Abstract
ABSTRACT Introduction The covalent Bruton’s tyrosine kinase (BTK) inhibitor ibrutinib has been approved in the USA for B cell malignancies for almost ten years and has improved the survival of patients with chronic lymphocytic leukemia (CLL)/small lymphocytic lymphoma (SLL). Orelabrutinib is a novel, highly selective covalent BTK inhibitor with proven efficacy and acceptable safety profile. In 2020, it was approved for the treatment of relapsed/refractory (R/R) CLL/SLL in China. Areas covered In this review, we summarized the current clinical trials exploring orelabrutinib monotherapy or orelabrutinib-based combination regimens in CLL/SLL, especially R/R CLL/SLL. Pharmacodynamics, pharmacokinetics, clinical efficacy and safety of orelabrutinib are also discussed. Expert opinion Orelabrutinib selectively inhibits BTK via covalent binding and exhibits linear pharmacokinetics. BTK is the only kinase targeted by orelabrutinib, and a few off-target toxicities of orelabrutinib have been reported. The phase I/II trial demonstrated the efficacy and safety of orelabrutinib in patients with R/R CLL/SLL; however, further clinical trials are needed to compare orelabrutinib with ibrutinib in patients with R/R CLL/SLL and to evaluate its efficacy and safety in patients with treatment-naive CLL/SLL.
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