Journal article

Phase 1 study of the selective BTK inhibitor zanubrutinib in B-cell malignancies and safety and efficacy evaluation in CLL

Constantine S Tam, Judith Trotman, Stephen Opat, Jan A Burger, Gavin Cull, David Gottlieb, Rosemary Harrup, Patrick B Johnston, Paula Marlton, Javier Munoz, John F Seymour, David Simpson, Alessandra Tedeschi, Rebecca Elstrom, Yiling Yu, Zhiyu Tang, Lynn Han, Jane Huang, William Novotny, Lai Wang Show all

Blood | AMER SOC HEMATOLOGY | Published : 2019

Abstract

Zanubrutinib is a potent and highly selective inhibitor of Bruton tyrosine kinase (BTK). In this first-in-human, open--label, multicenter, phase1 study, patients in part 1 (3+3) dose escalation) had relapsed/refractory B-cell malignancies and received zanubrutinib 40, 80, 160, or 320 mg once daily or 160 mg twice daily. Part 2 (expansion) consisted of disease--specific cohorts, including treatment-naïve or relapsed/refractory chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL). The primary end points were safety and tolerability, and definition of the maximum tolerated dose (part 1). Additional end points included pharmacokinetics/pharmacodynamics and preliminary efficacy. Repo..

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