gb1275

GB1275 is a first-in-class, orally active small molecule that acts as an allosteric agonist of CD11b (integrin alpha M), a receptor broadly expressed on immunosuppressive myeloid cells such as myeloid-derived suppressor cells (MDSCs) and tumor-associated macrophages (TAMs) within the tumor microenvironment. By activating CD11b, GB1275 reduces the recruitment and function of MDSCs and TAMs at the tumor site, repolarizes immunosuppressive M2 TAMs to a pro-inflammatory M1 phenotype, and increases infiltration of activated CD8+ T cells into tumors. These effects enhance antitumor immune responses and have shown synergy with checkpoint inhibitors like pembrolizumab in preclinical models. GB1275 was developed for use in advanced solid tumors resistant or less responsive to immuno-oncology therapies—including pancreatic cancer (with orphan drug status), microsatellite-stable colorectal cancer, gastric/gastroesophageal junction cancers, breast cancer, prostate cancer, and esophageal cancer—but its clinical development has been discontinued after phase I/II trials due to lack of observed benefit[1][2][3][6].

Other names

(Z)-Leukadherin-1 choline