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Acalabrutinib

Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia

N Engl J Med. 2016 Jan 28; 374(4): 323–332.

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Awan, F. T., Schuh, A., Brown, J. R., Furman, R. R., Pagel, J. M., Hillmen, P., ... & Frigault, M. M. (2019). Acalabrutinib monotherapy in patients with chronic lymphocytic leukemia who are intolerant to ibrutinib. Blood Advances, 3(9), 1553-1562

Wang, M., Rule, S., Zinzani, P. L., Goy, A., Casasnovas, O., Smith, S. D., ... & Panizo, C. (2018). Acalabrutinib in relapsed or refractory mantle cell lymphoma (ACE-LY-004): a single-arm, multicentre, phase 2 trial. The Lancet, 391(10121), 659-667

Patel VK, Lamothe B, Ayres ML, et al. Pharmacodynamics and proteomic analysis of acalabrutinib therapy: similarity of on-target effects to ibrutinib and rationale for combination therapy. Leukemia. 2018;32(4):920–930. doi:10.1038/leu.2017.321

Ward R and F Goldberg. 2018 Covalent Inhibition of Kinases. Kinase Drug Discovery. G de Bruin and T Barf. Royal Society of Chemistry.  Drug Discovery Series No. 67. Chapter 4: 61-96

Barf, T., Covey, T., Izumi, R., van de Kar, B., Gulrajani, M., van Lith, B., ... & Verkaik, S. (2017). Acalabrutinib (ACP-196): a covalent Bruton tyrosine kinase inhibitor with a differentiated selectivity and in vivo potency profile. Journal of Pharmacology and Experimental Therapeutics, 363(2), 240-252

Patel, V., Balakrishnan, K., Bibikova, E., Ayres, M., Keating, M. J., Wierda, W. G., & Gandhi, V. (2017). Comparison of acalabrutinib, a selective Bruton tyrosine kinase inhibitor, with ibrutinib in chronic lymphocytic leukemia cells. Clinical Cancer Research, 23(14), 3734-3743

T.  Barf, T. Covey, R. Izumi, B. van de Kar, M. Gulrajani, B. van Lith, M. van Hoek, E. de Zwart, D. Mittag, D. Demont, S. Verkaik, F. Krantz, P. G. Pearson, R. Ulrich, and A.Kaptein. (2017) Acalabrutinib (ACP-196): A Covalent Bruton Tyrosine Kinase Inhibitor with a Differentiated Selectivity and In Vivo Potency Profiles. J Pharmacol Exp Ther 363:240–252

Byrd JC, Harrington B, O'Brien S, et al. Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia. N Engl J Med. 2016; 374(4):323–332. doi:10.1056/NEJMoa1509981

T Barf and A. Kaptein (2012) Irreversible protein kinase inhibitors: balancing the benefits and risks. J Med Chem 55:6243–6262.