Ruxolitinib
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Also known as INC-424INC424INCB-018424INCB-18424INCB018424Jakavis-S-ruxolitinibJAKAFIRUXOLITINIB PHOSPHATEINCB-018424 SALTINCB018424(R)-RUXOLITINIBINCB018424 (RUXOLITINIB)RUXOLITINIB (INCB018424)(R)-RUXOLITINIBINCB18424RuxolitinibJakafiRuxolitinib phosphateÊRuxolitinib phosphateÂ
Summary
Ruxolitinib (CHEMBL1789941) is an approved small-molecule antineoplastic agent (ATC D11AH09) targeting JAK1, JAK2, and JAK3; indicated across 66 conditions including neoplasm and primary myelofibrosis; with CIViC clinical evidence for 13 variant-indication associations (e.g. PCM1::JAK2 Fusion OR BCR::JAK2 Fusion in myeloid neoplasm).
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: D11AH09 (+1 more)
- Targets: 4 (JAK1, JAK2, JAK3…)
- Indications: 66 conditions
- Clinical trials: 373
- Precision-oncology evidence (CIViC): 13 variant–indication associations
- Chemistry: 306.4 Da · C17H18N6
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1789941 |
| Name | Ruxolitinib |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 25126798 |
| ChEBI | CHEBI:66919 |
| ATC | D11AH09, L01EJ01 |
| Molecular formula | C17H18N6 |
| Molecular weight | 306.4 |
| InChIKey | HFNKQEVNSGCOJV-OAHLLOKOSA-N |
SMILES: C1CCC(C1)[C@@H](CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3
IUPAC name: (3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile
ChEBI definition: A pyrazole substituted at position 1 by a 2-cyano-1-cyclopentylethyl group and at position 3 by a pyrrolo[2,3-d]pyrimidin-4-yl group. Used as the phosphate salt for the treatment of patients with intermediate or high-risk myelofibrosis, including primary myelofibrosis, post-polycythemia vera myelofibrosis and post-essential thrombocythemia myelofibrosis.
Pharmacological roles (ChEBI): antineoplastic agent, EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor.
Also known as: INC-424, INC424, INCB-018424, INCB-18424, INCB018424, Jakavi, Ruxolitinib, s-, S-ruxolitinib, JAKAFI, RUXOLITINIB PHOSPHATE, INCB-018424 SALT
Parent form; salt/anhydrous children: CHEMBL1795071, CHEMBL4594381, CHEMBL4594382
Patent coverage: 4,564 distinct patent families (11,547 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 10,593 (92%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| JAK1 | Janus kinase 1 | Inhibition | 10.05 | 2.8% | P23458 |
| JAK2 | Janus kinase 2 | Inhibition | 8.05 | 0.7% | O60674 |
| JAK3 | Janus kinase 3 | Inhibition | 6.31 | 0.6% | P52333 |
| TYK2 | tyrosine kinase 2 | Inhibition | 7.52 | 0.8% | P29597 |
Broader ChEMBL bioactivity targets: 142 (assay-derived). Sample: Leucine-rich repeat serine/threonine-protein kinase 2, Rhodopsin kinase GRK7, Serine/threonine-protein kinase TAO2, Serine/threonine-protein kinase/endoribonuclease IRE1, Serine/threonine-protein kinase OSR1, STE20/SPS1-related proline-alanine-rich protein kinase, Mitogen-activated protein kinase kinase kinase 15, Microtubule-associated serine/threonine-protein kinase 1, Serine/threonine-protein kinase SBK1, Tyrosine-protein kinase JAK2.
Bioactivity
ChEMBL activities: 353 potent at pChembl ≥ 5 of 362 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| JAK2 | 10.44 | IC50 | 0.04 | nM | CHEMBL_ACT_25701597 |
| JAK2 | 10.44 | IC50 | 0.04 | nM | CHEMBL_ACT_25938456 |
| JAK2 | 10.44 | Kd | 0.04 | nM | CHEMBL_ACT_7571811 |
| JAK2 | 10.25 | IC50 | 0.06 | nM | CHEMBL_ACT_18141618 |
| JAK2 | 10.25 | IC50 | 0.06 | nM | CHEMBL_ACT_18665620 |
| JAK1 | 10.05 | Ki | 0.09 | nM | CHEMBL_ACT_12138162 |
| JAK1 | 10.05 | IC50 | 0.09 | nM | CHEMBL_ACT_25701589 |
| JAK1 | 10.05 | IC50 | 0.09 | nM | CHEMBL_ACT_25938455 |
| JAK2 | 10 | Ki | 0.1 | nM | CHEMBL_ACT_12069216 |
| JAK2 | 10 | Ki | 0.1 | nM | CHEMBL_ACT_13317341 |
| JAK2 | 9.92 | IC50 | 0.12 | nM | CHEMBL_ACT_16515204 |
| JAK1 | 9.7 | Ki | 0.2 | nM | CHEMBL_ACT_12069217 |
| JAK1 | 9.7 | Ki | 0.2 | nM | CHEMBL_ACT_13317342 |
| JAK2 | 9.7 | IC50 | 0.2 | nM | CHEMBL_ACT_15112131 |
| JAK2 | 9.62 | Ki | 0.24 | nM | CHEMBL_ACT_12138165 |
| TYK2 | 9.4 | IC50 | 0.4 | nM | CHEMBL_ACT_13901940 |
| JAK2 | 9.4 | IC50 | 0.4 | nM | CHEMBL_ACT_22812634 |
| TYK2 | 9.4 | IC50 | 0.4 | nM | CHEMBL_ACT_25701608 |
| JAK1 | 9.37 | IC50 | 0.43 | nM | CHEMBL_ACT_16515210 |
| TYK2 | 9.3 | Ki | 0.5 | nM | CHEMBL_ACT_12069214 |
| TYK2 | 9.3 | Ki | 0.5 | nM | CHEMBL_ACT_13317339 |
| TYK2 | 9.3 | Ki | 0.5 | nM | CHEMBL_ACT_13317472 |
| TYK2 | 9.26 | Ki | 0.55 | nM | CHEMBL_ACT_12138160 |
| JAK1 | 9.22 | IC50 | 0.6 | nM | CHEMBL_ACT_13902022 |
| JAK2 | 9.22 | IC50 | 0.6 | nM | CHEMBL_ACT_18992766 |
| JAK2 | 9.15 | IC50 | 0.7 | nM | CHEMBL_ACT_13901996 |
| TYK2 | 9.14 | IC50 | 0.72 | nM | CHEMBL_ACT_16515192 |
| JAK1 | 9.1 | IC50 | 0.8 | nM | CHEMBL_ACT_13282600 |
| JAK2 | 9.1 | Kd | 0.8 | nM | CHEMBL_ACT_25839811 |
| TYK2 | 9.05 | Kd | 0.9 | nM | CHEMBL_ACT_7571747 |
Target pathways
Aggregated over 4 target gene(s): JAK1, JAK2, JAK3, TYK2.
Top Reactome pathways
86 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Interleukin-4 and Interleukin-13 signaling | 4 | JAK1, JAK2, JAK3, TYK2 |
| Interleukin-20 family signaling | 4 | JAK1, JAK2, JAK3, TYK2 |
| Potential therapeutics for SARS | 4 | JAK1, JAK2, JAK3, TYK2 |
| Interleukin-6 signaling | 3 | JAK1, JAK2, TYK2 |
| MAPK3 (ERK1) activation | 3 | JAK1, JAK2, TYK2 |
| MAPK1 (ERK2) activation | 3 | JAK1, JAK2, TYK2 |
| Cytokine Signaling in Immune system | 3 | JAK1, JAK2, JAK3 |
| Signal Transduction | 3 | JAK1, JAK2, JAK3 |
| Disease | 3 | JAK1, JAK2, JAK3 |
| Immune System | 3 | JAK1, JAK2, JAK3 |
| Signaling by Interleukins | 3 | JAK1, JAK2, JAK3 |
| Interleukin-2 family signaling | 3 | JAK1, JAK2, JAK3 |
| Interleukin-3, Interleukin-5 and GM-CSF signaling | 3 | JAK1, JAK2, JAK3 |
| Infectious disease | 3 | JAK1, JAK2, JAK3 |
| RAF/MAP kinase cascade | 3 | JAK1, JAK2, JAK3 |
| MAPK family signaling cascades | 3 | JAK1, JAK2, JAK3 |
| MAPK1/MAPK3 signaling | 3 | JAK1, JAK2, JAK3 |
| IL-6-type cytokine receptor ligand interactions | 3 | JAK1, JAK2, TYK2 |
| Interleukin-35 Signalling | 3 | JAK1, JAK2, TYK2 |
| Interleukin-12 signaling | 3 | JAK1, JAK2, TYK2 |
| Interleukin-27 signaling | 3 | JAK1, JAK2, TYK2 |
| Interleukin receptor SHC signaling | 3 | JAK1, JAK2, JAK3 |
| Signaling by CSF3 (G-CSF) | 3 | JAK1, JAK2, TYK2 |
| SARS-CoV Infections | 3 | JAK1, JAK2, JAK3 |
| Inactivation of CSF3 (G-CSF) signaling | 3 | JAK1, JAK2, TYK2 |
| Viral Infection Pathways | 3 | JAK1, JAK2, JAK3 |
| Activation of STAT3 by cadherin engagement | 3 | JAK1, JAK2, TYK2 |
| RAF-independent MAPK1/3 activation | 2 | JAK1, JAK2 |
| Interleukin-7 signaling | 2 | JAK1, JAK3 |
| Interleukin-12 family signaling | 2 | JAK1, JAK2 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| protein phosphorylation | 4 |
| cell surface receptor signaling pathway via JAK-STAT | 4 |
| cytokine-mediated signaling pathway | 4 |
| cell differentiation | 4 |
| intracellular signal transduction | 4 |
| growth hormone receptor signaling pathway via JAK-STAT | 4 |
| regulation of cell-cell adhesion | 4 |
| type II interferon-mediated signaling pathway | 3 |
| cellular response to virus | 3 |
| regulation of receptor signaling pathway via JAK-STAT | 3 |
| regulation of alpha-beta T cell activation | 3 |
| interleukin-15-mediated signaling pathway | 2 |
| interleukin-4-mediated signaling pathway | 2 |
| interleukin-2-mediated signaling pathway | 2 |
| interleukin-7-mediated signaling pathway | 2 |
Indications & clinical
Indications
66 indications (3 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| neoplasm | 4 | MONDO:0005070 | EFO:0000616 |
| primary myelofibrosis | 3 | MONDO:0009692 | EFO:0002430 |
| graft versus host disease | 3 | MONDO:0013730 | EFO:0004599 |
| vitiligo | 3 | MONDO:0008661 | EFO:0004208 |
| essential thrombocythemia | 3 | MONDO:0005029 | EFO:0000479 |
| acquired polycythemia vera | 3 | MONDO:0009891 | EFO:0002429 |
| atopic eczema | 3 | MONDO:0004980 | EFO:0000274 |
| exocrine pancreatic carcinoma | 3 | MONDO:0005192 | EFO:0002618 |
| severe acute respiratory syndrome | 3 | MONDO:0005091 | EFO:0000694 |
| macrophage activation syndrome | 3 | MONDO:0015545 | EFO:1001806 |
| prurigo | 3 | MONDO:0021739 | MONDO:0021739 |
| head and neck squamous cell carcinoma | 2 | MONDO:0010150 | EFO:0000181 |
| leukemia | 2 | MONDO:0005059 | EFO:0000565 |
| Hodgkins lymphoma | 2 | MONDO:0004952 | EFO:0000183 |
| breast carcinoma | 2 | MONDO:0004989 | EFO:0000305 |
| psoriasis | 2 | MONDO:0005083 | EFO:0000676 |
| HIV infectious disease | 2 | MONDO:0005109 | EFO:0000764 |
| B-cell chronic lymphocytic leukemia | 2 | MONDO:0004948 | EFO:0000095 |
| alopecia areata | 2 | MONDO:0005340 | EFO:0004192 |
| rheumatoid arthritis | 2 | MONDO:0008383 | EFO:0000685 |
| acute lymphoblastic leukemia | 2 | MONDO:0004967 | EFO:0000220 |
| acute myeloid leukemia | 2 | MONDO:0018874 | EFO:0000222 |
| chronic myeloid leukemia | 2 | MONDO:0011996 | EFO:0000339 |
| lymphoma | 2 | MONDO:0005062 | EFO:0000574 |
| plasma cell myeloma | 2 | MONDO:0009693 | EFO:0001378 |
| non-small cell lung carcinoma | 2 | MONDO:0005233 | EFO:0003060 |
| inflammatory breast carcinoma | 2 | MONDO:0006804 | EFO:1000984 |
| colorectal carcinoma | 2 | MONDO:0024331 | EFO:1001951 |
| lymphoid neoplasm | 2 | MONDO:0005157 | EFO:0001642 |
| lichen planus | 2 | MONDO:0006572 | EFO:1000726 |
| hypereosinophilic syndrome | 2 | MONDO:0015691 | EFO:1001467 |
| breast neoplasm | 2 | MONDO:0021100 | MONDO:0007254 |
| hidradenitis suppurativa | 2 | MONDO:0006559 | EFO:1000710 |
| necrobiosis lipoidica | 2 | MONDO:0006583 | EFO:1000738 |
| bronchiolitis obliterans syndrome | 2 | MONDO:0015265 | EFO:0007183 |
| discoid lupus erythematosus | 2 | MONDO:0019558 | MONDO:0019558 |
| beta thalassemia | 2 | MONDO:0019402 | MONDO:0016486 |
| anemia | 2 | MONDO:0002280 | EFO:0004272 |
| lichen disease | 2 | MONDO:0006570 | EFO:1000724 |
| seborrheic dermatitis | 2 | MONDO:0006608 | EFO:1000764 |
| histiocytosis | 2 | MONDO:0002637 | HP:0100727 |
| hematopoietic and lymphoid system neoplasm | 2 | MONDO:0002334 | MONDO:0044881 |
| non-Hodgkin lymphoma | 1 | MONDO:0018908 | EFO:0005952 |
| T-cell acute lymphoblastic leukemia | 1 | MONDO:0004963 | EFO:0000209 |
| glioblastoma | 1 | MONDO:0018177 | EFO:0000519 |
| lung neoplasm | 1 | MONDO:0021117 | MONDO:0008903 |
| pneumonia | 1 | MONDO:0005249 | EFO:0003106 |
| dermatitis | 1 | MONDO:0002406 | MONDO:0002406 |
| neuromyelitis optica | 1 | MONDO:0019100 | EFO:0004256 |
| paraganglioma | 1 | MONDO:0000448 | EFO:1000453 |
| uveal melanoma | 1 | MONDO:0006486 | EFO:1000616 |
| pancreatic ductal adenocarcinoma | 1 | MONDO:0005184 | MONDO:0005184 |
| malignant atrophic papulosis | 1 | MONDO:0011208 | MONDO:0011208 |
13 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 373.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 154 |
| PHASE1 | 62 |
| PHASE1/PHASE2 | 55 |
| PHASE3 | 50 |
| Not specified | 29 |
| PHASE4 | 15 |
| PHASE2/PHASE3 | 5 |
| EARLY_PHASE1 | 3 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT02386800 | PHASE4 | ACTIVE_NOT_RECRUITING | CINC424A2X01B Rollover Protocol |
| NCT06364319 | PHASE4 | NOT_YET_RECRUITING | Efficacy and Safety of Anti-CD25 rhMAb in the Treatment of Steroid-Refractory cGVHD |
| NCT06462469 | PHASE4 | RECRUITING | Study of Efficacy and Safety of Ruxolitinib in Patients With Grade II to IV Steroid-refractory Acute Graft vs. Host Disease |
| NCT06824103 | PHASE4 | RECRUITING | Study of Efficacy and Safety of Ruxolitinib in Chinese Participants With Corticosteroid-refractory Chronic Graft vs. Host Disease |
| NCT07101588 | PHASE4 | RECRUITING | Ruxolitinib-Decitabine Intensified Conditioning Regimen for AML: A Randomized Trial |
| NCT07352566 | PHASE4 | NOT_YET_RECRUITING | Utilization of a Microdevice for Psoriasis and Atopic Dermatitis |
| NCT07498205 | PHASE4 | NOT_YET_RECRUITING | Comparing Momelotinib and Ruxolitinib in People With Untreated Myelofibrosis and Low Blood Cell Counts |
| NCT01558739 | PHASE4 | COMPLETED | Exploratory Phase II Study of INC424 Patients With Primary Myelofibrosis (PMF) or Post Polycythaemia Myelofibrosis (PPV MF) or Post Essential Thrombocythaemia Myelofibrosis (PET-MF) |
| NCT04446806 | PHASE4 | UNKNOWN | Prevention and Treatment of Differentiation Syndrome in Patients With Acute Promyelocytic Leukemia |
| NCT04999878 | PHASE4 | UNKNOWN | A Prospective Clinical Study of Ruxolitinib and Etoposide Combined With DDGP Regimen (RUE-DDGP) in Induction Therapy of T/NK Cell Lymphoma-associated Hemophagocytic Syndrome. |
| NCT05021276 | PHASE4 | UNKNOWN | Basiliximab Combined With Ruxolitinib as Second-line Treatment of Grade 3-4 Steroid-resistant aGVHD |
| NCT05447260 | PHASE4 | UNKNOWN | A New Prognostic Stratification-based Safety and Efficacy Study of Ruxolitinib in Myelofibrosis |
| NCT05491304 | PHASE4 | UNKNOWN | Cytokine Guided Risk Stratification and Treatment in Pediatric Hemophagocytic Lymphohistiocytosis |
| NCT05696392 | PHASE4 | TERMINATED | The Purpose of This Study is to Evaluate the Effects of Ruxolitinib Cream on Adults With Atopic Dermatitis Experiencing Sleep Disturbance. |
| NCT07368673 | PHASE4 | COMPLETED | Comparative Effectiveness of Ruxolitinib Monotherapy Versus Its Combination With Tacrolimus and Corticosteroids in the Management of Vitiligo: A Randomized Controlled Trial |
| NCT03117751 | PHASE2/PHASE3 | ACTIVE_NOT_RECRUITING | Total Therapy XVII for Newly Diagnosed Patients With Acute Lymphoblastic Leukemia and Lymphoma |
| NCT04116502 | PHASE3 | RECRUITING | MITHRIDATE: Ruxolitinib Versus Hydroxycarbamide or Interferon as First Line Therapy in High Risk Polycythemia Vera |
| NCT04468984 | PHASE3 | ACTIVE_NOT_RECRUITING | Study of Oral Navitoclax Tablet in Combination With Oral Ruxolitinib Tablet Versus Best Available Therapy to Assess Change in Spleen Volume in Adult Participants With Relapsed/Refractory Myelofibrosis |
| NCT04562389 | PHASE3 | ACTIVE_NOT_RECRUITING | Study of Selinexor in Combination With Ruxolitinib in Myelofibrosis |
| NCT04603495 | PHASE3 | ACTIVE_NOT_RECRUITING | Phase 3 Study of Pelabresib (CPI-0610) in Myelofibrosis (MF) (MANIFEST-2) |
| NCT06079879 | PHASE3 | RECRUITING | A Study of Bomedemstat (IMG-7289/MK-3543) Compared to Best Available Therapy (BAT) in Participants With Essential Thrombocythemia and an Inadequate Response or Intolerance of Hydroxyurea (MK-3543-006) |
| NCT06479135 | PHASE3 | RECRUITING | Study of Navtemadlin add-on to Ruxolitinib in JAK Inhibitor-Naïve Patients With Myelofibrosis Who Have a Suboptimal Response to Ruxolitinib |
| NCT06548360 | PHASE3 | RECRUITING | A Study to Evaluate the Safety and Efficacy of Ruxolitinib Cream in Pediatric Participants With Nonsegmental Vitiligo |
| NCT06615050 | PHASE3 | RECRUITING | A Study of Tacrolimus/Methotrexate/Ruxolitinib Versus Post-Transplant Cyclophosphamide/Tacrolimus/Mycophenolate Mofetil in Non-Myeloablative/Reduced Intensity Conditioning Allogeneic Peripheral Blood Stem Cell Transplantation (BMT CTN 2203) |
| NCT06804811 | PHASE3 | RECRUITING | A Study to Evaluate the Efficacy and Safety of Ruxolitinib Cream in Children (6 to < 12 Years Old) With Nonsegmental Vitiligo |
| NCT06832618 | PHASE3 | RECRUITING | A Study to Assess the Efficacy and Safety of Ruxolitinib Cream in Children and Adolescents (6 to <18 Years Old) With Moderate Atopic Dermatitis |
| NCT06958211 | PHASE3 | RECRUITING | Study to Evaluate the Efficacy and Safety of Ruxolitinib Cream in Participants With Hidradenitis Suppurativa (TRuE-HS2) |
| NCT06959225 | PHASE3 | RECRUITING | Study to Evaluate the Efficacy and Safety of Ruxolitinib Cream in Participants With Hidradenitis Suppurativa (TRuE-HS1) |
| NCT07297914 | PHASE2/PHASE3 | NOT_YET_RECRUITING | Framework for Optimizing, Refining, and Unifying Management of HSCT in Pediatric ALL |
| NCT07317700 | PHASE3 | RECRUITING | A Clinical Trial of Flonoltinib Maleate for Intermediate or High-Risk Myelofibrosis |
| NCT07357727 | PHASE3 | RECRUITING | A Phase 3 Study of Pelabresib (DAK539) and Ruxolitinib in Myelofibrosis (MF) |
| NCT07366801 | PHASE2/PHASE3 | RECRUITING | Co-infusion of Treg-enriched Donor Lymphocytes With CD3-depleted Hematopoietic Stem Cell Graft to Prevent Graft-versus Host Disease After Allogeneic Hematopoietic Stem Cell Transplantation Among Children With Hematologic Malignancies |
| NCT07588945 | PHASE3 | NOT_YET_RECRUITING | daGOAT-Guided Prevention of Severe aGVHD After Allo-HSCT |
| NCT07595939 | PHASE3 | NOT_YET_RECRUITING | Efficacy and Safety of Ruxolitinib Cream in Chinese Children Aged 2-11 Years With Non-segmental Vitiligo |
| NCT00934544 | PHASE3 | COMPLETED | Controlled Myelofibrosis Study With Oral Janus-associated Kinase (JAK) Inhibitor Treatment-II: The COMFORT-II Trial |
| NCT00952289 | PHASE3 | COMPLETED | COntrolled MyeloFibrosis Study With ORal JAK Inhibitor Treatment: The COMFORT-I Trial |
| NCT01243944 | PHASE3 | COMPLETED | Study of Efficacy and Safety in Polycythemia Vera Subjects Who Are Resistant to or Intolerant of Hydroxyurea: JAK Inhibitor INC424 (INCB018424) Tablets Versus Best Available Care: (The RESPONSE Trial) |
| NCT01493414 | PHASE3 | COMPLETED | INC424 for Patients With Primary Myelofibrosis, Post Polycythemia Myelofibrosis or Post-essential Thrombocythemia Myelofibrosis. |
| NCT01632904 | PHASE3 | COMPLETED | Randomized Switch Study From Hydroxyurea to Ruxolitinib for RELIEF of Polycythemia Vera Symptoms: The Relief Study |
| NCT01969838 | PHASE3 | COMPLETED | Momelotinib Versus Ruxolitinib in Subjects With Myelofibrosis |
Clinical evidence (CIViC)
Variant × indication × effect (13 predictive associations from 14 curated evidence items):
| Variant | Indication | Effect | Therapy | Level | CIViC |
|---|---|---|---|---|---|
| PCM1::JAK2 Fusion OR BCR::JAK2 Fusion | Myeloid Neoplasm | Sensitivity/Response | Ruxolitinib | CIViC B | EID11325 |
| CSF3R T618I | Chronic Neutrophilic Leukemia | Sensitivity/Response | Ruxolitinib | CIViC C | EID6381 +1 |
| GOLGA5::JAK2 Fusion | B-lymphoblastic Leukemia/lymphoma, BCR-ABL1–like | Sensitivity/Response | Ruxolitinib | CIViC C | EID7007 |
| JAK1 OVEREXPRESSION | Sarcoma | Sensitivity/Response | Ruxolitinib | CIViC C | EID7852 |
| JAK2 F694L | Childhood B-cell Acute Lymphoblastic Leukemia | Sensitivity/Response | Ruxolitinib | CIViC C | EID7021 |
| SSBP2::JAK2 Fusion | B-lymphoblastic Leukemia/lymphoma, BCR-ABL1–like | Sensitivity/Response | Ruxolitinib | CIViC C | EID7257 |
| VHL R200W (c.598C>T) | Chuvash Polycythemia | Sensitivity/Response | Ruxolitinib | CIViC C | EID1608 |
| IGH::CRLF2 Fusion | Acute Lymphoblastic Leukemia | Sensitivity/Response | Ruxolitinib | CIViC D | EID8540 |
| JAK1 A1086S | Hepatocellular Carcinoma | Sensitivity/Response | Ruxolitinib | CIViC D | EID10058 |
| JAK1 E483D | Hepatocellular Carcinoma | Sensitivity/Response | Ruxolitinib | CIViC D | EID10057 |
| JAK1 N451S | Hepatocellular Carcinoma | Sensitivity/Response | Ruxolitinib | CIViC D | EID10056 |
| JAK1 S646F | B-lymphoblastic Leukemia/lymphoma, BCR-ABL1–like | Sensitivity/Response | Ruxolitinib | CIViC D | EID7957 |
| JAK1 S703I | Hepatocellular Carcinoma | Sensitivity/Response | Ruxolitinib | CIViC D | EID1900 |
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
126 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| CRIZOTINIB | ChEMBL + PubChem | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| DEUCRAVACITINIB | ChEMBL + PubChem | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| Pazopanib | ChEMBL + PubChem | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| RITLECITINIB | ChEMBL + PubChem | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| ABROCITINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| BARICITINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| FEDRATINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| FILGOTINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| MIDOSTAURIN | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| MOMELOTINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| NINTEDANIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| PACRITINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| PEFICITINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| SUNITINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| TOFACITINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| UPADACITINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| BREPOCITINIB | ChEMBL | Phase 3 | JAK1, JAK2, JAK3, TYK2 |
| DELGOCITINIB | ChEMBL | Phase 3 | JAK1, JAK2, JAK3, TYK2 |
| DOVITINIB | ChEMBL | Phase 3 | JAK1, JAK2, JAK3, TYK2 |
| ITACITINIB | ChEMBL | Phase 3 | JAK1, JAK2, JAK3, TYK2 |
| LESTAURTINIB | ChEMBL | Phase 3 | JAK1, JAK2, JAK3, TYK2 |
| AT-9283 | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| ATINVICITINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| AZD-1480 | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| BMS-911543 | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| CC-401 | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| CERDULATINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| DECERNOTINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| GANDOTINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| GOLIDOCITINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| GUSACITINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| IFIDANCITINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| IZENCITINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| NEZULCITINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| NS-018 | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| OCLACITINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| R-406 | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| ROPSACITINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| SOLCITINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| SU-014813 | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| TOZASERTIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| Afatinib | PubChem | Approved | JAK1, JAK2, JAK3, TYK2 |
| Gefitinib | PubChem | Approved | JAK1, JAK2, JAK3, TYK2 |
| Idelalisib | PubChem | Approved | JAK1, JAK2, JAK3, TYK2 |
| Selumetinib | PubChem | Approved | JAK1, JAK2, JAK3, TYK2 |
| dacomitinib | ChEMBL + PubChem | Phase 4 (approved) | JAK1, JAK3, TYK2 |
| IMATINIB | ChEMBL + PubChem | Phase 4 (approved) | JAK1, JAK2, TYK2 |
| AXITINIB | ChEMBL | Phase 4 (approved) | JAK2, JAK3, TYK2 |
| BOSUTINIB | ChEMBL | Phase 4 (approved) | JAK2, JAK3, TYK2 |
| CERITINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3 |
| DASATINIB | ChEMBL | Phase 4 (approved) | JAK2, JAK3, TYK2 |
| ENTRECTINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3 |
| ERLOTINIB | ChEMBL | Phase 4 (approved) | JAK2, JAK3, TYK2 |
| ABIVERTINIB | ChEMBL | Phase 3 | JAK1, JAK2, JAK3 |
| ALVOCIDIB | ChEMBL | Phase 3 | JAK2, JAK3, TYK2 |
| DEFACTINIB | ChEMBL | Phase 3 | JAK2, JAK3, TYK2 |
| BMS-919373 | ChEMBL | Phase 2 | JAK2, JAK3, TYK2 |
| CENISERTIB | ChEMBL | Phase 2 | JAK2, JAK3, TYK2 |
| LONDAMOCITINIB | ChEMBL | Phase 2 | JAK1, JAK2, TYK2 |
| belumosudil | PubChem | Approved | JAK2, JAK3, TYK2 |
Related Atlas pages
- Genes: JAK1, JAK2, JAK3, TYK2
- Diseases: neoplasm, primary myelofibrosis, graft versus host disease, vitiligo, essential thrombocythemia, acquired polycythemia vera, atopic eczema, exocrine pancreatic carcinoma, severe acute respiratory syndrome, macrophage activation syndrome, prurigo, myeloid neoplasm, chronic neutrophilic leukemia, B-lymphoblastic leukemia/lymphoma, BCR-ABL1–like, sarcoma, Chuvash polycythemia, acute lymphoblastic leukemia, hepatocellular carcinoma
- Drugs: Crizotinib, Deucravacitinib, Pazopanib, Ritlecitinib, Abrocitinib, Baricitinib, Fedratinib, Filgotinib, Midostaurin, Momelotinib, Nintedanib, Pacritinib, Peficitinib, Sunitinib, Tofacitinib, Upadacitinib, Brepocitinib, Delgocitinib, Dovitinib, Itacitinib, Lestaurtinib, Afatinib, Gefitinib, Idelalisib, Selumetinib, dacomitinib, Imatinib, Axitinib, Bosutinib, Ceritinib, Dasatinib, Entrectinib, Erlotinib, Abivertinib, Alvocidib, Defactinib, belumosudil
- Biomarker genes: CSF3R, VHL