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.
Schwarzwald-Baar Klinikum, Klinik für Innere Medizin II, Villingen-Schwenningen, Germany
Rems-Murr-Klinikum gGmbH Winnenden, Winnenden, Germany
Studienzentrum Aschaffenburg, Aschaffenburg, Germany
Boston Medical Center, Boston, Massachusetts, United States
Children's National Medical Center, Washington, District of Columbia, United States
Hospital Universitario 12 de Octubre, Madrid, Spain
University Medical Center Groningen, Groningen, Netherlands
Dana Farber Cancer Institute, Boston, Massachusetts, United States
Virginia Piper Cancer Institute, Coon Rapids, Minnesota, United States
Massachusetts General Hosptial, Boston, Massachusetts, United States
Emory University, Atlanta, Georgia, United States
University of Texas /MD Anderson CRC, Houston, Texas, United States
City of Hope National Medical Center, Duarte, California, United States
Kent & Canterbury Hospital, Canterbury, United Kingdom
Royal Liverpool Hospital, Liverpool, United Kingdom
Heartlands Hospitals, Birmingham, United Kingdom
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