Bortezomib is a dipeptide boronic acid derivative and proteasome inhibitor used to treat multiple myeloma and mantle cell lymphoma. The 26S proteasome is a protein complex that degrades ubiquitinated proteins in the ubiquitin-proteasome pathway: reversible inhibition of the 26S proteasome, leading to cell cycle arrest and apoptosis of cancer cells, is thought to be the main mechanism of action of bortezomib. However, multiple mechanisms may be involved in the anticancer activity of bortezomib.
Bortezomib was first synthesized in 1995. In May 2003, bortezomib became the first anticancer proteasome inhibitor that was approved by the FDA under the trade name VELCADE. Phase I, II, III, and IV clinical trials are undergoing to investigate the therapeutic efficacy of bortezomib in leukemia, myasthenia gravis, systemic lupus erythematosus, rheumatoid arthritis, and solid tumours.
Bortezomib is indicated for the treatment of adults with multiple myeloma or mantle cell lymphoma.
Masonic Cancer Center, University of Minnesota, Minneapolis, Minnesota, United States
Dana-Farber Cancer Institute, Boston, Massachusetts, United States
Mater Misericordiae University Hospital, Dublin, Ireland
Leeds Cancer Centre at St. James's University Hospital, Leeds, England, United Kingdom
Adelaide and Meath Hospital, Dublin Incorporating the National Children's Hospital, Dublin, Ireland
UT MD Anderson Cancer Center, Houston, Texas, United States
Emory University Winship Cancer Institute, Atlanta, Georgia, United States
Fred Hutchinson Cancer Research Center/University of Washington Cancer Consortium, Seattle, Washington, United States
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