What is the mechanism of action of bortezomib?

What is the mechanism of action of bortezomib?

Mechanism of Action Bortezomib is a selective inhibitor of the 26S proteasome, preventing the activation of NF-κB. It induces apoptosis of rapidly dividing, metabolically active cells with extensive protein synthesis.

Why does bortezomib work in multiple myeloma?

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 does bortezomib inhibit the proteasome?

The boronic acid group in bortezomib can bind and form a complex with the active site of threonine hydroxyl group in the β5-subunit and block the chymotrypsin-like activity of the proteasome (Fig. 2), which is responsible for its cell-death inducing capabilities [60–61].

What kind of drug is bortezomib?

Bortezomib is in a class of medications called antineoplastic agents. It works by killing cancer cells.

Is bortezomib a biologic?

Some intracellular peptides have been shown to be biologically active, and so the effect of bortezomib on the levels of intracellular peptides may contribute to the biological and/or side effects of the drug.

Is bortezomib an immunosuppressant?

Bortezomib has been shown to exert potent immunomodulatory effects, including the induction of apoptosis of dendritic cells, decrease in T cell costimulatory molecules and in inflammatory cytokine production, selective apoptosis of activated effector T cells, increase in effector function, and inhibition of NF-κB ( …

Why is bortezomib given?

Generic Name: bortezomib This medication is used to treat certain types of cancer (such as multiple myeloma, mantle cell lymphoma). It works by slowing or stopping the growth of cancer cells.

Is bortezomib chemotherapy or immunotherapy?

Bortezomib was the first proteasome inhibitor approved to treat patients who had already been treated with two other types of chemotherapy and whose cancer has still progressed after the most recent therapy.

Bortezomib is a Proteasome Inhibitor. The mechanism of action of bortezomib is as a Proteasome Inhibitor. Bortezomib is a proteasome inhibitor and antineoplastic agent that is used in treatment of refractory multiple myeloma and certain lymphomas.

How does bortezomib work on the 26S proteasome?

Bortezomib reversibly inhibits the 26S proteasome, a large protease complex that degrades ubiquinated proteins. By blocking the targeted proteolysis normally performed by the proteasome, bortezomib disrupts various cell signaling pathways, leading to cell cycle arrest, apoptosis, and inhibition of angiogenesis.

When was bortezomib approved to treat multiple myeloma?

Bortezomib showed remarkable clinical activity in patients with multiple myeloma and was rapidly approved by the FDA in 2003 to treat relapsed and refractory multiple myeloma.

Are there any phase 2 trials for bortezomib?

A randomized phase 2 study of erlotinib alone and in combination with bortezomib in previously treated advanced non-small cell lung cancer. J Thorac Oncol 2009;4:1002–9. A randomized phase II study of bortezomib and pemetrexed, in combination or alone, in patients with previously treated advanced non-small-cell lung cancer.

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