ponatinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 4716 943319-70-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ponatinib
  • iclusig
  • AP24534
  • ponatinib hydrochloride
  • ponatinib HCl
a pan-Bcr-Abl protein kinase Inhibitor
  • Molecular weight: 532.57
  • Formula: C29H27F3N6O
  • CLOGP: 6.11
  • LIPINSKI: 2
  • HAC: 7
  • HDO: 1
  • TPSA: 65.77
  • ALOGS: -5.26
  • ROTB: 7
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
45 mg O

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 4.474 Moderate 0.72
caco2-efflux Caco-2 efflux ratio (BA/AB) 4.446 Moderate 0.72
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 4.150 10^-6 cm/s Moderate 0.72
dh-clint Dog hepatocyte intrinsic clearance 12.589 uL/min/10^6 cells Moderate 0.72
dppb Dog plasma protein binding (% unbound) 0.610 % Moderate 0.72
fcs-ppb Fetal calf serum protein binding (% unbound) 3.100 % Moderate 0.72
herg hERG pIC50 5.293 pIC50 Moderate 0.72
hh-clint Human hepatocyte intrinsic clearance 3.027 uL/min/10^6 cells Moderate 0.72
hlm-clint Human liver microsomal intrinsic clearance 18.707 uL/min/mg protein Moderate 0.72
hppb Human plasma protein binding (% unbound) 0.480 % Moderate 0.72
kinase-safety-class ABL1,ABL2,ACVR2A,ACVR2B,ACVRL1,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,CAMK2B,CAMK2D,CDK1,CDK19,CDK5,CDK9,CHEK1,CSF1R,CSK,DDR1,EGFR,EIF2AK3,EPHA2,EPHB1,EPHB3,EPHB4,ERBB2,ERBB4,FGFR1,FGFR4,FLT1,FLT3,FLT4,FYN,GAK,GRK2,IKBKB,INSR,IRAK1,IRAK3,ITK,JAK1,JAK2,KDR,KIT,LCK,LYN,MAP2K1,MAP3K1,MAP3K10,MAP3K11,MAP3K2,MAP3K21,MAP3K3,MAP3K7,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK10,MAPK11,MAPK14,MAPK7,MAPK8,MAPK9,MAPKAPK2,MARK4,MELK,MET,MINK1,MKNK2,MST1R,MTOR,NTRK1,NTRK2,NTRK3,PAK4,PDGFRB,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PRKCD,PRKDC,PTK6,RET,RIPK3,RPS6KA1,SIK2,SIK3,SRC,STK10,STK33,SYK,TEK,TGFBR1,TNIK,TTK,TYRO3,ULK1,ULK2,YES1 110
kinase-selectivity-class ABL2,ALK,AURKB,AURKC,AXL,BLK,BMX,BRAF,BTK,CAMK2D,CDK4,CDK7,CDK8,CDK9,CSF1R,CSK,DDR1,EGFR,EIF2AK3,EPHA2,EPHB3,EPHB4,ERBB2,ERBB4,FGFR1,FGFR4,FLT1,FLT3,FLT4,FYN,GAK,IGF1R,INSR,IRAK1,JAK1,JAK2,KDR,KIT,LCK,LYN,MAP2K1,MAP3K11,MAP3K2,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAP4K5,MAPK11,MAPK12,MAPK14,MAPK7,MARK4,MET,MINK1,MKNK2,MST1R,MTOR,NTRK1,NTRK3,PAK4,PDGFRB,PDK1,PDK4,PIK3CA,PIK3CD,PRKCD,PRKDC,RET,RIPK3,SIK2,SIK3,SRC,STK10,STK33,STK4,SYK,TEK,TNIK,TNK1,TTK,TYRO3,ULK1,ULK2,YES1 85
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 10.889 Moderate 0.72
mh-clint Mouse hepatocyte intrinsic clearance 19.679 Moderate 0.72
mppb Mouse plasma protein binding (% unbound) 0.400 Moderate 0.72
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 23.281 Moderate 0.72
pfas-class PFAS structural alert (1 = True, 0 = False) 1
pppb Pig plasma protein binding (% unbound) 1.330 % Moderate 0.72
rh-clint Rat hepatocyte intrinsic clearance 20.091 uL/min/10^6 cells Moderate 0.72
rh-fuinc Rat hepatocyte fraction unbound in incubation 1.900 % Moderate 0.72
rppb Rat plasma protein binding (% unbound) 0.450 % Moderate 0.72
solubility-dd Solubility at pH 7.4 in DMSO 1.161 uM Moderate 0.72

Approvals:

DateAgencyCompanyOrphan
Dec. 14, 2012 FDA ARIAD

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
Acute lymphocytic leukaemia recurrent 348.43 21.67 74 8167 2647 90617559
Cytogenetic analysis abnormal 221.61 21.67 43 8198 967 90619239
Philadelphia chromosome positive 198.44 21.67 35 8206 455 90619751
Death 186.97 21.67 218 8023 456333 90163873
Blast crisis in myelogenous leukaemia 169.00 21.67 32 8209 629 90619577
Drug resistance 168.93 21.67 73 8168 30376 90589830
Chronic myeloid leukaemia recurrent 159.12 21.67 27 8214 275 90619931
Cytopenia 117.38 21.67 48 8193 17401 90602805
Thrombocytopenia 95.77 21.67 106 8135 208619 90411587
Neoplasm progression 95.37 21.67 56 8185 44430 90575776
Dry skin 90.00 21.67 70 8171 88003 90532203
Central nervous system leukaemia 88.88 21.67 16 8225 235 90619971
Haematotoxicity 86.07 21.67 35 8206 12500 90607706
Blast cell crisis 83.43 21.67 13 8228 73 90620133
Pericardial effusion 80.61 21.67 47 8194 36786 90583420
Graft versus host disease 74.50 21.67 28 8213 8116 90612090
Peripheral arterial occlusive disease 73.54 21.67 24 8217 4597 90615609
Leukaemia recurrent 70.44 21.67 18 8223 1449 90618757
Rash 68.55 21.67 192 8049 795908 89824298
Platelet count decreased 67.00 21.67 72 8169 136897 90483309
Lipase increased 66.07 21.67 28 8213 11083 90609123
Chronic myeloid leukaemia transformation 63.32 21.67 11 8230 130 90620076
Pleural effusion 60.34 21.67 62 8179 111929 90508277
Therapeutic response delayed 58.88 21.67 14 8227 836 90619370
Graft versus host disease in eye 57.89 21.67 10 8231 114 90620092
Pancytopenia 51.52 21.67 59 8182 120204 90500002
Stem cell transplant 50.29 21.67 15 8226 2139 90618067
Cytokine release syndrome 49.11 21.67 31 8210 27942 90592264
Philadelphia positive acute lymphocytic leukaemia 47.73 21.67 7 8234 24 90620182
Ischaemic stroke 45.12 21.67 27 8214 22139 90598067
Capillary leak syndrome 42.53 21.67 14 8227 2753 90617453
Bone pain 42.14 21.67 39 8202 61944 90558262
Product dose omission issue 41.90 21.67 86 8155 291601 90328605
Skin toxicity 40.02 21.67 17 8224 6762 90613444
Ichthyosis acquired 39.18 21.67 5 8236 3 90620203
Malignant neoplasm progression 38.47 21.67 48 8193 106822 90513384
Catabolic state 36.77 21.67 6 8235 47 90620159
Pancreatitis 36.40 21.67 38 8203 69788 90550418
Myalgia 35.63 21.67 60 8181 175065 90445141
Device related bacteraemia 34.82 21.67 8 8233 411 90619795
Minimal residual disease 34.54 21.67 8 8233 426 90619780
Ichthyosis 34.45 21.67 6 8235 72 90620134
Renal artery stenosis 33.40 21.67 11 8230 2166 90618040
Pyrexia 33.12 21.67 133 8108 660352 89959854
Product administered to patient of inappropriate age 31.96 21.67 13 8228 4640 90615566
Haemophagocytic lymphohistiocytosis 31.90 21.67 19 8222 15440 90604766
Febrile neutropenia 31.87 21.67 54 8187 158295 90461911
Cerebrovascular stenosis 31.01 21.67 5 8236 36 90620170
Off label use 30.95 21.67 188 8053 1102064 89518142
Skin exfoliation 30.22 21.67 34 8207 67879 90552327
Joint swelling 29.80 21.67 5 8236 503295 90116911
Hepatotoxicity 29.53 21.67 28 8213 45814 90574392
Hypertension 29.51 21.67 100 8141 457432 90162774
Graft versus host disease in skin 27.27 21.67 11 8230 3842 90616364
Chemotherapy 27.10 21.67 9 8232 1818 90618388
Peripheral artery stenosis 26.81 21.67 7 8234 613 90619593
Pityriasis rubra pilaris 25.69 21.67 5 8236 114 90620092
Swelling 25.16 21.67 4 8237 419054 90201152
Drug hypersensitivity 24.54 21.67 6 8235 463603 90156603
Granulicatella infection 24.34 21.67 5 8236 151 90620055
Chronic myeloid leukaemia 23.78 21.67 9 8232 2655 90617551
Hepatic function abnormal 23.78 21.67 25 8216 46263 90573943
Constipation 23.33 21.67 67 8174 280328 90339878
Blast cell count increased 23.01 21.67 6 8235 523 90619683
Platelet count abnormal 22.74 21.67 10 8231 4325 90615881
Sepsis 22.31 21.67 50 8191 179764 90440442
Splenomegaly 21.87 21.67 14 8227 12910 90607296

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
Acute lymphocytic leukaemia recurrent 397.14 20.70 105 10190 3586 42607454
Drug resistance 231.58 20.70 128 10167 34120 42576920
Philadelphia chromosome positive 221.89 20.70 47 10248 594 42610446
Blast crisis in myelogenous leukaemia 214.43 20.70 46 10249 620 42610420
Cytogenetic analysis abnormal 185.63 20.70 42 10253 733 42610307
Chronic myeloid leukaemia recurrent 167.59 20.70 32 10263 228 42610812
Neoplasm progression 147.13 20.70 90 10205 28910 42582130
Death 138.51 20.70 331 9964 470854 42140186
Drug intolerance 98.81 20.70 109 10186 80315 42530725
Blast cell crisis 84.79 20.70 16 10279 106 42610934
Autoimmune lymphoproliferative syndrome 81.36 20.70 17 10278 200 42610840
Lipase increased 67.24 20.70 38 10257 10528 42600512
Pancreatitis 64.40 20.70 65 10230 43203 42567837
Loss of therapeutic response 63.55 20.70 20 10275 1271 42609769
Central nervous system neoplasm 62.29 20.70 12 10283 90 42610950
Thrombocytopenia 61.21 20.70 139 10156 190140 42420900
Chronic myeloid leukaemia transformation 59.22 20.70 13 10282 196 42610844
Blast cells present 57.08 20.70 15 10280 498 42610542
Gallbladder oedema 56.80 20.70 13 10282 239 42610801
Viral haemorrhagic cystitis 56.45 20.70 20 10275 1834 42609206
Pleural effusion 56.01 20.70 91 10204 97075 42513965
Minimal residual disease 54.24 20.70 15 10280 606 42610434
Cytopenia 54.19 20.70 40 10255 17457 42593583
Peripheral arterial occlusive disease 47.34 20.70 26 10269 6812 42604228
Central nervous system leukaemia 46.18 20.70 12 10283 381 42610659
Hepatotoxicity 45.32 20.70 42 10253 25125 42585915
Acute lymphocytic leukaemia 44.52 20.70 20 10275 3411 42607629
Platelet count decreased 43.13 20.70 100 10195 138481 42472559
Stem cell transplant 42.57 20.70 18 10277 2654 42608386
Chronic myeloid leukaemia 40.41 20.70 17 10278 2475 42608565
Loss of CAR T-cell persistence 40.04 20.70 7 10288 28 42611012
Treatment failure 39.29 20.70 61 10234 62563 42548477
Leukaemic infiltration extramedullary 38.99 20.70 9 10286 172 42610868
Graft versus host disease 38.79 20.70 29 10266 12896 42598144
Periarthritis calcarea 38.78 20.70 8 10287 88 42610952
Articular calcification 38.45 20.70 8 10287 92 42610948
Cytokine release syndrome 36.13 20.70 49 10246 44478 42566562
Clonal evolution 36.06 20.70 8 10287 127 42610913
Renal artery stenosis 34.90 20.70 15 10280 2302 42608738
Myopathy toxic 34.49 20.70 11 10284 730 42610310
Hepatic calcification 33.20 20.70 9 10286 337 42610703
Adrenal cyst 33.09 20.70 8 10287 188 42610852
Bone marrow transplant 32.89 20.70 12 10283 1197 42609843
Haematopoietic stem cell mobilisation 32.80 20.70 9 10286 353 42610687
Bone pain 32.23 20.70 34 10261 23758 42587282
Gastrointestinal wall thickening 31.35 20.70 13 10282 1826 42609214
Costal cartilage fracture 31.28 20.70 8 10287 238 42610802
Adrenomegaly 31.18 20.70 9 10286 425 42610615
Renal artery angioplasty 31.15 20.70 5 10290 10 42611030
Post transplant lymphoproliferative disorder 30.85 20.70 22 10273 9098 42601942
Metamyelocyte count increased 30.51 20.70 9 10286 459 42610581
Immature granulocyte count increased 30.46 20.70 8 10287 265 42610775
Product dose omission issue 30.36 20.70 94 10201 154271 42456769
Renal artery stent placement 30.24 20.70 5 10290 13 42611027
Myeloid leukaemia 30.14 20.70 9 10286 479 42610561
Pericardial effusion 29.70 20.70 36 10259 29239 42581801
Epstein-Barr virus infection 29.60 20.70 22 10273 9696 42601344
Ichthyosis 29.57 20.70 7 10288 150 42610890
Hypertension 29.42 20.70 98 10197 167106 42443934
Dry skin 28.81 20.70 46 10249 48292 42562748
Red cell distribution width increased 28.76 20.70 19 10276 6945 42604095
Transplant 27.94 20.70 10 10285 944 42610096
Leukaemia recurrent 27.78 20.70 12 10283 1864 42609176
Pancytopenia 27.25 20.70 76 10219 117667 42493373
Myelocyte count increased 27.06 20.70 8 10287 411 42610629
Diarrhoea 26.70 20.70 44 10251 460805 42150235
Activated partial thromboplastin time shortened 25.80 20.70 8 10287 484 42610556
White blood cell count increased 25.63 20.70 42 10253 45045 42565995
Haematotoxicity 25.11 20.70 21 10274 10964 42600076
Adrenal adenoma 25.11 20.70 8 10287 529 42610511
Bone neoplasm 25.05 20.70 7 10288 294 42610746
Polymerase chain reaction positive 24.74 20.70 6 10289 143 42610897
Philadelphia positive acute lymphocytic leukaemia 24.23 20.70 5 10290 55 42610985
Malignant neoplasm progression 24.13 20.70 69 10226 108331 42502709
Leukaemic infiltration 23.71 20.70 6 10289 171 42610869
Graft versus host disease in gastrointestinal tract 23.62 20.70 15 10280 5128 42605912
Peripheral vascular disorder 23.16 20.70 15 10280 5302 42605738
Leukocytosis 23.05 20.70 32 10263 29676 42581364
Nephrocalcinosis 21.95 20.70 8 10287 795 42610245
Diaphragmatic disorder 21.94 20.70 9 10286 1230 42609810

FDA Adverse Event Reporting System (Geriatric)

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
Acute lymphocytic leukaemia recurrent 577.30 19.02 137 14253 5650 110569259
Drug resistance 295.68 19.02 145 14245 56229 110518680
Blast crisis in myelogenous leukaemia 289.48 19.02 57 14333 951 110573958
Philadelphia chromosome positive 283.58 19.02 55 14335 845 110574064
Death 210.93 19.02 347 14043 698522 109876387
Cytogenetic analysis abnormal 201.98 19.02 44 14346 1225 110573684
Chronic myeloid leukaemia recurrent 186.73 19.02 34 14356 363 110574546
Neoplasm progression 146.48 19.02 96 14294 64499 110510410
Thrombocytopenia 128.13 19.02 190 14200 348695 110226214
Lipase increased 122.24 19.02 56 14334 18616 110556293
Platelet count decreased 115.56 19.02 146 14244 230297 110344612
Central nervous system leukaemia 113.94 19.02 24 14366 567 110574342
Pleural effusion 107.73 19.02 124 14266 177585 110397324
Blast cell crisis 102.35 19.02 18 14372 155 110574754
Peripheral arterial occlusive disease 101.27 19.02 40 14350 9240 110565669
Cytopenia 99.62 19.02 57 14333 30059 110544850
Autoimmune lymphoproliferative syndrome 90.35 19.02 17 14373 220 110574689
Pericardial effusion 79.09 19.02 63 14327 57154 110517755
Graft versus host disease 77.07 19.02 41 14349 18765 110556144
Renal artery stenosis 74.08 19.02 25 14365 3701 110571208
Dry skin 73.55 19.02 80 14310 107573 110467336
Cytokine release syndrome 69.75 19.02 64 14326 70242 110504667
Stem cell transplant 66.11 19.02 24 14366 4403 110570506
Hepatotoxicity 65.41 19.02 59 14331 63341 110511568
Chronic myeloid leukaemia transformation 61.59 19.02 13 14377 310 110574599
Ichthyosis 60.83 19.02 12 14378 202 110574707
Pancytopenia 58.69 19.02 101 14289 209512 110365397
Minimal residual disease 57.06 19.02 15 14375 938 110573971
Haematotoxicity 56.90 19.02 35 14355 21047 110553862
Viral haemorrhagic cystitis 56.69 19.02 20 14370 3379 110571530
Leukaemia recurrent 54.43 19.02 19 14371 3112 110571797
Philadelphia positive acute lymphocytic leukaemia 52.22 19.02 9 14381 68 110574841
Pancreatitis 51.20 19.02 62 14328 93471 110481438
Febrile neutropenia 50.75 19.02 121 14269 316646 110258263
Loss of therapeutic response 50.52 19.02 17 14373 2493 110572416
Rash 47.68 19.02 222 14168 820742 109754167
Therapeutic response delayed 47.07 19.02 14 14376 1376 110573533
Graft versus host disease in eye 46.42 19.02 11 14379 449 110574460
Product administered to patient of inappropriate age 46.08 19.02 22 14368 8014 110566895
Bone marrow transplant 44.62 19.02 14 14376 1646 110573263
Neutrophil count decreased 44.45 19.02 66 14324 120875 110454034
Hypertension 43.97 19.02 156 14234 509928 110064981
Bone pain 43.76 19.02 48 14342 65085 110509824
Hepatic function abnormal 43.76 19.02 56 14334 89239 110485670
Neutropenia 43.57 19.02 127 14263 374493 110200416
Periarthritis calcarea 43.23 19.02 8 14382 94 110574815
Peripheral artery stenosis 43.10 19.02 13 14377 1341 110573568
Chronic myeloid leukaemia 41.71 19.02 17 14373 4256 110570653
Clonal evolution 41.57 19.02 9 14381 243 110574666
Pneumonia fungal 41.11 19.02 25 14365 14729 110560180
Adrenomegaly 40.60 19.02 10 14380 481 110574428
Joint swelling 40.50 19.02 5 14385 442840 110132069
Venoocclusive liver disease 40.41 19.02 25 14365 15182 110559727
Amylase increased 39.54 19.02 23 14367 12496 110562413
Drug hypersensitivity 39.46 19.02 6 14384 454084 110120825
Infusion related reaction 38.26 19.02 3 14387 381159 110193750
Hepatic calcification 38.25 19.02 9 14381 356 110574553
Gene mutation 38.18 19.02 15 14375 3414 110571495
Loss of CAR T-cell persistence 38.03 19.02 6 14384 24 110574885
Acute lymphocytic leukaemia 36.81 19.02 17 14373 5748 110569161
Haematopoietic stem cell mobilisation 36.72 19.02 9 14381 424 110574485
Articular calcification 35.98 19.02 8 14382 245 110574664
Costal cartilage fracture 35.73 19.02 8 14382 253 110574656
Adrenal cyst 35.67 19.02 8 14382 255 110574654
Pyrexia 35.13 19.02 218 14172 898047 109676862
Leukocytosis 35.01 19.02 39 14351 53789 110521120
Carotid artery stenosis 34.61 19.02 19 14371 9244 110565665
Swelling 34.57 19.02 3 14387 351038 110223871
Myeloid leukaemia 34.54 19.02 10 14380 895 110574014
Cerebral infarction 34.47 19.02 38 14352 51800 110523109
Ischaemic stroke 34.15 19.02 34 14356 41229 110533680
Blast cells present 33.77 19.02 10 14380 968 110573941
Leukaemic infiltration extramedullary 33.35 19.02 8 14382 344 110574565
Ichthyosis acquired 33.06 19.02 5 14385 14 110574895
Capillary leak syndrome 32.99 19.02 15 14375 4893 110570016
Coronary artery stenosis 32.51 19.02 21 14369 13737 110561172
Central nervous system neoplasm 32.48 19.02 7 14383 185 110574724
Metamyelocyte count increased 32.36 19.02 9 14381 697 110574212
Catabolic state 31.79 19.02 6 14384 79 110574830
Chronic graft versus host disease 31.53 19.02 18 14372 9439 110565470
Epstein-Barr virus infection 31.07 19.02 23 14367 18715 110556194
Renal artery angioplasty 30.62 19.02 5 14385 26 110574883
Post transplant lymphoproliferative disorder 30.09 19.02 21 14369 15592 110559317
Off label use 30 19.02 312 14078 1499873 109075036
Bone marrow leukaemic cell infiltration 29.93 19.02 6 14384 110 110574799
Pityriasis rubra pilaris 29.92 19.02 7 14383 270 110574639
Malignant neoplasm progression 29.35 19.02 68 14322 174499 110400410
Moyamoya disease 28.93 19.02 6 14384 131 110574778
Activated partial thromboplastin time shortened 28.77 19.02 9 14381 1048 110573861
Blast cell count increased 28.71 19.02 10 14380 1627 110573282
Skin toxicity 27.88 19.02 18 14372 11765 110563144
Full blood count decreased 27.59 19.02 27 14363 32072 110542837
Cerebrovascular stenosis 27.50 19.02 6 14384 168 110574741
Myopathy toxic 26.77 19.02 9 14381 1316 110573593
Immature granulocyte count increased 26.30 19.02 8 14382 849 110574060
Neoplasm recurrence 26.03 19.02 13 14377 5219 110569690
Carotid arteriosclerosis 25.92 19.02 11 14379 3046 110571863
Myelocyte count increased 25.79 19.02 8 14382 906 110574003
Splenomegaly 25.65 19.02 23 14367 24475 110550434
Red cell distribution width increased 25.64 19.02 20 14370 17582 110557327
Product dose omission issue 25.63 19.02 96 14294 321686 110253223
Peripheral vascular disorder 25.10 19.02 15 14375 8561 110566348
Renal artery stent placement 25.03 19.02 5 14385 90 110574819
Mesenteric arterial occlusion 24.79 19.02 6 14384 268 110574641
Blood bilirubin increased 24.44 19.02 39 14351 75933 110498976
Vascular occlusion 24.24 19.02 9 14381 1758 110573151
Skin exfoliation 24.19 19.02 42 14348 87609 110487300
White blood cell count decreased 24.02 19.02 75 14315 229315 110345594
Disease progression 23.93 19.02 78 14312 243956 110330953
Fall 23.88 19.02 26 14364 603456 109971453
Transaminases increased 23.86 19.02 35 14355 63355 110511554
Vomiting 23.82 19.02 52 14338 910623 109664286
Diaphragmatic disorder 23.67 19.02 9 14381 1877 110573032
Acquired gene mutation 23.65 19.02 10 14380 2744 110572165
Musculoskeletal stiffness 23.61 19.02 4 14386 279818 110295091
Abdominal discomfort 23.38 19.02 11 14379 393847 110181062
Graft versus host disease in skin 23.03 19.02 14 14376 8240 110566669
Confusional state 22.34 19.02 17 14373 468663 110106246
Bone marrow necrosis 22.09 19.02 6 14384 425 110574484
Granulicatella infection 22.07 19.02 5 14385 167 110574742
Adrenal adenoma 21.95 19.02 8 14382 1484 110573425
Condition aggravated 21.76 19.02 39 14351 734797 109840112
Constipation 21.59 19.02 98 14292 357688 110217221
Activated partial thromboplastin time prolonged 21.47 19.02 20 14370 22348 110552561
Angina pectoris 21.46 19.02 33 14357 62262 110512647
Acute coronary syndrome 20.91 19.02 20 14370 23092 110551817
Septic shock 20.82 19.02 56 14334 157472 110417437
Pancreatic enzymes increased 20.80 19.02 8 14382 1721 110573188
Wheezing 20.77 19.02 4 14386 255226 110319683
Maternal exposure during pregnancy 20.73 19.02 4 14386 254879 110320030
Nasopharyngitis 20.52 19.02 13 14377 394348 110180561
Bone marrow failure 20.43 19.02 31 14359 57817 110517092
Nephrocalcinosis 20.42 19.02 8 14382 1806 110573103
Urticaria 20.36 19.02 8 14382 318849 110256060
Abdominal pain 20.29 19.02 125 14265 512864 110062045
Haemangioma 20.18 19.02 9 14381 2807 110572102
Procalcitonin increased 19.95 19.02 10 14380 4046 110570863
Peripheral artery occlusion 19.91 19.02 9 14381 2896 110572013
Blister 19.75 19.02 3 14387 227373 110347536
Device related bacteraemia 19.61 19.02 7 14383 1223 110573686
Graft versus host disease in gastrointestinal tract 19.51 19.02 13 14377 8955 110565954
Transplant 19.37 19.02 7 14383 1267 110573642
Peripheral ischaemia 19.30 19.02 14 14376 11044 110563865
Acute myocardial infarction 19.14 19.02 37 14353 83740 110491169
Pancreatitis chronic 19.04 19.02 10 14380 4455 110570454

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EA05 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
BCR-ABL tyrosine kinase inhibitors
FDA MoA N0000175076 Protein Kinase Inhibitors
MeSH PA D000092004 Tyrosine Kinase Inhibitors
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D047428 Protein Kinase Inhibitors
FDA EPC N0000175605 Kinase Inhibitor
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:38637 tyrosine kinase inhibitor

Related Drugs by ATC class:

L01EA BCR-ABL tyrosine kinase inhibitors 5 drugs
asciminibbosutinibdasatinibimatinibnilotinib

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Chronic myeloid leukemia indication 92818009 DOID:8552
Philadelphia chromosome-positive acute lymphoblastic leukemia indication 425688002




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.98 acidic
pKa2 8.49 Basic
pKa3 5.58 Basic
pKa4 4.36 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 10MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 18, 2020 RX TABLET ORAL 9029533 Dec. 22, 2026 A METHOD FOR THE TREATMENT OF LEUKEMIAS
EQ 10MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 18, 2020 RX TABLET ORAL 9029533 Dec. 22, 2026 A METHOD FOR TREATING ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 10MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 18, 2020 RX TABLET ORAL 9029533 Dec. 22, 2026 A METHOD FOR TREATING LEUKEMIA RESULTING FROM A MUTATION IN THE BCR-ABL KINASE DOMAIN
EQ 10MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 18, 2020 RX TABLET ORAL 9029533 Dec. 22, 2026 A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 10MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 18, 2020 RX TABLET ORAL 9029533 Dec. 22, 2026 A METHOD OF TREATING CHRONIC MYELOGENOUS LEUKEMIA
EQ 15MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 9029533 Dec. 22, 2026 A METHOD FOR THE TREATMENT OF LEUKEMIAS
EQ 15MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 9029533 Dec. 22, 2026 A METHOD FOR TREATING ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 15MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 9029533 Dec. 22, 2026 A METHOD FOR TREATING LEUKEMIA RESULTING FROM A MUTATION IN THE BCR-ABL KINASE DOMAIN
EQ 15MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 9029533 Dec. 22, 2026 A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 15MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 9029533 Dec. 22, 2026 A METHOD OF TREATING CHRONIC MYELOGENOUS LEUKEMIA
EQ 30MG BASE ICLUSIG TAKEDA PHARMS USA N203469 April 23, 2015 RX TABLET ORAL 9029533 Dec. 22, 2026 A METHOD FOR THE TREATMENT OF LEUKEMIAS
EQ 30MG BASE ICLUSIG TAKEDA PHARMS USA N203469 April 23, 2015 RX TABLET ORAL 9029533 Dec. 22, 2026 A METHOD FOR TREATING ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 30MG BASE ICLUSIG TAKEDA PHARMS USA N203469 April 23, 2015 RX TABLET ORAL 9029533 Dec. 22, 2026 A METHOD FOR TREATING LEUKEMIA RESULTING FROM A MUTATION IN THE BCR-ABL KINASE DOMAIN
EQ 30MG BASE ICLUSIG TAKEDA PHARMS USA N203469 April 23, 2015 RX TABLET ORAL 9029533 Dec. 22, 2026 A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 30MG BASE ICLUSIG TAKEDA PHARMS USA N203469 April 23, 2015 RX TABLET ORAL 9029533 Dec. 22, 2026 A METHOD OF TREATING CHRONIC MYELOGENOUS LEUKEMIA
EQ 45MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 9029533 Dec. 22, 2026 A METHOD FOR THE TREATMENT OF LEUKEMIAS
EQ 45MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 9029533 Dec. 22, 2026 A METHOD FOR TREATING ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 45MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 9029533 Dec. 22, 2026 A METHOD FOR TREATING LEUKEMIA RESULTING FROM A MUTATION IN THE BCR-ABL KINASE DOMAIN
EQ 45MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 9029533 Dec. 22, 2026 A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 45MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 9029533 Dec. 22, 2026 A METHOD OF TREATING CHRONIC MYELOGENOUS LEUKEMIA
EQ 10MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 18, 2020 RX TABLET ORAL 11192895 Dec. 12, 2033 A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 10MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 18, 2020 RX TABLET ORAL 11192895 Dec. 12, 2033 A METHOD FOR TREATING LEUKEMIA RESULTING FROM A MUTATION IN THE BCR-ABL KINASE DOMAIN
EQ 10MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 18, 2020 RX TABLET ORAL 11192895 Dec. 12, 2033 A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 10MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 18, 2020 RX TABLET ORAL 11192897 Dec. 12, 2033 A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 10MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 18, 2020 RX TABLET ORAL 11192897 Dec. 12, 2033 A METHOD FOR TREATING LEUKEMIA RESULTING FROM A MUTATION IN THE BCR-ABL KINASE DOMAIN
EQ 10MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 18, 2020 RX TABLET ORAL 11192897 Dec. 12, 2033 A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 10MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 18, 2020 RX TABLET ORAL 11384086 Dec. 12, 2033 A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 10MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 18, 2020 RX TABLET ORAL 11384086 Dec. 12, 2033 A METHOD FOR TREATING LEUKEMIA RESULTING FROM A MUTATION IN THE BCR-ABL KINASE DOMAIN
EQ 10MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 18, 2020 RX TABLET ORAL 11384086 Dec. 12, 2033 A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 10MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 18, 2020 RX TABLET ORAL 9493470 Dec. 12, 2033 A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 10MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 18, 2020 RX TABLET ORAL 9493470 Dec. 12, 2033 A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 15MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 11192895 Dec. 12, 2033 A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 15MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 11192895 Dec. 12, 2033 A METHOD FOR TREATING LEUKEMIA RESULTING FROM A MUTATION IN THE BCR-ABL KINASE DOMAIN
EQ 15MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 11192895 Dec. 12, 2033 A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 15MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 11192897 Dec. 12, 2033 A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 15MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 11192897 Dec. 12, 2033 A METHOD FOR TREATING LEUKEMIA RESULTING FROM A MUTATION IN THE BCR-ABL KINASE DOMAIN
EQ 15MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 11192897 Dec. 12, 2033 A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 15MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 11384086 Dec. 12, 2033 A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 15MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 11384086 Dec. 12, 2033 A METHOD FOR TREATING LEUKEMIA RESULTING FROM A MUTATION IN THE BCR-ABL KINASE DOMAIN
EQ 15MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 11384086 Dec. 12, 2033 A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 15MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 9493470 Dec. 12, 2033 A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 15MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 9493470 Dec. 12, 2033 A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 30MG BASE ICLUSIG TAKEDA PHARMS USA N203469 April 23, 2015 RX TABLET ORAL 11192895 Dec. 12, 2033 A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 30MG BASE ICLUSIG TAKEDA PHARMS USA N203469 April 23, 2015 RX TABLET ORAL 11192895 Dec. 12, 2033 A METHOD FOR TREATING LEUKEMIA RESULTING FROM A MUTATION IN THE BCR-ABL KINASE DOMAIN
EQ 30MG BASE ICLUSIG TAKEDA PHARMS USA N203469 April 23, 2015 RX TABLET ORAL 11192895 Dec. 12, 2033 A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 30MG BASE ICLUSIG TAKEDA PHARMS USA N203469 April 23, 2015 RX TABLET ORAL 11192897 Dec. 12, 2033 A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 30MG BASE ICLUSIG TAKEDA PHARMS USA N203469 April 23, 2015 RX TABLET ORAL 11192897 Dec. 12, 2033 A METHOD FOR TREATING LEUKEMIA RESULTING FROM A MUTATION IN THE BCR-ABL KINASE DOMAIN
EQ 30MG BASE ICLUSIG TAKEDA PHARMS USA N203469 April 23, 2015 RX TABLET ORAL 11192897 Dec. 12, 2033 A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 30MG BASE ICLUSIG TAKEDA PHARMS USA N203469 April 23, 2015 RX TABLET ORAL 11384086 Dec. 12, 2033 A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 30MG BASE ICLUSIG TAKEDA PHARMS USA N203469 April 23, 2015 RX TABLET ORAL 11384086 Dec. 12, 2033 A METHOD FOR TREATING LEUKEMIA RESULTING FROM A MUTATION IN THE BCR-ABL KINASE DOMAIN
EQ 30MG BASE ICLUSIG TAKEDA PHARMS USA N203469 April 23, 2015 RX TABLET ORAL 11384086 Dec. 12, 2033 A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 30MG BASE ICLUSIG TAKEDA PHARMS USA N203469 April 23, 2015 RX TABLET ORAL 9493470 Dec. 12, 2033 A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 30MG BASE ICLUSIG TAKEDA PHARMS USA N203469 April 23, 2015 RX TABLET ORAL 9493470 Dec. 12, 2033 A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 45MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 11192895 Dec. 12, 2033 A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 45MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 11192895 Dec. 12, 2033 A METHOD FOR TREATING LEUKEMIA RESULTING FROM A MUTATION IN THE BCR-ABL KINASE DOMAIN
EQ 45MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 11192895 Dec. 12, 2033 A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 45MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 11192897 Dec. 12, 2033 A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 45MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 11192897 Dec. 12, 2033 A METHOD FOR TREATING LEUKEMIA RESULTING FROM A MUTATION IN THE BCR-ABL KINASE DOMAIN
EQ 45MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 11192897 Dec. 12, 2033 A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 45MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 11384086 Dec. 12, 2033 A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 45MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 11384086 Dec. 12, 2033 A METHOD FOR TREATING LEUKEMIA RESULTING FROM A MUTATION IN THE BCR-ABL KINASE DOMAIN
EQ 45MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 11384086 Dec. 12, 2033 A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 45MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 9493470 Dec. 12, 2033 A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 45MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL 9493470 Dec. 12, 2033 A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 10MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 18, 2020 RX TABLET ORAL March 19, 2027 TREATMENT OF ADULT PATIENTS WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA (PH+ ALL) IN COMBINATION WITH CHEMOTHERAPY
EQ 15MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL March 19, 2027 TREATMENT OF ADULT PATIENTS WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA (PH+ ALL) IN COMBINATION WITH CHEMOTHERAPY
EQ 30MG BASE ICLUSIG TAKEDA PHARMS USA N203469 April 23, 2015 RX TABLET ORAL March 19, 2027 TREATMENT OF ADULT PATIENTS WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA (PH+ ALL) IN COMBINATION WITH CHEMOTHERAPY
EQ 45MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL March 19, 2027 TREATMENT OF ADULT PATIENTS WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA (PH+ ALL) IN COMBINATION WITH CHEMOTHERAPY
EQ 10MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 18, 2020 RX TABLET ORAL March 19, 2031 TREATMENT OF ADULT PATIENTS WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA (PH+ ALL)
EQ 15MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL March 19, 2031 TREATMENT OF ADULT PATIENTS WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA (PH+ ALL)
EQ 30MG BASE ICLUSIG TAKEDA PHARMS USA N203469 April 23, 2015 RX TABLET ORAL March 19, 2031 TREATMENT OF ADULT PATIENTS WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA (PH+ ALL)
EQ 45MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL March 19, 2031 TREATMENT OF ADULT PATIENTS WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA (PH+ ALL)

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Tyrosine-protein kinase ABL1 Kinase INHIBITOR IC50 9.43 WOMBAT-PK CHEMBL
Breakpoint cluster region protein Kinase INHIBITOR Kd 7.30 CHEMBL CHEMBL
Platelet-derived growth factor receptor beta Kinase IC50 8.92 CHEMBL
Mast/stem cell growth factor receptor Kit Kinase INHIBITOR IC50 7.90 WOMBAT-PK
Proto-oncogene tyrosine-protein kinase Src Kinase IC50 8.52 CHEMBL
Tyrosine-protein kinase Lck Kinase Kd 7.62 CHEMBL
Tyrosine-protein kinase Yes Kinase Kd 6.66 CHEMBL
Tyrosine-protein kinase Fyn Kinase Kd 7.44 CHEMBL
Ephrin type-A receptor 2 Kinase Kd 7.57 CHEMBL
Serine/threonine-protein kinase B-raf Kinase Kd 5.92 CHEMBL
Receptor-type tyrosine-protein kinase FLT3 Kinase IC50 9.52 CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret Kinase IC50 7.59 CHEMBL
Vascular endothelial growth factor receptor 1 Kinase IC50 8.43 CHEMBL
Vascular endothelial growth factor receptor 2 Kinase INHIBITOR IC50 8.82 WOMBAT-PK
Macrophage colony-stimulating factor 1 receptor Kinase IC50 8.07 CHEMBL
Platelet-derived growth factor receptor alpha Kinase INHIBITOR IC50 8.96 WOMBAT-PK
Myosin light chain kinase, smooth muscle Kinase Kd 7 CHEMBL
Fibroblast growth factor receptor 3 Kinase IC50 8.03 CHEMBL
Tyrosine-protein kinase HCK Kinase Kd 7.09 CHEMBL
Tyrosine-protein kinase JAK1 Kinase IC50 7.49 CHEMBL
High affinity nerve growth factor receptor Kinase IC50 7.94 CHEMBL
Tyrosine-protein kinase JAK2 Kinase IC50 6.77 CHEMBL
Tyrosine-protein kinase CSK Kinase INHIBITOR IC50 8.27 WOMBAT-PK
Tyrosine-protein kinase Lyn Kinase INHIBITOR IC50 9.62 WOMBAT-PK
Fibroblast growth factor receptor 1 Kinase INHIBITOR IC50 8.66 WOMBAT-PK
Abelson tyrosine-protein kinase 2 Kinase Kd 7.70 CHEMBL
Mitogen-activated protein kinase 11 Kinase Kd 6 CHEMBL
Ephrin type-A receptor 5 Kinase Kd 8.10 CHEMBL
Ephrin type-A receptor 4 Kinase Kd 4.77 CHEMBL
Fibroblast growth factor receptor 2 Kinase IC50 8.89 CHEMBL
TRAF2 and NCK-interacting protein kinase Kinase Kd 6.42 CHEMBL
Tyrosine-protein kinase Fgr Kinase Kd 7.42 CHEMBL
Mitogen-activated protein kinase 14 Kinase Kd 6.81 CHEMBL
Tyrosine-protein kinase FRK Kinase Kd 7.03 CHEMBL
Cyclin-G-associated kinase Kinase Kd 5.73 CHEMBL
Receptor-interacting serine/threonine-protein kinase 2 Kinase IC50 8.17 CHEMBL
Cyclin-dependent kinase 8 Kinase INHIBITOR Kd 8.17 IUPHAR
Cyclin-dependent kinase 16 Kinase Kd 5.76 CHEMBL
Mitogen-activated protein kinase 9 Kinase Kd 5.10 CHEMBL
Calcium/calmodulin-dependent protein kinase kinase 2 Kinase Kd 5.75 CHEMBL
Epithelial discoidin domain-containing receptor 1 Kinase Kd 7.75 CHEMBL
Ephrin type-B receptor 4 Kinase Kd 5.83 CHEMBL
TGF-beta receptor type-2 Kinase Kd 5.75 CHEMBL
MAP kinase-activated protein kinase 2 Kinase Kd 6.33 CHEMBL
Tyrosine-protein kinase BTK Kinase Kd 5.74 CHEMBL
Ephrin type-B receptor 2 Kinase Kd 5.73 CHEMBL
Non-receptor tyrosine-protein kinase TNK1 Kinase Kd 7.08 CHEMBL
Cyclin-dependent kinase 17 Kinase Kd 6.47 CHEMBL
Mitogen-activated protein kinase kinase kinase MLT Kinase Kd 7.39 CHEMBL
Protein-tyrosine kinase 2-beta Kinase Kd 6.53 CHEMBL
Maternal embryonic leucine zipper kinase Kinase Kd 5.53 CHEMBL
Discoidin domain-containing receptor 2 Kinase Kd 7.06 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 1 Kinase Kd 6.11 CHEMBL
cAMP-dependent protein kinase catalytic subunit alpha Kinase IC50 6.21 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 4 Kinase Kd 6.51 CHEMBL
Cyclin-dependent kinase 19 Kinase INHIBITOR Kd 7.92 IUPHAR
Ephrin type-A receptor 1 Kinase Kd 5.94 CHEMBL
Ephrin type-B receptor 3 Kinase Kd 6.26 CHEMBL
Receptor-interacting serine/threonine-protein kinase 1 Kinase INHIBITOR IC50 7.92 IUPHAR
Fibroblast growth factor receptor 4 Kinase IC50 8.15 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 2 Kinase Kd 7.39 CHEMBL
Interleukin-1 receptor-associated kinase 4 Kinase Kd 5.66 CHEMBL
Interleukin-1 receptor-associated kinase 1 Kinase Kd 6.16 CHEMBL
Serine/threonine-protein kinase TAO3 Kinase Kd 5.67 CHEMBL
Serine/threonine-protein kinase ULK3 Kinase Kd 5.76 CHEMBL
Mitogen-activated protein kinase kinase kinase 1 Kinase Kd 6.31 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 5 Kinase Kd 5.53 CHEMBL
Leucine-rich repeat serine/threonine-protein kinase 2 Kinase IC50 7.51 CHEMBL
Bcr/Abl fusion protein Kinase IC50 9.30 CHEMBL
Receptor-interacting serine/threonine-protein kinase 3 Kinase INHIBITOR Ki 8.80 IUPHAR
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 6.11 CHEMBL
ATP-dependent RNA helicase DDX1 Enzyme Kd 7.07 CHEMBL
ATP-binding cassette sub-family G member 2 Transporter IC50 7.40 CHEMBL
Proto-oncogene tyrosine-protein kinase Src Kinase IC50 9.05 CHEMBL

External reference:

IDSource
4340891KFS UNII
D09950 KEGG_DRUG
4032031 VUID
N0000186141 NUI
4032031 VANDF
C2987417 UMLSCUI
CHEBI:78543 CHEBI
0LI PDB_CHEM_ID
CHEMBL1171837 ChEMBL_ID
24826799 PUBCHEM_CID
DB08901 DRUGBANK_ID
CHEMBL2105708 ChEMBL_ID
9362 INN_ID
C545373 MESH_SUPPLEMENTAL_RECORD_UI
5890 IUPHAR_LIGAND_ID
1114544-31-8 SECONDARY_CAS_RN
1364347 RXNORM
196462 MMSL
29016 MMSL
31534 MMSL
d07936 MMSL
014797 NDDF
014798 NDDF
703796003 SNOMEDCT_US
703797007 SNOMEDCT_US
703798002 SNOMEDCT_US
4340891KFS INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Iclusig HUMAN PRESCRIPTION DRUG LABEL 1 63020-533 TABLET, FILM COATED 30 mg ORAL NDA 33 sections
Iclusig HUMAN PRESCRIPTION DRUG LABEL 1 63020-533 TABLET, FILM COATED 30 mg ORAL NDA 33 sections
Iclusig HUMAN PRESCRIPTION DRUG LABEL 1 63020-534 TABLET, FILM COATED 45 mg ORAL NDA 33 sections
Iclusig HUMAN PRESCRIPTION DRUG LABEL 1 63020-534 TABLET, FILM COATED 45 mg ORAL NDA 33 sections
Iclusig HUMAN PRESCRIPTION DRUG LABEL 1 63020-535 TABLET, FILM COATED 15 mg ORAL NDA 33 sections
Iclusig HUMAN PRESCRIPTION DRUG LABEL 1 63020-535 TABLET, FILM COATED 15 mg ORAL NDA 33 sections
Iclusig HUMAN PRESCRIPTION DRUG LABEL 1 63020-536 TABLET, FILM COATED 10 mg ORAL NDA 33 sections
Iclusig HUMAN PRESCRIPTION DRUG LABEL 1 63020-536 TABLET, FILM COATED 10 mg ORAL NDA 33 sections