Published data for lead compound, the fumaramide PLpro inhibitor Jun13728, demonstrate potent inhibition of SARS-CoV2 variants including nirmatrelvir-resistant mutant (light blue). Link to paper below.
Invention Summary:
The COVID-19 pandemic significantly accelerated the development of antiviral therapies and vaccines. Recent efforts for research to support pandemic preparedness have focused on developing oral antiviral medications that target highly conserved viral components, including polymerases and proteases essential for replication. For example, nirmatrelvir, an inhibitor of the SARS-CoV-2 main protease (Mpro) and a component of Pfizer’s Paxlovid drug product, exhibits broad-spectrum activity against coronaviruses. However, additional antivirals with new mechanisms of action are needed to combat viruses for which no antivirals are available or for which there is known danger of drug resistance.
Researchers at Rutgers have designed and tested fumarimide inhibitors that target the papain-like protease (PLpro) of SARS-CoV-2 and demonstrate high potency. Supported by in vitro and in vivo PK data, results demonstrate effective inhibition and promising drug exposure characteristics.
Market Applications:
Therapeutic Development for Drug-Resistant Coronaviruses
Pandemic Preparedness and Response
Advantages:
Novel Mechanism of Action
Potent and Bioavailable
Publications:
• J. Med. Chem. 2024, 67, 22, 20399–20420
Intellectual Property & Development Status: Non-Provisional application filed. Patent pending. Available for licensing and/or research collaboration. For any business development and other collaborative partnerships, contact: marketingbd@research.rutgers.edu