Drug Information

Drug General Information
Drug ID
D04LKS
Former ID
DNCL003509
Drug Name
Ruxolitinib
Synonyms
Ruxolitinib (JAK inhibitor)
Drug Type
Small molecular drug
Indication High-risk myelofibrosis [ICD10:C94.4, D47.4] Approved [524601], [533122], [541031], [556264]
Essential thrombocythemia [ICD9: 238.71, 289.9; ICD10:D47.3, D75.2, D75.8] Phase 4 [523729], [541031]
Pancreatic cancer [ICD9: 140-199, 140-229, 157, 210-229; ICD10:C25] Phase 3 [524723], [541031]
Company
Incyte
Formula
C17H18N6
InChI
InChI=1S/C17H18N6/c18-7-5-15(12-3-1-2-4-12)23-10-13(9-22-23)16-14-6-8-19-17(14)21-11-20-16/h6,8-12,15H,1-5H2,(H,19,20,21)/t15-/m1/s1
InChIKey
HFNKQEVNSGCOJV-OAHLLOKOSA-N
CAS Number
CAS 941678-49-5
PubChem Compound ID
25126798
PubChem Substance ID
81071277, 85921742, 104253171, 131480859, 134339114, 134449640, 135263142, 135626684, 135693443, 135727401, 136367406, 136378506, 136920365, 136959525, 137168066, 137237509, 137275864, 137875640, 144116074, 152212763, 152258834, 152344048, 152344083, 160645455, 160647685, 162011537, 162038073, 162197164, 163913900, 164193924, 164764917, 165238055, 170502151, 172919539, 174006685, 174474441, 175267965, 175427129, 177748964, 178102315, 186005338, 188376260, 198992749, 208265517, 223617460, 223723945, 224411802, 226532797, 247725985, 249737056
ChEBI ID
ChEBI:66919
SuperDrug ATC ID
L01XE18
Drug Resistance Mutation (DRM)
DRM DRM Info
Target and Pathway
Target(s) Tyrosine-protein kinase JAK2 Target Info Modulator [531783]
JAK1 Target Info Modulator [531783]
KEGG Pathway Chemokine signaling pathway
PI3K-Akt signaling pathway
Signaling pathways regulating pluripotency of stem cells
Jak-STAT signaling pathway
Cholinergic synapse
Prolactin signaling pathway
Adipocytokine signaling pathway
Leishmaniasis
Toxoplasmosis
Tuberculosis
Measles
Influenza A
Herpes simplex infectionhsa04151:PI3K-Akt signaling pathway
Osteoclast differentiation
Hepatitis C
Hepatitis B
HTLV-I infection
Herpes simplex infection
Epstein-Barr virus infection
Pathways in cancer
Viral carcinogenesis
Pancreatic cancer
NetPath Pathway IL2 Signaling Pathway
PANTHER Pathway Inflammation mediated by chemokine and cytokine signaling pathway
Interferon-gamma signaling pathway
JAK/STAT signaling pathway
PDGF signaling pathway
PI3 kinase pathway
CCKR signaling map STP00005:Angiogenesis
Pathway Interaction Database Endothelins
ErbB4 signaling events
GMCSF-mediated signaling events
IL4-mediated signaling events
IL27-mediated signaling events
Signaling events mediated by PTP1B
IL12-mediated signaling events
S1P3 pathway
SHP2 signaling
CXCR4-mediated signaling events
IL5-mediated signaling events
IFN-gamma pathway
ErbB2/ErbB3 signaling events
IL3-mediated signaling events
IL6-mediated signaling events
PDGFR-beta signaling pathway
IL23-mediated signaling events
Signaling events mediated by Stem cell factor receptor (c-Kit)
EPO signaling pathway
Notch-mediated HES/HEY networkp73pathway:p73 transcription factor network
Signaling events mediated by TCPTP
IL2-mediated signaling events
IL2 signaling events mediated by PI3K
PDGFR-alpha signaling pathway
IL2 signaling events mediated by STAT5
Reactome Interleukin-6 signaling
MAPK3 (ERK1) activation
MAPK1 (ERK2) activation
GPVI-mediated activation cascade
Prolactin receptor signaling
RMTs methylate histone arginines
G beta:gamma signalling through PI3Kgamma
Interleukin-3, 5 and GM-CSF signaling
RAF activation
RAF/MAP kinase cascade
Interferon gamma signaling
Regulation of IFNG signaling
Interleukin receptor SHC signaling
Growth hormone receptor signaling
Factors involved in megakaryocyte development and platelet productionR-HSA-1059683:Interleukin-6 signaling
ISG15 antiviral mechanism
Interleukin-7 signaling
Interleukin-2 signaling
Interferon alpha/beta signaling
Regulation of IFNA signaling
WikiPathways Serotonin Receptor 2 and STAT3 Signaling
Type II interferon signaling (IFNG)
Notch Signaling Pathway
EPO Receptor Signaling
EGF/EGFR Signaling Pathway
IL-4 Signaling Pathway
IL-6 signaling pathway
Kit receptor signaling pathway
IL-3 Signaling Pathway
Mesodermal Commitment Pathway
Interleukin-2 signaling
Signaling by SCF-KIT
Prolactin receptor signaling
Growth hormone receptor signaling
JAK/STAT
BDNF signaling pathway
Oncostatin M Signaling Pathway
Interleukin-11 Signaling Pathway
AGE/RAGE pathway
TSLP Signaling Pathway
IL17 signaling pathway
Leptin signaling pathway
TSH signaling pathway
Interleukin-3, 5 and GM-CSF signaling
Interferon gamma signaling
Factors involved in megakaryocyte development and platelet production
IL-5 Signaling PathwayWP619:Type II interferon signaling (IFNG)
Interferon type I signaling pathways
TGF Beta Signaling Pathway
IL-2 Signaling Pathway
TCA Cycle Nutrient Utilization and Invasiveness of Ovarian Cancer
Interleukin-7 signaling
PDGF Pathway
Prostate Cancer
IL-9 Signaling Pathway
Type III interferon signaling
IL-7 Signaling Pathway
Integrated Breast Cancer Pathway
Integrated Cancer pathway
Interferon alpha/beta signaling
IL-5 Signaling Pathway
References
Ref 523729ClinicalTrials.gov (NCT01493414) INC424 for Patients With Myelofibrosis, Post Polycythemia Myelofibrosis or Post-essential Thrombocythemia Myelofibrosis. U.S. National Institutes of Health.
Ref 524601ClinicalTrials.gov (NCT02038036) Ruxolitinib Efficacy and Safety in Patients With HU Resistant or Intolerant Polycythemia Vera vs Best Available Therapy.. U.S. National Institutes of Health.
Ref 524723ClinicalTrials.gov (NCT02117479) Study of Ruxolitinib in Pancreatic Cancer Patients (Janus 1). U.S. National Institutes of Health.
Ref 533122Ruxolitinib versus standard therapy for the treatment of polycythemia vera. N Engl J Med. 2015 Jan 29;372(5):426-35.
Ref 541031(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5688).
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
Ref 5317832011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.

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