eltanexor

Eltanexor is an orally bioavailable, second-generation selective inhibitor of nuclear export (SINE) that targets the exportin 1 protein (XPO1/CRM1). By binding to XPO1, eltanexor blocks the nuclear export of tumor suppressor proteins such as p53, p73, BRCA1/2, pRB, and FOXO. This leads to their accumulation in the nucleus and reactivation of their tumor-suppressing functions, resulting in apoptosis of cancer cells while sparing normal cells. Eltanexor has a broad therapeutic window with minimal blood-brain barrier penetration and is being developed primarily for hematologic malignancies and solid tumors. It is under investigation for diseases including myelodysplastic syndromes (MDS), multiple myeloma, colorectal cancer, nasopharyngeal cancer, prostate cancer, squamous cell carcinoma, acute myeloid leukemia (AML), and solid tumors. The drug has received orphan drug designation from the FDA for MDS but is not yet approved by any regulatory agency[1][2][3][4][5][6].

Other names

eltanexor