- |||||||||| 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
- |||||||||| 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
- |||||||||| Journal: Screening of pharmaceutical and personal care products (PPCPs) along wastewater treatment system equipped with root zone treatment: A potential model for domestic waste leachate management. (Pubmed Central) - Mar 14, 2023
In general, carbamazepine, ibuprofen, acetaminophen, trimethoprim, sulfamethoxazole, caffeine, triclocarban, and triclosan are often reported in wastewater systems...In essence, RZT-based WWTP was found to be effective in removing the PPCPs and other organic contaminants in the study but results in stress the need for further comprehensive research on RZT system to conclude the exact removal efficacy and fate of PPCPs during treatment in the system. As a current research gap, the study also recommended RZT to be appraised for PPCPs in-situ remediation from landfill leachates, an underestimated source of PPCPs intrusion in the environment.
- |||||||||| 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.
- |||||||||| Review, Journal: Interactions of Antiretroviral Drugs with Food, Beverages, Dietary Supplements, and Alcohol: A Systematic Review and Meta-analyses. (Pubmed Central) - Nov 2, 2022
Didanosine, zalcitabine, zidovudine, efavirenz, amprenavir, fosamprenavir, and indinavir should be taken on an empty stomach for maximum patient benefit...There is insufficient evidence available to make recommendations about consuming juice or alcohol with antiretroviral drugs. Resolving drug-food interactions may contribute to maximized cART effectiveness and safety.
- |||||||||| 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.
- |||||||||| 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.
- |||||||||| 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.
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