title: Ibrutinib: from bench side to clinical implications.
abstract: The activation of the B cell receptor (BCR) is nowadays known to play a primary role in the etiopathogenesis of a multitude of B cell malignancies, being one of the main factors responsible for the enhanced proliferation and survival of transformed cells. Thanks to the characterization and continuous discovery of the pathways driving B cell proliferation in consequence to BCR activation, it has been possible to develop a small molecule inhibitor specifically antagonizing the Bruton's tyrosine kinase (BTK), an enzyme located in an early strategic position within the whole pathway. Ibrutinib, formerly PCI-32765, is a first in class, potent, specific, irreversible and relatively safe BTK inhibitor, demonstrating so far an impressive efficacy in the treatment of chronic lymphocytic leukemia, diffuse large B cell lymphoma, follicular lymphoma, mantle cell lymphoma (MCL), Waldenström macroglobulinemia and multiple myeloma. This review will summarize the most important pharmacological evidences available as of today and will take in consideration the latest findings regarding the mechanism of action of ibrutinib.
authors.affiliation: Department of Biotechnology and Translational Medicine, University of Milan, Milan, Italy.
authors.forename: Davide
authors.initials: D
authors.lastname: Grisafi
authors.forename: Alessandra
authors.initials: A
authors.lastname: Maestro
authors.forename: Camilla
authors.initials: C
authors.lastname: Grumi
authors.forename: Ludovica
authors.initials: L
authors.lastname: Piazzoni
authors.forename: Giampaolo
authors.initials: G
authors.lastname: Tirone
authors.forename: Walter
authors.initials: W
authors.lastname: Fiore
authors.forename: Roberto
authors.initials: R
authors.lastname: Tessari
authors.forename: Valeria
authors.initials: V
authors.lastname: Gianardi
authors.forename: Milo
authors.initials: M
authors.lastname: Gatti
authors.forename: Francesca
authors.initials: F
authors.lastname: Tasca
authors.forename: Daniele
authors.initials: D
authors.lastname: Generali
authors.forename: Andrea
authors.initials: A
authors.lastname: Ravelli
authors.forename: Francesco
authors.initials: F
authors.lastname: Lanza
authors.forename: Francesco
authors.initials: F
authors.lastname: Scaglione
mesh_terms: D000225:Adenine / Q000031:analogs & derivatives; D000970:Antineoplastic Agents; D035843:Biomedical Research; D006801:Humans; D015451:Leukemia, Lymphocytic, Chronic, B-Cell / Q000188:drug therapy; D008223:Lymphoma / Q000188:drug therapy; D010880:Piperidines; D011720:Pyrazoles; D011743:Pyrimidines
chemical_list: D000970:Antineoplastic Agents; D010880:Piperidines; D011720:Pyrazoles; D011743:Pyrimidines; C551803:ibrutinib; D000225:Adenine