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  • ||||||||||  Paxlovid (nirmatrelvir/ritonavir) / Pfizer
    Review, Journal:  New Insights into the Cooperativity and Dynamics of Dimeric Enzymes. (Pubmed Central) -  Aug 24, 2023   
    These advancements not only provide essential case studies and theoretical support for comprehending dimeric enzyme catalysis but also serve as a foundation for designing highly efficient catalysts, such as dimeric organic catalysts. Moreover, these developments have significant implications for drug design, as exemplified by Paxlovid, which was designed for the homodimeric main protease of SARS-CoV-2.
  • ||||||||||  Paxlovid (nirmatrelvir/ritonavir) / Pfizer
    Journal:  Multicomponent Synthesis of the SARS-CoV-2 Main Protease Inhibitor Nirmatrelvir. (Pubmed Central) -  Aug 22, 2023   
    We report a new synthesis of nirmatrelvir featuring a highly enantioselective biocatalytic desymmetrization (>99% ee) and a highly diastereoselective multicomponent reaction (>25:1 dr) as the key steps. Our route avoids the use of transition metals and peptide coupling reagents, resulting in an overall highly efficient and atom-economic process.
  • ||||||||||  Lagevrio (molnupiravir) / Ridgeback Biotherap, Merck (MSD)
    Journal, Real-world evidence, Real-world:  Real-World Utilization of Molnupiravir during the COVID-19 Omicron Surge in Israel. (Pubmed Central) -  Aug 22, 2023   
    At 28 days post-MOV dispensation, the cumulative incidence (95% CI) of COVID-19-related hospitalization and/or all-cause mortality was 3.6% (2.5%, 4.6%), with similar rates across sexes and age groups (18-64 vs. ?65 years), and lower rates among recently vaccinated and/or recently SARS-CoV-2-infected patients. These data describe the characteristics and outcomes for MOV-treated patients in Israel, whose clinical characteristics may preclude the use of nirmatrelvir/ritonavir to treat their COVID-19 infection.
  • ||||||||||  Paxlovid (nirmatrelvir/ritonavir) / Pfizer
    Journal:  Exploring diverse reactive warheads for the design of SARS-CoV-2 main protease inhibitors. (Pubmed Central) -  Aug 22, 2023   
    SARS-CoV-2 main protease (M) is a validated antiviral drug target of nirmatrelvir, the active ingredient in Pfizer's oral drug Paxlovid...X-ray crystal structures of M with Jun10541R and Jun10221 revealed covalent modification of Cys145. These M inhibitors with diverse reactive warheads collectively represent promising candidates for further development.
  • ||||||||||  Paxlovid (nirmatrelvir/ritonavir) / Pfizer
    Journal:  Le nirmatrelvir-ritonavir pour les patients non hospitalis (Pubmed Central) -  Aug 20, 2023   
    Based on the predicted biological activities and binding affinities of NMV to WT and mutant (C145A & C145S) M, it can be stipulated that NMV may have conventional potency to act as an anti-viral agent against WT M, while the catalytic-dyad mutations may show substantial mutation-induced drug resistance.Communicated by Ramaswamy H. Sarma. No abstract available
  • ||||||||||  Paxlovid (nirmatrelvir/ritonavir) / Pfizer, Lagevrio (molnupiravir) / Ridgeback Biotherap, Merck (MSD)
    Journal:  Pyronaridine tetraphosphate is an efficacious antiviral and anti-inflammatory active against multiple highly pathogenic coronaviruses. (Pubmed Central) -  Aug 15, 2023   
    Additionally, we find that pyronaridine additively combines with current COVID-19 treatments such as nirmatrelvir (protease inhibitor in Paxlovid) and molnupiravir to further inhibit SARS-CoV-2 infections. There are many antiviral compounds that demonstrate efficacy in cellular models, but few that show this level of impact in multiple mouse models and represent a promising therapeutic for the current coronavirus pandemic as well as future outbreaks as well.
  • ||||||||||  Paxlovid (nirmatrelvir/ritonavir) / Pfizer
    Journal:  Deuteration for Metabolic Stabilization of SARS-CoV-2 Inhibitors GC373 and Nirmatrelvir. (Pubmed Central) -  Aug 14, 2023   
    Hydrogens can be replaced with deuterium in nirmatrelvir and GC373 to slow oxidation. Results show that deuterium slows oxidation of nirmatrelvir adjacent to nitrogen by ?40% and that the type of warhead can switch the site of oxidative metabolism.
  • ||||||||||  Paxlovid (nirmatrelvir/ritonavir) / Pfizer
    An Infectious Rise in Fats - Severe Hypertriglyceridemia Secondary to SARS-CoV-2 Infection (Zone 4, Science and Technology Hall, Level 2) -  Aug 12, 2023 - Abstract #AHA2023AHA_5829;    
    He was prescribed paxlovid and discharged home...Further research is needed to deduce how infectious processes can lead to elevated TG levels. Treatment consists of initiating a low-fat diet and may include fibrates.
  • ||||||||||  Paxlovid (nirmatrelvir and ritonavir) / Pfizer, Lagevrio (molnupiravir) / Ridgeback Biotherap, Merck (MSD)
    Journal, Real-world evidence, Real-world effectiveness, Real-world:  Real-world effectiveness of molnupiravir and nirmatrelvir/ritonavir as treatments for COVID-19 in high-risk patients. (Pubmed Central) -  Aug 11, 2023   
    Nirmatrelvir-ritonavir treatment was associated with reduced hospitalization in high-risk COVID-19 patients even in highly vaccinated populations. Collectively, these real-world findings suggest that although the risks of hospitalization and death due to COVID-19 have been reduced, antivirals can provide additional benefits to members of highly vulnerable patient populations.
  • ||||||||||  LB Abstract 2 TBD 3 (254 AB) -  Aug 11, 2023 - Abstract #IDWeek2023IDWeek_431;    
  • ||||||||||  Paxlovid (nirmatrelvir and ritonavir) / Pfizer, Lagevrio (molnupiravir) / Ridgeback Biotherap, Merck (MSD)
    Journal:  Anthracyclines inhibit SARS-CoV-2 infection. (Pubmed Central) -  Aug 7, 2023   
    Six compounds were found to inhibit SARS-CoV-2 at the half maximal inhibitory concentration (IC50) below 1 ?M, including the anthracycline drug aclarubicin that markedly reduced viral RNA-dependent RNA polymerase (RdRp)-mediated gene expression, whereas other anthracyclines inhibited SARS-CoV-2 by activating the expression of interferon and antiviral genes. As the most commonly prescribed anti-cancer drugs, anthracyclines hold the promise of becoming new SARS-CoV-2 inhibitors.
  • ||||||||||  Paxlovid (nirmatrelvir and ritonavir) / Pfizer
    Journal:  DNA-encoded chemical libraries yield non-covalent and non-peptidic SARS-CoV-2 main protease inhibitors. (Pubmed Central) -  Aug 5, 2023   
    Furthermore, these compounds demonstrate efficacy against mutant forms of M that have shown resistance to the standard-of-care drug nirmatrelvir. Overall, this work demonstrates that DEC-Tec can efficiently generate novel and potent inhibitors without preliminary chemical or structural information.
  • ||||||||||  GOOD C-OP, BAD C-OP? (Convention Center Exhibit Hall) -  Aug 4, 2023 - Abstract #CHEST2023CHEST_2184;    
  • ||||||||||  Journal:  Medication safety in chronic kidney disease. (Pubmed Central) -  Aug 3, 2023   
    Several medications increase the risk of development of acute kidney injury or progression of CKD. Close attention is needed to select the appropriate dose or safer alternatives to reduce the risk of drug-induced harm in patients with CKD.