ASP3082 + pembrolizumab

ASP3082 + pembrolizumab is an investigational combination therapy intended for advanced solid tumors with KRAS G12D mutation, particularly non-small cell lung cancer (NSCLC) and other solid tumors. ASP3082 is a novel small molecule proteolysis-targeting chimera (PROTAC) degrader that selectively binds and promotes degradation of KRAS G12D-mutated protein by recruiting E3 ubiquitin ligases, leading to its destruction. Pembrolizumab is a monoclonal antibody checkpoint inhibitor targeting programmed cell death protein 1 (PD-1), thus enhancing anti-tumor immunity. The combination aims to provide a targeted antineoplastic effect by both directly degrading oncogenic KRAS G12D and promoting anti-tumor immune activity. ASP3082 is developed by Astellas Pharma. The combination is being evaluated by intravenous route in clinical trials for safety, tolerability, and anti-tumor efficacy in patients with advanced solid tumors, particularly NSCLC, harboring KRAS G12D mutation[1][3][4].