Eltanexor (KPT-8602) is a second-generation SINE, orally bioavailable Exportin 1 (XPO1,CRM1) inhibitor with markedly reduced brain penetration compared to selinexor (30-fold less).
Eltanexor (KPT-8602) inhibits viability of human AML cell lines in vitro with IC50 of 20−211 nM, more active than the first-generation XPO1 inhibitor, selinexor.
Eltanexor (KPT-8602) exhibits greater anti-leukemic efficacy against both leukemic blasts and LICs in AML patient-derived xenograft models, with no effect on normal hematopoietic stem and progenitor cell (HSPC) frequency.
