ponatinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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

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 215.16 22.15 49 5724 1926 50597425
Philadelphia chromosome positive 172.95 22.15 31 5742 348 50599003
Chronic myeloid leukaemia recurrent 120.96 22.15 21 5752 193 50599158
Blast crisis in myelogenous leukaemia 114.55 22.15 23 5750 489 50598862
Cytogenetic analysis abnormal 105.92 22.15 23 5750 723 50598628
Neoplasm progression 97.27 22.15 53 5720 29104 50570247
Dry skin 92.67 22.15 59 5714 43132 50556219
Drug resistance 78.93 22.15 40 5733 18949 50580402
Rash 77.38 22.15 160 5613 437311 50162040
Death 73.37 22.15 132 5641 325247 50274104
Peripheral arterial occlusive disease 70.44 22.15 23 5750 3514 50595837
Blast cell crisis 66.79 22.15 11 5762 71 50599280
Therapeutic response delayed 61.51 22.15 14 5759 547 50598804
Stem cell transplant 55.12 22.15 16 5757 1652 50597699
Thrombocytopenia 54.72 22.15 70 5703 127603 50471748
Cytopenia 50.14 22.15 23 5750 8752 50590599
Hypertension 46.58 22.15 85 5688 211118 50388233
Pleural effusion 41.90 22.15 49 5724 81405 50517946
Leukaemia recurrent 41.31 22.15 12 5761 1242 50598109
Off label use 41.25 22.15 133 5640 474293 50125058
Platelet count decreased 41.21 22.15 54 5719 100672 50498679
Graft versus host disease 41.09 22.15 18 5755 6148 50593203
Catabolic state 41.07 22.15 7 5766 57 50599294
Ichthyosis acquired 38.05 22.15 5 5768 3 50599348
Lipase increased 35.49 22.15 18 5755 8523 50590828
Pyrexia 34.27 22.15 108 5665 380095 50219256
Pancytopenia 32.74 22.15 44 5729 83986 50515365
Product administered to patient of inappropriate age 32.58 22.15 12 5761 2618 50596733
Chemotherapy 31.76 22.15 10 5763 1359 50597992
Chronic myeloid leukaemia transformation 30.93 22.15 6 5767 106 50599245
Central nervous system leukaemia 30.46 22.15 6 5767 115 50599236
Soft tissue necrosis 28.23 22.15 7 5766 396 50598955
Ischaemic stroke 27.42 22.15 19 5754 15929 50583422
Peripheral artery stenosis 26.34 22.15 7 5766 522 50598829
Philadelphia positive acute lymphocytic leukaemia 26.09 22.15 4 5769 15 50599336
Pancreatitis 25.93 22.15 28 5745 42586 50556765
Capillary leak syndrome 24.81 22.15 9 5764 1881 50597470
Skin exfoliation 23.89 22.15 24 5749 33588 50565763
Bone pain 23.58 22.15 28 5745 47201 50552150
Skin wrinkling 22.79 22.15 7 5766 876 50598475
Graft versus host disease in skin 22.17 22.15 9 5764 2547 50596804

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 227.90 21.34 63 7357 2453 29564654
Drug resistance 200.75 21.34 101 7319 21439 29545668
Neoplasm progression 181.45 21.34 90 7330 18522 29548585
Cytogenetic analysis abnormal 152.24 21.34 34 7386 536 29566571
Blast crisis in myelogenous leukaemia 126.34 21.34 29 7391 520 29566587
Chronic myeloid leukaemia recurrent 114.60 21.34 22 7398 155 29566952
Loss of therapeutic response 90.10 21.34 20 7400 306 29566801
Philadelphia chromosome positive 79.53 21.34 18 7402 302 29566805
Blast cell crisis 68.69 21.34 13 7407 84 29567023
Lipase increased 65.77 21.34 35 7385 8302 29558805
Autoimmune lymphoproliferative syndrome 61.72 21.34 13 7407 153 29566954
Drug intolerance 61.53 21.34 68 7352 48311 29518796
Death 60.29 21.34 205 7215 341879 29225228
Blast cells present 57.17 21.34 15 7405 476 29566631
Peripheral arterial occlusive disease 47.78 21.34 24 7396 5052 29562055
Viral haemorrhagic cystitis 47.54 21.34 15 7405 925 29566182
Pleural effusion 47.29 21.34 73 7347 71835 29495272
Chronic myeloid leukaemia transformation 45.61 21.34 10 7410 144 29566963
Hepatotoxicity 43.55 21.34 36 7384 17831 29549276
Gallbladder oedema 42.86 21.34 10 7410 193 29566914
Pancreatitis 41.26 21.34 47 7373 34467 29532640
Stem cell transplant 40.01 21.34 16 7404 1971 29565136
Loss of CAR T-cell persistence 39.78 21.34 7 7413 28 29567079
Cytokine release syndrome 39.64 21.34 30 7390 13089 29554018
Central nervous system neoplasm 39.54 21.34 8 7412 76 29567031
Bone marrow transplant 39.37 21.34 13 7407 927 29566180
Haematopoietic stem cell mobilisation 39.06 21.34 9 7411 164 29566943
Platelet count decreased 38.99 21.34 83 7337 104589 29462518
Renal artery stenosis 36.77 21.34 15 7405 1946 29565161
Thrombocytopenia 36.15 21.34 94 7326 134729 29432378
Clonal evolution 35.93 21.34 8 7412 124 29566983
Graft versus host disease 35.87 21.34 25 7395 9603 29557504
Cytopenia 35.34 21.34 25 7395 9834 29557273
Central nervous system leukaemia 35.24 21.34 9 7411 256 29566851
Hepatic calcification 32.92 21.34 9 7411 335 29566772
Adrenomegaly 32.59 21.34 9 7411 348 29566759
Acute lymphocytic leukaemia 32.53 21.34 15 7405 2616 29564491
Metamyelocyte count increased 31.89 21.34 9 7411 377 29566730
Renal artery stent placement 30.97 21.34 5 7415 10 29567097
Renal artery angioplasty 30.97 21.34 5 7415 10 29567097
Costal cartilage fracture 30.76 21.34 8 7412 245 29566862
Transplant 30.64 21.34 10 7410 687 29566420
Periarthritis calcarea 29.85 21.34 6 7414 55 29567052
Post transplant lymphoproliferative disorder 29.65 21.34 18 7402 5475 29561632
Articular calcification 29.56 21.34 6 7414 58 29567049
Graft versus host disease in gastrointestinal tract 29.48 21.34 15 7405 3243 29563864
Dry skin 28.29 21.34 32 7388 23275 29543832
Immature granulocyte count increased 28.00 21.34 6 7414 77 29567030
Myelocyte count increased 27.90 21.34 8 7412 355 29566752
Adrenal cyst 27.65 21.34 6 7414 82 29567025
Bone pain 27.06 21.34 28 7392 18424 29548683
Red cell distribution width increased 26.90 21.34 16 7404 4691 29562416
Epstein-Barr virus infection 26.55 21.34 18 7402 6611 29560496
Off label use 26.15 21.34 146 7274 300654 29266453
Hypertension 25.96 21.34 76 7344 116538 29450569
Gastrointestinal wall thickening 25.60 21.34 10 7410 1158 29565949
Bone neoplasm 25.41 21.34 7 7413 268 29566839
Treatment failure 24.94 21.34 38 7382 36901 29530206
Peripheral vascular disorder 24.74 21.34 15 7405 4552 29562555
Diaphragmatic disorder 23.64 21.34 9 7411 973 29566134
Graft versus host disease in skin 23.35 21.34 13 7407 3366 29563741
Monocyte count decreased 22.66 21.34 9 7411 1089 29566018
Activated partial thromboplastin time prolonged 21.84 21.34 17 7403 7725 29559382

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 321.20 20.16 83 10242 3943 64484464
Drug resistance 196.84 20.16 101 10224 35001 64453406
Philadelphia chromosome positive 182.42 20.16 37 10288 580 64487827
Blast crisis in myelogenous leukaemia 172.43 20.16 37 10288 772 64487635
Neoplasm progression 160.56 20.16 93 10232 40871 64447536
Cytogenetic analysis abnormal 122.54 20.16 29 10296 952 64487455
Chronic myeloid leukaemia recurrent 120.12 20.16 23 10302 263 64488144
Peripheral arterial occlusive disease 97.16 20.16 38 10287 6949 64481458
Lipase increased 85.20 20.16 43 10282 14359 64474048
Platelet count decreased 83.95 20.16 118 10207 167593 64320814
Pleural effusion 80.22 20.16 100 10225 126459 64361948
Dry skin 75.92 20.16 64 10261 51097 64437310
Blast cell crisis 75.38 20.16 14 10311 134 64488273
Stem cell transplant 70.68 20.16 25 10300 3456 64484951
Thrombocytopenia 68.68 20.16 126 10199 223675 64264732
Autoimmune lymphoproliferative syndrome 66.14 20.16 13 10312 172 64488235
Death 64.40 20.16 196 10129 482509 64005898
Rash 60.02 20.16 185 10140 458364 64030043
Hypertension 59.17 20.16 129 10196 259132 64229275
Cytopenia 57.59 20.16 34 10291 15437 64472970
Renal artery stenosis 55.29 20.16 20 10305 2949 64485458
Loss of therapeutic response 54.84 20.16 12 10313 275 64488132
Cytokine release syndrome 50.67 20.16 35 10290 20794 64467613
Therapeutic response delayed 50.50 20.16 14 10311 868 64487539
Graft versus host disease 50.48 20.16 30 10295 13783 64474624
Bone marrow transplant 49.53 20.16 15 10310 1272 64487135
Central nervous system leukaemia 46.10 20.16 11 10314 374 64488033
Viral haemorrhagic cystitis 46 20.16 15 10310 1620 64486787
Off label use 44.97 20.16 210 10115 632596 63855811
Product administered to patient of inappropriate age 43.51 20.16 19 10306 4582 64483825
Neutrophil count decreased 42.60 20.16 57 10268 77139 64411268
Peripheral artery stenosis 41.90 20.16 13 10312 1196 64487211
Adrenomegaly 41.11 20.16 10 10315 369 64488038
Haematopoietic stem cell mobilisation 41.09 20.16 9 10316 207 64488200
Clonal evolution 40.61 20.16 9 10316 219 64488188
Chronic myeloid leukaemia transformation 40.08 20.16 9 10316 233 64488174
Loss of CAR T-cell persistence 36.79 20.16 6 10319 24 64488383
Hepatic calcification 36.42 20.16 9 10316 355 64488052
Hepatotoxicity 36.15 20.16 38 10287 39924 64448483
Central nervous system neoplasm 35.58 20.16 7 10318 93 64488314
Catabolic state 35.58 20.16 7 10318 93 64488314
Costal cartilage fracture 34.27 20.16 8 10317 247 64488160
Renal artery angioplasty 33.21 20.16 5 10320 10 64488397
Ichthyosis acquired 33.21 20.16 5 10320 10 64488397
Blast cells present 33.16 20.16 10 10315 836 64487571
Amylase increased 32.71 20.16 20 10305 9665 64478742
Periarthritis calcarea 32.54 20.16 6 10319 55 64488352
Philadelphia positive acute lymphocytic leukaemia 32.16 20.16 6 10319 59 64488348
Metamyelocyte count increased 31.54 20.16 9 10316 620 64487787
Pancytopenia 31.14 20.16 70 10255 143239 64345168
Hepatic function abnormal 30.26 20.16 44 10281 64269 64424138
Adrenal cyst 30.01 20.16 6 10319 87 64488320
Articular calcification 29.58 20.16 6 10319 94 64488313
Renal artery stent placement 29.27 20.16 5 10320 28 64488379
Skin exfoliation 29.24 20.16 36 10289 44849 64443558
Pyrexia 28.95 20.16 170 10155 558474 63929933
Leukaemia recurrent 28.79 20.16 12 10313 2582 64485825
Acute lymphocytic leukaemia 28.65 20.16 14 10311 4357 64484050
Carotid artery stenosis 28.37 20.16 17 10308 7924 64480483
Pancreatitis 28.36 20.16 41 10284 59566 64428841
Chronic graft versus host disease 26.57 20.16 15 10310 6261 64482146
Neutropenia 26.11 20.16 91 10234 239533 64248874
Liver disorder 25.83 20.16 37 10288 53314 64435093
Epstein-Barr virus infection 25.80 20.16 19 10306 12469 64475938
Myelocyte count increased 25.70 20.16 8 10317 744 64487663
Post transplant lymphoproliferative disorder 25.50 20.16 17 10308 9527 64478880
Cerebral infarction 25.26 20.16 32 10293 41012 64447395
Abdominal pain 24.56 20.16 107 10218 312268 64176139
Malignant neoplasm progression 24.36 20.16 55 10270 112816 64375591
Diaphragmatic disorder 24.29 20.16 9 10316 1419 64486988
Red cell distribution width increased 23.80 20.16 18 10307 12291 64476116
Febrile neutropenia 23.76 20.16 75 10250 187582 64300825
Activated partial thromboplastin time prolonged 23.14 20.16 18 10307 12813 64475594
Bone pain 23.04 20.16 33 10292 47539 64440868
Fall 22.74 20.16 20 10305 416806 64071601
Chronic myeloid leukaemia 22.70 20.16 11 10314 3363 64485044
Ichthyosis 22.32 20.16 5 10320 128 64488279
Soft tissue necrosis 22.18 20.16 7 10318 681 64487726
Peripheral vascular disorder 22.01 20.16 14 10311 7247 64481160
Blast cell count increased 21.53 20.16 8 10317 1271 64487136
Activated partial thromboplastin time shortened 21.27 20.16 7 10318 778 64487629
Drug hypersensitivity 21.03 20.16 6 10319 237809 64250598
Carotid arteriosclerosis 21.01 20.16 9 10316 2070 64486337
Blood bilirubin increased 20.96 20.16 35 10290 57518 64430889
White blood cell count decreased 20.82 20.16 64 10261 157773 64330634
Coronary artery stenosis 20.76 20.16 16 10309 11232 64477175
Graft versus host disease in skin 20.55 20.16 12 10313 5335 64483072
Transplant 20.50 20.16 7 10318 871 64487536

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 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 agents
CHEBI has role CHEBI:38637 tyrosine kinase inhibitors

Drug Use (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 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 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 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 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 Dec. 18, 2023 CHRONIC PHASE (CP) CHRONIC MYELOID LEUKEMIA (CML) WITH RESISTANCE OR INTOLERANCE TO AT LEAST TWO PRIOR KINASE INHIBITORS
EQ 15MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL Dec. 18, 2023 CHRONIC PHASE (CP) CHRONIC MYELOID LEUKEMIA (CML) WITH RESISTANCE OR INTOLERANCE TO AT LEAST TWO PRIOR KINASE INHIBITORS
EQ 30MG BASE ICLUSIG TAKEDA PHARMS USA N203469 April 23, 2015 RX TABLET ORAL Dec. 18, 2023 CHRONIC PHASE (CP) CHRONIC MYELOID LEUKEMIA (CML) WITH RESISTANCE OR INTOLERANCE TO AT LEAST TWO PRIOR KINASE INHIBITORS
EQ 45MG BASE ICLUSIG TAKEDA PHARMS USA N203469 Dec. 14, 2012 RX TABLET ORAL Dec. 18, 2023 CHRONIC PHASE (CP) CHRONIC MYELOID LEUKEMIA (CML) WITH RESISTANCE OR INTOLERANCE TO AT LEAST TWO PRIOR KINASE INHIBITORS

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Breakpoint cluster region protein Kinase INHIBITOR Kd 7.30 CHEMBL CHEMBL
Tyrosine-protein kinase ABL1 Kinase INHIBITOR IC50 9.43 WOMBAT-PK CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret Kinase IC50 7.59 CHEMBL
Vascular endothelial growth factor receptor 1 Kinase IC50 8.43 CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 6.11 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
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
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 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
Cyclin-dependent kinase 8 Kinase INHIBITOR Kd 8.17 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
Bcr/Abl fusion protein Kinase IC50 9.30 CHEMBL
Receptor-interacting serine/threonine-protein kinase 3 Kinase INHIBITOR Ki 8.80 IUPHAR
Vascular endothelial growth factor receptor 2 Kinase INHIBITOR IC50 8.82 WOMBAT-PK
ATP-dependent RNA helicase DDX1 Enzyme Kd 7.07 CHEMBL
Platelet-derived growth factor receptor alpha Kinase INHIBITOR IC50 8.96 WOMBAT-PK
Proto-oncogene tyrosine-protein kinase Src Kinase IC50 9.05 CHEMBL

External reference:

IDSource
4340891KFS UNII
D09950 KEGG_DRUG
4032031 VUID
N0000186141 NUI
1114544-31-8 SECONDARY_CAS_RN
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
1364347 RXNORM
196462 MMSL
29016 MMSL
31534 MMSL
d07936 MMSL
014797 NDDF
014798 NDDF
703796003 SNOMEDCT_US
703797007 SNOMEDCT_US
703798002 SNOMEDCT_US

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