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.
Roswell Park Medical Center, Buffalo, New York, United States
University of Wisconsin, Madison, Wisconsin, United States
Hackensack University Medical Center, Hackensack, New Jersey, United States
Sparrow Regional Cancer Center, Lansing, Michigan, United States
University of California Davis Cancer Center, Sacramento, California, United States
University of California Davis Cancer Center, Sacramento, California, United States
Moffitt Cancer Center, Tampa, Florida, United States
Children's Oncology Group, Philadelphia, Pennsylvania, United States
Asan Medical Center, University of Ulsan College of Medicine, Seoul, Korea, Republic of
Asan Medical Cener, Seoul, Korea, Republic of
Massachusetts General Hospital, Boston, Massachusetts, United States
Dana-Farber Cancer Institute, Boston, Massachusetts, United States
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