Invention Summary:
RifaAAPs are novel dual-targeted, low-resistance-emergence, orally-available compounds for treatment of tuberculosis (TB) and non-tuberculous mycobacterial (NTM) infections--including drug-resistant, multi-drug-resistant (MDR), and extensively-drug-resistant (XDR) strains.
Researchers indicate that RifaAAPs comprise the core pharmacophore of rifampin (Rif; a first-line anti-TB drug that binds to the mycobacterial RNA polymerase active center and sterically blocks RNA synthesis) covalently linked to an N-aroyl-N-aryl-phenylalaninamide (AAP; a proprietary synthetic anti-TB agent that binds to a different site on mycobacterial RNA polymerase and allosterically blocks RNA synthesis). RifaAAPs inhibit mycobacterial RNA polymerase through two different binding sites (the Rif and AAP binding sites) and two different mechanisms (the Rif and AAP mechanisms). As a result, RifaAAPs overcome Rif-resistance and overcome AAP-resistance. As a further result, RifaAAPs exhibit much lower--orders of magnitude lower--resistance emergence than Rif and AAP. RifaAAPs potently inhibit Mycobacterium tuberculosis RNA polymerase, exhibit potent in vitro antibacterial activity against Mycobacterium tuberculosis and non-tuberculous mycobacteria--including drug-susceptible, drug-resistant, and multidrug-resistant strains--and exhibit potent in vivo efficacy in oral treatment of mouse Mycobacterium tuberculosis acute infection and mouse Mycobacterium tuberculosis chronic infection (ED = 12.5 mg/kg PO).
Market Applications:
- Oral treatment of drug-susceptible, drug-resistant, multi-drug-resistant, and extensively-drug-resistant TB.
- Oral or parenteral treatment of drug-susceptible, drug-resistant, multi-drug-resistant, and extensively-drug-resistant NTM infections, including Mycobacterium avium infections and Mycobacterium abscessus infections.
Advantages:
- Potent in vitro activity against drug-susceptible, drug-resistant, and multi-drug-resistant TB and NTM infections, including Mycobacterium avium complex and Mycobacterium abscessus.
- Potent in vivo efficacy in treatment of mouse Mycobacterium tuberculosis acute infection and chronic infection.
- Dual-targeted. Novel chemical scaffold and novel mechanism.
- Low resistance emergence.
- High oral availability
Intellectual Property & Development Status: 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
Researchers at Rutgers University have designed a novel two-phase, environmentally friendly, low-cost air purification device that could run off a backup battery for emergencies.
Market Applications:
• Air purification in wildfire smoke environments
Advantages:
• Low-cost
Publications: • Low-cost
Intellectual Property & Development Status: 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
Researchers at Rutgers University have designed a novel two-phase, environmentally friendly, low-cost air purification device that could run off a backup battery for emergencies.
Market Applications:
• Air purification in wildfire smoke environments
Advantages:
• Low-cost
Publications: • Low-cost
Intellectual Property & Development Status: Issued US and EP patents and pending US, EP, and Chinese patents. Available for licensing or research collaboration. This is a late-stage preclinical program with in vitro and in vivo proof of concept, ADME, safety pharmacology, and PK. For business development or other collaborative partnerships, contact marketingbd@research.rutgers.edu
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