Eltanexor (ATG-016) is a second-generation Selective Inhibitor of Nuclear Export (SINE) compound. The agent is currently in Phase 1/2 clinical studies for the treatment of hematological and solid tumor malignancies.
SINE compounds inhibit nuclear export through covalent binding to cysteine 528 (Cys528) in the cargo-binding pocket of Exportin 1 (XPO1/CRM1) and promote cancer cell death through apoptosis. The XPO1 inhibitors block the nuclear export of tumor suppressor proteins and other growth regulatory proteins, leading to accumulation of these proteins in the nucleus and enhancing their anti-cancer activity through apoptosis.
We are in partnership with Karyopharm Therapeutics for clinical development, manufacturing and commercialization of eltanexor in mainland China and Macau. We expect to initiate Phase 2 clinical trials in both hematological malignancies and solid tumors in 2018.