Table 1.
Proteasome inhibitors used in clinical practice or in clinical trials for the treatment of multiple myeloma
| Compound | Chemical | Binding | Adm | Status | Proteasome inhibition |
|---|---|---|---|---|---|
| Bortezomib (PS-341) | Boronate | Reversible | IV/SC | FDA approved | β5/β5i > β1/β1i > β2i |
| CEP-18770 | Boronate | Reversible | IV/oral | Phase 1–2 | β5/β5i > β1/β1i |
| MLN-9708 | Boronate | Reversible | Oral/IV | Phase 1–2 | β5/β5i > β1/β1i |
| Carfilzomib (PR-171) | Epoxyketone | Irreversible | IV | FDA approved | β5/β5i > > β2i~β1i |
| Oprozomib (ONX-0912) | Epoxyketone | Irreversible | Oral/IV | Phase 1 | β5/β5i |
| Marizomib (NPI-0052) | β-lactone | Irreversible | IV/oral | Phase 1 | β5/β5i > β2/β2i > β1/β1i |
Note: © 2012, Elsevier. Adapted with permission from Kisselev AF, van der Linden WA, Overkleeft HS. Proteasome inhibitors: an expanding army attacking a unique target. Chem Biol. 2012;19(1):99–115.34
Abbreviations: Adm, administration; IV, intravenous; SC, subcutaneous.