Ibrutinib: from bench side to clinical implications

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From: Medical Oncology(Vol. 32, Issue 9)
Publisher: Springer
Document Type: Report
Length: 278 words

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Byline: Davide Grisafi (1), Alessandra Maestro (1), Camilla Grumi (1), Ludovica Piazzoni (1), Giampaolo Tirone (1), Walter Fiore (1), Roberto Tessari (1), Valeria Gianardi (1), Milo Gatti (1), Francesca Tasca (1), Daniele Generali (1,2), Andrea Ravelli (3), Francesco Lanza (3), Francesco Scaglione (1) Keywords: Ibrutinib; Bruton's tyrosine kinase; Chronic lymphocytic leukemia; Follicular lymphoma; Mantle cell lymphoma; Non-Hodgkin lymphoma 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), Waldenstrom 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. Author Affiliation: (1) Department of Biotechnology and Translational Medicine, University of Milan, Milan, Italy (2) Molecular Therapy and Pharmacogemomic Unit, AO Istituti Ospitalieri di Cremona, Viale Concordia 1, 26100, Cremona, Italy (3) Hematology CTMO Unit, AO Istituti Ospitalieri di Cremona, Cremona, Italy Article History: Registration Date: 16/07/2015 Received Date: 07/07/2015 Accepted Date: 16/07/2015 Online Date: 30/07/2015

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Gale Document Number: GALE|A423693303