Abstract
Bortezomib was the first proteasome inhibitor (PI) discovered and demonstrated great efficacy in myeloma, both in vitro and in patients. However, still many patients ultimately relapse and there is the need for novel therapies. A second generation of PI have been discovered, potentially more effective ands some also orally administered. Carfilzomib is an irreversible proteasome inhibitor that showed great efficacy in clinical studies. Ixazomib is an oral compound that has been introduced recently in the therapeutic spectrum. Novel agents such as Marizomib seem promising in the fact that can also pass through the blood brain barrier and maybe effective also in CNS muyeloma. This review focus on all proteasome inhibitors available in clinics and the new ones coming soon.
Keywords: Myeloma, bortezomib, new proteasome inhibitors, carfilzomib, oprozomib.
Graphical Abstract
Anti-Cancer Agents in Medicinal Chemistry
Title:Second Generation Proteasome Inhibitors in Multiple Myeloma
Volume: 17 Issue: 7
Author(s): Alessandro Gozzetti*, Giulia Papini, Veronica Candi, Corrado Zuanelli Brambilla, Santina Sirianni and Monica Bocchia
Affiliation:
- Hematology, Policlinico “Santa Maria alle Scotte”, Viale Bracci 16, 53100 Siena,Italy
Keywords: Myeloma, bortezomib, new proteasome inhibitors, carfilzomib, oprozomib.
Abstract: Bortezomib was the first proteasome inhibitor (PI) discovered and demonstrated great efficacy in myeloma, both in vitro and in patients. However, still many patients ultimately relapse and there is the need for novel therapies. A second generation of PI have been discovered, potentially more effective ands some also orally administered. Carfilzomib is an irreversible proteasome inhibitor that showed great efficacy in clinical studies. Ixazomib is an oral compound that has been introduced recently in the therapeutic spectrum. Novel agents such as Marizomib seem promising in the fact that can also pass through the blood brain barrier and maybe effective also in CNS muyeloma. This review focus on all proteasome inhibitors available in clinics and the new ones coming soon.
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Cite this article as:
Gozzetti Alessandro*, Papini Giulia, Candi Veronica, Brambilla Zuanelli Corrado, Sirianni Santina and Bocchia Monica, Second Generation Proteasome Inhibitors in Multiple Myeloma, Anti-Cancer Agents in Medicinal Chemistry 2017; 17 (7) . https://dx.doi.org/10.2174/1871520616666160902101622
DOI https://dx.doi.org/10.2174/1871520616666160902101622 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
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