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Remdesivir - PubAg

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Last Updated: 15 October 2021

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Remdesivir: From Ebola to COVID-19

Human coronaviruses were discovered in the 1960s and were originally believed to cause just moderate top respiratory system conditions in immunocompetent hosts. Despite the value of these pathogens, no accepted antiviral medications for the treatment of human coronavirus infections appeared. Remdesivir, a nucleotide analogue prodrug initially developed for the treatment of Ebola virus, was found to hinder the replication of a wide variety of human and animal coronaviruses in vitro and in preclinical studies. It is therefore not unexpected that when the extremely pathogenic SARS-CoV-2 coronavirus emerged in late 2019 in China, triggering worldwide health and wellness issue due to the virus strong human-to-human transmission capacity, remdesivir was just one of the first scientific candidates that obtained focus. After in vitro studies had shown its antiviral activity against SARS-CoV-2, and a first individual was successfully treated with the medicine in the USA, a variety of trials on remdesivir were initiated.

Source link: https://pubag.nal.usda.gov/catalog/7184294


Sulfobutylether-beta-cyclodextrin-enabled antiviral remdesivir: Characterization of electrospun- and lyophilized formulations

Making use of solubilizing carbohydrate resulted in a 300-fold renovation of the aqueous solubility of REM, and improved dissolution rate of the drug allowing the prep work of steady infusion options for therapy. 2D ROESY NMR spectroscopy given details on the nature of REM-- excipient interaction and suggested the existence of addition phenomenon and the electrostatic destination in between anionic SBECD and nitrogen-containing REM in liquid remedy.

Source link: https://pubag.nal.usda.gov/catalog/7339970


Selecting a stable solid form of remdesivir using microcrystal electron diffraction and crystal structure prediction

We present the MicroED frameworks of remdesivir forms II and IV and end that form II is a lot more stable than form IV at ambient temperature in contract with experimental observations.

Source link: https://pubag.nal.usda.gov/catalog/7373045


Remdesivir: A potential game-changer or just a myth? A systematic review and meta-analysis

Professional renovation on day 28, day 14 scientific healing, and day 14 discharge rate were much better among remdesivir team. Earlier clinical enhancement; and scientific recovery were seen amongst the remdesivir group. Longer course of remdesivir showed a higher discharge rate at day 14, however there were significantly greater rates of serious unfavorable impacts, and medication discontinuation than the 5-day course. Remdesivir revealed a much better 14 days death account, clinical recuperation, and discharge rate.

Source link: https://pubag.nal.usda.gov/catalog/7159522


Rapid determination of remdesivir (SARS-CoV-2 drug) in human plasma for therapeutic drug monitoring in COVID-19-Patients

To take on the unsafe consequences of the extensive COVID-19 pandemic, a broad-spectrum anti-viral medicine remdesivir has gotten miraculous focus recently as a result of its encouraging application in dealing with COVID-19 patients. A fast and sensitive analytical method is vital to monitor RDV medicine account in human plasma for pharmacokinetics and therapeutic medicine monitoring. Under the ideal VA-SI-LLME conditions, method validation results suggested a superb correlation coefficient of 0. 9969 for UHPLC-PDA and 0. 9990 for UHPLC-MS/MS. The established technique showed exceptional removal recoveries between 90. 79-- 116. 74 % and 85. 68-- 101. 34 % with intraday and interday accuracy ≤ 9. 59 for both methods. These outcomes proved that the developed approach is a basic, fast, and delicate logical method that can be applied as a conventional analytical device for PK and TDM studies of RDV in scientific tests during the current around the world episode.

Source link: https://pubag.nal.usda.gov/catalog/7221887


The folate antagonist methotrexate diminishes replication of the coronavirus SARS-CoV-2 and enhances the antiviral efficacy of remdesivir in cell culture models

We examined restraint of host cell nucleotide synthesis as a promising strategy to reduce the replication of SARS-CoV-2-RNA, hence decreasing the formation of virus progeny. Strikingly, the duplication of SARS-CoV-2 was prevented by MTX in therapeutic focus around 1 µM, leading to greater than 1000-fold reductions in virus kids in Vero C1008 and ~ 100-fold reductions in Calu-3 cells. Infection duplication was much more conscious comparable focus of MTX than of the well established antiviral agent remdesivir. MTX highly diminished the synthesis of viral structural healthy proteins and the amount of released virus RNA. Virus replication and healthy protein synthesis were saved by folinic acid and by inosine, indicating that purine depletion is the primary mechanism that enables MTX to decrease virus RNA synthesis. The combination of MTX with remdesivir caused synergistic problems of virus replication, also at 100 nM MTX.

Source link: https://pubag.nal.usda.gov/catalog/7410724


Development and validation of a simple, selective, and sensitive LC-MS/MS assay for the quantification of remdesivir in human plasma

Remdesivir, formerly GS-5734, has lately ended up being the first antiviral medicine accepted by the U. S. Food and Drug Administration to treat COVID-19, the illness triggered by SARS-CoV-2. Healing dosing and pharmacokinetic studies require an easy, sensitive, and discerning confirmed assay to evaluate drug focus in scientific samples. We created a fast and delicate LC-MS/MS assay for the quantification of remdesivir in human plasma with its deuterium-labeled analog, remdesivir- ² H5, as the interior standard.

Source link: https://pubag.nal.usda.gov/catalog/7307811


Effect of remdesivir on patients with COVID-19: A network meta-analysis of randomized control trials

Thus, we performed a network meta-analysis comparing the rate of medical enhancement amongst patients with COVID-19 that got 5-day course of remdesivir versus 10-day course of remdesivir versus conventional care. Our evaluation demonstrated that the usage of remdesivir for patients with COVID-19 was connected with the significantly greater scientific enhancement rate contrasted with standard care alone.

Source link: https://pubag.nal.usda.gov/catalog/7087827


A Chemoenzymatic Synthesis of the (RP)-Isomer of the Antiviral Prodrug Remdesivir

Like various other ProTide prodrugs, remdesivir includes a chiral phosphorus facility. However, both presently known enzymes liable for the preliminary activation action of remdesivir are each stereoselective and show differential tissue circulation. Provided the capacity of the COVID-19 infection to contaminate a wide range of cells types, addition of the -diastereomer may be of scientific importance.

Source link: https://pubag.nal.usda.gov/catalog/7084164


Current knowledge about the antivirals remdesivir (GS-5734) and GS-441524 as therapeutic options for coronaviruses

Remdesivir is a broad-spectrum antiviral medication that is now being checked as a potential treatment for COVID-19 in global, multi-site clinical tests. It is critical for public health specialists and the One Health community to stay up to day on one of the most encouraging potential restorative options that are under examination. Thus, the purpose of this evaluation is to manufacture the expertise to day about remdesivir as a healing option for coronaviruses, with a special focus on info pertinent to the One Health community.

Source link: https://pubag.nal.usda.gov/catalog/6980179

* Please keep in mind that all text is summarized by machine, we do not bear any responsibility, and you should always check original source before taking any actions

* Please keep in mind that all text is summarized by machine, we do not bear any responsibility, and you should always check original source before taking any actions