| Nature of inhibition |
Irreversible inhibition |
Reversible inhibition |
Reversible inhibition |
Irreversible inhibition |
Irreversible inhibition |
| Chemical structure |
Tetrapeptide epoxyketone |
Boronic acid |
Boronic acid derivative |
Salinosporamide |
Tripeptide epoxyketone |
| specificity |
Highly selective for chymotrypsin-like active site, β-5 |
Inhibits both chymotrypsin-like and caspase-like sites, β-5 and β-1 |
Preferentially inhibits chymotrypsin-like site, β-5 |
Inhibits all three subunits of the proteasome, β-5, β-1 and β-2 |
Highly selective for chymotrypsin-like active site, β-5 |
| Route of administration |
Intravenous |
Intravenous or subcutaneous |
Oral |
Intravenous |
Oral |
| Side effects/neuropathy risk |
Minimal peripheral neuropathy |
Risk of peripheral neuropathy |
Mild neuropathy and gastrointestinal side effects |
Peripheral neuropathy uncommon |
Gastrointestinal side effects, no neuropathy |
| Recommended dosing schedule |
20/27 mg m−2 On days 1, 2, 8, 9, 15 and 16 every 28 days |
0.7–1.3 mg m−2 Once weekly days 1, 8, 15 and 22 every 28 days |
4 mg Once weekly on days 1, 8 and 15 every 28 days |
0.5 mg m−2 Over 120 min days 1, 4, 8 and 11 of a 21-day cycle |
240/300 mg Per day twice a week, or 150/180 mg per day, 5 days in 2 weeks |
| US Food and Drug Administration approval status |
Approved |
Approved |
Approved |
Not approved |
Not approved |
