Table 1. JAK inhibitors, their targets, and their applications to pathologies.

Inhibitors	Selectivity	Off- target	Diseases	Clinical phases
Type I
Ruxolitinib	JAK2>JAK1>JAK3		MF and hydroxyurea resistant or intolerant PV Refractory leukemia (post-MPN leukemia) Pancreatic cancers Corticosteroid refractory-GVHD Psoriasis Alopecia Vitiligo	FDA-approved 77– 79 Phase 2 80 Phase 2 in combination with capecitabine (after gemcitabine failure) 81 In evaluation 82 Phase 2 83 Open-label clinical trial 84 Case report 85
Momelotinib (CYT-387)	JAK2>JAK1>JAK3	ALK-2 TBK1 IKKε	PMF Post PV/ET MF PV/ET	Phase 3 - SIMPLIFY-1/2 (Stopped) 86 Phase 2 (terminated) 87
AZD1480	JAK2>JAK1	Aurora A FGFR1 FLT4	PMF Post PV/ET MF B-ALL Solid tumors	Phase 1 (completed) 88 In evaluation (preclinic) 89 Phase 1 (terminated) 90
Baricitinib (INCB-028050)	JAK2>JAK1		Rheumatoid arthritis Psoriasis	Phase 3 (FDA approval in process, EMA-approved) 91 Phase 2 92
Tofacitinib	JAK1>JAK3		Methothrexate-resistant rheumatoid arthritis Crohn’s Psoriasis Alopecia areata Dermatomyositis, vitiligo	FDA-approved 93 Phase 2 94 Phase 3 95 Phase 2 96 Case report 96
Gandotinib (LY2784544)	Pan-JAK JAK2V617F>JAK2		JAK2V617F-positive MF, ET and PV patients	Phase 1 97 Phase 2 (in progress)
XL019	Pan-JAK		PV, MF	Phase 1 (terminated) 98
NVP-BSK805	JAK2		JAK2V617F	Cellular models 99
NS-018	JAK2V617F>JAK2	Src	PMF, post PV/ET MF patients JAK2V617F selective	Phase 2 12 In vitro 100
Pacritinib (SB11518)	JAK2	FLT3	MF	Phase 3 PERSIST-1 101, PERSIST-2 102 PAC203 study evaluating the effect of lower doses
CEP-33779	JAK2		Rheumatoid arthritis, colorectal cancer, lupus nephritis	Preclinical mouse models 103
NVP-BVB808	JAK2	FLT3	MPN	Cell lines 104
TG101209	JAK2	FLT3	MPN, systemic sclerosis	Cellular models 105
Fedratinib (TG101348)	JAK2	FLT3 BRD4	MF	Phase 3 JAKARTA 106 FDA removed the clinical hold in August 2017
AZ960	JAK2		ATL, other leukemia	Cell lines
Filgotinib (GLPG0634)	JAK1>JAK2		Rheumatoid arthritis Bowel and Crohn’s diseases Lupus and psoriasis	Phase 3 107 Phase 2 108 Phase 2 109
Itacitinib (INCB-039110)	JAK1		MF Psoriasis Non-small cell lung cancer GVHD B-cell lymphoma BRAF-mutant melanoma and other solid tumors	Phase 2 (alone or in combination with low-dose of ruxolitinib) 110 Phase 2 111 Phase 2 (combination with EGFR inhibitor, osimertinib) (in progress) Phase 3 (combination with corticosteroids) (in progress) Phase 1/2 (combination with BTK inhibitor, ibrutinib) (in progress) Phase 1 (in combination with MAPK inhibitors, dabrafenib or trametinib) (in progress)
INCB52793	JAK1		Advanced malignancies	Phase 1 (in progress)
PF-04965842	JAK1		Moderate to severe psoriasis	Phase 2 112
Upadacitinib (ABT-494)	JAK1		Rheumatoid arthritis	Phase 2 113 Phase 3 (in progress)
Decernotinib (VX-509)	JAK3		Rheumatoid arthritis	Phase 2/3 114
WHI-P131/ JANEX-1	JAK3		GVHD	Preclinical mouse model 115
JAK3-IN-1	JAK3		N/A	N/A
Peficitinib (ASP015K)	JAK3		Psoriasis Rheumatoid arthritis	Phase 2 116 Phase 2 117
Type II
NVP-BBT594	JAK2	BCR-ABL KDR FLT3 RET		Cellular models 14
NVP-CHZ868	JAK2	KIT, PDGFR VEGFR	MPN B-ALL	Preclinical mouse models 75
Allosteric inhibitors
LS104	JAK2	BCR- ABL	MPN	JAK2V617F cell lines 118
ON044580	JAK2	BCR- ABL	MPN	BCR-ABL cell lines 119

ATL, adult T-cell leukemia; B-ALL, B-cell acute lymphoblastic leukemia; BTK, Bruton’s tyrosine kinase; EGFR, epidermal growth factor receptor; EMA, European Medicines Agency; ET, essential thrombocythemia; FDA, US Food and Drug Administration; GVHD, graft-versus-host disease; JAK, Janus kinase; MAPK, mitogen-activated protein kinase; MF, myelofibrosis; MPN, myeloproliferative neoplasm; N/A, not applicable; PMF, primary myelofibrosis; PV, polycythemia vera.