Second Generation Proteasome Inhibitors in Multiple Myeloma.
Bortezomib was the first proteasome inhibitor (PI) discovered and demonstrated great efficacy in myeloma, both in vitro and in patients. However, still many patients ultimately relapse and there is the need for novel therapies. A second generation of PI have been discovered, potentially more effective ands some also orally administered. Carfilzomib is an irreversible proteasome inhibitor that showed great efficacy in clinical studies. Ixazomib is an oral compound that has been introduced recently in the therapeutic spectrum. Novel agents such as Marizomib seem promising in the fact that can also pass through the blood brain barrier and maybe effective also in CNS muyeloma. This review focus on all proteasome inhibitors available in clinics and the new ones coming soon.
Hematology, Policlinico "Santa Maria alle Scotte", Viale Bracci 16, 53100 Siena, Italy.
Alessandro
A
Gozzetti
Hematology, Azienda Ospedaliera Universitaria Senese, Policlinico "Santa Maria alle Scotte", Siena, Italy.
Giulia
G
Papini
Hematology, Azienda Ospedaliera Universitaria Senese, Policlinico "Santa Maria alle Scotte", Siena, Italy.
Veronica
V
Candi
Hematology, Azienda Ospedaliera Universitaria Senese, Policlinico "Santa Maria alle Scotte", Siena, Italy.
Corrado Zuanelli
CZ
Brambilla
Hematology, Azienda Ospedaliera Universitaria Senese, Policlinico "Santa Maria alle Scotte", Siena, Italy.
Santina
S
Sirianni
Hematology, Azienda Ospedaliera Universitaria Senese, Policlinico "Santa Maria alle Scotte", Siena, Italy.
Monica
M
Bocchia
D000818:Animals; D001897:Boronic Acids / Q000494:pharmacology / Q000627:therapeutic use; D000069286:Bortezomib / Q000494:pharmacology / Q000627:therapeutic use; D016543:Central Nervous System Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D055808:Drug Discovery; D006801:Humans; D007783:Lactones / Q000494:pharmacology / Q000627:therapeutic use; D009101:Multiple Myeloma / Q000188:drug therapy* / Q000378:metabolism; D009364:Neoplasm Recurrence, Local / Q000188:drug therapy; D009842:Oligopeptides / Q000494:pharmacology / Q000627:therapeutic use; D061988:Proteasome Inhibitors / Q000494:pharmacology / Q000627:therapeutic use*; D011758:Pyrroles / Q000494:pharmacology / Q000627:therapeutic use; D013912:Threonine / Q000031:analogs & derivatives / Q000494:pharmacology / Q000627:therapeutic use
D001897:Boronic Acids; D007783:Lactones; C554738:ONX 0912; D009842:Oligopeptides; D061988:Proteasome Inhibitors; D011758:Pyrroles; D013912:Threonine; D000069286:Bortezomib; C527966:delanzomib; C475865:marizomib; C524865:carfilzomib
Myeloma; bortezomib; carfilzomib; new proteasome inhibitors; oprozomib