A novel proteasome inhibitor NPI-0052 as an anticancer therapy
Open Access
- 17 October 2006
- journal article
- review article
- Published by Springer Nature in British Journal of Cancer
- Vol. 95 (8) , 961-965
- https://doi.org/10.1038/sj.bjc.6603406
Abstract
Proteasome inhibitor Bortezomib/Velcade has emerged as an effective anticancer therapy for the treatment of relapsed and/or refractory multiple myeloma (MM), but prolonged treatment can be associated with toxicity and development of drug resistance. In this review, we discuss the recent discovery of a novel proteasome inhibitor, NPI-0052, that is distinct from Bortezomib in its chemical structure, mechanisms of action, and effects on proteasomal activities; most importantly, it overcomes resistance to conventional and Bortezomib therapies. In vivo studies using human MM xenografts shows that NPI-0052 is well tolerated, prolongs survival, and reduces tumour recurrence. These preclinical studies provided the basis for Phase-I clinical trial of NPI-0052 in relapsed/refractory MM patients.Keywords
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