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 | |
GDC-0834 | Phase I | Rheumatoid Arthritis | 5.9 nM | |
RN-486 | Preclinical | Rheumatoid Arthritis, SLE | 4.0 nM | |
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 | |
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 |