DGIdb - RUXOLITINIB Drug Record

RUXOLITINIB chembl:CHEMBL1789941 ApprovedAntineoplasticImmunotherapy

Alternate Names:

JAKAVI
INCB018424
INC-424
INCB-18424
INC424
INCB-018424
RUXOLITINIB
INCB424
JAKAFI®
JAKAVI®
INCB 18424
(R)-RUXOLITINIB
chembl:CHEMBL1789941
drugbank:08877
pubchem.compound:25126798
chemidplus:941678-49-5
rxcui:1193326

Drug Info:

FDA Approval	Myelofibrosis
Drug Class	Kinase Inhibitors

(7 More Sources)

Publications:

Mazzacurati et al., 2015, The PIM inhibitor AZD1208 synergizes with ruxolitinib to induce apoptosis of ruxolitinib sensitive and resistant JAK2-V617F-driven cells and inhibit colony formation of primary MPN cells., Oncotarget
Hornakova et al., 2011, Oncogenic JAK1 and JAK2-activating mutations resistant to ATP-competitive inhibitors., Haematologica
Choong et al., 2013, Combination treatment for myeloproliferative neoplasms using JAK and pan-class I PI3K inhibitors., J. Cell. Mol. Med.
Deshpande et al., 2012, Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms., Leukemia
Weigert et al., 2012, Genetic resistance to JAK2 enzymatic inhibitors is overcome by HSP90 inhibition., J. Exp. Med.
Marty et al., 2014, Germ-line JAK2 mutations in the kinase domain are responsible for hereditary thrombocytosis and are resistant to JAK2 and HSP90 inhibitors., Blood
Roberts et al., 2014, Targetable kinase-activating lesions in Ph-like acute lymphoblastic leukemia., N. Engl. J. Med.
Tan L et al., 2015, Development of Selective Covalent Janus Kinase 3 Inhibitors., J Med Chem
Dusa et al., 2010, JAK2 V617F constitutive activation requires JH2 residue F595: a pseudokinase domain target for specific inhibitors., PLoS ONE
Bercovich et al., 2008, Mutations of JAK2 in acute lymphoblastic leukaemias associated with Down's syndrome., Lancet
Maude et al., 2012, Targeting JAK1/2 and mTOR in murine xenograft models of Ph-like acute lymphoblastic leukemia., Blood
Man et al., 2012, Sorafenib treatment of FLT3-ITD(+) acute myeloid leukemia: favorable initial outcome and mechanisms of subsequent nonresponsiveness associated with the emergence of a D835 mutation., Blood
Mullighan et al., 2009, JAK mutations in high-risk childhood acute lymphoblastic leukemia., Proc. Natl. Acad. Sci. U.S.A.
Kilpivaara et al., 2009, A germline JAK2 SNP is associated with predisposition to the development of JAK2(V617F)-positive myeloproliferative neoplasms., Nat. Genet.
Kiladjian et al., 2006, High molecular response rate of polycythemia vera patients treated with pegylated interferon alpha-2a., Blood
Ismael et al., 2012, De novo childhood myelodysplastic/myeloproliferative disease with unique molecular characteristics., Br. J. Haematol.
Paschka et al., 2013, Secondary genetic lesions in acute myeloid leukemia with inv(16) or t(16;16): a study of the German-Austrian AML Study Group (AMLSG)., Blood
Wernig et al., 2008, Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera., Cancer Cell
Nagao et al., 2014, Proliferation and survival signaling from both Jak2-V617F and Lyn involving GSK3 and mTOR/p70S6K/4EBP1 in PVTL-1 cell line newly established from acute myeloid leukemia transformed from polycythemia vera., PLoS ONE
MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
Rumi et al., 2014, Clinical effect of driver mutations of JAK2, CALR, or MPL in primary myelofibrosis., Blood
Yoshiki et al., 2011, A case of myeloid sarcoma with correlation to JAK2V617F mutation, complicated by myelofibrosis and secondary acute myeloid leukemia., Intern. Med.
Novotny-Diermayr et al., 2012, The oral HDAC inhibitor pracinostat (SB939) is efficacious and synergistic with the JAK2 inhibitor pacritinib (SB1518) in preclinical models of AML., Blood Cancer J
Wang et al., 2010, AML1 is overexpressed in patients with myeloproliferative neoplasms and mediates JAK2V617F-independent overexpression of NF-E2., Blood
Levine et al., 2005, The JAK2V617F activating mutation occurs in chronic myelomonocytic leukemia and acute myeloid leukemia, but not in acute lymphoblastic leukemia or chronic lymphocytic leukemia., Blood
Malak et al., Long term follow up of 93 families with myeloproliferative neoplasms: life expectancy and implications of JAK2V617F in the occurrence of complications., Blood Cells Mol. Dis.
Jekarl et al., 2010, JAK2 V617F mutation in myelodysplastic syndrome, myelodysplastic syndrome/myeloproliferative neoplasm, unclassifiable, refractory anemia with ring sideroblasts with thrombocytosis, and acute myeloid leukemia., Korean J Hematol
Campbell et al., 2006, V617F mutation in JAK2 is associated with poorer survival in idiopathic myelofibrosis., Blood
Baxter et al., Acquired mutation of the tyrosine kinase JAK2 in human myeloproliferative disorders., Lancet
Eghtedar et al., 2012, Phase 2 study of the JAK kinase inhibitor ruxolitinib in patients with refractory leukemias, including postmyeloproliferative neoplasm acute myeloid leukemia., Blood
Roug et al., 2011, A patient with a 20-year lag phase between JAK2-V617F+ myeloproliferation and NPM1-mutated AML arguing against a common origin of disease., Eur. J. Haematol.
Passamonti et al., 2010, A prospective study of 338 patients with polycythemia vera: the impact of JAK2 (V617F) allele burden and leukocytosis on fibrotic or leukemic disease transformation and vascular complications., Leukemia
Yang et al., 2012, Ruxolitinib: in the treatment of myelofibrosis., Drugs
Cervantes et al., 2013, Myelofibrosis: an update on current pharmacotherapy and future directions., Expert Opin Pharmacother
Lierman et al., 2012, Ruxolitinib inhibits transforming JAK2 fusion proteins in vitro and induces complete cytogenetic remission in t(8;9)(p22;p24)/PCM1-JAK2-positive chronic eosinophilic leukemia., Blood
Chase et al., 2013, Ruxolitinib as potential targeted therapy for patients with JAK2 rearrangements., Haematologica
Ding YY et al., 2018, Clinical efficacy of ruxolitinib and chemotherapy in a child with Philadelphia chromosome-like acute lymphoblastic leukemia with <i>GOLGA5-JAK2</i> fusion and induction failure., Haematologica
Yang et al., 2016, Activating JAK1 mutation may predict the sensitivity of JAK-STAT inhibition in hepatocellular carcinoma., Oncotarget
Newton Y et al., 2018, Comparative RNA-Sequencing Analysis Benefits a Pediatric Patient With Relapsed Cancer., JCO Precis Oncol
Losdyck et al., 2015, Distinct Acute Lymphoblastic Leukemia (ALL)-associated Janus Kinase 3 (JAK3) Mutants Exhibit Different Cytokine-Receptor Requirements and JAK Inhibitor Specificities., J. Biol. Chem.
Maxson et al., 2016, The Colony-Stimulating Factor 3 Receptor T640N Mutation Is Oncogenic, Sensitive to JAK Inhibition, and Mimics T618I., Clin. Cancer Res.
Dao KH et al., 2014, Significant clinical response to JAK1/2 inhibition in a patient with CSF3R-T618I-positive atypical chronic myeloid leukemia., Leuk Res Rep
Fleischman et al., 2013, The CSF3R T618I mutation causes a lethal neutrophilic neoplasia in mice that is responsive to therapeutic JAK inhibition., Blood
2013, Genomic and epigenomic landscapes of adult de novo acute myeloid leukemia., N. Engl. J. Med.
Maxson et al., 2013, Oncogenic CSF3R mutations in chronic neutrophilic leukemia and atypical CML., N. Engl. J. Med.
Zhou et al., 2016, Clinical Improvement with JAK2 Inhibition in Chuvash Polycythemia., N. Engl. J. Med.

RUXOLITINIB CRLF2

Interaction Score: 13.74

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22955920

Sources:
CIViC
RUXOLITINIB CSF3R

Interaction Score: 7.85

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

Approval Status Preclinical

PMIDs:
26475333 25180155 24081659 23634996 23656643

Sources:
JAX-CKB DoCM CIViC
RUXOLITINIB JAK2

Interaction Score: 4.99

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type hematologic cancer

Response Type decreased response

Approval Status Preclinical

PMIDs:
26472029 21393331 24251790 21926964 22271575 24398328 25207766 26258521 20585391 18805579 22955920 22368270 19470474 19287384 16709929 22571758 23115274 18394554 24404189 25157968 24986690 22041374 22829971 20339092 16081687 22818858 21120162 16293597 15781101 22422826 21689158 20631743 23061804 23514013 22899477 22875628 29773603

Sources:
DTC MyCancerGenome JAX-CKB DoCM CIViC MyCancerGenomeClinicalTrial TTD OncoKB
RUXOLITINIB JAK1

Interaction Score: 3.43

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Clinical Status preclinical

Pathway activation

Variant Effect gain-of-function

PMIDs:
22955920 18805579 23061804 23514013 26701727 31372595

Sources:
MyCancerGenome DoCM CIViC TTD
RUXOLITINIB PLAUR

Interaction Score: 2.29

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
RUXOLITINIB MPL

Interaction Score: 1.25

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Ruxolitinib + TGX-221

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

PMIDs:
24251790

Sources:
JAX-CKB
RUXOLITINIB VHL

Interaction Score: 0.92

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27518686

Sources:
CIViC
RUXOLITINIB JAK3

Interaction Score: 0.86

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Evidence Type Actionable

Indication/Tumor Type Advanced Solid Tumor

Response Type decreased response

PMIDs:
26258521 26446793

Sources:
DTC JAX-CKB
RUXOLITINIB CYP3A4

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB

MyCancerGenome: RUXOLITINIB
- Version: 20-Jun-2017
Alternate Names:

INCB18424 Development Name

RUXOLITINIB Generic Name

JAKAFI Trade Name

Drug Info:

Drug Class Kinase Inhibitors

FDA Approval Myelofibrosis

Publications:
DTC: RUXOLITINIB
- Version: 02-September-2020
Alternate Names:

CHEMBL1789941 ChEMBL Drug ID

Drug Info:

Publications:

Tan L et al., 2015, Development of Selective Covalent Janus Kinase 3 Inhibitors., J Med Chem

JAX-CKB: Ruxolitinib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Maxson et al., 2016, The Colony-Stimulating Factor 3 Receptor T640N Mutation Is Oncogenic, Sensitive to JAK Inhibition, and Mimics T618I., Clin. Cancer Res.

Choong et al., 2013, Combination treatment for myeloproliferative neoplasms using JAK and pan-class I PI3K inhibitors., J. Cell. Mol. Med.

Marty et al., 2014, Germ-line JAK2 mutations in the kinase domain are responsible for hereditary thrombocytosis and are resistant to JAK2 and HSP90 inhibitors., Blood

DoCM: RUXOLITINIB

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Maude et al., 2012, Targeting JAK1/2 and mTOR in murine xenograft models of Ph-like acute lymphoblastic leukemia., Blood

2013, Genomic and epigenomic landscapes of adult de novo acute myeloid leukemia., N. Engl. J. Med.

Maxson et al., 2013, Oncogenic CSF3R mutations in chronic neutrophilic leukemia and atypical CML., N. Engl. J. Med.

CIViC: RUXOLITINIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Zhou et al., 2016, Clinical Improvement with JAK2 Inhibition in Chuvash Polycythemia., N. Engl. J. Med.

Dao KH et al., 2014, Significant clinical response to JAK1/2 inhibition in a patient with CSF3R-T618I-positive atypical chronic myeloid leukemia., Leuk Res Rep

Fleischman et al., 2013, The CSF3R T618I mutation causes a lethal neutrophilic neoplasia in mice that is responsive to therapeutic JAK inhibition., Blood

TTD: Ruxolitinib
- Version: 2020.06.01
Alternate Names:

D04LKS TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL1789941
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
MyCancerGenomeClinicalTrial: INCB018424
- Version: 30-February-2014
Alternate Names:

Drug Info:

Publications:
OncoKB: Ruxolitinib
- Version: 23-July-2020
Alternate Names:

Drug Info:

Publications:
MyCancerGenomeClinicalTrial: RUXOLITINIB
- Version: 30-February-2014
Alternate Names:

Drug Info:

Publications:
PharmGKB: ruxolitinib
- Version: 18-August-2020
Alternate Names:

Drug Info:

Publications:

Indication/Tumor Type	Advanced Solid Tumor
Response Type	sensitive
Approval Status	Preclinical

Indication/Tumor Type	hematologic cancer
Response Type	decreased response
Approval Status	Preclinical

Clinical Status	preclinical
Pathway	activation
Variant Effect	gain-of-function

combination therapy	Ruxolitinib + TGX-221
Indication/Tumor Type	Advanced Solid Tumor
Response Type	sensitive

Evidence Type	Actionable
Indication/Tumor Type	Advanced Solid Tumor
Response Type	decreased response

INCB18424	Development Name
RUXOLITINIB	Generic Name
JAKAFI	Trade Name

RUXOLITINIB Drug Record

RUXOLITINIB chembl:CHEMBL1789941 ApprovedAntineoplasticImmunotherapy

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22955920

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type Advanced Solid Tumor Response Type sensitive Approval Status Preclinical

PMIDs: 26475333 25180155 24081659 23634996 23656643

Sources: JAX-CKB DoCM CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Indication/Tumor Type hematologic cancer Response Type decreased response Approval Status Preclinical

Sources: DTC MyCancerGenome JAX-CKB DoCM CIViC MyCancerGenomeClinicalTrial TTD OncoKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Clinical Status preclinical Pathway activation Variant Effect gain-of-function

PMIDs: 22955920 18805579 23061804 23514013 26701727 31372595

Sources: MyCancerGenome DoCM CIViC TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Ruxolitinib + TGX-221 Indication/Tumor Type Advanced Solid Tumor Response Type sensitive

PMIDs: 24251790

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 27518686

Sources: CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Evidence Type Actionable Indication/Tumor Type Advanced Solid Tumor Response Type decreased response

PMIDs: 26258521 26446793

Sources: DTC JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

MyCancerGenome: RUXOLITINIB

Alternate Names: INCB18424 Development Name RUXOLITINIB Generic Name JAKAFI Trade Name

Drug Info: Drug Class Kinase Inhibitors FDA Approval Myelofibrosis

Publications:

DTC: RUXOLITINIB

Alternate Names: CHEMBL1789941 ChEMBL Drug ID

Drug Info:

Publications: Tan L et al., 2015, Development of Selective Covalent Janus Kinase 3 Inhibitors., J Med Chem

JAX-CKB: Ruxolitinib

Alternate Names:

Drug Info:

DoCM: RUXOLITINIB

Alternate Names:

Drug Info:

CIViC: RUXOLITINIB

Alternate Names:

Drug Info:

TTD: Ruxolitinib

Alternate Names: D04LKS TTD Drug ID

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL1789941

Alternate Names:

Drug Info:

Publications:

MyCancerGenomeClinicalTrial: INCB018424

Alternate Names:

Drug Info:

Publications:

OncoKB: Ruxolitinib

Alternate Names:

Drug Info:

Publications:

MyCancerGenomeClinicalTrial: RUXOLITINIB

Alternate Names:

Drug Info:

Publications:

PharmGKB: ruxolitinib

Alternate Names:

Drug Info:

Interaction Types & Directionality:

n/a

PMIDs:
22955920

Sources:
CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

Approval Status Preclinical

PMIDs:
26475333 25180155 24081659 23634996 23656643

Sources:
JAX-CKB DoCM CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type hematologic cancer

Response Type decreased response

Approval Status Preclinical

Sources:
DTC MyCancerGenome JAX-CKB DoCM CIViC MyCancerGenomeClinicalTrial TTD OncoKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Clinical Status preclinical

Pathway activation

Variant Effect gain-of-function

PMIDs:
22955920 18805579 23061804 23514013 26701727 31372595

Sources:
MyCancerGenome DoCM CIViC TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Ruxolitinib + TGX-221

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

PMIDs:
24251790

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

PMIDs:
27518686

Sources:
CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Evidence Type Actionable

Indication/Tumor Type Advanced Solid Tumor

Response Type decreased response

PMIDs:
26258521 26446793

Sources:
DTC JAX-CKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Alternate Names:

INCB18424 Development Name

RUXOLITINIB Generic Name

JAKAFI Trade Name

Drug Info:

Drug Class Kinase Inhibitors

FDA Approval Myelofibrosis

Alternate Names:

CHEMBL1789941 ChEMBL Drug ID

Publications:

Tan L et al., 2015, Development of Selective Covalent Janus Kinase 3 Inhibitors., J Med Chem

Alternate Names:

D04LKS TTD Drug ID