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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 [7678]
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 [8183]
  1. NR not reported.