Ixazomib (MLN2238) is a potent, selective, orally bioavailable proteasome inhibitor with IC50 of 3.4 nM.
Ixazomib binds to and inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with Ki of 0.93 nM, weakly inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites (IC50 of 31 and 3,500 n M).
Ixazomib inhibits growth and induces apoptosis in MM cells.
Ixazomib shows improved antitumor activity in models of lymphoma compared with bortezomib.
