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Overview

Basic Info

Drug Type

Drug conjugates

Synonyms-

Target

COX-2 x RdRp

Mechanism

COX-2 inhibitors(Cyclooxygenase-2 inhibitors), RdRp inhibitors(RNA-directed RNA polymerase inhibitors)

Therapeutic Areas

Infectious Diseases

Active Indication

Coronavirus Infections

Inactive Indication-

Originator Organization

Southern University of Science & Technology

Active Organization

Southern University of Science & Technology

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Structure

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Coronaviruses (CoVs) infect a broad range of hosts, including humans and various animals, with a tendency to cross the species barrier, causing severe harm to human society and fostering the need for effective anti-coronaviral drugs. GS-441524 is a broad-spectrum antiviral nucleoside with potent anti-CoVs activities. However, its application is limited by poor oral bioavailability. Herein, we designed and synthesized several conjugates via covalently binding NSAIDs to 5'-OH of GS-441524 through ester bonds. The ibuprofen conjugate, ATV041, exhibited potent in vitro anti-coronaviral efficacy against four zoonotic coronaviruses in the alpha- and beta-genera. Oral-dosed ATV041 resulted in favorable bioavailability and rapid tissue distribution of GS-441524 and ibuprofen. In MHV-A59 infected mice, ATV041 dose-dependently decreased viral RNA replication and significantly reduced the proinflammatory cytokines in the liver and the lung at 3 dpi. As a result, the MHV-A59-induced lung and liver inflammatory injury was significantly alleviated. Taken together, this work provides a novel drug conjugate strategy to improve oral PK and offers a potent anti-coronaviral lead compound for further studies.

100 Deals associated with ATV041

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