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.
M D Anderson Cancer Center, Houston, Texas, United States
City of Hope, Duarte, California, United States
Mayo Clinic, Rochester, Minnesota, United States
Gynecologic Oncology Group, Philadelphia, Pennsylvania, United States
Cancer Care Ontario-Hamilton Regional Cancer Centre, Hamilton, Ontario, Canada
Cancer Care Ontario-London Regional Cancer Centre, London, Ontario, Canada
Ottawa Regional Cancer Centre, Ottawa, Ontario, Canada
Abramson Cancer Center of The University of Pennsylvania, Philadelphia, Pennsylvania, United States
North Central Cancer Treatment Group, Rochester, Minnesota, United States
Kaiser Permanente Oncology Clinical Trials, Vallejo, California, United States
Texas Oncology at Medical City Dallas Hospital, Dallas, Texas, United States
Western Pennsylvania Hospital, Dept. of Human Oncology, Pittsburgh, Pennsylvania, United States
National Institutes of Health Clinical Center, 9000 Rockville Pike, Bethesda, Maryland, United States
National Institutes of Health Clinical Center, 9000 Rockville Pike, Bethesda, Maryland, United States
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