KTN0182A

KTN0182A is an investigational antibody-drug conjugate (ADC) developed by Kolltan Pharmaceuticals for KIT-positive malignancies. It consists of the humanized IgG1κ monoclonal antibody KTN0158, which binds the membrane-proximal D4 domain of KIT to inhibit receptor dimerization, conjugated via a cathepsin-cleavable valine/alanine linker to the pyrrolobenzodiazepine (PBD) dimer payload SG3227 (with average DAR ~2). The PBD binds DNA minor groove to cross-link strands, causing lethal lesions, demonstrating potent antitumor activity in vitro and in vivo against broad tumor types, including as primary therapy or to overcome resistance to small molecule KIT inhibitors.[1][8][9]