Details of the Drug

General Information of Drug (ID: DM7Q98D)

Drug Name
Ruxolitinib
Synonyms Ruxolitinib (JAK inhibitor)
Indication
Disease Entry ICD 11 Status REF
Essential thrombocythemia 3B63.1Z Approved [1]
High-risk myelofibrosis 2A20.2 Approved [2], [3], [4], [5]
Pancreatic cancer 2C10 Phase 3 [2], [6]
Atopic dermatitis EA80 Phase 1/2 [7]
Vitiligo ED63.0 Phase 1/2 [7]
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 306.4
Topological Polar Surface Area (xlogp) 2.1
Rotatable Bond Count (rotbonds) 4
Hydrogen Bond Donor Count (hbonddonor) 1
Hydrogen Bond Acceptor Count (hbondacc) 4
Chemical Identifiers
Formula
C17H18N6
IUPAC Name
(3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile
Canonical SMILES
C1CCC(C1)[C@@H](CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3
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
Cross-matching ID
PubChem CID
25126798
ChEBI ID
CHEBI:66919
CAS Number
941678-49-5
DrugBank ID
DB08877
TTD ID
D04LKS
ACDINA ID
D00611

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Janus kinase 1 (JAK-1) TT6DM01 JAK1_HUMAN Modulator [8]
Janus kinase 2 (JAK-2) TTRMX3V JAK2_HUMAN Modulator [8]
Urokinase plasminogen activator surface receptor (PLAUR) TTPRL03 UPAR_HUMAN Inhibitor [9]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Ruxolitinib
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Fedratinib DM4ZBK6 Minor Decreased metabolism of Ruxolitinib caused by Fedratinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [23]
Coadministration of a Drug Treating the Disease Different from Ruxolitinib (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Ivosidenib DM8S6T7 Moderate Increased metabolism of Ruxolitinib caused by Ivosidenib mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [24]
Arn-509 DMT81LZ Moderate Increased metabolism of Ruxolitinib caused by Arn-509 mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [24]
Pexidartinib DMS2J0Z Moderate Increased metabolism of Ruxolitinib caused by Pexidartinib mediated induction of CYP450 enzyme. Bone/articular cartilage neoplasm [2F7B] [24]
Tucatinib DMBESUA Major Decreased metabolism of Ruxolitinib caused by Tucatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [24]
Palbociclib DMD7L94 Minor Decreased metabolism of Ruxolitinib caused by Palbociclib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [23]
Levomilnacipran DMV26S8 Moderate Increased risk of bleeding by the combination of Ruxolitinib and Levomilnacipran. Chronic pain [MG30] [25]
Regorafenib DMHSY1I Major Increased risk of bleeding by the combination of Ruxolitinib and Regorafenib. Colorectal cancer [2B91] [23]
Lumacaftor DMCLWDJ Moderate Increased metabolism of Ruxolitinib caused by Lumacaftor mediated induction of CYP450 enzyme. Cystic fibrosis [CA25] [24]
MK-8228 DMOB58Q Minor Decreased metabolism of Ruxolitinib caused by MK-8228 mediated inhibition of CYP450 enzyme. Cytomegaloviral disease [1D82] [23]
Vortioxetine DM6F1PU Moderate Increased risk of bleeding by the combination of Ruxolitinib and Vortioxetine. Depression [6A70-6A7Z] [25]
Apigenin DMI3491 Minor Increased risk of bleeding by the combination of Ruxolitinib and Apigenin. Discovery agent [N.A.] [26]
Stiripentol DMMSDOY Minor Decreased metabolism of Ruxolitinib caused by Stiripentol mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [23]
Tazemetostat DMWP1BH Moderate Increased metabolism of Ruxolitinib caused by Tazemetostat mediated induction of CYP450 enzyme. Follicular lymphoma [2A80] [24]
Avapritinib DMK2GZX Major Increased risk of bleeding by the combination of Ruxolitinib and Avapritinib. Gastrointestinal stromal tumour [2B5B] [23]
Cobicistat DM6L4H2 Major Decreased metabolism of Ruxolitinib caused by Cobicistat mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [24]
Teriflunomide DMQ2FKJ Major Additive immunosuppressive effects by the combination of Ruxolitinib and Teriflunomide. Hyper-lipoproteinaemia [5C80] [27]
Berotralstat DMWA2DZ Minor Decreased metabolism of Ruxolitinib caused by Berotralstat mediated inhibition of CYP450 enzyme. Innate/adaptive immunodeficiency [4A00] [23]
Suvorexant DM0E6S3 Minor Decreased metabolism of Ruxolitinib caused by Suvorexant mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [23]
Ceritinib DMB920Z Major Decreased metabolism of Ruxolitinib caused by Ceritinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [24]
PF-06463922 DMKM7EW Moderate Increased metabolism of Ruxolitinib caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [24]
Selpercatinib DMZR15V Minor Decreased metabolism of Ruxolitinib caused by Selpercatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [23]
Idelalisib DM602WT Major Decreased metabolism of Ruxolitinib caused by Idelalisib mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [24]
IPI-145 DMWA24P Minor Decreased metabolism of Ruxolitinib caused by IPI-145 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [23]
Acalabrutinib DM7GCVW Major Increased risk of bleeding by the combination of Ruxolitinib and Acalabrutinib. Mature B-cell lymphoma [2A85] [28]
Ibrutinib DMHZCPO Major Increased risk of bleeding by the combination of Ruxolitinib and Ibrutinib. Mature B-cell lymphoma [2A85] [29]
Ponatinib DMYGJQO Major Increased risk of bleeding by the combination of Ruxolitinib and Ponatinib. Mature B-cell lymphoma [2A85] [30]
Vemurafenib DM62UG5 Moderate Increased metabolism of Ruxolitinib caused by Vemurafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [24]
Dabrafenib DMX6OE3 Moderate Increased metabolism of Ruxolitinib caused by Dabrafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [24]
Tecfidera DM2OVDT Moderate Additive immunosuppressive effects by the combination of Ruxolitinib and Tecfidera. Multiple sclerosis [8A40] [31]
Siponimod DM2R86O Major Additive immunosuppressive effects by the combination of Ruxolitinib and Siponimod. Multiple sclerosis [8A40] [32]
Ocrelizumab DMEZ2KH Moderate Additive immunosuppressive effects by the combination of Ruxolitinib and Ocrelizumab. Multiple sclerosis [8A40] [33]
Ozanimod DMT6AM2 Major Additive immunosuppressive effects by the combination of Ruxolitinib and Ozanimod. Multiple sclerosis [8A40] [23]
Netupitant DMEKAYI Minor Decreased metabolism of Ruxolitinib caused by Netupitant mediated inhibition of CYP450 enzyme. Nausea/vomiting [MD90] [23]
Entrectinib DMMPTLH Minor Decreased metabolism of Ruxolitinib caused by Entrectinib mediated inhibition of CYP450 enzyme. Non-small cell lung cancer [2C25] [23]
Rucaparib DM9PVX8 Minor Decreased metabolism of Ruxolitinib caused by Rucaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [23]
Abametapir DM2RX0I Moderate Decreased metabolism of Ruxolitinib caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [34]
Lefamulin DME6G97 Moderate Decreased metabolism of Ruxolitinib caused by Lefamulin mediated inhibition of CYP450 enzyme. Pneumonia [CA40] [23]
Enzalutamide DMGL19D Moderate Increased metabolism of Ruxolitinib caused by Enzalutamide mediated induction of CYP450 enzyme. Prostate cancer [2C82] [24]
Anthrax vaccine DM9GSWY Moderate Antagonize the effect of Ruxolitinib when combined with Anthrax vaccine. Sepsis [1G40-1G41] [35]
Voxelotor DMCS6M5 Minor Decreased metabolism of Ruxolitinib caused by Voxelotor mediated inhibition of CYP450 enzyme. Sickle-cell disorder [3A51] [23]
Telotristat ethyl DMDIYFZ Moderate Increased metabolism of Ruxolitinib caused by Telotristat ethyl mediated induction of CYP450 enzyme. Small intestine developmental anomaly [DA90] [23]
Larotrectinib DM26CQR Minor Decreased metabolism of Ruxolitinib caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [23]
LEE011 DMMX75K Minor Decreased metabolism of Ruxolitinib caused by LEE011 mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [23]
Fostamatinib DM6AUHV Moderate Decreased metabolism of Ruxolitinib caused by Fostamatinib mediated inhibition of CYP450 enzyme. Thrombocytopenia [3B64] [36]
Elagolix DMB2C0E Moderate Increased metabolism of Ruxolitinib caused by Elagolix mediated induction of CYP450 enzyme. Uterine fibroid [2E86] [24]
Betrixaban DM2C4RF Major Increased risk of bleeding by the combination of Ruxolitinib and Betrixaban. Venous thromboembolism [BD72] [37]
⏷ Show the Full List of 46 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
Hydroxypropyl cellulose E00632 Not Available Binding agent; Coating agent; Emulsifying agent; Film/Membrane-forming agent; Modified-release agent; Suspending agent; Viscosity-controlling agent
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Povidone E00667 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Silicon dioxide E00670 Not Available Anticaking agent; Opacifying agent; Viscosity-controlling agent
Hydrophobic colloidal silica E00285 24261 Anticaking agent; Emulsion stabilizing agent; Glidant; Suspending agent; Viscosity-controlling agent
Cellulose microcrystalline E00698 Not Available Adsorbent; Suspending agent; Diluent
⏷ Show the Full List of 7 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Ruxolitinib Phosphate eq 5mg base tablet eq 5mg base Tablet Oral
Ruxolitinib Phosphate eq 10mg base tablet eq 10mg base Tablet Oral
Ruxolitinib Phosphate eq 15mg base tablet eq 15mg base Tablet Oral
Ruxolitinib Phosphate eq 20mg base tablet eq 20mg base Tablet Oral
Ruxolitinib Phosphate eq 25mg base tablet eq 25mg base Tablet Oral
Ruxolitinib 10 mg tablet 10 mg Oral Tablet Oral
Ruxolitinib 15 mg tablet 15 mg Oral Tablet Oral
Ruxolitinib 20 mg tablet 20 mg Oral Tablet Oral
Ruxolitinib 25 mg tablet 25 mg Oral Tablet Oral
Ruxolitinib 5 mg tablet 5 mg Oral Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
2 URL: 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).
3 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.
4 Ruxolitinib versus standard therapy for the treatment of polycythemia vera. N Engl J Med. 2015 Jan 29;372(5):426-35.
5 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
6 ClinicalTrials.gov (NCT02117479) Study of Ruxolitinib in Pancreatic Cancer Patients (Janus 1). U.S. National Institutes of Health.
7 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
8 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
9 Urokinase-type plasminogen activator receptor signaling is critical in nasopharyngeal carcinoma cell growth and metastasis.Cell Cycle. 2014;13(12):1958-69.
10 Selective JAK inhibitors in development for rheumatoid arthritis. Expert Opin Investig Drugs. 2014 Aug;23(8):1067-77.
11 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
12 Genetic determinants of response and survival in momelotinib-treated patients with myelofibrosis.Leukemia.2015 Mar;29(3):741-4.
13 Emerging drugs for the therapy of primary and post essential thrombocythemia, post polycythemia vera myelofibrosis. Expert Opin Emerg Drugs. 2009 Sep;14(3):471-9.
14 National Cancer Institute Drug Dictionary (drug id 609888).
15 Company report (Portola Pharmaceuticals)
16 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
17 URL: 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. (Target id: 2048).
18 Clinical pipeline report, company report or official report of Concert Pharmaceuticals.
19 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
20 URL: 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. (Target id: 2047).
21 Clinical pipeline report, company report or official report of Aclaris Therapeutics.
22 ClinicalTrials.gov (NCT03759340) ATI-502 Topical Solution for the Treatment of Alopecia Areata (AA), Alopecia Universalis (AU) and Alopecia Totalis (AT). U.S. National Institutes of Health.
23 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
24 Product Information. Jakafi (ruxolitinib). Incyte Corporation, Wilmington, DE.
25 Alderman CP, Moritz CK, Ben-Tovim DI "Abnormal platelet aggregation associated with fluoxetine therapy." Ann Pharmacother 26 (1992): 1517-9. [PMID: 1482806]
26 Heck AM, DeWitt BA, Lukes AL "Potential interactions between alternative therapies and warfarin." Am J Health Syst Pharm 57 (2000): 1221-7 quiz 1228-30. [PMID: 10902065]
27 Product Information. Arava (leflunomide). Hoechst Marion-Roussel Inc, Kansas City, MO.
28 Product Information. Calquence (acalabrutinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
29 Agencia Espaola de Medicamentos y Productos Sanitarios Healthcare "Centro de informacion online de medicamentos de la AEMPS - CIMA.".
30 Product Information. Iclusig (ponatinib). Ariad Pharmaceuticals Inc, Cambridge, MA.
31 Product Information. Vumerity (diroximel fumarate). Alkermes, Inc, Cambridge, MA.
32 Cerner Multum, Inc. "Australian Product Information.".
33 Product Information. Ocrevus (ocrelizumab). Genentech, South San Francisco, CA.
34 Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
35 CDC. Centers for Disease Control and Prevention/ "Recommendations of the advisory committtee on immunization practices (ACIP): use of vaccines and immune globulins in persons with altered immunocompetence." MMWR Morb Mortal Wkly Rep 42(RR-04) (1993): 1-18. [PMID: 20300058]
36 Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.
37 Product Information. Bevyxxa (betrixaban). Portola Pharmaceuticals, South San Francisco, CA.