Ibrutinib for mantle cell lymphoma.
Plymouth, United Kingdom. In Future Oncol, Feb 2016
Ibrutinib is a first-in-class, oral inhibitor of Bruton's tyrosine kinase which acts by downstream inhibition of the B-cell receptor.
Mantle Cell Lymphoma.
Australia. In J Clin Oncol, Feb 2016
In particular, agents recently approved by the Food and Drug Administration include the proteasome inhibitor bortezomib, immunomodulator lenalidomide, and Bruton's tyrosine kinase inhibitor ibrutinib.
The role of B-cell receptor inhibitors in the treatment of patients with chronic lymphocytic leukemia.
Bethesda, United States. In Haematologica, Dec 2015
Spleen tyrosine kinase, Bruton's tyrosine kinase, and the phosphatidylinositol 3-kinase (PI3K) δ isoform are essential for B-cell receptor signal transduction but also mediate the effect of other pathways engaged in chronic lymphocytic leukemia cells in the tissue-microenvironment. Orally bioavailable inhibitors of spleen tyrosine kinase, Bruton's tyrosine kinase, or PI3Kδ, induce high rates of durable responses.
Covalent targeting of acquired cysteines in cancer.
Utrecht, Netherlands. In Curr Opin Chem Biol, Dec 2015
For example, targeting cysteine residues in the ATP-binding pockets of kinases with thiol-reactive molecules has afforded increased selectivity and potency to drugs like imbrutinib, which inhibits the oncogene BTK, and CO-1686 and AZD9291 that target oncogenic mutant EGFR.