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.
Novartis Investigative Site, Tokushima, Japan
Site 2, Nashville, Tennessee, United States
Colorado Blood Cancer Institute, Denver, Colorado, United States
Oncology Hematology Care, Cincinnati, Ohio, United States
Tennessee Oncology, Chattanooga, Tennessee, United States
Thomas Jefferson University, Philadelphia, Pennsylvania, United States
Gustave Roussy, Villejuif, Val de Marne, France
University of Florida College of Medicine (Shands), Gainesville, Florida, United States
Virginia Commonwealth University MCV Hospitals, Richmond, Virginia, United States
University of North Carolina Hospital at Chapel Hill, Chapel Hill, North Carolina, United States
Hopital Necker Enfants-malades, Paris, France
Universitaetsspital-Basel, Basel, Switzerland
Istituto Oncologico Svizzera Italiana IOSI, Bellinzona, Switzerland
Hopital Fribourgeois, Fribourg, Switzerland
Connecticut Children's Hospital, Hartford, Connecticut, United States
Arkansas Children's Hospital, Little Rock, Arkansas, United States
Helen DeVos Children's Hospital, Grand Rapids, Michigan, United States
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