Ruxolitinib
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2011
- First approval year
- 2011
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Ruxolitinib
- Molecular weight
- 306.37
- Structure (SMILES)
- N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1
- jakavi
- Jakavi
- (R)-RUXOLITINIB
- 1h pyrazole 1 propanenitrile beta cyclopentyl 4 7h pyrrolo 2 3 d pyrimidin 4 yl beta r
- 1H-PYRAZOLE-1-PROPANENITRILE, .BETA.-CYCLOPENTYL-4-(7H-PYRROLO(2,3-D)PYRIMIDIN-4-YL)-, (.BETA.R)-
- drug inc424
- inc 424
- INC-424
- inc424
- INC424
- incb 018424
- incb 018424 salt
- incb 18424
- INCB-018424
- INCB-018424 SALT
- INCB-18424
- incb018424
- INCB018424
- INCB018424 (RUXOLITINIB)
- incb018424 r ruxolitinib
- incb018424 ruxolitinib
- INCB018424(R)-RUXOLITINIB
- incb18424
- INCB18424
- jakafi
- JAKAFI
- jakavi
And 26 more, listed on the interactive page.
- CAS registry numbers
- 941678-49-5
- ChEMBL ID
- CHEMBL1789941
- InChIKey
- HFNKQEVNSGCOJV-OAHLLOKOSA-N
- PubChem compound IDs
- 25126798
- FDA ingredient codes (UNII)
- 82S8X8XX8H
- D11AH09
- L01EJ01
Sources for recorded values
- 1193325
- 1193326
- Applicant
- INCYTE CORP
- Approval date
- 16 Nov 2011
- Application number
- NDA202192
- Status
- Authorised
- Status date
- 23 Aug 2012
- Authorisation date
- 23 Aug 2012
- Approved indications
- Myelofibrosis (MF)Jakavi is indicated for the treatment of disease related splenomegaly or symptoms in adult patients with primary myelofibrosis (also known as chronic idiopathic myelofibrosis), post polycythaemia vera myelofibrosis or post essential thrombocythaemia myelofibrosis.Polycythaemia vera (PV)Jakavi is indicated for the treatment of adult patients with polycythaemia vera who are resistant to or intolerant of hydroxyurea.Graft versus host disease (GvHD)Acute GvHDJakavi is indicated for the treatment of adults and paediatric patients aged 28 days and older with acute graft versus host disease who have inadequate response to corticosteroids or other systemic therapies (see section 5.1).Chronic GvHDJakavi is indicated for the treatment of adults and paediatric patients aged 6 months and older with chronic graft versus host disease who have inadequate response to corticosteroids or other systemic therapies (see section 5.1). Myelofibrosis (MF)Jakavi is indicated for the treatment of disease related splenomegaly or symptoms in adult patients with primary myelofibrosis (also known as chronic idiopathic myelofibrosis), post polycythaemia vera myelofibrosis or post essential thrombocythaemia myelofibrosis.Polycythaemia vera (PV)Jakavi is indicated for the treatment of adult patients with polycythaemia vera who are resistant to or intolerant of hydroxyurea.Graft versus host disease (GvHD)Acute GvHDJakavi is indicated for the treatment of adults and paediatric patients aged 28 days and older with acute graft versus host disease who have inadequate response to corticosteroids or other systemic therapies (see section 5.1).Chronic GvHDJakavi is indicated for the treatment of adults and paediatric patients aged 6 months and older with chronic graft versus host disease who have inadequate response to corticosteroids or other systemic therapies (see section 5.1).
- Product number
- EMEA/H/C/002464
- Authorisation holder
- Novartis Europharm Limited
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 0
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- No
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Graft vs Host Disease
- Myeloproliferative Disorders
- Polycythemia Vera
European medicines record
- Patents
- 0
- Designations
- 5
- First in class
- Yes
- Fast track
- Yes
- Breakthrough designation
- Yes
- Orphan designation
- No
- Priority review
- Yes
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Boxed warning
- Yes
- Pharmacology name
- ruxolitinib
- Type
- Synthetic organic
- Drug name stem
- -tinib
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- topical
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- Janus kinase 2
- Gene symbol
- JAK2
- Protein identifier
- O60674
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- Janus kinase 2
- Gene symbol
- JAK2
- Protein identifier
- O60674
- Median affinity
- 8.05
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- Janus kinase 1
- Gene symbol
- JAK1
- Protein identifier
- P23458
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- Janus kinase 1
- Gene symbol
- JAK1
- Protein identifier
- P23458
- Median affinity
- 8.22
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- tyrosine kinase 2
- Gene symbol
- TYK2
- Protein identifier
- P29597
- Median affinity
- 7.52
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- tyrosine kinase 2
- Gene symbol
- TYK2
- Protein identifier
- P29597
- Median affinity
- 9.26
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- Janus kinase 3
- Gene symbol
- JAK3
- Protein identifier
- P52333
- Median affinity
- 6.31
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- Janus kinase 3
- Gene symbol
- JAK3
- Protein identifier
- P52333
- Median affinity
- 8.49
- Affinity units
- pIC50
- Mechanism
- Tyrosine-protein kinase JAK1 inhibitor
- Action type
- Inhibitor
- Target
- Tyrosine-protein kinase JAK1
- Mechanism
- Tyrosine-protein kinase JAK2 inhibitor
- Action type
- Inhibitor
- Target
- Tyrosine-protein kinase JAK2
- Mechanism
- Tyrosine-protein kinase JAK3 inhibitor
- Action type
- Inhibitor
- Target
- Tyrosine-protein kinase JAK3
- Mechanism
- Tyrosine-protein kinase TYK2 inhibitor
- Action type
- Inhibitor
- Target
- Non-receptor tyrosine-protein kinase TYK2
- Action type
- Inhibitor
- Gene symbol
- JAK2
- Protein identifier
- O60674
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- JAK1
- Protein identifier
- P23458
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- Leukemia, Lymphocytic, Chronic, B-Cell
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000095
- Subject identifier
- D015451
- Condition
- Carcinoma, Squamous Cell
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000181
- Subject identifier
- D002294
- Condition
- Hodgkin Disease
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000183
- Subject identifier
- D006689
- Condition
- Leukemia, Biphenotypic, Acute
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000209
- Subject identifier
- D015456
- Condition
- Precursor Cell Lymphoblastic Leukemia-Lymphoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000220
- Subject identifier
- D054198
- Condition
- Leukemia, Myeloid, Acute
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000222
- Subject identifier
- D015470
- Condition
- Dermatitis, Atopic
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000274
- Subject identifier
- D003876
- Condition
- Breast Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000305
- Subject identifier
- D001943
- Condition
- Leukemia, Myelogenous, Chronic, BCR-ABL Positive
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000339
- Subject identifier
- D015464
- Condition
- Thrombocythemia, Essential
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000479
- Subject identifier
- D013920
- Condition
- Glioblastoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000519
- Subject identifier
- D005909
- Condition
- Leukemia
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000565
- Subject identifier
- D007938
- Condition
- Lymphoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000574
- Subject identifier
- D008223
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Psoriasis
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000676
- Subject identifier
- D011565
- Condition
- Arthritis, Rheumatoid
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000685
- Subject identifier
- D001172
- Condition
- Severe Acute Respiratory Syndrome
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000694
- Subject identifier
- D045169
- Condition
- HIV Infections
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000764
- Subject identifier
- D015658
- Condition
- Multiple Myeloma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0001378
- Subject identifier
- D009101
- Condition
- Hematologic Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0001642
- Subject identifier
- D019337
- Condition
- Polycythemia Vera
- Highest recorded phase
- 3
- Condition identifier
- EFO:0002429
- Subject identifier
- D011087
- Condition
- Primary Myelofibrosis
- Highest recorded phase
- 3
- Condition identifier
- EFO:0002430
- Subject identifier
- D055728
- Condition
- Pancreatic Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0002618
- Subject identifier
- D010190
- Condition
- Carcinoma, Non-Small-Cell Lung
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003060
- Subject identifier
- D002289
- Condition
- Pneumonia
- Highest recorded phase
- 1
- Condition identifier
- EFO:0003106
- Subject identifier
- D011014
And 41 more, listed on the interactive page.
- Condition identifier
- EFO_0000095
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000181
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000183
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000198
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000222
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000274
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000305
- Condition identifier
- EFO_0000339
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000398
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000479
- Condition identifier
- EFO_0000565
- Condition identifier
- EFO_0000574
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0000676
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000685
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000694
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000764
- Highest recorded phase
- 2
- Condition identifier
- EFO_0001378
- Highest recorded phase
- 2
- Condition identifier
- EFO_0002429
- Highest recorded phase
- 3
- Condition identifier
- EFO_0002430
- Highest recorded phase
- 3
- Condition identifier
- EFO_0002618
- Highest recorded phase
- 3
- Condition identifier
- EFO_0003060
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003860
- Highest recorded phase
- 3
- Condition identifier
- EFO_0004192
- Highest recorded phase
- 2
- Condition identifier
- EFO_0004208
And 135 more, listed on the interactive page.
- Warning
- Black Box Warning
- Country
- United States
- Warning
- Black Box Warning
- Effect
- infectious disease
- Country
- United States
- Event
- acute myeloid leukaemia
- Reports
- 173
- Reporting signal score
- 316.379
- Event
- anaemia
- Reports
- 1,171
- Reporting signal score
- 1,037.85
- Event
- blast cell count increased
- Reports
- 83
- Reporting signal score
- 280.026
- Event
- blood count abnormal
- Reports
- 305
- Reporting signal score
- 593.793
- Event
- blood lactate dehydrogenase increased
- Reports
- 154
- Reporting signal score
- 181.919
- Event
- contusion
- Reports
- 343
- Reporting signal score
- 292.158
- Event
- drug hypersensitivity
- Reports
- 14
- Reporting signal score
- 196.816
- Event
- fatigue
- Reports
- 1,106
- Reporting signal score
- 222.261
- Event
- febrile neutropenia
- Reports
- 302
- Reporting signal score
- 191.291
- Event
- haematocrit decreased
- Reports
- 182
- Reporting signal score
- 208.568
- Event
- haemoglobin decreased
- Reports
- 990
- Reporting signal score
- 1,251.47
- Event
- injection site pain
- Reports
- 2
- Reporting signal score
- 186.564
- Event
- myelofibrosis
- Reports
- 233
- Reporting signal score
- 827.201
- Event
- night sweats
- Reports
- 179
- Reporting signal score
- 210.937
- Event
- platelet count decreased
- Reports
- 977
- Reporting signal score
- 1,273.84
- Event
- platelet count increased
- Reports
- 419
- Reporting signal score
- 1,041.99
- Event
- primary myelofibrosis
- Reports
- 44
- Reporting signal score
- 184.83
- Event
- red blood cell count decreased
- Reports
- 259
- Reporting signal score
- 367.117
- Event
- second primary malignancy
- Reports
- 300
- Reporting signal score
- 764.502
- Event
- splenomegaly
- Reports
- 541
- Reporting signal score
- 1,542
- Event
- squamous cell carcinoma
- Reports
- 143
- Reporting signal score
- 227.727
- Event
- thrombocytopenia
- Reports
- 608
- Reporting signal score
- 406.87
- Event
- weight increased
- Reports
- 518
- Reporting signal score
- 317.511
- Event
- white blood cell count increased
- Reports
- 408
- Reporting signal score
- 555.89
- NCT00044304
- NCT00550043
- NCT00617994
- NCT00820950
- NCT00638378
- NCT00639002
- NCT03110822
- NCT03773107
- NCT06209606
- NCT06225310
- NCT00726232
- NCT00952289
- NCT01348490
- NCT01375140
- NCT02076191
- NCT02267278
- NCT02718300
- NCT03123588
- NCT03144687
- NCT00934544
- NCT01317875
- NCT01340651
- NCT01369498
- NCT01433445
- NCT01493414
And 180 more, listed on the interactive page.
- Route
- Topical
- How often
- Twice daily
- Apply a thin layer
- Do not use with occlusive dressings
- Hydrogen bond acceptors
- 5
- Hydrogen bond donors
- 1
- Polar surface area
- 83.18
- Calculated partition coefficient (ALogP)
- 3.47
- Calculated partition coefficient (XLogP)
- 2.1
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 4
- Heavy atoms
- 23
- Molecular formula
- C17H18N6
- Monoisotopic mass
- 306.15929460
- Natural product
- Yes
- 50881-005
- 50881-010
- 50881-011
- 50881-015
- 50881-020
- 50881-022
- 50881-025
- 50881-033
- 50881-044
- 50881-055
- Recorded assays
- 1,828
- Active assays
- 483
- Confirmatory
- Other
- Screening
These details could not be displayed.
Related records
Trials (32)
- A Phase 1 Study of Ruxolitinib, Steroids and Lenalidomide for Relapsed/Refractory Multiple Myeloma (RRMM) Patients
- A Phase Ib/II Dose-finding Study to Assess the Safety and Efficacy of LDE225 + INC424 in Patients With MF
- A Real-world Study on the Influencing Factors of Efficacy of Ruxolitinib Cream in Vitiligo
- A Study to Assess Efficacy and Safety of CGB-500, 1% Tofacitinib Versus an Active Comparator for Atopic Dermatitis
- A Study to Evaluate the Safety and Efficacy of Ruxolitinib Cream With Phototherapy in Participants With Vitiligo
- A Study to Evaluate the Safety and Efficacy of Ruxolitinib Phosphate Cream Applied Topically to Adults With Atopic Dermatitis
- A Study to Evaluate the Safety and Tolerability of Maximal Use Ruxolitinib Cream
- A Study to Find the Maximum Tolerated Dose of the Experimental Combination of the Drugs INC424 and BKM120 in Patients With Primary or Secondary Myelofibrosis
- A Study, Comparing Ruxolitinib Topical Cream 1.5% (Taro Pharmaceuticals U.S.A, Inc.) to OPZELURA (Ruxolitinib) Cream for the Treatment of Mild-to-Moderate Atopic Dermatitis.
- A Trial Using ANAKINRA, TOCILIZUMAB Alone or in Association With RUXOLITINIB in Severe Stage 2b and 3 of COVID19-associated Disease
- Activity, Safety and Pharmacokinetics in Pediatric Subjects With Moderate and Severe Chronic Graft vs. Host Disease After Allogeneic Stem Cell Transplant
- Comparing the Therapeutic Effects of Using Ruxolitinib and Steroids Concurrently to Steroids Alone as Initial Treatment In Patients Diagnosed With Chronic Graft-versus-host Disease at a Grade of Moderate or Higher Severity
- Efficacy and Safety of Ruxolitinib Cream in Chinese Children Aged 2-11 Years With Non-segmental Vitiligo
- Exploratory Phase II Study of INC424 Patients With Primary Myelofibrosis (PMF) or Post Polycythaemia Myelofibrosis (PPV MF) or Post Essential Thrombocythaemia Myelofibrosis (PET-MF)
- INC424 for Patients With Primary Myelofibrosis, Post Polycythemia Myelofibrosis or Post-essential Thrombocythemia Myelofibrosis.
- Low Dose Ruxolitinib in Combination With Methylprednisolone
- Phase I Study of the Combination of Afatinib and Ruxolitinib in Patients With Treatment-refractory Non-Small Cell Lung Cancer (NSCLC)
- Pilot Study Using Changes in Serum BCMA to Determine Disease Progression in Multiple Myeloma
- Ruxolitinib and Chidamide for Acute T Cell Lymphoblast Leukemia/ Lymphoblastic Lymphoma
- Ruxolitinib and Chidamide Intensified Bu/CY Conditioning Regimen
Approved for (2)
- Cancer
- Neoplasm
In development for (69)
- Acquired polycythemia vera Phase 3
- Acute lymphoblastic leukemia Phase 2
- Acute myeloid leukemia Phase 2
- Alopecia areata Phase 2
- Anemia Phase 2
- Atopic eczema Phase 3
- B-cell chronic lymphocytic leukemia Phase 2
- Beta-thalassemia major Phase 2
- Bone marrow neoplasm Phase 3
- Breast cancer Phase 2
- Breast carcinoma Phase 2
- Bronchiolitis obliterans syndrome Phase 2
- Chronic graft versus host disease Phase 2
- Chronic myeloid leukemia Phase 2
- Classic Hodgkin lymphoma Phase 2
- Colorectal carcinoma Phase 2
- COVID-19 Phase 3
- Dermatitis Phase 1
- Dermatomyositis Phase 2
- Discoid lupus erythematosus Phase 2
Other linked conditions (2)
- Acute graft versus host disease
- Chuvash polycythemia