bgb-10188

BGB-10188 is a highly selective, oral small molecule inhibitor of phosphatidylinositol 3-kinase delta (PI3Kδ). It binds selectively to PI3Kδ and inhibits the PI3K/AKT signaling pathway, leading to decreased proliferation and increased cell death in tumor cells that overexpress PI3Kδ[1][2][6]. Preclinical studies show that BGB-10188 has more than 3000-fold selectivity for PI3Kδ over other isoforms (PI3Kα, β, γ) and does not significantly inhibit other kinases or lipid kinases[2][6]. The drug demonstrates potent antitumor activity as monotherapy and in combination with zanubrutinib (a BTK inhibitor) or tislelizumab (a PD-1 antibody), particularly in models of malignant B-cell neoplasms[3][5]. Clinical trials are ongoing for various hematologic malignancies and solid tumors. Developed by BeiGene, it is currently being evaluated in Phase I/II clinical trials for diseases including relapsed/refractory mature B-cell malignancies, follicular lymphoma, mantle cell lymphoma, diffuse large B-cell lymphoma, chronic lymphocytic leukemia, melanoma, non-small cell lung cancer, small cell lung cancer, advanced malignant solid neoplasms—including gastroesophageal junction carcinomas—and others[2][4][7].