Acalabrutinib (ACP-196): a selective second-generation BTK inhibitor

Jingjing Wu; Mingzhi Zhang; Delong Liu

doi:10.1186/s13045-016-0250-9

Acalabrutinib (ACP-196): a selective second-generation BTK inhibitor

J Hematol Oncol. 2016 Mar 9:9:21. doi: 10.1186/s13045-016-0250-9.

Authors

Jingjing Wu¹, Mingzhi Zhang¹, Delong Liu²

Affiliations

¹ Department of Oncology, The first Affiliated Hospital of Zhengzhou University, Zhengzhou, 450052, China.
² Department of Oncology, The first Affiliated Hospital of Zhengzhou University, Zhengzhou, 450052, China. Delong_liu@nymc.edu.

Abstract

More and more targeted agents become available for B cell malignancies with increasing precision and potency. The first-in-class Bruton's tyrosine kinase (BTK) inhibitor, ibrutinib, has been in clinical use for the treatment of chronic lymphocytic leukemia, mantle cell lymphoma, and Waldenstrom's macroglobulinemia. More selective BTK inhibitors (ACP-196, ONO/GS-4059, BGB-3111, CC-292) are being explored. Acalabrutinib (ACP-196) is a novel irreversible second-generation BTK inhibitor that was shown to be more potent and selective than ibrutinib. This review summarized the preclinical research and clinical data of acalabrutinib.

Publication types

Research Support, Non-U.S. Gov't
Review

MeSH terms

Agammaglobulinaemia Tyrosine Kinase
Animals
Benzamides / therapeutic use*
Clinical Trials as Topic
Hematologic Neoplasms / drug therapy*
Hematologic Neoplasms / enzymology
Hematologic Neoplasms / pathology
Humans
Protein Kinase Inhibitors / therapeutic use*
Protein-Tyrosine Kinases / antagonists & inhibitors*
Protein-Tyrosine Kinases / metabolism
Pyrazines / therapeutic use*
Treatment Outcome
Xenograft Model Antitumor Assays

Substances

Benzamides
Protein Kinase Inhibitors
Pyrazines
Protein-Tyrosine Kinases
Agammaglobulinaemia Tyrosine Kinase
BTK protein, human
acalabrutinib