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.
Shanghai Jiaotong University School of Medicine, Shanghai, Shanghai, China
Sun Yat-sen University Cancer Center; State Key Laboratory of Oncology in South China,, Guangzhou, Guangdong, China
Guangdong Provincial Peoples Hospital, Guangzhou, Guangdong, China
Sun Yat-sen Memorial Hospital, Sun Yat-sen University, Guangzhou, Guangdong, China
Mayo Clinic in Rochester, Rochester, Minnesota, United States
Ruijin Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai, Shanghai, China
M D Anderson Cancer Center, Houston, Texas, United States
Northwell Health, New Hyde Park, New York, United States
Princess Margaret Hospital, Toronto, Ontario, Canada
London Health Sciences Centre, London, Ontario, Canada
University of Arkansas, Little Rock, Arkansas, United States
City of Hope, Duarte, California, United States
UC San Diego Health Moores Cancer Center, San Diego, California, United States
City of Hope, Duarte, California, United States
Smilow Cancer Hospital/Yale Cancer Center, New Haven, Connecticut, United States
Moffitt Cancer Center, Tampa, Florida, United States
Peking Union Medical College Hospital, Beijing, China
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