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BPI-371153 is a novel, orally bioavailable small molecule inhibitor of programmed cell death ligand 1 (PD-L1, also known as CD274). Developed by Betta Pharmaceuticals, it is designed to disrupt the interaction between PD-L1 and its receptor PD-1, thereby blocking an important immune checkpoint pathway that tumors exploit to evade immune surveillance. Preclinical data indicate that BPI-371153 induces and stabilizes PD-L1 dimer formation and endocytosis, effectively inhibiting the immunosuppressive function of PD-L1. The drug is being investigated for its antineoplastic activity in patients with locally advanced or metastatic solid tumors and relapsed/refractory lymphoma. Early clinical results show manageable safety, favorable pharmacokinetics (half-life 20.8–26.2 hours), immunomodulatory effects (increased IL-18, IL-2, IL-6, CXCL9), and promising antitumor activity—particularly in patients with high PD-L1 expression or high tumor mutational burden[1][3][5][6].
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