Selinexor

Advances in the understanding of the pathophysiology, molecular biology and genetics of solid tumors and hematological malignancies have culminated in the development of novel targeted therapeutic agents leading to improved prognosis and quality of life for cancer patients. Despite these advances, prognosis remains poor for many cancer patients, and there is an unmet need for new therapeutic options. Exportin-1 (XPO1) is a nuclear export receptor that is responsible for exporting proteins, including tumor suppressor proteins, out of the nucleus. Nuclear export of tumor suppressor proteins is an important mechanism by which cancer cells avoid apoptosis and cell death. Overexpression of XPO1 imparts poor prognosis, indicating that XPO1 inhibition can be a potential therapeutic target. Recently, selective inhibitors of nuclear export (SINE) drugs have been developed. Selinexor (KPT-330) is an oral SINE with a favorable toxicity profile and demonstrated to have preclinical and clinical activity against a broad range of solid tumors and hematological malignancies.