Sograzepide (Netazepide) is a potent, selective, and orally bioavailable gastrin/CCK-B receptor antagonist. It suppresses gastrin-mediated signaling and pappalysin 2 expression, demonstrating the ability to induce regression of type 1 gastric neuroendocrine tumors (gNETs) in clinical research. This small molecule is a valuable tool for investigating gastrin biology and gNET pathogenesis in both in vitro and in vivo models.