Abstract
Bortezomib is the first-in-class proteasome inhibitor which has been used worldwide for the treatment of multiple myeloma and mantle cell lymphoma. Bortezomib is under evaluation as a single agent or in combination with other drugs for solid cancers and stem cell transplantation in clinical settings. However, adverse effects and drug resistance have been observed in patients, which is now emerging as a great challenge for the extended application of bortezomib. In this review, we will comprehensively discuss the development of bortezomib, the mechanism underlying its therapeutics, adverse effects and resistance. Second generation of bortezomib and its future directions will also be discussed.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Animals
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Antineoplastic Agents / adverse effects
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Antineoplastic Agents / pharmacology*
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Antineoplastic Agents / therapeutic use
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Boronic Acids / adverse effects
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Boronic Acids / pharmacology
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Boronic Acids / therapeutic use*
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Bortezomib
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Drug Design
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Drug Resistance, Neoplasm
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Humans
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Lymphoma, Mantle-Cell / drug therapy
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Lymphoma, Mantle-Cell / pathology
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Multiple Myeloma / drug therapy
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Multiple Myeloma / pathology
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Proteasome Endopeptidase Complex / drug effects
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Proteasome Endopeptidase Complex / metabolism
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Proteasome Inhibitors / adverse effects
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Proteasome Inhibitors / pharmacology
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Proteasome Inhibitors / therapeutic use*
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Pyrazines / adverse effects
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Pyrazines / pharmacology
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Pyrazines / therapeutic use*
Substances
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Antineoplastic Agents
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Boronic Acids
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Proteasome Inhibitors
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Pyrazines
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Bortezomib
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Proteasome Endopeptidase Complex