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.
Henry Ford hospital, Detroit, Michigan, United States
State Key Laboratory of Experimental Haematology, Department of Paediatric Haematology, Institute of Haematology and Blood Diseases Hospital, Chinese Academy of Medical Sciences and Peking Union Medical College, Tanjin, Tianjin, China
GSK Investigational Site, Tokyo, Japan
Mayo Clinic, Jacksonville, Florida, United States
Mayo Clinic in Rochester, Rochester, Minnesota, United States
M D Anderson Cancer Center, Houston, Texas, United States
National University Hospital, Singapore, Singapore
Hospital de la Santa Creu i Sant Pau, Barcelona, Spain
Hospital Universitario de Cruces, Bilbao, Spain
Complejo Hospitalario Regional Reina Sofía, Córdoba, Spain
SBMU, Tehran, Iran, Islamic Republic of
University Of Chicago Medicine Comprehensive Cancer Center, Chicago, Illinois, United States
Indiana University/Melvin and Bren Simon Cancer Center, Indianapolis, Indiana, United States
Aurora Cancer Care-Milwaukee West, Wauwatosa, Wisconsin, United States
Mayo Clinic, Rochester, Minnesota, United States
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