Bruton’s tyrosine kinase in chronic inflammation: from pathophysiology to therapy

Figures & data

Table 1 Btk inhibitors in development for immune-mediated inflammatory disorders

Compound	Irreversible/reversible	IC50	Tested in animal models for	Clinical stage
CG11746	Reversible	1.9 nM	RA	Preclinical
RN486	Reversible	4 nM	RA SLE	Preclinical
Ibrutinib	Irreversible	0.5 nM	RA, SLE	Preclinical
ONO-4059	Reversible	2.2 nM	RA	Preclinical
CC-292	Irreversible	5.9 nM	RA	Phase IIa
GDC-0834	Reversible	5.9 nM	RA	Phase I
HM-71224	Irreversible	2 nM	RA	Phase I
PF-06250112	Reversible	0.5 nM	SLE	Preclinical

Abbreviations: IC₅₀, half maximal inhibitory concentration; RA, rheumatoid arthritis; SLE, systemic lupus erythematosus.