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, Hokkaido, Japan
GSK Investigation Site, Fukushima City, Fukushima-Ken, Japan
Sun Yat-Sen University Cancer Center, Guangzhou, Guangdong, China
GSK Investigational Site, Zhengzhou, China
GSK Investigational Site, Yokohama, Japan
Taipei Medical University Hospital, Taipei, Taiwan
Fuxing Hospital affiliated to Capital Medical University, Beijing, Beijing, China
Peking University People's Hospital, Beijing, Beijing, China
Hosp. Univ. 12 de Octubre, Madrid, Spain
City of Hope, Duarte, California, United States
University of California San Francisco, San Francisco, California, United States
First Affiliated Hospital of Zhejiang University Schlool of Medicine, Hangzhou, Zhejiang, China
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