Skip to main content

Table 1 BTK Inhibitors in preclinical and clinical development

From: Ibrutinib and novel BTK inhibitors in clinical development

BTK inhibitor

Stage of development

Disease(s)

IC50

Reference

Ibrutinib

Phase II/III

CLL/SLL, MCL, WM, ABC-DLBCL, MM

0.5 nM

[54, 57, 58, 60]

GDC-0834

Phase I

Rheumatoid Arthritis

5.9 nM

[70, 71]

RN-486

Preclinical

Rheumatoid Arthritis, SLE

4.0 nM

[72, 73]

CGI-560

Preclinical

NR

400 nM

[74]

CGI-1746

Preclinical

Rheumatoid Arthritis

1.9 nM

[74]

HM-71224

Phase I

Rheumatoid Arthritis

NR

[75]

CC-292

Phase I

CLL/B-NHL

< 0.5 nM

[76–78]

ONO-4059

Phase I

CLL

2.2 nM

[79]

CNX-774

Preclinical

Autoimmune Diseases, B-cell NHL

< 1 nM

[80]

LFM-A13

Preclinical

B-cell NHL

17.2 μM

[81–83]

  1. NR not reported.