NS3 protease and NS3 helicase functions, respectively. These high-confidence candidate molecules will be useful for developing effective anti-DENV therapy to combat dengue infection.Communicated by Ramaswamy H. Sarma.
  • ||||||||||  Crixivan (indinavir sulfate) / Merck (MSD)
    Preclinical, Journal:  The Dynamic Intestinal Absorption Model (Diamod (Pubmed Central) -  Jul 3, 2023   
    Molecular docking revealed only ?-sitosterol- 3-O-?-D-glucopyranoside with a lower docking score of - 9.712 kcal/mol than positive control of indinavir...Root Mean Square Fluctuation of catalytic sites HIS41 and CYS145 was 0.756 The Diamod
  • ||||||||||  cyclosporine / Generic mfg.
    Treatment of ingrown nails and periungual pyogenic granuloma-like lesions by partial nail avulsion and chemical matricectomy in a patient on cyclosporine treatment due to graft-versus-host disease () -  Jul 3, 2023 - Abstract #WCD2023WCD_6189;    
    Although improper nail trimming appears to be the most common cause, the other causes were reported as poor hygiene, tight-fitting shoes, hyperhidrosis, trauma, and some drugs including epidermal growth factor receptor inhibitors (gefitinib, cetuximab), retinoids, cyclosporine, indinavir, azidothymidine (AZT), fluorouracil (5FU), methotrexate, capecitabine, doxorubicin, and docetaxel...At the time of the submission to our clinic, she has been treated with prednisone and cyclosporine (100 mg/day) for 4 months...Although discontinuation of the drug is needed for the treatment, it may not be possible in every situation due to vital expectations from the drug in cases such as ours. A surgical approach including the removal of the excessive tissue and partial nail avulsion with a matricectomy should be one of the considered approaches in such cases that are unresponsive to conservative treatments
  • ||||||||||  Crixivan (indinavir sulfate) / Merck (MSD)
    Journal:  Involvement of CYP3A4 and MDR1 in altered metabolism and transport of indinavir in 1,25(OH)D-treated Caco-2 cells. (Pubmed Central) -  Mar 2, 2023   
    Similarly, plasma levels of the metabolite increased in 1,25(OH)D-treated rats; however, systemic exposure to indinavir led to insignificant alterations. Considering the overlapping substrate specificities for CYP3A4 and MDR1 and their significant roles in drug pharmacokinetics, VDR may play an important role in drug interactions of CYP3A4 and MDR1 substrates for accessing more effective and safe disease treatments.
  • ||||||||||  Prezista (darunavir) / J&J, Invirase (saquinavir) / Roche, Crixivan (indinavir sulfate) / Merck (MSD)
    Journal:  HIV protease inhibitor attenuated astrocyte autophagy involvement in inflammation via p38 MAPK pathway. (Pubmed Central) -  Nov 15, 2022   
    In the following study, we verified the results from RNA-sequence using the liquid chip technique, qRT-PCR, Elisa, and western blots, which suggested that LPV induced inflammatory response and the p38 MAPK pathway was involved in this process. Collectively, we demonstrated that PIs attenuated the involvement of astrocyte autophagy in inflammation via the p38 MAPK pathway, providing new insights into the mechanism of HAND.
  • ||||||||||  Journal:  Discovery of Novel HIV Protease Inhibitors Using Modern Computational Techniques. (Pubmed Central) -  Oct 28, 2022   
    HPS/002 and HPS/004 have been found to be most promising in terms of IC/percent inhibition (90.15%) of HIV-1 PR, in addition to their drug metabolism and safety profile. These hit candidates should be investigated further as possible HIV-1 PIs with improved efficacy and low toxicity through in vitro experiments and clinical trial investigations.
  • ||||||||||  Crixivan (indinavir sulfate) / Merck (MSD)
    Mathematical Representation of Drug Induced Crystal Nephropathy Using a Quantitative Systems Toxicology Approach (Exhibit Hall, Orange County Convention Center, West Building) -  Oct 13, 2022 - Abstract #KIDNEYWEEK2022KIDNEY_WEEK_3512;    
    Conclusion The crystal nephropathy model in RENAsym does a reasonable job of representing EG-induced CaOx crystal formation and its nephrotoxic effects. The model shows promise in its ability to predict kidney injury due to other compounds that can precipitate in the kidney tubule, such as indinavir.
  • ||||||||||  Edsivo (celiprolol) / Acer Therap, Invirase (saquinavir) / Roche, Crixivan (indinavir sulfate) / Merck (MSD)
    Review, Journal:  Phytochemicals That Interfere With Drug Metabolism and Transport, Modifying Plasma Concentration in Humans and Animals. (Pubmed Central) -  Sep 29, 2022   
    Interactions between Pchs and drugs affect the gene expression and enzymatic activity of CYP3A and P-gp transporter, which has an impact on their bioavailability; such that co-administration of drugs with food, beverages and food supplements can cause a subtherapeutic effect or overdose. Therefore, it is important for the clinician to consider these interactions to obtain a better therapeutic effect.
  • ||||||||||  Anti-retroviral repurposing for treatment of glioblastoma (West/Central Hall) -  Sep 28, 2022 - Abstract #SNO2022SNO_659;    
    We identified six potential antiretrovirals among several drug classes with significant anti-glioma activity: abacavir (ABC), lamivudine (LMV), raltegravir (RLT), darunavir (DAR), indinavir (IND), and etravirine (ETV)...Synergy assessment of ETV with standard of care temozolomide (TMZ) demonstrated that these drugs work independently of one another (Bliss score of -0.39 and -0.83 in GBM 28 and GBM 43, respectively)...Overall, several antiretroviral drugs could be repositioned for glioblastoma therapy. Given its ideal therapeutic index and ability to penetrate the blood-brain barrier, ETV may be a promising candidate for future clinical trials in neuro-oncology.
  • ||||||||||  Crixivan (indinavir sulfate) / Merck (MSD)
    Journal:  Antiretroviral drug activity and potential for pre-exposure prophylaxis against COVID-19 and HIV infection. (Pubmed Central) -  Sep 14, 2022   
    Existing or new combinations of antiretroviral drugs could potentially prevent or ameliorate the course of COVID-19 if shown to inhibit SARS-CoV-2 in vitro and in clinical trials. Further studies are needed to establish the activity of ARVs for treatment or prevention of SARS-CoV-2 infection .Communicated by Ramaswamy H. Sarma.
  • ||||||||||  Tekturna (aliskiren) / PDL, Crixivan (indinavir sulfate) / Merck (MSD)
    Regio- and diastereoselective rhodium-catalyzed allylic substitution with unstabilized benzyl nucleophiles (Virtual-only (Zoom)) -  Aug 9, 2022 - Abstract #ACSFall2022ACS_Fall_2771;    
    This seminar will also outline the development of a diastereoselective variant, which permits both acyclic and cyclic allylic carbonates bearing a homoallylic stereocenter to undergo benzylation with high levels of diastereocontrol. Hence, this approach provides a rare example of 1,2-stereoinduction in transition metal-catalyzed allylic substitution.
  • ||||||||||  Crixivan (indinavir sulfate) / Merck (MSD)
    Coupled cluster benchmarking of large noncovalent complexes (S404bc (McCormick Place Convention Center)) -  Aug 9, 2022 - Abstract #ACSFall2022ACS_Fall_276;    
    In this work, benchmark binding energies for large noncovalent complexes in two popular datasets, L7 and S12L, a C60 dimer, the DNA-ellipticine intercalation complex, and the largest system of the study, the HIV-indinavir system, using a focal point method that relies on the canonical form of second-order Møller-Plesset theory and the domain based local pair natural orbital scheme for the coupled cluster with single double and perturbative triple excitations [CCSD(T)] extrapolated to the complete basis set (CBS) limit are reported...r2SCAN-3c and B97M-V work well in large noncovalent complexes in this work, and GFN2-xTB performs well in π-π stacking complexes. The benchmark interaction energies of these host-guest, molecular materials, and biological complexes provide crucial reference data for the development/improvement of current and future lower-cost computational methods.
  • ||||||||||  Crixivan (indinavir sulfate) / Merck (MSD)
    Journal:  Coupled Cluster Benchmarking of Large Noncovalent Complexes in L7 and S12L as Well as the C Dimer, DNA-Ellipticine, and HIV-Indinavir. (Pubmed Central) -  Jul 17, 2022   
    B97M-V is the most reliable computationally efficient approach to predicting noncovalent interactions for large complexes, being the only one to have binding errors within the so-called 1 kcal/mol "chemical accuracy". The benchmark interaction energies of these host-guest complexes, molecular materials, and biological systems with electronic and medicinal implications provide crucial reference data for the improvement of current and future lower-cost methods.
  • ||||||||||  Crixivan (indinavir sulfate) / Merck (MSD)
    Journal:  A novel phenolic formulation for treating hepatic and peripheral insulin resistance by regulating GLUT4-mediated glucose uptake. (Pubmed Central) -  May 10, 2022   
    We report here that a formula consisting of resveratrol, ferulic acid and epigallocatechin-3-O-gallate is more effective in ameliorating muscle and hepatic insulin resistance than the anti-diabetic drugs, metformin and AICAR...On the other hand, this formula also showed anti-diabetic potential by the reduction of lipid content in the myotubes, hepatocytes, and adipocytes. This study demonstrated that the three phenolic compounds in the formula could work in distinct mechanisms and enhance both insulin-dependent and independent vesicles trafficking and glucose transport mechanisms to improve carbohydrate and lipid metabolism.
  • ||||||||||  Crixivan (indinavir sulfate) / Merck (MSD)
    Journal:  Hybrid QM/MM Free-Energy Evaluation of Drug-Resistant Mutational Effect on the Binding of an Inhibitor Indinavir to HIV-1 Protease. (Pubmed Central) -  Mar 25, 2022   
    Through the free-energy calculations of protonation states of catalytic groups at the binding pocket and of the ligand-binding affinity changes upon the mutations, we successfully reproduced the experimentally observed significant reduction of the binding affinity upon the drug-resistant mutations and elucidated the underlying molecular mechanism. The present study opens the way for understanding the molecular mechanism of drug resistance through the direct quantitative comparison of ligand binding and enzymatic reaction with the same accuracy.
  • ||||||||||  Tybost (cobicistat) / Gilead, Crixivan (indinavir sulfate) / Merck (MSD)
    FDA event, Journal:  Whole genome analysis and homology modeling of SARS-CoV-2 Indian isolate reveals potent FDA approved drug choice for treating COVID-19. (Pubmed Central) -  Feb 11, 2022   
    Overall our present research findings is that three proposed drugs namely cobicistat, remdesivir and indinavir showed higher interaction with the model SARS-CoV-2 viral target proteins from the Indian nCoV-19 isolate. These compounds could be used as a starting point for the creation of active antiviral drugs to combat the deadly COVID-19 virus during global pandemic and its subsequent viral infection waves across the globe.Communicated by Ramaswamy H. Sarma.
  • ||||||||||  ritonavir / Generic mfg.
    Journal:  Potential protease inhibitors and their combinations to block SARS-CoV-2. (Pubmed Central) -  Jan 29, 2022   
    These results suggest that protease inhibitors particularly Ritonavir, either alone or in combination with other drugs such as Atazanavir, have the potential to treat COVID 19. Communicated by Ramaswamy H. Sarma.
  • ||||||||||  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.
  • ||||||||||  Crixivan (indinavir sulfate) / Merck (MSD), Tetralysal (lymecycline) / Galderma
    Clinical, Journal:  Untargeted Metabolic Profiling of Extracellular Vesicles of SARS-CoV-2-Infected Patients Shows Presence of Potent Anti-Inflammatory Metabolites. (Pubmed Central) -  Oct 22, 2021   
    These findings suggest that EVs not only carry active drug molecules but also anti-inflammatory metabolites, clearly suggesting that exosomes might play a crucial role in negotiating with heightened inflammation during COVID-19 infection. These preliminary results could also pave the way for the identification of novel metabolites that might act as critical regulators of inflammatory pathways during viral infections.