Selinexor is a first-in-class SINE compound targeting XPO1, a key nuclear export protein. It is the first and only SINE compound approved by the FDA. Selinexor is approved for use in the treatment of two hematologic malignancies, namely multiple myeloma (MM) and DLBCL and is the only single-agent, orally-available therapy approved for the treatment of patients with R/R DLBCL. In addition to R/R MM and R/R DLBCL, promising research and data highlight the anti-cancer potential of selinexor for a wide range of cancer types, including both solid tumors and hematological malignancies.
Selinexor functions by selectively binding to residue cysteine 528 (Cys528) in the cargo-binding groove of XPO1, inhibiting cargo binding and exporting by XPO1. Through inhibition of XPO1,selinexor blocks the nuclear export of tumor suppressors, growth regulators and anti-inflammatory proteins, leading to the accumulation of these proteins in the nucleus and enhancing anti-cancer activity in the cell.
We are in partnership with Karyopharm Therapeutics for clinical development, manufacturing and commercialization of selinexor in Greater China (mainland China, Hong Kong, Taiwan, Macau), Australia, New Zealand, South Korea, and the ASEAN countries. Antengene is conducting multiple clinical studies (including two registrational studies) of selinexor in China.