BSI-401

BSI-401 is an orally active small molecule inhibitor of Poly (ADP-Ribose) polymerase 1 (PARP-1), initially developed by BiPar Sciences (later acquired by Sanofi). As a derivative of 6-iodo-5-amino-1,2-benzopyrone, it functions by non-covalently binding to PARP-1, an enzyme essential for sensing and repairing single-strand DNA breaks. By blocking this repair mechanism, BSI-401 promotes genomic instability and apoptosis in malignant cells, particularly those already burdened by DNA damage. It was positioned as a second-generation PARP inhibitor following iniparib (BSI-201) and has demonstrated preclinical activity in pancreatic and other digestive cancers, both as a monotherapy and in combination with platinum-based chemotherapeutics like oxaliplatin.

Other names

5-amino-6-iodo-1,2-benzopyrone5-amino-6-iodo-2H-1-benzopyran-2-one6-iodo-5-amino-1,2-benzopyrone derivative