ruxolitinib Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 4190 941678-49-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ruxolitinib
  • jakafi
  • INCB 018424
  • ruxolitinib phosphate
  • jakavi
a kinase inhibitor, inhibits Janus Associated Kinases (JAKs) JAK1 and JAK2 which mediate the signaling of a number of cytokines and growth factors that are important for hematopoiesis and immune function
  • Molecular weight: 306.37
  • Formula: C17H18N6
  • CLOGP: 2.22
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 1
  • TPSA: 83.18
  • ALOGS: -3.42
  • ROTB: 4

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Nov. 16, 2011 FDA INCYTE CORP

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Haemoglobin decreased 891.91 35.81 281 3997 17870 2335937
Platelet count decreased 882.71 35.81 270 4008 15543 2338264
Platelet count increased 680.65 35.81 148 4130 2089 2351718
Anaemia 670.76 35.81 269 4009 34523 2319284
Fatigue 653.64 35.81 346 3932 84527 2269280
Weight increased 625.33 35.81 227 4051 22110 2331697
Death 558.73 35.81 308 3970 81160 2272647
Product dose omission 526.36 35.81 233 4045 38024 2315783
Splenomegaly 501.68 35.81 108 4170 1443 2352364
Blood count abnormal 476.00 35.81 111 4167 2171 2351636
Contusion 467.88 35.81 159 4119 12651 2341156
Dizziness 414.77 35.81 227 4051 58438 2295369
Headache 366.41 35.81 234 4044 79945 2273862
White blood cell count increased 359.87 35.81 113 4165 6965 2346842
Diarrhoea 304.40 35.81 212 4066 83352 2270455
Myelofibrosis 301.72 35.81 55 4223 283 2353524
Red blood cell count decreased 280.23 35.81 83 4195 4183 2349624
Thrombocytopenia 279.50 35.81 122 4156 19009 2334798
Asthenia 241.02 35.81 148 4130 46778 2307029
Dyspnoea 225.41 35.81 173 4105 78560 2275247
Nausea 204.58 35.81 190 4088 111999 2241808
Flatulence 195.84 35.81 64 4214 4461 2349346
Pneumonia 183.06 35.81 127 4151 49169 2304638
Abdominal distension 180.25 35.81 75 4203 10336 2343471
Muscle spasms 178.09 35.81 93 4185 21473 2332334
Increased appetite 177.69 35.81 46 4232 1394 2352413
Constipation 174.97 35.81 92 4186 21537 2332270
Fall 171.68 35.81 120 4158 46979 2306828
Acute myeloid leukaemia 170.33 35.81 51 4227 2659 2351148
Malaise 162.66 35.81 124 4154 55461 2298346
Haematocrit decreased 158.65 35.81 54 4224 4264 2349543
Night sweats 153.41 35.81 50 4228 3450 2350357
Abdominal pain 152.47 35.81 99 4179 34275 2319532
Epistaxis 151.10 35.81 65 4213 9714 2344093
White blood cell count decreased 148.75 35.81 78 4200 18130 2335677
Pain 132.32 35.81 115 4163 61742 2292065
Pyrexia 125.32 35.81 105 4173 53603 2300204
Bone pain 123.37 35.81 55 4223 8941 2344866
Herpes zoster 122.41 35.81 56 4222 9669 2344138
Pruritus 118.52 35.81 93 4185 43247 2310560
Abdominal discomfort 118.05 35.81 66 4212 17390 2336417
Pain in extremity 115.70 35.81 91 4187 42449 2311358
Peripheral swelling 112.14 35.81 64 4214 17533 2336274
Haemorrhage 109.63 35.81 54 4224 10985 2342822
Urinary tract infection 108.15 35.81 76 4202 29866 2323941
Alopecia 101.41 35.81 65 4213 21936 2331871
Arthralgia 98.33 35.81 92 4186 54193 2299614
Cough 92.45 35.81 72 4206 33045 2320762
Memory impairment 90.43 35.81 50 4228 12873 2340934
Vomiting 88.95 35.81 99 4179 71503 2282304
Nasopharyngitis 86.66 35.81 59 4219 21997 2331810
Feeling abnormal 83.10 35.81 59 4219 23522 2330285
Pancytopenia 82.01 35.81 45 4233 11407 2342400
Rash 80.26 35.81 86 4192 59472 2294335
Transfusion 78.50 35.81 26 4252 1882 2351925
Off label use 78.34 35.81 94 4184 73504 2280303
Therapeutic response unexpected 77.62 35.81 31 4247 3828 2349979
Gout 76.96 35.81 24 4254 1431 2352376
Sepsis 76.30 35.81 51 4227 18437 2335370
Decreased appetite 72.43 35.81 59 4219 28832 2324975
Weight decreased 69.14 35.81 57 4221 28314 2325493
Incorrect dose administered 69.14 35.81 38 4240 9657 2344150
Hospitalisation 68.66 35.81 44 4234 14809 2338998
Back pain 67.71 35.81 59 4219 31600 2322207
Oedema peripheral 64.80 35.81 51 4227 23712 2330095
Oropharyngeal pain 63.04 35.81 38 4240 11480 2342327
Platelet count abnormal 60.68 35.81 17 4261 696 2353111
Blood lactate dehydrogenase increased 59.85 35.81 25 4253 3459 2350348
Insomnia 59.07 35.81 50 4228 25737 2328070
Infection 58.65 35.81 43 4235 17986 2335821
Medication error 57.87 35.81 29 4249 6102 2347705
Somnolence 56.81 35.81 47 4231 23438 2330369
Leukocytosis 55.91 35.81 24 4254 3552 2350255
Stomatitis 53.04 35.81 32 4246 9678 2344129
Blood iron decreased 51.07 35.81 17 4261 1248 2352559
Abdominal pain upper 50.90 35.81 43 4235 22057 2331750
Second primary malignancy 50.72 35.81 16 4262 990 2352817
Chills 50.36 35.81 37 4241 15515 2338292
Pollakiuria 48.37 35.81 22 4256 3734 2350073
Leukaemia 45.83 35.81 14 4264 778 2353029
Disease progression 45.09 35.81 36 4242 17059 2336748
Myalgia 44.91 35.81 41 4237 23292 2330515
Haematoma 44.76 35.81 23 4255 5098 2348709
Hypoaesthesia 43.83 35.81 38 4240 20177 2333630
Primary myelofibrosis 43.72 35.81 7 4271 13 2353794
Splenectomy 43.65 35.81 10 4268 178 2353629
Respiratory failure 43.37 35.81 32 4246 13496 2340311
Vision blurred 43.26 35.81 33 4245 14635 2339172
Fluid retention 43.13 35.81 25 4253 7021 2346786
Influenza 42.29 35.81 31 4247 12947 2340860
Oral herpes 41.89 35.81 17 4261 2185 2351622
Bronchitis 38.57 35.81 30 4248 13684 2340123
Red blood cell count increased 38.15 35.81 10 4268 317 2353490
Visual impairment 38.12 35.81 28 4250 11727 2342080
Balance disorder 38.04 35.81 26 4252 9721 2344086
Hepatomegaly 37.99 35.81 15 4263 1794 2352013
Arthritis 37.51 35.81 26 4252 9942 2343865
Wrong technique in product usage process 36.63 35.81 34 4244 19714 2334093
Feeling cold 36.03 35.81 17 4261 3133 2350674

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Death 967.13 37.68 545 4011 86898 1655327
Platelet count decreased 843.96 37.68 303 4253 16220 1726005
Haemoglobin decreased 729.68 37.68 275 4281 16839 1725386
Anaemia 703.20 37.68 312 4244 29145 1713080
Splenomegaly 661.56 37.68 159 4397 1961 1740264
Fatigue 577.47 37.68 325 4231 50456 1691769
Myelofibrosis 439.08 37.68 85 4471 325 1741900
White blood cell count increased 404.82 37.68 143 4413 7169 1735056
Pneumonia 403.45 37.68 250 4306 45932 1696293
Product dose omission 400.21 37.68 195 4361 22245 1719980
Platelet count increased 351.76 37.68 91 4465 1530 1740695
Blood count abnormal 346.52 37.68 88 4468 1369 1740856
Acute myeloid leukaemia 269.90 37.68 85 4471 2956 1739269
Diarrhoea 251.42 37.68 199 4357 53653 1688572
Weight increased 236.19 37.68 110 4446 11247 1730978
Red blood cell count decreased 234.09 37.68 80 4476 3606 1738619
Contusion 230.76 37.68 87 4469 5222 1737003
Dyspnoea 229.25 37.68 186 4370 51873 1690352
Asthenia 226.36 37.68 157 4399 34513 1707712
Thrombocytopenia 212.46 37.68 126 4430 21123 1721102
Second primary malignancy 203.37 37.68 54 4502 1005 1741220
Dizziness 199.67 37.68 145 4411 34216 1708009
Headache 197.33 37.68 144 4412 34232 1707993
Pyrexia 173.32 37.68 151 4405 46249 1695976
Epistaxis 164.92 37.68 78 4478 8228 1733997
Haematocrit decreased 164.00 37.68 64 4492 4209 1738016
Night sweats 162.58 37.68 54 4502 2222 1740003
White blood cell count decreased 144.43 37.68 83 4473 13066 1729159
Leukocytosis 139.38 37.68 54 4502 3479 1738746
Flatulence 134.33 37.68 50 4506 2884 1739341
Weight decreased 129.49 37.68 95 4461 22658 1719567
Malaise 126.02 37.68 104 4452 29461 1712764
Febrile neutropenia 121.66 37.68 70 4486 11030 1731195
Off label use 115.31 37.68 111 4445 38460 1703765
Infection 112.12 37.68 69 4487 12291 1729934
Abdominal pain 105.09 37.68 82 4474 21408 1720817
Haemorrhage 102.41 37.68 60 4496 9769 1732456
Blast cell count increased 99.92 37.68 22 4534 175 1742050
Fall 98.05 37.68 87 4469 27127 1715098
Transfusion 97.98 37.68 31 4525 1088 1741137
Oedema peripheral 97.66 37.68 69 4487 15481 1726744
Nasopharyngitis 96.18 37.68 58 4498 9952 1732273
Acute leukaemia 95.91 37.68 24 4532 348 1741877
Abdominal discomfort 90.82 37.68 54 4502 9027 1733198
Herpes zoster 90.82 37.68 43 4513 4530 1737695
Muscle spasms 90.67 37.68 59 4497 11562 1730663
Decreased appetite 87.31 37.68 77 4479 23794 1718431
Sepsis 86.06 37.68 70 4486 19368 1722857
Gout 85.76 37.68 35 4521 2581 1739644
Pancytopenia 84.55 37.68 56 4500 11301 1730924
Respiratory failure 83.35 37.68 61 4495 14444 1727781
Pain 81.93 37.68 78 4478 26579 1715646
Nausea 79.82 37.68 105 4451 51091 1691134
Pain in extremity 76.48 37.68 64 4492 18408 1723817
Iron overload 75.84 37.68 17 4539 148 1742077
Constipation 74.89 37.68 58 4498 14942 1727283
Leukaemia 73.57 37.68 23 4533 775 1741450
Arthralgia 70.86 37.68 68 4488 23376 1718849
Insomnia 70.71 37.68 58 4498 16218 1726007
Increased appetite 69.14 37.68 23 4533 948 1741277
Nocardiosis 69.10 37.68 20 4536 515 1741710
Abdominal distension 68.82 37.68 40 4516 6404 1735821
Blood lactate dehydrogenase increased 68.22 37.68 33 4523 3642 1738583
Peripheral swelling 65.91 37.68 42 4514 7929 1734296
Disease progression 65.69 37.68 57 4499 17206 1725019
Back pain 65.54 37.68 56 4500 16557 1725668
Influenza 64.41 37.68 39 4517 6728 1735497
Cough 64.36 37.68 59 4497 19138 1723087
Primary myelofibrosis 64.15 37.68 11 4545 16 1742209
Platelet count abnormal 63.53 37.68 19 4537 550 1741675
Blood creatinine increased 63.31 37.68 51 4505 13895 1728330
Drug ineffective 62.16 37.68 105 4451 63696 1678529
Pruritus 62.07 37.68 63 4493 23159 1719066
Squamous cell carcinoma 61.20 37.68 25 4531 1846 1740379
Haematoma 60.16 37.68 31 4525 3914 1738311
Hospitalisation 58.82 37.68 47 4509 12653 1729572
Bone pain 55.87 37.68 28 4528 3334 1738891
Therapeutic response unexpected 54.97 37.68 25 4531 2399 1739826
Cardiac failure 54.89 37.68 45 4511 12557 1729668
Skin cancer 54.06 37.68 21 4535 1358 1740867
Blast cells present 53.54 37.68 11 4545 60 1742165
Haematocrit increased 51.67 37.68 14 4542 281 1741944
Nephrolithiasis 51.33 37.68 28 4528 3964 1738261
Tuberculosis 51.19 37.68 22 4534 1844 1740381
Skin lesion 50.11 37.68 25 4531 2947 1739278
Chills 49.36 37.68 41 4515 11646 1730579
Rash 49.12 37.68 72 4484 38621 1703604
Septic shock 48.56 37.68 35 4521 8074 1734151
General physical health deterioration 45.25 37.68 41 4515 13077 1729148
Pleural effusion 44.90 37.68 38 4518 11072 1731153
Blood potassium increased 44.78 37.68 22 4534 2508 1739717
Splenic infarction 44.04 37.68 13 4543 359 1741866
Early satiety 43.63 37.68 10 4546 97 1742128
Abdominal pain upper 43.17 37.68 37 4519 10964 1731261
Ascites 42.62 37.68 28 4528 5558 1736667
Dyspnoea exertional 42.22 37.68 25 4531 4136 1738089
Acne 42.10 37.68 19 4537 1789 1740436
Memory impairment 40.44 37.68 29 4527 6634 1735591
Vomiting 39.78 37.68 65 4491 38250 1703975
Product use in unapproved indication 39.66 37.68 33 4523 9389 1732836
Cytopenia 39.35 37.68 15 4541 921 1741304
Basal cell carcinoma 39.26 37.68 20 4536 2463 1739762
Red blood cell count increased 39.05 37.68 11 4545 256 1741969
Gait disturbance 38.68 37.68 37 4519 12633 1729592
Dehydration 38.44 37.68 43 4513 17615 1724610
Graft versus host disease 38.33 37.68 17 4539 1536 1740689
Polycythaemia vera 38.32 37.68 9 4547 98 1742127

Pharmacologic Action:

SourceCodeDescription
ATC L01XE18 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Protein kinase inhibitors
FDA EPC N0000175605 Kinase Inhibitor
FDA MoA N0000175076 Protein Kinase Inhibitors
CHEBI has role CHEBI:35610 antineoplastic agent

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Myelofibrosis indication 52967002 DOID:4971
Polycythemia vera indication 109992005
Myeloproliferative disorder indication 425333006
Coronavirus infection off-label use 186747009

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 6.44 acidic
pKa2 4.6 Basic
pKa3 2.37 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 10MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 9079912 Dec. 12, 2026 USE OF RUXOLITINIB (JAKAFI) FOR BLOCKING SIGNAL TRANSDUCTION OF JANUS ASSOCIATED KINASES (JAKS) JAK1 AND/OR JAK2
EQ 10MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 9079912 Dec. 12, 2026 USE OF RUXOLITINIB (JAKAFI) FOR INHIBITING JANUS ASSOCIATED KINASES (JAKS) JAK1 AND/OR JAK2.
EQ 10MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 9814722 Dec. 12, 2026 FOR TREATMENT OF STEROID-REFRACTORY ACUTE GRAFT-VERSUS-HOST DISEASE
EQ 15MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 9079912 Dec. 12, 2026 USE OF RUXOLITINIB (JAKAFI) FOR BLOCKING SIGNAL TRANSDUCTION OF JANUS ASSOCIATED KINASES (JAKS) JAK1 AND/OR JAK2
EQ 15MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 9079912 Dec. 12, 2026 USE OF RUXOLITINIB (JAKAFI) FOR INHIBITING JANUS ASSOCIATED KINASES (JAKS) JAK1 AND/OR JAK2.
EQ 15MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 9814722 Dec. 12, 2026 FOR TREATMENT OF STEROID-REFRACTORY ACUTE GRAFT-VERSUS-HOST DISEASE
EQ 20MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 9079912 Dec. 12, 2026 USE OF RUXOLITINIB (JAKAFI) FOR BLOCKING SIGNAL TRANSDUCTION OF JANUS ASSOCIATED KINASES (JAKS) JAK1 AND/OR JAK2
EQ 20MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 9079912 Dec. 12, 2026 USE OF RUXOLITINIB (JAKAFI) FOR INHIBITING JANUS ASSOCIATED KINASES (JAKS) JAK1 AND/OR JAK2.
EQ 20MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 9814722 Dec. 12, 2026 FOR TREATMENT OF STEROID-REFRACTORY ACUTE GRAFT-VERSUS-HOST DISEASE
EQ 25MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 9079912 Dec. 12, 2026 USE OF RUXOLITINIB (JAKAFI) FOR BLOCKING SIGNAL TRANSDUCTION OF JANUS ASSOCIATED KINASES (JAKS) JAK1 AND/OR JAK2
EQ 25MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 9079912 Dec. 12, 2026 USE OF RUXOLITINIB (JAKAFI) FOR INHIBITING JANUS ASSOCIATED KINASES (JAKS) JAK1 AND/OR JAK2.
EQ 25MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 9814722 Dec. 12, 2026 FOR TREATMENT OF STEROID-REFRACTORY ACUTE GRAFT-VERSUS-HOST DISEASE
EQ 5MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 9079912 Dec. 12, 2026 USE OF RUXOLITINIB (JAKAFI) FOR BLOCKING SIGNAL TRANSDUCTION OF JANUS ASSOCIATED KINASES (JAKS) JAK1 AND/OR JAK2
EQ 5MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 9079912 Dec. 12, 2026 USE OF RUXOLITINIB (JAKAFI) FOR INHIBITING JANUS ASSOCIATED KINASES (JAKS) JAK1 AND/OR JAK2.
EQ 5MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 9814722 Dec. 12, 2026 FOR TREATMENT OF STEROID-REFRACTORY ACUTE GRAFT-VERSUS-HOST DISEASE
EQ 10MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 7598257 Dec. 24, 2027 FOR THE TREATMENT OF INTERMEDIATE OR HIGH-RISK MYELOFIBROSIS
EQ 10MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 7598257 Dec. 24, 2027 FOR THE TREATMENT OF POLYCYTHEMIA VERA
EQ 15MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 7598257 Dec. 24, 2027 FOR THE TREATMENT OF INTERMEDIATE OR HIGH-RISK MYELOFIBROSIS
EQ 15MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 7598257 Dec. 24, 2027 FOR THE TREATMENT OF POLYCYTHEMIA VERA
EQ 20MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 7598257 Dec. 24, 2027 FOR THE TREATMENT OF INTERMEDIATE OR HIGH-RISK MYELOFIBROSIS
EQ 20MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 7598257 Dec. 24, 2027 FOR THE TREATMENT OF POLYCYTHEMIA VERA
EQ 25MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 7598257 Dec. 24, 2027 FOR THE TREATMENT OF INTERMEDIATE OR HIGH-RISK MYELOFIBROSIS
EQ 25MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 7598257 Dec. 24, 2027 FOR THE TREATMENT OF POLYCYTHEMIA VERA
EQ 5MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 7598257 Dec. 24, 2027 FOR THE TREATMENT OF INTERMEDIATE OR HIGH-RISK MYELOFIBROSIS
EQ 5MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 7598257 Dec. 24, 2027 FOR THE TREATMENT OF POLYCYTHEMIA VERA
EQ 10MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 10016429 June 12, 2028 FOR TREATMENT OF STEROID-REFRACTORY ACUTE GRAFT-VERSUS-HOST DISEASE
EQ 10MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 8822481 June 12, 2028 USE OF RUXOLITINIB (JAKAFI) FOR INHIBITING JANUS ASSOCIATED KINASES (JAKS) JAK1 AND/OR JAK2.
EQ 10MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 8829013 June 12, 2028 FOR THE TREATMENT OF INTERMEDIATE OR HIGH-RISK MYELOFIBROSIS
EQ 10MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 8829013 June 12, 2028 FOR THE TREATMENT OF POLYCYTHEMIA VERA
EQ 15MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 10016429 June 12, 2028 FOR TREATMENT OF STEROID-REFRACTORY ACUTE GRAFT-VERSUS-HOST DISEASE
EQ 15MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 8822481 June 12, 2028 USE OF RUXOLITINIB (JAKAFI) FOR INHIBITING JANUS ASSOCIATED KINASES (JAKS) JAK1 AND/OR JAK2.
EQ 15MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 8829013 June 12, 2028 FOR THE TREATMENT OF INTERMEDIATE OR HIGH-RISK MYELOFIBROSIS
EQ 15MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 8829013 June 12, 2028 FOR THE TREATMENT OF POLYCYTHEMIA VERA
EQ 20MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 10016429 June 12, 2028 FOR TREATMENT OF STEROID-REFRACTORY ACUTE GRAFT-VERSUS-HOST DISEASE
EQ 20MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 8822481 June 12, 2028 USE OF RUXOLITINIB (JAKAFI) FOR INHIBITING JANUS ASSOCIATED KINASES (JAKS) JAK1 AND/OR JAK2.
EQ 20MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 8829013 June 12, 2028 FOR THE TREATMENT OF INTERMEDIATE OR HIGH-RISK MYELOFIBROSIS
EQ 20MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 8829013 June 12, 2028 FOR THE TREATMENT OF POLYCYTHEMIA VERA
EQ 25MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 10016429 June 12, 2028 FOR TREATMENT OF STEROID-REFRACTORY ACUTE GRAFT-VERSUS-HOST DISEASE
EQ 25MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 8822481 June 12, 2028 USE OF RUXOLITINIB (JAKAFI) FOR INHIBITING JANUS ASSOCIATED KINASES (JAKS) JAK1 AND/OR JAK2.
EQ 25MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 8829013 June 12, 2028 FOR THE TREATMENT OF INTERMEDIATE OR HIGH-RISK MYELOFIBROSIS
EQ 25MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 8829013 June 12, 2028 FOR THE TREATMENT OF POLYCYTHEMIA VERA
EQ 5MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 10016429 June 12, 2028 FOR TREATMENT OF STEROID-REFRACTORY ACUTE GRAFT-VERSUS-HOST DISEASE
EQ 5MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 8822481 June 12, 2028 USE OF RUXOLITINIB (JAKAFI) FOR INHIBITING JANUS ASSOCIATED KINASES (JAKS) JAK1 AND/OR JAK2.
EQ 5MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 8829013 June 12, 2028 FOR THE TREATMENT OF INTERMEDIATE OR HIGH-RISK MYELOFIBROSIS
EQ 5MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL 8829013 June 12, 2028 FOR THE TREATMENT OF POLYCYTHEMIA VERA

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 10MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL Dec. 4, 2021 TREATMENT OF PATIENTS WITH POLYCYTHEMIA VERA WHO HAVE HAD AN INADEQUATE RESPONSE TO OR ARE INTOLERANT OF HYDROXYUREA
EQ 15MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL Dec. 4, 2021 TREATMENT OF PATIENTS WITH POLYCYTHEMIA VERA WHO HAVE HAD AN INADEQUATE RESPONSE TO OR ARE INTOLERANT OF HYDROXYUREA
EQ 20MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL Dec. 4, 2021 TREATMENT OF PATIENTS WITH POLYCYTHEMIA VERA WHO HAVE HAD AN INADEQUATE RESPONSE TO OR ARE INTOLERANT OF HYDROXYUREA
EQ 25MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL Dec. 4, 2021 TREATMENT OF PATIENTS WITH POLYCYTHEMIA VERA WHO HAVE HAD AN INADEQUATE RESPONSE TO OR ARE INTOLERANT OF HYDROXYUREA
EQ 5MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL Dec. 4, 2021 TREATMENT OF PATIENTS WITH POLYCYTHEMIA VERA WHO HAVE HAD AN INADEQUATE RESPONSE TO OR ARE INTOLERANT OF HYDROXYUREA
EQ 10MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL May 24, 2022 TREATMENT OF STEROID-REFRACTORY ACUTE GRAFT-VERSUS-HOST DISEASE (GVHD) IN ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER
EQ 15MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL May 24, 2022 TREATMENT OF STEROID-REFRACTORY ACUTE GRAFT-VERSUS-HOST DISEASE (GVHD) IN ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER
EQ 20MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL May 24, 2022 TREATMENT OF STEROID-REFRACTORY ACUTE GRAFT-VERSUS-HOST DISEASE (GVHD) IN ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER
EQ 25MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL May 24, 2022 TREATMENT OF STEROID-REFRACTORY ACUTE GRAFT-VERSUS-HOST DISEASE (GVHD) IN ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER
EQ 5MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL May 24, 2022 TREATMENT OF STEROID-REFRACTORY ACUTE GRAFT-VERSUS-HOST DISEASE (GVHD) IN ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER
EQ 10MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL May 24, 2026 TREATMENT OF STEROID-REFRACTORY ACUTE GRAFT-VERSUS-HOST DISEASE (GVHD) IN ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER
EQ 15MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL May 24, 2026 TREATMENT OF STEROID-REFRACTORY ACUTE GRAFT-VERSUS-HOST DISEASE (GVHD) IN ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER
EQ 20MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL May 24, 2026 TREATMENT OF STEROID-REFRACTORY ACUTE GRAFT-VERSUS-HOST DISEASE (GVHD) IN ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER
EQ 25MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL May 24, 2026 TREATMENT OF STEROID-REFRACTORY ACUTE GRAFT-VERSUS-HOST DISEASE (GVHD) IN ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER
EQ 5MG BASE JAKAFI INCYTE CORP N202192 Nov. 16, 2011 RX TABLET ORAL May 24, 2026 TREATMENT OF STEROID-REFRACTORY ACUTE GRAFT-VERSUS-HOST DISEASE (GVHD) IN ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Tyrosine-protein kinase JAK1 Kinase INHIBITOR Ki 10.05 CHEMBL CHEMBL
Tyrosine-protein kinase JAK2 Kinase INHIBITOR Kd 10.44 CHEMBL CHEMBL
Phosphatidylinositol 4-kinase beta Kinase Kd 5.47 CHEMBL
Serine/threonine-protein kinase DCLK1 Kinase Kd 7.17 CHEMBL
Calcium/calmodulin-dependent protein kinase type 1 Kinase Kd 6.33 CHEMBL
SRSF protein kinase 1 Kinase Kd 5.68 CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 2 Kinase Kd 5.43 CHEMBL
Serine/threonine-protein kinase RIO3 Kinase Kd 5.70 CHEMBL
Serine/threonine-protein kinase Nek3 Kinase Kd 5.96 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 3 Kinase Kd 6.33 CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit beta Kinase Kd 6.51 CHEMBL
Ribosomal protein S6 kinase alpha-6 Kinase Kd 6.82 CHEMBL
Ribosomal protein S6 kinase alpha-1 Kinase Kd 6.92 CHEMBL
Cyclin-G-associated kinase Kinase Kd 7 CHEMBL
Serine/threonine-protein kinase SBK1 Kinase Kd 5.89 CHEMBL
Mitogen-activated protein kinase kinase kinase 15 Kinase Kd 5.96 CHEMBL
Microtubule-associated serine/threonine-protein kinase 1 Kinase Kd 6.28 CHEMBL
JAK2/TYK2 Kinase IC50 6.09 CHEMBL
JAK1/JAK2/TYK2 Kinase IC50 6.53 CHEMBL
JAK1/TYK2 Kinase IC50 6.71 CHEMBL
Homeodomain-interacting protein kinase 3 Kinase Kd 5.92 CHEMBL
Homeodomain-interacting protein kinase 2 Kinase Kd 6 CHEMBL
Maternal embryonic leucine zipper kinase Kinase Kd 5.66 CHEMBL
Serine/threonine-protein kinase PLK1 Kinase Kd 6.89 CHEMBL
Serine/threonine-protein kinase TBK1 Kinase Kd 5.77 CHEMBL
Serine/threonine-protein kinase Nek7 Kinase Kd 5.31 CHEMBL
Serine/threonine-protein kinase/endoribonuclease IRE1 Kinase Kd 5.60 CHEMBL
Serine/threonine-protein kinase B-raf Kinase Kd 5.66 CHEMBL
Serine/threonine-protein kinase OSR1 Kinase Kd 5.57 CHEMBL
STE20/SPS1-related proline-alanine-rich protein kinase Kinase Kd 5.72 CHEMBL
Mitogen-activated protein kinase kinase kinase 7 Kinase Kd 6.14 CHEMBL
Dual specificity protein kinase CLK2 Kinase Kd 6.34 CHEMBL
G protein-coupled receptor kinase 7 Kinase Kd 6.27 CHEMBL
Homeodomain-interacting protein kinase 1 Kinase Kd 5.92 CHEMBL
JAK3/JAK1 Kinase IC50 7.64 CHEMBL
Dual specificity protein kinase TTK Kinase Kd 6.32 CHEMBL
JAK2/JAK1 Kinase IC50 7.51 CHEMBL
Ephrin type-A receptor 3 Kinase Kd 5.21 CHEMBL
Serine/threonine-protein kinase 16 Kinase Kd 6.31 CHEMBL
Serine/threonine-protein kinase 17B Kinase Kd 5.46 CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit gamma Kinase Kd 7 CHEMBL
Serine/threonine-protein kinase PLK4 Kinase Kd 6.70 CHEMBL
AP2-associated protein kinase 1 Kinase Kd 6.92 CHEMBL
Serine/threonine-protein kinase MARK2 Kinase Kd 6.18 CHEMBL
Protein kinase C epsilon type Kinase Kd 6.28 CHEMBL
Tyrosine-protein kinase JAK3 Kinase Kd 8.70 CHEMBL
Ribosomal protein S6 kinase alpha-5 Kinase Kd 6.85 CHEMBL
Casein kinase II subunit alpha' Kinase Kd 5.48 CHEMBL
Serine/threonine-protein kinase TAO1 Kinase Kd 5.89 CHEMBL
Aurora kinase C Kinase Kd 5.06 CHEMBL
Phosphorylase b kinase gamma catalytic chain, liver/testis isoform Kinase Kd 6 CHEMBL
High affinity nerve growth factor receptor Kinase Kd 5.82 CHEMBL
Rho-associated protein kinase 1 Kinase Kd 7.22 CHEMBL
Ankyrin repeat and protein kinase domain-containing protein 1 Kinase Kd 6.41 CHEMBL
Serine/threonine-protein kinase 25 Kinase Kd 5.20 CHEMBL
Myosin light chain kinase, smooth muscle Kinase Kd 6.44 CHEMBL
Serine/threonine-protein kinase DCLK2 Kinase Kd 6.12 CHEMBL
Leucine-rich repeat serine/threonine-protein kinase 2 Kinase Kd 7.05 CHEMBL
Serine/threonine-protein kinase PAK 6 Kinase Kd 5.54 CHEMBL
Mast/stem cell growth factor receptor Kit Kinase Kd 5.20 CHEMBL
BMP-2-inducible protein kinase Kinase Kd 6.68 CHEMBL
Serine/threonine-protein kinase PAK 7 Kinase Kd 5.89 CHEMBL
Serine/threonine-protein kinase 17A Kinase Kd 5.21 CHEMBL
Ribosomal protein S6 kinase alpha-4 Kinase Kd 6.47 CHEMBL
Dual specificity protein kinase CLK4 Kinase Kd 5.77 CHEMBL
MAP kinase-interacting serine/threonine-protein kinase 2 Kinase Kd 6.70 CHEMBL
Death-associated protein kinase 2 Kinase Kd 7.01 CHEMBL
Bone morphogenetic protein receptor type-1B Kinase Kd 5.74 CHEMBL
Non-receptor tyrosine-protein kinase TYK2 Kinase Ki 9.30 CHEMBL
Interleukin-1 receptor-associated kinase 1 Kinase Kd 6.54 CHEMBL
Calcium/calmodulin-dependent protein kinase type 1D Kinase Kd 6.92 CHEMBL
Calcium/calmodulin-dependent protein kinase type 1G Kinase Kd 5.66 CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit beta Kinase Kd 5.64 CHEMBL
Serine/threonine-protein kinase TAO2 Kinase Kd 6.51 CHEMBL
Ribosomal protein S6 kinase alpha-2 Kinase Kd 6.82 CHEMBL
Serine/threonine-protein kinase ULK2 Kinase Kd 6.72 CHEMBL
Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform Kinase Kd 5.24 CHEMBL
Activated CDC42 kinase 1 Kinase Kd 5.59 CHEMBL
Casein kinase II subunit alpha Kinase Kd 5.38 CHEMBL
NT-3 growth factor receptor Kinase Kd 6.48 CHEMBL
Rhodopsin kinase Kinase Kd 6.14 CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit alpha Kinase Kd 7.34 CHEMBL
G protein-coupled receptor kinase 4 Kinase Kd 5.21 CHEMBL
Mitogen-activated protein kinase kinase kinase 2 Kinase Kd 7.39 CHEMBL
Serine/threonine-protein kinase ULK3 Kinase Kd 5.62 CHEMBL
Serine/threonine-protein kinase 26 Kinase Kd 5.51 CHEMBL
Serine/threonine-protein kinase PLK2 Kinase Kd 5.82 CHEMBL
Bone morphogenetic protein receptor type-2 Kinase Kd 6.03 CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit epsilon Kinase Kd 5.92 CHEMBL
Peripheral plasma membrane protein CASK Kinase Kd 5.82 CHEMBL
Ephrin type-B receptor 6 Kinase Kd 5.51 CHEMBL
Mitogen-activated protein kinase 8 Kinase Kd 5.32 CHEMBL
Serine/threonine-protein kinase TAO3 Kinase Kd 6.23 CHEMBL
Casein kinase I isoform alpha Kinase Kd 5.74 CHEMBL
Mitogen-activated protein kinase kinase kinase 1 Kinase Kd 5.38 CHEMBL
Cyclin-dependent kinase 7 Kinase Kd 5.48 CHEMBL
Serine/threonine-protein kinase SIK3 Kinase Kd 5.89 CHEMBL
Rho-associated protein kinase 2 Kinase Kd 7.28 CHEMBL
Death-associated protein kinase 1 Kinase Kd 7.14 CHEMBL
Uncharacterized serine/threonine-protein kinase SBK3 Kinase Kd 5.24 CHEMBL
Death-associated protein kinase 3 Kinase Kd 7.05 CHEMBL
Serine/threonine-protein kinase PAK 4 Kinase Kd 5.80 CHEMBL
Serine/threonine-protein kinase DCLK3 Kinase Kd 6.59 CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 1A Kinase Kd 6.04 CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret Kinase Kd 6.72 CHEMBL
Myotonin-protein kinase Kinase Kd 5.46 CHEMBL
Leukocyte tyrosine kinase receptor Kinase Kd 6.36 CHEMBL
Mitogen-activated protein kinase kinase kinase 19 Kinase Kd 6.57 CHEMBL
Serine/threonine-protein kinase PLK3 Kinase Kd 6.15 CHEMBL
BDNF/NT-3 growth factors receptor Kinase Kd 6.44 CHEMBL
NUAK family SNF1-like kinase 2 Kinase Kd 6.49 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 2 Kinase Kd 5.40 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 4 Kinase Kd 5.74 CHEMBL
SRSF protein kinase 3 Kinase Kd 5.48 CHEMBL
Serine/threonine-protein kinase VRK2 Kinase Kd 5.40 CHEMBL
ALK tyrosine kinase receptor Kinase Kd 5.82 CHEMBL
Mitogen-activated protein kinase kinase kinase 3 Kinase Kd 6.82 CHEMBL
Serine/threonine-protein kinase RIO1 Kinase Kd 5.60 CHEMBL
Serine/threonine-protein kinase RIO2 Kinase Kd 5.92 CHEMBL
Serine/threonine-protein kinase ULK1 Kinase Kd 6.52 CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit delta Kinase Kd 7.05 CHEMBL
cGMP-dependent protein kinase 2 Kinase Kd 6.16 CHEMBL
Receptor-interacting serine/threonine-protein kinase 4 Kinase Kd 5.68 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 1 Kinase Kd 5.72 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 2 Kinase Kd 5.70 CHEMBL
Tyrosine-protein kinase ABL1 Kinase Kd 5.96 CHEMBL
Serine/threonine-protein kinase PknB Kinase Kd 5.38 CHEMBL

External reference:

IDSource
4031235 VUID
N0000184017 NUI
C2931926 UMLSCUI
D09959 KEGG_DRUG
436LRU32H5 UNII
1092939-17-7 SECONDARY_CAS_RN
703779004 SNOMEDCT_US
1193326 RXNORM
014040 NDDF
28206 MMSL
d07812 MMSL
4031235 VANDF
702806008 SNOMEDCT_US
9287 INN_ID
RXT PDB_CHEM_ID
DB08877 DRUGBANK_ID
CHEBI:66919 CHEBI
C540383 MESH_SUPPLEMENTAL_RECORD_UI
CHEMBL1789941 ChEMBL_ID
CHEMBL1795071 ChEMBL_ID
25126798 PUBCHEM_CID
5688 IUPHAR_LIGAND_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
JAKAFI HUMAN PRESCRIPTION DRUG LABEL 1 50881-005 TABLET 5 mg ORAL NDA 18 sections
JAKAFI HUMAN PRESCRIPTION DRUG LABEL 1 50881-010 TABLET 10 mg ORAL NDA 18 sections
JAKAFI HUMAN PRESCRIPTION DRUG LABEL 1 50881-015 TABLET 15 mg ORAL NDA 18 sections
JAKAFI HUMAN PRESCRIPTION DRUG LABEL 1 50881-020 TABLET 20 mg ORAL NDA 18 sections
JAKAFI HUMAN PRESCRIPTION DRUG LABEL 1 50881-025 TABLET 25 mg ORAL NDA 18 sections