Efficacy of THB001, a Potent and Selective Oral Small Molecule Inhibitor of Wild Type KIT Receptor Tyrosine Kinase, in a Rat Passive Cutaneous Anaphylaxis Model

Abstract

Mast cells play a central role in the pathophysiology of allergic inflammation. Mast cell activation, migration, proliferation and survival are dependent on KIT (CD117) signaling. THB001 is a potent and selective inhibitor of wild type KIT being studied clinically as a therapy for mast cell driven diseases. The current study correlated target engagement, mast cell depletion and efficacy in an in vivo model of anaphylaxis.