Zetomipzomib (KZR-616) is a first-in-class inhibitor of immunoproteasome, dually inhibits immunoproteasome subunits LMP7 (IC50, 39/57 nM, hLMP7/mLMP7) and LMP2 (IC50, 131/179 nM, hLMP2/mLMP2).
Zetomipzomib (KZR-616) also potently inhibits MECL-1 subunit (IC50=623 nM) and constitutive proteasome β5 subunit (IC50=688 nM), and maintains LMP7 and LMP2 selective inhibition in MOLT-4 cells.
Zetomipzomib (KZR-616) exhibits potent cytokine expression inhibition and in vivo efficacy in an inflammatory disease model.
