What is proteasome inhibitor bortezomib?
The proteasome inhibitor, bortezomib, a boronic dipeptide which reversibly inhibit the chymotrypsin-like activity at the β5-subunit of proteasome (PSMB5), has marked efficacy against multiple myeloma and several non-Hodgkin’s lymphoma subtypes, and has a potential therapeutic role against other malignancy diseases.
What is the role of bortezomib?
Bortezomib is a type of treatment for myeloma called a proteasome inhibitor. Proteasomes are enzymes found in all cells and play an important role in cell function and growth. Cancer cells are more sensitive to the effects of bortezomib, causing cancer cells to die or not grow any further.
How is bortezomib excreted?
The drug is metabolized by the CYP3A4 and CYP2C19 enzymes in the liver. The metabolites are inactive and are excreted by the kidney.
What does a proteasome inhibitor do?
Proteasome inhibitors are a type of drug that prevents proteasomes, the garbage disposal system of the cell, from chewing up excess proteins. The proteins build up and kill the myeloma cells.
Is bortezomib a chemotherapy drug?
Bortezomib is a type of cancer treatment drug called a proteasome inhibitor. Proteasomes are in cells. They help to break down proteins that the cell doesn’t need. Bortezomib blocks the proteasomes so the proteins build up inside the cell.
How often is bortezomib given?
VELCADE is administered twice weekly for two weeks (Days 1, 4, 8, and 11) followed by a ten day rest period on Days 12 to 21. For patients with a response first documented at cycle 6, two additional VcR-CAP cycles are recommended. At least 72 hours should elapse between consecutive doses of VELCADE.
How long is bortezomib in system?
Bortezomib is rapidly distributed into tissues after administration of a single dose, with an initial plasma distribution half-life of less than 10 minutes, followed by a terminal elimination half-life of more than 40 hours.
What are the most common clinical toxicities of proteasome inhibitors?
The first-generation proteasome inhibitor, bortezomib, induces significant gastrointestinal side effects including nausea, vomiting, diarrhoea, and constipation, occurring in up to 84% of patients.
Are proteasome inhibitors chemo?
The success of bortezomib has shown that proteasome inhibitors are sufficiently safe for clinical application as chemotherapeutic drugs [24], [25]. Inhibitors against the 20S proteolytic core of the proteasome have been the most extensively investigated.