APG-1387 + pembrolizumab

APG-1387 + pembrolizumab is an investigational combination therapy being evaluated for the treatment of advanced solid tumors. APG-1387 is a small-molecule, bivalent inhibitor of apoptosis proteins (IAP antagonist), which acts as a second mitochondrial-derived activator of caspases (SMAC) mimetic. It induces rapid degradation of cellular IAP1 and X-linked IAP, leading to enhanced apoptosis of cancer cells and immune modulation. Pembrolizumab is a monoclonal antibody immune checkpoint inhibitor targeting programmed death-1 (PD-1), thereby enhancing T-cell-mediated antitumor immune responses. The combination aims to synergistically induce cancer cell apoptosis and enhance antitumor immunity. Clinical studies have shown that the combination is generally well tolerated and has demonstrated promising preliminary antitumor effects—including partial responses and disease control in patients with cancers such as breast cancer, colorectal cancer (CRC), and non-small cell lung cancer (NSCLC)—with manageable adverse events[1][2][3].