Table 1 Key features of different... | American Society of Hematology

Table 1

Key features of different proteasome inhibitors^8-10

Characteristic	Bortezomib	MLN9708	Carfilzomib	Marizomib
Active moiety	Boronate	Boronate	Epoxyketone	β-lactone
Subunits inhibited
Constitutive proteasome	β5, β1	β5	β5	β5 and β2
Immunoproteasome	β5i	NR	β5i	NR
IC₅₀, nM
Chymotrypsin	2.4-7.9	3.4	6	3.5
Trypsin	590-4200	3500	3600	28
Caspase	24-74	31	2400	430
IC₅₀ against RPMI 8226 MM cell line, nM	5.7	NR	5	9.1
Binding kinetics	Slowly reversible	Reversible	Irreversible	Irreversible
Half-life, minutes	110	18	< 30	< 10-15
Route of administration	IV/SC	Oral/IV	IV	IV

Characteristic	Bortezomib	MLN9708	Carfilzomib	Marizomib
Active moiety	Boronate	Boronate	Epoxyketone	β-lactone
Subunits inhibited
Constitutive proteasome	β5, β1	β5	β5	β5 and β2
Immunoproteasome	β5i	NR	β5i	NR
IC₅₀, nM
Chymotrypsin	2.4-7.9	3.4	6	3.5
Trypsin	590-4200	3500	3600	28
Caspase	24-74	31	2400	430
IC₅₀ against RPMI 8226 MM cell line, nM	5.7	NR	5	9.1
Binding kinetics	Slowly reversible	Reversible	Irreversible	Irreversible
Half-life, minutes	110	18	< 30	< 10-15
Route of administration	IV/SC	Oral/IV	IV	IV

IC₅₀ indicates half-maximal inhibitory concentration; and NR, not reported.