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Table 1 Comparison of ibrutinib with second- generation BTK inhibitors

From: Second-generation inhibitors of Bruton tyrosine kinase

 

Ibrutinib

ACP-196

ONO/GS-4059

BGB-3111

Target

BTK

BTK

BTK

BTK

Major off-targets

EGFR, ITK, TEC

Minimal

TEC (weak)

ITK (weak)

Activity on C481S

No

Yes

Yes

Yes

Platelet inhibition

Yes

No

NA

NA

Atrial fibrillation

Observed

Not observed

Observeda

NA

Approved indications

CLL/SLL, MCL,WM

None

None

None

  1. BTK Bruton tyrosine kinase, NA not available /reported, CLL chronic lymphoid leukemia, SLL small lymphoid leukemia, MCL mantle cell lymphoma, WM Waldenstrom’s macroglobulinemia
  2. aThe atrial fibrillation was not thought to be drug-related