Ibrutinib

Ibrutinib in the glossary for Waldenström's macroglobulinemia

A small molecule inhibitor of Bruton's tyrosine kinase

Ibrutinib is an orally bioavailable, first generation, small-molecule inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity. Upon oral administration, ibrutinib binds to and irreversibly inhibits BTK activity, thereby preventing both B-cell activation and B-cell-mediated signalling. This leads to an inhibition of the growth of malignant B cells that overexpress BTK. Ibrutinib is used to treat patients with chronic graft-versus-host (cGVHD) disease, chronic lymphocytic leukemia (CLL), mantle cell lymphoma (MCL), marginal zone lymphoma (MZL) and Waldenström's macroglobulinemia. It was approved for Waldenström's macroglobulinemia in 2015. In August 2018, ibrutinib in combination with rituximab was approved in the United States for the treatment of adults with Waldenström's macroglobulinemia (Ibrutinib SmPC). Ibrutinib is authorized for use in the EU (ibrutinib SmPC).