| 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 |
[1],
[2],
[3],
[4]
|
|---|
|
Essential thrombocythemia [ICD9: 238.71, 289.9; ICD10:D47.3, D75.2, D75.8]
|
Phase 4 |
[5],
[3]
|
|
Pancreatic cancer [ICD9: 140-199, 140-229, 157, 210-229; ICD10:C25]
|
Phase 3 |
[6],
[3]
|
| Company |
Incyte
|
| Structure |
|
Download
2D MOL
3D MOL
|
| 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 |
|
| 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 |
[7]
|
|---|
| JAK1 |
Target Info |
Modulator |
[7]
|
|
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 1 | ClinicalTrials.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 2 | Ruxolitinib versus standard therapy for the treatment of polycythemia vera. N Engl J Med. 2015 Jan 29;372(5):426-35. |
|---|
| REF 3 | (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 4 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. |
|---|
| REF 5 | ClinicalTrials.gov (NCT01493414) INC424 for Patients With Myelofibrosis, Post Polycythemia Myelofibrosis or Post-essential Thrombocythemia Myelofibrosis. U.S. National Institutes of Health. |
|---|
| REF 6 | ClinicalTrials.gov (NCT02117479) Study of Ruxolitinib in Pancreatic Cancer Patients (Janus 1). U.S. National Institutes of Health. |
|---|
| REF 7 | 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4. |
|---|
