Skip to main content
. 2023 Mar 6;28(5):2400. doi: 10.3390/molecules28052400

Table 1.

Summary of approved BTKIs [5,14,20,75,76,77,78].

Name Synonyms Type of Inhibitor Indications Year of Approval Activity (IC50)
Ibrutinib Imbruvica® CRA-032765
PC-32765
PCI-32765
PCI-32765-00
Irreversible MCL, CLL, SLL, WM, MZL, GVHD 2013 BTK IC50 = 0.47 nM
ITK IC50 = 55 nM
TEC IC50 = 3.2 nM
Acalabrutinib Calquence® ACP-196 Irreversible CLL, SLL, MCL 2017 BTK IC50 = 2.5 nM
ITK IC50 > 20,000 nM
TEC IC50 = 37 nM
Zanubrutinib Brukinsa® BGB-3111 Irreversible NHL, CLL, MCL 2019 BTK IC50 = 0.3 nM
ITK IC50 = 56 nM
TEC IC50 = 2 nM
Tirabrutinib
Velexbru®
ONO-4059 Irreversible CNS lymphoma, WM, CLL 2020 BTK IC50 = 6.8 nM
ITK IC50 > 20,000 nM
TEC IC50 = 48 nM
Orelabrutinib ICP-022 Irreversible MCL, CLL, SLL 2020 BTK IC50 = 1.6 nM