Table 2.

JAKinib IC₅₀ values in B-cells, neutrophils and CD8+ T-cells from whole blood assays

Stimulation/pSTAT	B-cells					Neutrophils					CD8+ T-cells
	BARI	FIL	MET	TOFA	UPA	BARI	FIL	MET	TOFA	UPA	BARI	FIL	MET	TOFA	UPA
	IC50, nM
JAK2/JAK2 or JAK2/TYK2-dependent cytokines
G-CSF/pSTAT3	NS					404	16 717	158 111	1245	369	NS
GM-CSF/pSTAT5	NS					66	3436	40 925	143	21	NS
IL-23/pSTAT3*	NS					NS					210	15 040	138 638	970	368
JAK1/JAK2/TYK2-dependent cytokines
IFNα/pSTAT1	156	2957	54 052	322	112	NS					80	1809	27 730	163	56
IFNα/pSTAT3	28	588	9777	62	20	47	833	13 438	66	18	35	795	10 617	73	23
IFNα/pSTAT5	23	436	7524	44	16	NS					27	607	8231	46	17
IFNγ/pSTAT1	22	900	12 820	61	21	78	3137	42 649	152	46	NS
JAK1/JAK3-dependent cytokines
IL-2/pSTAT5	NS					NS					32	809	11 046	33	21
IL-4/pSTAT6	295	6426	164 309	356	162	71	1200	37 069	106	37	47	1022	25 900	51	26
IL-15/pSTAT5	NS					NS					56	1459	19 958	56	32

G-CSF, GM-CSF, IFNα, IFNγ, IL-2, IL-4 and IL-15 reported IC₅₀ values are based on the average of duplicates from 6–10 healthy volunteer whole blood.

*Memory CD8+ T-cells.

BARI, baricitinib; FIL, filgotinib; G-CSF, granulocyte colony stimulating factor; GM-CSF, granulocyte-macrophage colony-stimulating factor; IC₅₀, half maximum inhibitory concentration; IFN, interferon; IL, interleukin; JAK, Janus kinase; JAKinib, Janus kinase inhibitor; MET, major metabolite of filgotinib (GS-829845); NS, not sampled; pSTAT, phosphorylated signal transducer and activator of transcription; TOFA, tofacitinib; TYK2, tyrosine kinase 2; UPA, upadacitinib.