Öйú365betÖÐÎĹÙÍø

Scientists continue to develop potential treatments for and vaccines against COVID-19 at a breathtaking pace. Among the most recent reports, Timothy O. Sheahan and Ralph S. Baric at the University of North Carolina at Chapel Hill, George Painter at Emory University (Atlanta), and colleagues there and at Vanderbilt University (Nashville, TN) and the Centers for Disease Control and Prevention (Atlanta) found that an existing antiviral prodrug shows promise against the SARS-CoV-2 virus.

The authorsâ€� work originated with a broad-spectrum antiviral compound called EIDD-1931 (β-d-N⁴-hydroxycytidine or uridine 4-oxime) that Painter and co-workers began to investigate in the early 2010s as a coronavirus treatment. (EIDD stands for the Emory Institute for Drug Development.) The molecule worked well against the SARS-CoV virus (which causes the severe acute and Middle East respiratory syndromes) in mice and dogs, but not monkeys.

Finding that the hydroxyl group in EIDD-1931 was being phosphorylated in monkeys� stomachs and could not get to infected cells, the researchers sought a way to block phosphorylation. They esterified the hydroxyl group in EIDD-1931 with 2-methylpropanoic acid to produce the molecule EIDD-2801 [uridine 5�-(2-methylpropanoate), 4-oxime], which not only prevented phosphorylation, but also made the prospective prodrug more lipid-soluble and therefore more available orally. Enzymes in the bloodstream hydrolyze EIDD-2801 to liberate the active agent EIDD-1931.

Following on the success of EIDD-2801 against SARS-CoV, the researchers turned their attention to the novel coronavirus. In April, they were able to state that the administration of EIDD-2801 is � . . . in primary human epithelial cell cultures without cytotoxicity.�

Things happened fast after that discovery. The scientists ; and the US Food and Drug Administration approved the application in a near-record 7 days. Drug Innovation Ventures at Emory (DRIVE), a spin-off from the university, then licensed EIDD-2801 to Ridgeback Biotherapeutics (Miami, FL) for human studies.

Painter believes that EIDD-2801 could work as a treatment for COVID-19 and other coronaviral diseases and, even better, as a prophylactic for individuals who have been exposed to a coronavirus.