First-in-human Safety, Pharmacokinetics and Pharmacodynamics of THB001: An Orally Available, Potent and Highly Selective Small Molecule Inhibitor of Wild Type KIT Receptor Tyrosine Kinase

Mast cells play a central role in the pathophysiology of allergic diseases. Mast cell activation, proliferation and survival is dependent on KIT (CD117) signaling. THB001 is an inhibitor of wild type KIT being developed as a potential therapy for mast cell driven diseases. A first-in-human study was performed to determine the safety, pharmacokinetics (PK) and pharmacodynamics (PD) of THB001.