• Featured Technology

    Compounds for Acute Lung Inflammation and Other Inflammatory Diseases

  • Blocking damage due to the activation of the NADPH complex is a potential strategy for treating many diseases. Current NADPH oxidase inhibitors lack specificity or potency, thus there is need to develop alternative therapeutics suitable for clinical testing. Researchers at Cincinnati Children’s have designed inhibitors of the small GTPase Rac-p67phox interaction that interacts with p67phox such that it prevents the binding of activated Rac1, abrogating superoxide production. Disruption of the GTPase Rac-p67phox interaction inhibits NOX2 enzyme assembly, thereby preventing NADPH oxidase activation.

    One inhibitor suppressed lipid oxidation and reduced inflammation in mouse lung tissue.

    A novel confidential lead compound has a Kd ~0.1microM.

    • NADPH activation is associated with tissue damage, mediation of innate immunity, inflammatory disorders, hyperproliferative disorders, fibrotic disease, and reperfusion injury.
    • More potent than available treatments
    • Acts with more specificity than available treatments
    • Potential for multiple delivery modes: oral, IV, or topical

    For an in-depth market overview, please click here.

    • The anti-inflammatory therapeutics market is estimated to reach $85.9B in 2017.
    • There are over 180 conditions that cause chronic or acute lung inflammation.
    • Asthma and COPD are two of the most common causes of lung inflammation and affect more than 10M people in the US.

    US Non-Provisional Patent Pending

    Canada Patent Pending

    European Patent Pending

    Priority Date: 02/14/2012

    Bosco, E. E., Kumar, S., Marchioni, F., Biesiada, J., Kordos, M., Szczur, K., … Zheng, Y. (2012). Rational design of small molecule inhibitors targeting the Rac GTPase - p67phox signaling axis in inflammation. Chemistry & Biology, 19(2), 228–242. doi:10.1016/j.chembiol.2011.12.017

  • For more information, please contact CTC Business Development at partnering@cchmc.org or 513-636-4285.