Oral IRAK1/4 Inhibitor for the Treatment of Autoimmune and Inflammatory Diseases:

  • The investigational candidate, R835, is an orally available, potent and selective inhibitor of interleukin receptor associated kinase (IRAK)1 and IRAK4 that blocks inflammatory cytokine production in response to toll-like receptor (TLR) and interleukin-1 receptor family (IL-1R) signaling.
  • TLRs and IL-1Rs play a critical role in the innate immune response. Dysregulation of the TLR and IL-1R pathways may be associated with a variety of inflammatory conditions including psoriasis, rheumatoid arthritis, lupus and gout (among others).
  • Through inhibition of TLR and IL1R signaling, R835 blocks both IL-23 production and TH17 cell differentiation providing a strong rationale for its use in the treatment of IL23/IL17-mediated diseases, such as psoriasis.
  • Rigel has an ongoing Phase 1 study to assess the safety, tolerability, and pharmacokinetics of R835 in healthy subjects.