Table 1.
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 |