KPT-276 is a selective inhibitor of nuclear export (SINE) compound that targets the nuclear export protein exportin 1 (XPO1/CRM1). It has been primarily investigated for its potential in cancer therapy, particularly in hematologic malignancies and solid tumors. By blocking XPO1, KPT-276 promotes the retention of tumor suppressor proteins and growth regulatory proteins in the nucleus, leading to cell cycle arrest and apoptosis in cancer cells. It has shown preclinical activity in models of multiple myeloma, acute myeloid leukemia, lymphoma, and certain solid tumors, especially those with dysregulated tumor suppressor pathways such as p53. KPT-276 enhances the anti-tumor effects of other agents such as proteasome inhibitors and chemotherapeutics, making it a candidate for combination regimens. Due to its mechanism of action and selectivity, KPT-276 is being explored as a therapeutic option in cancers resistant to conventional treatments. Its development supports ongoing research into targeted therapies that exploit nucleocytoplasmic transport dysregulation in cancer.