Abstract
Mantle cell lymphoma (MCL) is a rare and aggressive form of non-Hodgkin lymphoma. Ibrutinib is a first-in-class, oral inhibitor of Bruton's tyrosine kinase which acts by downstream inhibition of the B-cell receptor. Early clinical trials have demonstrated excellent tolerability and a modest side-effect profile in relapsed/refractory MCL. Although the majority of disease responses are partial, efficacy data are impressive with more than two-thirds of patients demonstrating a durable response. This article focuses on all aspects of ibrutinib in the context of MCL, including a summary of the basic pharmacology and pharmacokinetics; a review of the safety and efficacy data published to date and a discussion of the future implications in MCL.
Keywords:
Bruton's tyrosine kinase; ibrutinib; mantle cell lymphoma.
MeSH terms
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Adenine / analogs & derivatives
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Agammaglobulinaemia Tyrosine Kinase
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Animals
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology
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Antineoplastic Agents / therapeutic use*
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Antineoplastic Combined Chemotherapy Protocols / therapeutic use
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Clinical Trials as Topic
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Drug Evaluation, Preclinical
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Drug Resistance, Neoplasm
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Humans
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Lymphoma, Mantle-Cell / drug therapy*
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Lymphoma, Mantle-Cell / metabolism
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Lymphoma, Mantle-Cell / pathology
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Piperidines
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Protein Kinase Inhibitors / chemistry
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Protein Kinase Inhibitors / pharmacology
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Protein Kinase Inhibitors / therapeutic use*
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Protein-Tyrosine Kinases / antagonists & inhibitors
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Pyrazoles / chemistry
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Pyrazoles / pharmacology
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Pyrazoles / therapeutic use*
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Pyrimidines / chemistry
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Pyrimidines / pharmacology
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Pyrimidines / therapeutic use*
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Receptors, Antigen, B-Cell / metabolism
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Recurrence
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Treatment Outcome
Substances
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Antineoplastic Agents
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Piperidines
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Protein Kinase Inhibitors
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Pyrazoles
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Pyrimidines
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Receptors, Antigen, B-Cell
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ibrutinib
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Protein-Tyrosine Kinases
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Agammaglobulinaemia Tyrosine Kinase
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Adenine