Novel compounds and their use as an inhibitor for SARS-CoV-2.
Invention Summary:
Two oral SARS-CoV-2 antivirals are available, molnupiravir and Paxlovid. However, the limited efficacy, drug-drug interaction, and drug resistance are main challenges facing these two drugs. Additional oral antivirals with novel mechanisms of actions are clearly needed. The papain-like protease (PLpro) of SARS‐CoV‐2 is a validated antiviral drug target inhibiting viral replication and there are no FDA approved inhibitors in this class.
Rutgers researchers have designed a battery of PLpro inhibitors with nanomolar IC50 values, representing the most potent PLpro inhibitors that can be used alone or in combination with the main protease inhibitors. The compounds are designed to target a new binding pocket and the mechanism of action has been characterized by X-ray crystallography, enzymatic assay, cell based FlipGFP PLpro assay, binding assay, and antiviral assay. Several lead compounds also showed favorable in vitro and in vivo PK properties.
Market Applications:
- Antiviral treatment for SARS-CoV-2 infection.
- Stand-alone treatment or can be used in combination with other available treatments.
Advantages:
- Potent antiviral activity (EC50 = 0.1 to 1 µM) and favorable in vitro and in vivo PK properties (i.p. and p.o.).
- Effective against multiple variants of SARS-CoV-2.
- Effective against nirmatrelvir resistant SARS-CoV-2 viruses.
- Orally bioavailable.
Intellectual Property & Development Status: Provisional patent application filed, patent pending. Available for licensing and/or research collaboration. For any business development and other collaborative partnerships contact marketingbd@research.rutgers.edu.
