The Center for Drug Evaluation (CDE) of the National Food and Drug Administration of China announced that the fumaric acid BGB-10188 capsule declared by BeiGene has obtained the implied license of two clinical trials, and it is planned to be developed for the treatment of advanced malignant tumors. Public information shows that BGB-10188 is a PI3Kδ inhibitor independently developed by BeiGene. This is the first time the drug has been approved for clinical use in China.

Phosphatidylinositol 3-kinase (PI3K) is a key regulatory kinase in the PI3K/AKT/mTOR signaling pathway. The PI3K signaling pathway plays an important role in regulating cell growth, movement, survival, metabolism and angiogenesis. In human cancers such as breast cancer, colorectal cancer, and blood cancer, almost all PI3K signaling pathways are dysregulated. Studies have found that the overactivity of the PI3K signaling pathway is significantly correlated with tumor progression, increase in tumor microvessel density, and enhanced chemotaxis and invasiveness of cancer cells.

BGB-10188 is a highly selective PI3Kδ inhibitor independently developed by BeiGene and one of the important drugs in BeiGene's early independent research and development projects. PI3Kδ is a subtype of PI3K kinase. It mainly exists in immune cells and blood cells. It participates in the signal transduction of B cell antigen receptor (BCR) in B cells and controls the development and maturation of B cells in the body.

According to public information from BeiGene, compared with other similar drugs, the safety of BGB-10188 is improved, and it shows anti-tumor activity in the body. At present, BeiGene is carrying out BGB-10188 monotherapy in Australia, and combined with tislelizumab (anti-PD-1 monoclonal antibody) or zebutinib (BTK inhibitor) in the treatment of B-cell malignancies and solid tumors In the phase 1 clinical trial, 150 subjects will be enrolled in the research plan. This clinical approval in China means that BGB-10188 will also carry out clinical research in China.

Public information shows that in addition to PI3Kδ inhibitors, BeiGene's early independent research and development projects also include: BGB-A445, a non-ligand-competitive anti-OX40 monoclonal antibody under development, which is planned to be developed as a single agent or in combination with Tiramer Lilizumab for the treatment of solid tumors has just been approved for clinical studies in China; BGB-15025, a hematopoietic stem cell kinase 1 (HPK1) inhibitor under development, is to be developed as a single agent or combined with tislelizumab to treat the entity Tumor; BGB-16673, an investigational chimeric degradation activation complex targeting BTK, has been declared for clinical use in China in October this year; BGB-A425, an investigational TIM3 monoclonal antibody.