TABLE 4

Proteasome inhibitors in clinical testing

InhibitorClassIC50 In Vitro Peptidase ActivityHalf-LifeRouteBindingReference
CT-LC-LT-L
nMmin
BortezomibBoronate7.953590110i.v./s.c.Slowly reversibleCauhan et al. (2005)
CarfilzomibEpoxyketone624003600<30i.v.IrreversibleKuhn et al. (2007)
IxazomibBoronate3.431350018p.o.ReversibleCauhan et al. (2005), Kupperman et al. (2010)
Marizomibβ-lactone3.54302810–15i.v.IrreversibleFeling et al. (2003)
OprozomibEpoxyketone36 (β5) NDND30–90p.o.IrreversibleZhou et al. (2009), Roccaro et al. (2010)
82 (β5i)
  • C-L, caspase-like activity (β1); CT-L, chymotrypsin-like activity (β5); ND, not determined; T-L, trypsin-like activity (β2).