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.
Wake Forest Baptist Health, Winston-Salem, North Carolina, United States
Pacific Oncology/Hematology Associates, Encinitas, California, United States
Seoul National University Hospital, Seoul, Korea, Republic of
Fakultní nemocnice Brno, Brno, Czechia
Fakultní nemocnice Hradec Králové, Nový Hradec Králové, Czechia
Fakultní nemocnice Ostrava, Ostrava-Poruba, Czechia
Tianjin Medical University General Hospital, Tianjin, Tianjin, China
Emory University/Winship Cancer Institute, Atlanta, Georgia, United States
Shuhua Yi, Tianjin, China
Stanford University Medical Center, Stanford, California, United States
University of Washington School of Medicine in St. Louis, Saint Louis, Missouri, United States
Washington University School of Medicine, Saint Louis, Missouri, United States
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