The predominant role of BRCA1/2 genes in DNA repair process, as well as their functional failure in BRCA1/2-associated breast cancer, has been the basis for developing novel therapeutic approaches directly or indirectly targeting this pathway, including specific cytotoxic agents such as platinum compound and poly(ADP-ribose) polymerase (PARP) inhibitors. This evidence concerns the gene BRCA1 and breast cancer.