PIPELINE ATG-008 (CC-223) ATG-010 (Selinexor) ATG-016 (Eltanexor) ATG-527 (Verdinexor) ATG-019 (KPT-9274) DISCOVERY DEVELOPMENT MANUFACTURING

ATG-010 (Selinexor)

Selinexor (ATG-010) is a first-in-class Selective Inhibitor of Nuclear Export (SINE) compound, being evaluated in multiple late-stage clinical trials in patients with relapsed and/or refractory hematological and solid tumor malignancies. We are in partnership with Karyopharm Therapeutics for clinical development, manufacturing and commercialization of selinexor in mainland China and Macau. Selinexor has been studied in over 40 clinical trials in over 10 cancer types, with more than 2,400 patients treated.

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.

Selinexor has received Fast Track designation from the U.S. Food and Drug Administration for the treatment of patients with penta-refractory multiple myeloma. We plan to initiate registrational studies of selinexor in China in the second half of 2018.