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.
GSK Investigational Site, London, United Kingdom
Zhejiang Cancer Hospital, Hangzhou, Zhejiang, China
Icahn School of Medicine at Mount Sinai, New York, New York, United States
Ludwig-Maximilians-Universität München, Klinikum Großhadern, München, Bayern, Germany
Universitätsklinikum Würzburg, Würzburg, Bayern, Germany
Medizinische Hochschule Hannover, Hannover, Niedersachen, Germany
Local Institution - 110, Winston-Salem, North Carolina, United States
Local Institution - 802, Brno, Czechia
Local Institution - 801, Ostrava-Poruba, Czechia
Peking Union Medical College Hospital, Beijing, Beijing, China
American Oncology Partners of Maryland, PA, Bethesda, Maryland, United States
MD Anderson Cancer Center, Houston, Texas, United States
Pacific Cancer Care, Monterey, California, United States
New York University School of Medicine, New York, New York, United States
Emory University Hospital/Winship Cancer Institute, Atlanta, Georgia, United States
OHSU Knight Cancer Institute, Portland, Oregon, United States
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