title: Dissecting bortezomib: development, application, adverse effects and future direction.
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.
authors.affiliation: Cyrus Tang Hematology Center, Jiangsu Institute of Hematology, The First Affiliated Hospital, Soochow University, Suzhou, China.
authors.forename: Biyin
authors.initials: B
authors.lastname: Cao
authors.forename: Jie
authors.initials: J
authors.lastname: Li
authors.forename: Xinliang
authors.initials: X
authors.lastname: Mao
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use; D001897:Boronic Acids / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D000069286:Bortezomib; D015195:Drug Design; D019008:Drug Resistance, Neoplasm; D006801:Humans; D020522:Lymphoma, Mantle-Cell / Q000188:drug therapy / Q000473:pathology; D009101:Multiple Myeloma / Q000188:drug therapy / Q000473:pathology; D046988:Proteasome Endopeptidase Complex / Q000187:drug effects / Q000378:metabolism; D061988:Proteasome Inhibitors / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D011719:Pyrazines / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*
chemical_list: D000970:Antineoplastic Agents; D001897:Boronic Acids; D061988:Proteasome Inhibitors; D011719:Pyrazines; D000069286:Bortezomib; D046988:Proteasome Endopeptidase Complex