Kinase Inhibitor (brand name)(indication; main therapeutic targets) Selected Kinase Target Affinity(antiviral and pulmonary benefit)KINOMEscan(kd<100 nM) Anti-inflammatory activity, cytokine suppression, antifibrotic activity
Midostaurin (Rydapt)
(acute myeloid leukemia, systemic mastocytosis; multi-targeted; FLT3-ITD, D816V-c-KIT) AAK1, JAK2, JAK3,
Kd KIT (220nM),
Kd RET (350nM)
(48) Anti-inflammatory and cytokine suppression (107)
Lestaurtinib
(orphan drug status, acute myeloid leukemia; multi-targeted; FLT3, JAK2, TrkA, TrkB, TrkC) AAK1, AXL, FYN, GAK, JAK1, JAK2, JAK3, RET
Kd KIT (150nM)* Anti-inflammatory and cytokine suppression (107)
Gilteritinib (Xospata)
(acute myeloid leukemia;
FLT3-ITD; AXL) AXL
IC50 (41 nM)
(49)**
Dasatinib (Sprycel)
(chronic myeloid leukemia, Ph+acute lymphoblastic leukemia; multi-targeted; BCR-ABL, SRC) ABL1, ABL2, CSK, FYN, GAK, KIT, LYN, SRC, YES Anti-inflammatory, cytokine suppression, antifibrotic (100) (99) (102) (103) (104) (101)
Imatinib Mesylate (Gleevec (US)/Glivec (Europe/Australia)
(chronic myeloid leukemia, Ph+acute lymphoblastic leukemia, gastrointestinal stromal tumor, chronic eosinophilic leukemia, hypereosinophilic syndrome, systemic mastocytosis; myelodysplastic syndrome; BCR-ABL, KIT, FIP1L1-PDGFRalpha) ABL1, ABL2, KIT Anti-inflammatory, cytokine suppression/immunomodulatory, antifibrotic (91) (92) (90) (79) (94) (95) (96) (93) (77)
Nilotinib (Tasigna)
(chronic myeloid leukemia; BCR-ABL) ABL1, ABL2, KIT Antifibrotic ((80) (81) (82) (83) (84) (85) (86)
Ponatinib (Iclusig)
(chronic myeloid leukemia, Ph+ acute lymphoblastic leukemia; BCR-ABL) ABL1, ABL2, KIT, RET, SRC Cytokine suppression (78)
Saracatinib
(orphan drug status, idiopathic pulmonary fibrosis; ABL, SRC, LCK, FGR, BLK) ABL1
FYN, LYN, SRC, YES1
IC50 v-ABL (30 nM); IC50 FYN (10 nM); IC50 LYN (5 nM) (isolated protein kinase assay) (186)** Antifibrotic (100) (99) (105)
Bosutinib (Bosulif)
(chronic myeloid leukemia; ABL, SRC) ABL1, ABL2, AXL, CSK, EGFR, FYN, GAK, LYN, SRC, YES Anti-inflammatory, cytokine suppression, and antifibrotic (104) (87) (88)
Baricitinib (Olumiant)
(rheumatoid arthritis; JAK1, JAK2) JAK1, JAK2, TYK2
Kd AAK1 (17 nM); Kd GAK (136 nM) (cell-free assay) (47)** Anti-inflammatory and cytokine suppression (106) (107) (108)
Ruxolitinib (Jakafi)
(myelofibrosis, polycythemia vera; JAK1, JAK2) GAK, JAK1, JAK2, JAK3, TYK2
Kd AAK1 (100 nM); Kd GAK (120 nM) (cell-free assay) (47)** Anti-inflammatory and cytokine suppression, antifibrotic (107)
Fedratinib (Inrebic)
(myelofibrosis; JAK2) AAK1, ABL1, FYN, GAK, JAK2, SRC
Kd AAK1 32 nM; Kd GAK 1 nM (cell-free assay) (47)** Anti-inflammatory and cytokine suppression, (107) (115)
Tofacitinib (XELJANZ XR)
(ulcerative colitis, rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis; JAK1, JAK3) JAK1, JAK2, JAK3, TYK2
No AAK1 inhibitory activity (47) Anti-inflammatory and cytokine suppression (109) (110) (107) (111)
Gefitinib (Iressa)
(non-small cell lung cancer; EGFR) EGFR, GAK Antifibrotic (119) (116) (178) (118)
Afatinib (Gilotrif)
(non-small cell lung cancer, advanced squamous cell carcinoma; Her2/EGFR) EGFR, GAK Anti-inflammatory, antifibrotic (116) (178) (179)
Lapatinib (Tykerb and Tyverb)
(breast cancer; Erb1/Erb2, EGFR) EGFR Antifibrotic (116) (178)
Osimertinib (Tagrisso)’
(non-small cell lung cancer; EGFR) EGFR
(60)** AZ5104, active metabolite of osimertinib, downregulates Th17-related cytokine production via inhibition of SRC-ERK-STAT3
(127)
Erlotinib (Tarceva)
(non-small cell lung cancer, pancreatic cancer; Erb1, EGFR) EGFR, GAK
Kd ABL1 (310nM)
(48) Antifibrotic (116) (178)
Neratinib (Nerlynx)
(breast cancer; Her2/EGFR) EGFR
Pazopanib (Votrient)
(renal cell carcinoma, advanced soft tissue sarcoma; multi-targeted; c-KIT, FGFR, PDGFR, VEGFR) KIT Anti-inflammatory potential, antifibrotic
(136)
Sorafenib (Nexavar)
(renal cell carcinoma, hepatocellular carcinoma, thyroid cancer; multi-targeted; PDGFR, VEGFR, RAF) KIT, RET Antifibrotic (125) (126) (187)
Sunitinib malate (Sutent)
(renal cell carcinoma, gastrointestinal stromal tumor; multi-targeted; PDGFR, VEGFR) AAK1, AXL, GAK, JAK1, KIT, RET Anti-inflammatory potential, cytokine suppression, antifibrotic (137) (135) (107)
Axitinib (Inlyta)
(renal cell carcinoma; c-KIT, PDGFR, VEGFR1, VEGFR2, VEGFR3) ABL1, ABL2, KIT Anti-inflammatory and cytokine suppression (128)
Vandetanib (Caprelsa)
(medullary thyroid carcinoma; EGFR, RET, VEGFR) ABL2, EGFR, GAK, RET, SRC
Kd ABL1 (270nM) (48)
Regorafenib (Stivarga)
(colorectal cancer, gastrointestinal stromal tumor, hepatocellular cancer; PDGFRβ, Raf-1, TIE2, VEGFR1/2/3) KIT, RET
Ibrutinib (Imbruvica)
(mantel cell lymphoma, Waldenstrom macroglobulinemia, chronic lymphocytic leukemia, Small lymphocytic lymphoma, marginal zone lymphoma; BTK) EGFR, RET Anti-inflammatory (132) (133)
Palbociclib (Ibrance)
(breast cancer; CDK4, CDK6) CDK6
Abemaciclib (Verzenio and Verzenios)
(breast cancer, CDK4,CDK6) CDK6
IC50 (10 nmol/L)
CDK9
IC50 (57 nmol/L)
(188)** Abemaciclib in combination with anastrozole led to increased cytokine signaling and immune activation
(189)
Alvocidib
(orphan drug status, acute myeloid leukemia; CDK1, CDK2, CDK4, CDK9) CDK9 Anti-inflammatory (134)
Ceritinib (Zykadia)
(non-small cell lung cancer; ALK, IGF1R, InsR, STK22D)
Crizotinib (Xalkori)
(non-small cell lung cancer; ALK/ROS1) ABL1, AXL
Masitinib (Masivet)
(orphan drug status, potential amyotrophic lateral sclerosis drug; FAK, FGFR3, KIT, LCK, PDGFR) ABL1, KIT,
LYN
Nintedanib (Ofev and Vargatef)
(idiopathic pulmonary fibrosis, non-small cell lung cancer; FGFR, PDGFR, VEGFR) AAK1, ABL1, AXL, JAK2, JAK3, KIT, RET, YES1 Anti-inflammatory, cytokine suppression, antifibrotic (129) (130) (131)