Invention Summary:
AAPs are novel orally available compounds for treatment 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 AAPs potently inhibit mycobacterial RNA polymerase through a novel binding site and novel mechanism. AAPs exhibit potent in vitro antibacterial activity against Mycobacterium tuberculosis and non-tuberculous mycobacteria--including drug-susceptible, drug-resistant, and multidrug-resistant strains (MIC for Mycobacterium tuberculosis = 0.78 mg/ml; MIC for Mycobacterium avium = 0.39 mg/ml; MIC for Mycobacterium abscessus = 3.13 mg/ml). AAPs exhibit potent in vivo efficacy in oral treatment of mouse acute infection and chronic infection by drug-susceptible M. tuberculosis and multi-drug-resistant Mycobacterium tuberculosis (EDs = 50-100 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.
- Novel chemical scaffold, novel binding site, and novel mechanism.
- No cross-resistance with current antimycobacterial drugs.
- Oral availability.
Publications: • Low-cost
Intellectual Property & Development Status:
Issued US and European patents. Available for licensing or research collaboration. This is a late-stage preclinical program with in vitro and in vivo proof of concept, ADME, and PK (candidate-selection and de-risking stage). For business development or other collaborative partnerships, contact marketingbd@research.rutgers.edu
