Novel BTK Inhibitors and Combos May Hold the Key to B-Cell Malignancies

Jane de Lartigue, PhD
Published: Thursday, May 21, 2015
Dr. Jennifer R. Brown

Jennifer R. Brown, MD, PhD

The Bruton tyrosine kinase (BTK)-targeting drug ibrutinib has demonstrated substantial success as a single agent in advancing the treatment of B-cell malignancies, and a number of novel BTK-targeting agents are now hot on its heels. Yet the ultimate development of resistance to these inhibitors limits long-term curative potential.

Table 1. BTK-Targeting Agents in Development

*Trial is ongoing but not recruiting participants.

ABC indicates activated B cell; BTK, Bruton tyrosine kinase; CLL, chronic lymphocytic leukemia; DLBCL, diffuse large b-cell lymphoma; FL, follicular lymphoma; MCL, mantle cell lymphoma; NHL, non-Hodgkin lymphoma; PI3K, phosphatidylinositol 3-kinase; PLL, prolymphocytic leukemia; SLL, small lymphocytic leukemia.

Despite the impressive clinical efficacy and tolerability of BTK-targeted agents, further research is required to identify optimal dosing schedules and patients who are most likely to benefit from this type of therapy. Furthermore, BTK inhibitor monotherapy is not curative; approximately one-third of patients do not respond to ibrutinib therapy at all, and the majority of those who do ultimately develop resistance.

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TitleExpiration DateCME Credits
Community Practice Connections™: 22nd Annual International Congress on Hematologic Malignancies®: Focus on Leukemias, Lymphomas and MyelomaMay 30, 20192.0
Online Medical Crossfire®: 5th Annual Miami Lung Cancer ConferenceMay 30, 20196.5
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