TIE2 kinase inhibition for advanced or metastatic solid tumors

Rebastinib is a potential first-in-class investigational, orally administered, potent, and highly selective inhibitor of the TIE2 kinase that was discovered using our proprietary drug discovery platform. TIE2 is the receptor for angiopoietins ANG-1 and ANG-2, an important family of vascular growth factors. TIE2 receptors are expressed on endothelial cells and angiogenic macrophages promoting the survival, maturation, and functional integrity of the vasculature and play a key role in regulating tumor angiogenesis, invasiveness, and metastasis. Rebastinib binds potently into the switch pocket of TIE2, stabilizing the inhibitory switch and displacing the activation switch to block TIE2 signaling. Rebastinib is currently being evaluated in a Phase 1b/2 clinical study in combination with paclitaxel.