NC State University is seeking commercial partners to commercialize novel molecules which inhibit both TRYPV-1 and Janus Kinase to treat chronic pain and itch .
Chronic itch and pain can be debilitating for many people worldwide and share many common physiological pathways. Current itch management strategies involve corticosteroid creams, antibacterials or local anesthetics. If these treatments are not successful, medications to treat nerve pain are used such as Lyrica (pregabalin) or Neurontin (gabapentin), together with an antidepressant or nerve block. Chronic pain that is not responsive to over the counter medication can be treated with certain types of antidepressant, muscle relaxants, anti-seizure medication and opioid based drugs. All of these medications have side effects and opioid addiction has become an epidemic in the United States. In fact, the US Centers for Disease Control and Prevention recently reported that 91 Americans die a day from opioid dependence, totaling 33,000 deaths in 2015 – more than any year on record. Such drugs now kill more Americans than guns or car accidents. One of the newer therapies designed to target chronic itch and pain by reducing inflammation are Janus Kinase inhibitors (Jakinibs) which exert their effect by have their effect by reduction of signal transduction after binding of cytokines, such as IL-31, to their receptors. These molecules are proposed for the treatment of cancer and inflammatory diseases, such as atopic dermatitis (AD). The JAK inhibitor oclacitinib is currently approved for the treatment of lesions and pruritus in dogs with AD while tofacitinib is approved/under clinical development for human rheumatoid arthritis and inflammation and pruritus associated with atopic dermatitis and psoriasis.
Researchers at NC State University have identified that there is a much more comprehensive relief of itch by JAK inhibitors, mediated through TRPV1-receptors. In addition to itch inhibition, the reduced response to capsaicin by JAK inhibitors indicates an extension of possible benefit in attenuating pain transduction via TRPV1, as already documented in patients with rheumatoid arthritis. Based on this information, the inventors have designed a set of drug candidates that are likely to inhibit both Janus Kinase and TRPV-1 receptor activity with broader and more effective pain relieving properties.
- Novel inhibitors to reduce both pain, itch and inflammation through inhibition of TRPV1 and Janus Kinase
Related Patent Information
- A US Provisional Patent application related to this invention has been filed.
About the Inventors
Dr. Wolfgang Baeumer, DVM, Dr.Med.Vet..Habil., Dip. ECVPT is an Associate Professor in the Department of Molecular Biomedical Sciences in the College of Veterinary Medicine at NC State. Dr. Baeumer’s research is primarily focused on the field of immunopharmacology, specifically three pharmacological targets, the histamine H4 receptor, JAK-STAT-inhibitors and the chemokine thymic stromal lymphopoietin (TSLP) and their use to treat allergic skin diseases. He serves on the editorial board of the Journal of Asthma and Allergy.
Dr. Denis Fourches is an Assistant Professor in the Department of Chemistry in the College of Sciences at NC State. He joined North Carolina State University in January 2015 as a Chancellor’s Faculty Excellence Program cluster hire in Bioinformatics. His central research goal is to analyze, model, and forecast complex interactions between chemical structures and various types of biological targets to design novel compounds with the desired activity and safety profiles.
Dr. Joshua Pierce is an Assistant Professor in the Department of Chemistry in the College of Sciences at NC State. Professor Pierce’s research at NC State explores cutting edge problems in natural products synthesis and organic methods development with a constant goal of high impact contributions to chemistry, biology and materials science. He holds expertise in chemical synthesis (heterocycles, natural products, peptides; chemical structure elucidation (NMR, MS, etc); antimicrobial and anticancer compound development; chemical probe development for various biological pathways.