KTN0158

KTN0158 is a humanized IgG1 monoclonal antibody that targets the stem cell factor receptor KIT (also known as c-KIT or CD117). It binds to the extracellular immunoglobulin-like domain 4 (D4) of KIT, blocking receptor homodimerization and preventing interaction with its ligand, stem cell factor (SCF), thereby inhibiting downstream signaling. KTN0158 potently inhibits both wild-type and mutant forms of KIT phosphorylation and has demonstrated strong antitumor activity in preclinical models, particularly in canine mast cell tumors. The drug was developed as a potential therapy for cancers driven by aberrant KIT activation—including gastrointestinal stromal tumors (GIST) and other KIT-dependent malignancies—as well as for conditions like neurofibromatosis type 1. In preclinical studies, KTN0158 showed greater potency than small-molecule inhibitors such as imatinib or nilotinib[1][2][5][7].

Other names

anti-c-KIT monoclonal antibody