to change the course of inflammatory diseases at the optimal intervention point: targeting mast cells through KIT inhibition

Our current research and development efforts are focused on inflammatory diseases of the skin, airway, and gastrointestinal tract. These diseases collectively affect millions of people worldwide, and in their most severe forms, are associated with significant morbidity and mortality risk.

Mast cells are part of the immune system and act as a primary effector cell of certain inflammatory diseases, such as chronic urticaria. Current approaches to treating mast cell-mediated inflammation are mechanistically limited. These approaches target either specific upstream activators or downstream mediators of mast cell activity, leaving multiple, residual signaling pathways open to propagate the inflammatory response.

Targeting KIT
has been shown to broadly inhibit mast cell activity

A highly selective, oral approach to targeting KIT represents a novel therapeutic approach that offers the potential for a meaningful advancement in the treatment paradigm for mast-cell mediated inflammatory diseases. In addition to improved patient convenience versus injectable therapies, daily oral therapy creates the opportunity for finer dose titration, and via its intracellular mechanism of action, eliminates the risk of antibody-mediated mast cell activation and anaphylaxis, which can be associated with biologic treatment approaches.

KIT at-a-glance
  • KIT is a cell-surface receptor found on mast cells and other cell types in the body
  • For mast cells, KIT is a master regulator of proliferation, migration, activation, and survival
  • Inhibition of KIT drives both rapid inactivation and depletion of mast cells over time
Learn more about THB335