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.
Washington University School of Medicine, Saint Louis, Missouri, United States
Dana-Farber Cancer Institute, Boston, Massachusetts, United States
Mayo Clinic, Rochester, Minnesota, United States
Florida Cancer Specialists, Ft. Myers, Florida, United States
Hematology Oncology of the North Shore, Skokie, Illinois, United States
Holy Cross Hospital, Ft. Lauderdale, Florida, United States
Novartis Investigative Site, Wolverhampton, United Kingdom
UC San Diego Moores Cancer Center, La Jolla, California, United States
Johns Hopkins University/Sidney Kimmel Cancer Center, Baltimore, Maryland, United States
Boston Medical Center, Boston, Massachusetts, United States
Arizona Cancer Center, Tucson, Arizona, United States
The Western Pennsylvania Hospital, Pittsburgh, Pennsylvania, United States
University of Maryland School of Medicine - Marlene & Stewart Greenebaum Cancer Center, Baltimore, Maryland, United States
Dana Farber Cancer Institute, Boston, Massachusetts, United States
Keryx / AOI Pharmaceuticals Investigative Site, Dublin 7, Ireland
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