Since 2020, Remdesivir, an antiviral medicine, has helped treat patients hospitalized due to COVID-19. It is approved by the FDA to be administered intravenously, and now, researchers are modifying it to be given orally.
As indicated in a Science Daily report, during the onset of the pandemic, Remdesivir was tested as a potential treatment and discovered to measurably lessen recovery time for COVID-19 patients admitted at the hospital.
In the last quarter of 2020, the Food and Drug Administration authorized the use of the medicine. Until to date, Remdesivir has stayed the only FDA-approved antiviral drug for COVID-19 infection.
At present, Remdesivir, as described by the National Institutes of Health, needs to be given intravenously, a process that limits its use to patients hospitalized with somewhat severe or advanced COVID-19 infections. The FDA has authorized the use of the drug only for adult patients and children who are 12 years old and above.
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In a study, Rethinking Remdesivir: Synthesis, Antiviral Activity and Pharmacokinetics of Oral Lipid Prodrugs, published in the Antimicrobial Agents and Chemotherapy, University of California San Diego School of Medicine, researchers described cell and animal research demonstrating how lipid modifications of Remdesivir nucleoside can enhance delivery, efficacy, and toxicity of the drug compared to the now-available Remdesivir.
According to the study's co-first author Robert Schooley, MD professor of medicine at UC San Diego School of Medicine, even though the development of the COVID-19 vaccine has had a major effect on the pandemic, the virus has continued spreading and causing disease, especially among those who haven't been vaccinated.
The professor added, with the development of more communicable viral variants, breakthrough cases of the virus are being detected, some of which can be severe in patients who have underlying conditions.
He also said the need for efficient, well-tolerated antiviral drugs that can be administered to patients at great risk for severe infection at the illness's early stages stays high.
For Oral Administration
Professor of medicine Karl Hostetler, MD at UC San Diego School of Medicine, together with colleagues, synthesized three new lipid prodrugs, combining a therapeutic agent, specifically Remdesivir nucleoside, with one of many lipid-phosphate types.
As described in the study, the resulting conjugated molecules employ new pathways to penetrate cells, the portion of that lipid phosphate carrying along with the medicine.
Essentially, the Remdesivir nucleoside's lipid phosphate prodrugs can be orally taken, staying intact and bioactive in the body after getting absorbed from the digestive system.
Schooley explained, "COVID-19 is a two-stage disease." The rapid growth of the virus takes place shortly after infection. It can also stimulate a misdirected immune response that leads to inflammatory pneumonia in patients who are not doing well.
For this antiviral treatment to be extremely effective, it needs to be given early in the infection before the illness's inflammatory phase leads to hospital admission.
Such compounds are formulated as oral administration, quickly absorbed from the gastrointestinal tract, and greatly bypass the liver where most of the toxicity of Remdesivir is detected.
For Remdesivir to become active, it needs modification by multiple enzymes. This complex metabolism possibly adds to variable antiviral activity, not to mention toxicity in different types of cells.
For instance, Remdesivir is effective in lung cells, although less effective in other organs. More so, it is somewhat more toxic in the liver cells, which restricts the number of drugs given to patients.
Related information about Remdesivir is shown on ABC News Australia's YouTube video below:
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