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. 2019 Apr;71(2):170–197. doi: 10.1124/pr.117.015370

TABLE 4.

Proteasome inhibitors in clinical testing

Inhibitor Class IC50 In Vitro Peptidase Activity
Half-Life Route Binding Reference
CT-L C-L T-L
nM min
Bortezomib Boronate 7.9 53 590 110 i.v./s.c. Slowly reversible Cauhan et al. (2005)
Carfilzomib Epoxyketone 6 2400 3600 <30 i.v. Irreversible Kuhn et al. (2007)
Ixazomib Boronate 3.4 31 3500 18 p.o. Reversible Cauhan et al. (2005), Kupperman et al. (2010)
Marizomib β-lactone 3.5 430 28 10–15 i.v. Irreversible Feling et al. (2003)
Oprozomib Epoxyketone 36 (β5) ND ND 30–90 p.o. Irreversible Zhou 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).