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.
University of Wisconsin Hospital and Clinics, Madison, Wisconsin, United States
Warren Grant Magnuson Clinical Center - NCI Clinical Trials Referral Office, Bethesda, Maryland, United States
Tennessee Oncology, PLLC, Nashville, Tennessee, United States
Florida Cancer Specialists, Fort Myers, Florida, United States
Jonsson Comprehensive Cancer Center at UCLA, Los Angeles, California, United States
H. Lee Moffitt Cancer Center, Tampa, Florida, United States
Winship Cancer Center, Atlanta, Georgia, United States
Beth Israel Deaconess Medical Center, Boston, Massachusetts, United States
Memorial Sloan-Kettering Cancer Center, New York, New York, United States
Massachusetts General Hospital, Boston, Massachusetts, United States
Emory Winship Cancer Institute, Atlanta, Georgia, United States
Weill Medical College of Cornell University, New York, New York, United States
University of Cologne, Cologne, NRW, Germany
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