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

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 1932 641571-10-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • nilotinib hydrochloride hydrate
  • nilotinib
  • tasigna
  • nilotinib hydrochloride monohydrate
Nilotinib is an inhibitor of the BCR-ABL kinase. Nilotinib binds to and stabilizes the inactive conformation of the kinase domain of ABL protein. In vitro, nilotinib inhibited BCR-ABL mediated proliferation of murine leukemic cell lines and human cell lines derived from patients with Ph+ CML. Under the conditions of the assays, nilotinib was able to overcome imatinib resistance resulting from BCR-ABL kinase mutations, in 32 out of 33 mutations tested. In vivo, nilotinib reduced the tumor size in a murine BCR-ABL xenograft model.
  • Molecular weight: 529.53
  • Formula: C28H22F3N7O
  • CLOGP: 5.69
  • LIPINSKI: 2
  • HAC: 8
  • HDO: 2
  • TPSA: 97.62
  • ALOGS: -5.42
  • ROTB: 7
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.60 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 4 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 21.58 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 30 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 4.722 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 3.873 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 8.110 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 14.256 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 0.660 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 1.420 % High 1
herg hERG pIC50 5.637 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 12.331 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 84.528 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 0.380 % High 1
kinase-safety-class ACVR2B,ALK,AURKA,AXL,BLK,BRAF,CAMK2B,CAMK2D,CDK5,CDK9,CSF1R,DDR1,DYRK1B,EGFR,EIF2AK3,EPHA2,EPHB4,ERBB2,FLT3,FYN,GRK2,ITK,JAK1,KIT,LCK,LYN,MAP3K21,MAP4K1,MAPK10,MAPK11,MAPK7,MAPKAPK2,MET,NTRK2,NTRK3,PDK2,PDK4,PIK3CG,PRKCD,PRKDC,SIK2,SIK3,STK33,TTK,YES1 45
kinase-selectivity-class ABL2,ACVR2A,ALK,AURKA,AXL,BLK,BRAF,CAMK2B,CAMK2D,CDK9,CSF1R,DDR1,DYRK1B,EPHA2,EPHB4,FLT3,FYN,GRK2,JAK1,KIT,LYN,MAP3K21,MAP4K1,MAP4K3,MAPK7,MTOR,PDK4,PIK3CD,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK 34
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 11.194 High 1
mh-clint Mouse hepatocyte intrinsic clearance 34.754 High 1
mppb Mouse plasma protein binding (% unbound) 0.300 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 8.630 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 1
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 1 High 1
pppb Pig plasma protein binding (% unbound) 1.110 % High 1
rh-clint Rat hepatocyte intrinsic clearance 17.338 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 3.980 % High 1
rppb Rat plasma protein binding (% unbound) 0.350 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 0.608 uM High 1

Approvals:

DateAgencyCompanyOrphan
Oct. 29, 2007 FDA NOVARTIS

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
Cytogenetic analysis abnormal 709.17 16.76 135 23289 875 90604148
Peripheral arterial occlusive disease 402.59 16.76 113 23311 4508 90600515
Electrocardiogram QT prolonged 386.82 16.76 238 23186 72218 90532805
Blast crisis in myelogenous leukaemia 327.40 16.76 66 23358 595 90604428
Drug resistance 300.44 16.76 150 23274 30299 90574724
Pleural effusion 247.83 16.76 216 23208 111775 90493248
Lipase increased 236.96 16.76 94 23330 11017 90594006
Second primary malignancy 236.08 16.76 92 23332 10286 90594737
Chronic myeloid leukaemia transformation 226.15 16.76 38 23386 103 90604920
Philadelphia chromosome positive 225.34 16.76 46 23378 444 90604579
Myocardial infarction 164.53 16.76 168 23256 105804 90499219
Bone pain 156.38 16.76 129 23295 61854 90543169
Intermittent claudication 156.13 16.76 44 23380 1779 90603244
Blood bilirubin increased 152.40 16.76 110 23314 43360 90561663
Malignant neoplasm progression 140.32 16.76 155 23269 106715 90498308
Death 138.87 16.76 340 23084 456211 90148812
Peripheral artery stenosis 137.68 16.76 32 23392 588 90604435
Rash 136.57 16.76 483 22941 795617 89809406
Off label use 124.88 16.76 65 23359 1102187 89502836
Myalgia 121.14 16.76 185 23239 174940 90430083
Acute myocardial infarction 119.35 16.76 87 23337 34803 90570220
Chronic myeloid leukaemia recurrent 119.32 16.76 25 23399 277 90604746
Thrombocytopenia 117.79 16.76 201 23223 208524 90396499
Platelet count decreased 106.64 16.76 153 23271 136816 90468207
Pancreatitis 105.24 16.76 109 23315 69717 90535306
Haematotoxicity 104.05 16.76 55 23369 12480 90592543
Carotid artery stenosis 96.12 16.76 40 23384 5294 90599729
Arteriosclerosis 94.01 16.76 49 23375 10804 90594219
Cytopenia 87.12 16.76 55 23369 17394 90587629
Cerebrovascular accident 86.07 16.76 131 23293 123402 90481621
Pancytopenia 84.45 16.76 128 23296 120135 90484888
White blood cell count increased 82.18 16.76 94 23330 67147 90537876
Peripheral vascular disorder 79.49 16.76 37 23387 6394 90598629
Joint swelling 78.76 16.76 17 23407 503283 90101740
Systemic lupus erythematosus 77.10 16.76 4 23420 361892 90243131
Platelet count increased 75.87 16.76 54 23370 20805 90584218
Pericardial effusion 75.29 16.76 68 23356 36765 90568258
Acute lymphocytic leukaemia recurrent 72.21 16.76 27 23397 2694 90602329
Splenomegaly 70.24 16.76 43 23381 12881 90592142
Myocardial ischaemia 70.11 16.76 44 23380 13770 90591253
Blast cell crisis 69.85 16.76 13 23411 73 90604950
Arthropathy 69.59 16.76 7 23417 366235 90238788
Anaemia 68.88 16.76 224 23200 352578 90252445
Glossodynia 67.16 16.76 4 23420 321775 90283248
Angina pectoris 66.07 16.76 65 23359 39095 90565928
Hyperbilirubinaemia 62.35 16.76 41 23383 13895 90591128
Condition aggravated 58.96 16.76 41 23383 595504 90009519
Coronary artery disease 58.95 16.76 57 23367 33566 90571457
Thrombocytosis 58.90 16.76 31 23393 6970 90598053
Chronic myeloid leukaemia 58.40 16.76 23 23401 2641 90602382
Rheumatoid arthritis 57.20 16.76 12 23412 362602 90242421
Gene mutation identification test positive 56.70 16.76 12 23412 140 90604883
Blood glucose increased 55.33 16.76 93 23331 95153 90509870
Palpitations 53.82 16.76 113 23311 136615 90468408
Bone marrow failure 53.46 16.76 53 23371 32168 90572855
Amylase increased 53.00 16.76 29 23395 7043 90597980
Therapeutic response delayed 52.84 16.76 16 23408 834 90604189
Diabetes mellitus 51.22 16.76 73 23351 64802 90540221
Polymerase chain reaction positive 49.73 16.76 11 23413 160 90604863
Pruritus 49.06 16.76 272 23152 541253 90063770
Exposure via father 48.66 16.76 12 23412 286 90604737
Drug hypersensitivity 47.08 16.76 31 23393 463578 90141445
Exposure via partner 47.07 16.76 10 23414 119 90604904
Wound 45.82 16.76 11 23413 302969 90302054
Lower respiratory tract infection 44.58 16.76 6 23418 250653 90354370
Musculoskeletal stiffness 44.38 16.76 11 23413 296521 90308502
Labelled drug-food interaction medication error 44.34 16.76 11 23413 269 90604754
Peripheral artery occlusion 43.65 16.76 16 23408 1510 90603513
Impaired healing 43.13 16.76 5 23419 234194 90370829
Mobility decreased 42.30 16.76 7 23417 250727 90354296
Fibromyalgia 41.73 16.76 3 23421 206266 90398757
Discomfort 41.40 16.76 10 23414 274325 90330698
Arterial disorder 41.17 16.76 15 23409 1391 90603632
Concomitant disease aggravated 40.01 16.76 29 23395 11489 90593534
Xanthelasma 39.49 16.76 8 23416 74 90604949
Drug intolerance 39.29 16.76 223 23201 447368 90157655
Intentional product use issue 39.03 16.76 5 23419 216887 90388136
Atrial fibrillation 37.80 16.76 97 23327 133514 90471509
Concomitant disease progression 37.75 16.76 16 23408 2216 90602807
Acute coronary syndrome 37.05 16.76 27 23397 10786 90594237
Leukaemia recurrent 36.91 16.76 14 23410 1453 90603570
Irritable bowel syndrome 36.81 16.76 5 23419 207443 90397580
Ill-defined disorder 36.53 16.76 3 23421 184888 90420135
Basophil count increased 36.41 16.76 13 23411 1138 90603885
Product use issue 36.36 16.76 20 23404 329899 90275124
Sinusitis 36.10 16.76 22 23402 343066 90261957
Stomatitis 36.00 16.76 13 23411 274685 90330338
Transaminases increased 35.66 16.76 46 23378 37146 90567877
Hypersensitivity 35.63 16.76 39 23385 454638 90150385
Leukocytosis 35.63 16.76 42 23382 30948 90574075
Wheezing 35.29 16.76 9 23415 238071 90366952
Pericarditis 35.04 16.76 13 23411 270138 90334885
Gamma-glutamyltransferase increased 34.92 16.76 46 23378 37906 90567117
Dry skin 34.88 16.76 73 23351 88000 90517023
Skin disorder 34.57 16.76 45 23379 36661 90568362
Peripheral ischaemia 33.75 16.76 20 23404 5647 90599376
Cardiac failure 33.60 16.76 82 23342 109414 90495609
Abdominal pain 33.30 16.76 195 23229 395526 90209497
Confusional state 32.67 16.76 31 23393 386174 90218849
Normal newborn 32.56 16.76 35 23389 23327 90581696
Alanine aminotransferase increased 32.53 16.76 85 23339 118253 90486770
Therapeutic response decreased 31.68 16.76 71 23353 89658 90515365
Haemoglobin decreased 30.78 16.76 102 23322 161854 90443169
Osteoarthritis 29.79 16.76 7 23417 195723 90409300
Folliculitis 29.76 16.76 8 23416 204345 90400678
Dyslipidaemia 29.65 16.76 23 23401 10084 90594939
Swelling 29.58 16.76 39 23385 419019 90186004
Myelofibrosis 29.07 16.76 12 23412 1555 90603468
Gene mutation 28.66 16.76 13 23411 2117 90602906
Hyperglycaemia 28.57 16.76 49 23375 50921 90554102
Nausea 28.49 16.76 423 23001 1109893 89495130
Food interaction 28.01 16.76 11 23413 1253 90603770
Psoriasis 27.58 16.76 3 23421 147751 90457272
Arterial occlusive disease 27.46 16.76 24 23400 12422 90592601
Cerebral infarction 27.24 16.76 34 23390 26562 90578461
Exposure during pregnancy 26.92 16.76 14 23410 238396 90366627
Vertebral artery hypoplasia 26.81 16.76 4 23420 3 90605020
Neoplasm malignant 26.55 16.76 38 23386 33842 90571181
Blood lactate dehydrogenase increased 26.32 16.76 33 23391 25899 90579124
Vertebral artery stenosis 26.31 16.76 6 23418 101 90604922
Skin toxicity 25.69 16.76 18 23406 6761 90598262
Pregnancy of partner 25.56 16.76 5 23419 38 90604985
Hepatic function abnormal 25.29 16.76 44 23380 46244 90558779
Haemolytic transfusion reaction 25 16.76 4 23420 7 90605016
Coronary artery stenosis 24.80 16.76 16 23408 5250 90599773
Injury 24.75 16.76 10 23414 197339 90407684
Blast cell count increased 24.69 16.76 8 23416 521 90604502
Liver injury 24.23 16.76 7 23417 170560 90434463
Cerebral artery stenosis 23.82 16.76 8 23416 583 90604440
Pain in extremity 23.70 16.76 198 23226 450331 90154692
Jaundice 23.35 16.76 35 23389 32482 90572541
Collateral circulation 22.82 16.76 4 23420 15 90605008
Ischaemic stroke 22.17 16.76 28 23396 22138 90582885
Blister 22.10 16.76 20 23404 254978 90350045
Angiopathy 21.82 16.76 15 23409 5465 90599558
Chylothorax 21.82 16.76 7 23417 442 90604581
Oncologic complication 21.67 16.76 6 23418 227 90604796
Infarction 21.60 16.76 12 23412 3001 90602022
Gangrene 21.02 16.76 21 23403 12855 90592168
Abdominal discomfort 20.94 16.76 59 23365 477269 90127754
Pancreatic enzymes increased 20.80 16.76 8 23416 862 90604161
Keratosis pilaris 20.09 16.76 5 23419 124 90604899
Fluid retention 19.98 16.76 59 23365 88032 90516991
Overdose 19.76 16.76 8 23416 157701 90447322
Cerebrovascular stenosis 19.75 16.76 4 23420 37 90604986
Aspartate aminotransferase increased 19.70 16.76 65 23359 102872 90502151
Skin sensitisation 19.60 16.76 8 23416 1007 90604016
Gastrointestinal tract irritation 19.53 16.76 7 23417 619 90604404
Hypotension 19.36 16.76 34 23390 325363 90279660
Peripheral artery thrombosis 19.20 16.76 10 23414 2200 90602823
Calculus bladder 19.16 16.76 7 23417 654 90604369
Neutropenia 18.99 16.76 111 23313 224793 90380230
Myelodysplastic syndrome 18.71 16.76 25 23399 20878 90584145
Asthma 18.69 16.76 21 23403 242139 90362884
Headache 18.41 16.76 319 23105 862427 89742596
Chest pain 18.15 16.76 143 23281 319502 90285521
Hepatotoxicity 18.15 16.76 38 23386 45804 90559219
Incorrect dose administered 18.02 16.76 53 23371 78877 90526146
Infection 17.99 16.76 42 23382 362052 90242971
Muscle spasms 17.94 16.76 119 23305 251764 90353259
Neoplasm progression 17.76 16.76 37 23387 44449 90560574
Product use in unapproved indication 17.52 16.76 38 23386 336198 90268825
Acute myeloid leukaemia 17.43 16.76 24 23400 20616 90584407
Extremity necrosis 17.42 16.76 9 23415 1948 90603075
Delirium 17.40 16.76 3 23421 104356 90500667
Capillary leak syndrome 17.10 16.76 10 23414 2757 90602266
Therapeutic product effect incomplete 17.05 16.76 15 23409 193881 90411142

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
Cytogenetic analysis abnormal 476.24 15.01 107 25315 668 42595245
Blast crisis in myelogenous leukaemia 464.52 15.01 102 25320 564 42595349
Electrocardiogram QT prolonged 395.55 15.01 283 25139 47662 42548251
Second primary malignancy 392.83 15.01 164 25258 9411 42586502
Peripheral arterial occlusive disease 388.02 15.01 148 25274 6690 42589223
Drug resistance 295.82 15.01 208 25214 34040 42561873
Pleural effusion 270.74 15.01 311 25111 96855 42499058
Angina pectoris 250.25 15.01 185 25237 32711 42563202
Myocardial infarction 232.77 15.01 326 25096 123683 42472230
Intermittent claudication 220.00 15.01 75 25347 2440 42593473
Off label use 217.58 15.01 57 25365 638278 41957635
Drug intolerance 216.49 15.01 253 25169 80171 42515742
Philadelphia chromosome positive 203.90 15.01 52 25370 589 42595324
Death 174.52 15.01 645 24777 470540 42125373
Rash 162.73 15.01 445 24977 276509 42319404
Lipase increased 161.09 15.01 92 25330 10474 42585439
Chronic myeloid leukaemia transformation 140.14 15.01 31 25391 178 42595735
Coronary artery stenosis 136.17 15.01 82 25340 10297 42585616
Chronic myeloid leukaemia recurrent 117.66 15.01 28 25394 232 42595681
Blood bilirubin increased 113.67 15.01 133 25289 42119 42553794
Acute myocardial infarction 113.50 15.01 156 25266 58009 42537904
Pancreatitis 107.84 15.01 131 25291 43137 42552776
Myocardial ischaemia 106.90 15.01 87 25335 17675 42578238
Malignant neoplasm progression 106.03 15.01 213 25209 108187 42487726
Peripheral artery stenosis 103.22 15.01 33 25389 874 42595039
White blood cell count increased 98.80 15.01 128 25294 44959 42550954
Coronary artery disease 98.72 15.01 140 25282 53580 42542333
Carotid artery stenosis 95.59 15.01 52 25370 5384 42590529
Arterial disorder 95.55 15.01 34 25388 1258 42594655
Peripheral vascular disorder 93.88 15.01 51 25371 5266 42590647
Acute kidney injury 87.24 15.01 56 25366 367281 42228632
Gene mutation identification test positive 84.98 15.01 21 25401 207 42595706
Platelet count decreased 81.37 15.01 223 25199 138358 42457555
Acute coronary syndrome 75.42 15.01 66 25356 14799 42581114
Hypotension 70.19 15.01 33 25389 257598 42338315
Abdominal pain upper 69.84 15.01 153 25269 82456 42513457
Chest pain 67.91 15.01 210 25212 139320 42456593
Blast cell crisis 65.01 15.01 15 25407 107 42595806
Concomitant disease progression 64.54 15.01 31 25391 2472 42593441
Thrombocytopenia 63.69 15.01 253 25169 190026 42405887
Splenomegaly 62.13 15.01 63 25359 16984 42578929
Concomitant disease aggravated 61.47 15.01 42 25380 6544 42589369
Toxicity to various agents 61.40 15.01 30 25392 229106 42366807
Peripheral artery occlusion 60.78 15.01 27 25395 1799 42594114
Loss of therapeutic response 59.33 15.01 24 25398 1267 42594646
Arterial stenosis 57.74 15.01 23 25399 1166 42594747
Polymerase chain reaction positive 56.93 15.01 14 25408 135 42595778
Arteriosclerosis 55.79 15.01 61 25361 17928 42577985
Bone pain 52.80 15.01 68 25354 23724 42572189
Cerebral artery stenosis 52.26 15.01 16 25406 366 42595547
Angina unstable 50.53 15.01 47 25375 11401 42584512
Cerebral infarction 49.67 15.01 76 25346 31093 42564820
Condition aggravated 49.01 15.01 50 25372 260704 42335209
Exposure via father 47.12 15.01 12 25410 135 42595778
Myalgia 46.13 15.01 144 25278 95936 42499977
Chronic myeloid leukaemia 44.26 15.01 24 25398 2468 42593445
Labelled drug-food interaction medication error 42.97 15.01 9 25413 38 42595875
Cerebrovascular accident 40.69 15.01 139 25283 97021 42498892
Peripheral ischaemia 39.50 15.01 32 25390 6453 42589460
Confusional state 39.06 15.01 26 25396 167571 42428342
Overdose 38.36 15.01 8 25414 105256 42490657
Pericardial effusion 37.94 15.01 65 25357 29210 42566703
Infarction 37.29 15.01 23 25399 3012 42592901
Hypercholesterolaemia 37.14 15.01 42 25380 12807 42583106
Acoustic neuroma 37.13 15.01 10 25412 142 42595771
Gene mutation 36.87 15.01 19 25403 1762 42594151
Therapeutic response decreased 35.24 15.01 72 25350 36940 42558973
Leukocytosis 34.67 15.01 63 25359 29645 42566268
Amylase increased 34.37 15.01 30 25392 6699 42589214
Hyperglycaemia 34.35 15.01 81 25341 45778 42550135
Blood glucose increased 32.22 15.01 107 25315 73592 42522321
Carotid arteriosclerosis 32.07 15.01 19 25403 2313 42593600
Coronary artery occlusion 30.18 15.01 35 25387 10962 42584951
Fall 30.08 15.01 59 25363 234461 42361452
Drug hypersensitivity 29.80 15.01 11 25411 99378 42496535
Drug interaction 29.46 15.01 73 25349 266926 42328987
Treatment failure 29.25 15.01 93 25329 62531 42533382
Pruritus 28.82 15.01 202 25220 188569 42407344
Tremor 28.61 15.01 11 25411 96918 42498995
Arterial thrombosis 28.50 15.01 16 25406 1760 42594153
Muscle spasms 27.58 15.01 113 25309 85931 42509982
Hyponatraemia 27.57 15.01 13 25409 101449 42494464
Pulmonary hypertension 27.53 15.01 50 25372 23519 42572394
Cytopenia 26.94 15.01 42 25380 17455 42578458
Ischaemia 26.79 15.01 23 25399 5024 42590889
Fatigue 26.52 15.01 385 25037 435256 42160657
Gangrene 26.48 15.01 23 25399 5103 42590810
Haematotoxicity 25.32 15.01 32 25390 10953 42584960
Paternal exposure during pregnancy 25.21 15.01 7 25415 112 42595801
Myopathy toxic 24.80 15.01 11 25411 730 42595183
Oedematous pancreatitis 24.52 15.01 11 25411 750 42595163
Product blister packaging issue 24.39 15.01 7 25415 127 42595786
Clonal evolution 24.34 15.01 7 25415 128 42595785
Intentional product misuse 24.05 15.01 4 25418 61896 42534017
Hallucination 24.01 15.01 3 25419 57504 42538409
Dehydration 23.53 15.01 30 25392 141737 42454176
Cardiovascular disorder 23.30 15.01 34 25388 13331 42582582
Arterial occlusive disease 23.04 15.01 20 25402 4433 42591480
Gamma-glutamyltransferase increased 22.82 15.01 56 25366 32441 42563472
Karyotype analysis abnormal 22.76 15.01 6 25416 78 42595835
Febrile neutropenia 22.71 15.01 48 25374 185655 42410258
Asthma 22.16 15.01 5 25417 62309 42533604
Acquired gene mutation 22.06 15.01 13 25409 1567 42594346
Diabetes mellitus 21.75 15.01 82 25340 60005 42535908
Blast cells present 21.74 15.01 9 25413 504 42595409
Pain in extremity 21.71 15.01 159 25263 150445 42445468
Arteritis 21.69 15.01 9 25413 507 42595406
Atrial fibrillation 21.65 15.01 150 25272 139443 42456470
Headache 21.64 15.01 228 25194 239141 42356772
Agitation 21.25 15.01 6 25416 64308 42531605
Bone marrow failure 21.13 15.01 55 25367 33038 42562875
Haemoglobin decreased 20.93 15.01 143 25279 132328 42463585
Intentional overdose 20.73 15.01 3 25419 51453 42544460
Chloroma 20.72 15.01 9 25413 568 42595345
Central nervous system leukaemia 20.48 15.01 8 25414 385 42595528
Pulmonary embolism 20.17 15.01 25 25397 119587 42476326
Leukaemia recurrent 20.01 15.01 13 25409 1863 42594050
Loss of personal independence in daily activities 19.85 15.01 3 25419 49813 42546100
Angiopathy 19.82 15.01 20 25402 5357 42590556
Necrosis 19.66 15.01 22 25400 6629 42589284
Gelatinous transformation of the bone marrow 19.48 15.01 4 25418 15 42595898
Hepatotoxicity 19.43 15.01 45 25377 25122 42570791
Somnolence 19.40 15.01 34 25388 141071 42454842
Pancreatic fibrosis 19.28 15.01 3 25419 0 42595913
Oncologic complication 19.21 15.01 8 25414 455 42595458
Delirium 19.11 15.01 4 25418 52515 42543398
Abdominal pain 18.43 15.01 184 25238 190287 42405626
Basophil count increased 18.28 15.01 9 25413 757 42595156
Alopecia 18.02 15.01 48 25374 29228 42566685
Oxygen saturation decreased 18.02 15.01 8 25414 64679 42531234
Myeloproliferative neoplasm 17.95 15.01 9 25413 788 42595125
Vascular stenosis 17.90 15.01 6 25416 185 42595728
Rectosigmoid cancer 17.87 15.01 6 25416 186 42595727
B-cell small lymphocytic lymphoma 17.78 15.01 6 25416 189 42595724
Chest discomfort 17.65 15.01 80 25342 63536 42532377
Pancreatic enzymes increased 17.05 15.01 9 25413 876 42595037
Intentional product use issue 16.91 15.01 11 25411 71822 42524091
Platelet count increased 16.90 15.01 26 25396 10677 42585236
Cytogenetic response 16.74 15.01 3 25419 4 42595909
Wheezing 16.52 15.01 6 25416 54775 42541138
Blood bilirubin unconjugated increased 16.10 15.01 8 25414 687 42595226
Vertebral artery occlusion 16.04 15.01 6 25416 256 42595657
Rheumatoid arthritis 15.93 15.01 3 25419 42437 42553476
Blood creatine phosphokinase increased 15.89 15.01 64 25358 48274 42547639
Neoplasm malignant 15.76 15.01 39 25383 22704 42573209
Gait apraxia 15.67 15.01 3 25419 7 42595906
Arrhythmia 15.41 15.01 56 25366 40261 42555652
Renal artery stenosis 15.32 15.01 12 25410 2305 42593608
Transformation to acute myeloid leukaemia 15.19 15.01 9 25413 1096 42594817
Pancreatic toxicity 15.18 15.01 4 25418 52 42595861
Metabolic acidosis 15.10 15.01 6 25416 51852 42544061

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
Cytogenetic analysis abnormal 907.81 15.38 177 33596 1092 110554434
Blast crisis in myelogenous leukaemia 543.03 15.38 111 33662 897 110554629
Peripheral arterial occlusive disease 500.70 15.38 163 33610 9117 110546409
Electrocardiogram QT prolonged 484.88 15.38 340 33433 108620 110446906
Drug resistance 458.51 15.38 258 33515 56116 110499410
Second primary malignancy 446.30 15.38 178 33595 17890 110537636
Pleural effusion 417.36 15.38 381 33392 177328 110378198
Philadelphia chromosome positive 334.84 15.38 73 33700 827 110554699
Lipase increased 301.32 15.38 136 33637 18536 110536990
Chronic myeloid leukaemia transformation 286.63 15.38 54 33719 269 110555257
Myocardial infarction 280.87 15.38 319 33454 191764 110363762
Blood bilirubin increased 220.60 15.38 184 33589 75788 110479738
Intermittent claudication 220.02 15.38 70 33703 3631 110551895
Death 205.26 15.38 570 33203 698299 109857227
Angina pectoris 204.31 15.38 162 33611 62133 110493393
Off label use 194.46 15.38 109 33664 1500076 109055450
Platelet count decreased 191.74 15.38 290 33483 230153 110325373
Rash 187.73 15.38 613 33160 820351 109735175
Acute myocardial infarction 187.40 15.38 175 33598 83602 110471924
Malignant neoplasm progression 162.96 15.38 232 33541 174335 110381191
Peripheral artery stenosis 152.51 15.38 42 33731 1312 110554214
Carotid artery stenosis 147.93 15.38 67 33706 9196 110546330
Chronic myeloid leukaemia recurrent 135.47 15.38 30 33743 367 110555159
Myocardial ischaemia 132.02 15.38 89 33684 26595 110528931
Thrombocytopenia 129.32 15.38 311 33462 348574 110206952
Pancreatitis 127.56 15.38 150 33623 93383 110462143
White blood cell count increased 126.62 15.38 152 33621 96690 110458836
Bone pain 124.81 15.38 125 33648 65008 110490518
Myalgia 117.65 15.38 229 33544 222152 110333374
Acute coronary syndrome 111.75 15.38 76 33697 23036 110532490
Coronary artery stenosis 106.45 15.38 61 33712 13697 110541829
Arterial disorder 103.75 15.38 35 33738 2184 110553342
Gene mutation identification test positive 103.44 15.38 23 33750 287 110555239
Coronary artery disease 101.12 15.38 117 33656 71573 110483953
Arteriosclerosis 91.16 15.38 69 33704 24698 110530828
Cerebral infarction 89.37 15.38 94 33679 51744 110503782
Splenomegaly 87.42 15.38 67 33706 24431 110531095
Pericardial effusion 86.83 15.38 97 33676 57120 110498406
Peripheral vascular disorder 85.62 15.38 45 33728 8531 110546995
Condition aggravated 79.25 15.38 65 33708 734771 109820755
Polymerase chain reaction positive 79.11 15.38 19 33754 339 110555187
Blood glucose increased 76.89 15.38 142 33631 132354 110423172
Joint swelling 75.32 15.38 21 33752 442824 110112702
Rheumatoid arthritis 72.08 15.38 5 33768 299608 110255918
Drug intolerance 71.43 15.38 279 33494 406233 110149293
Acute lymphocytic leukaemia recurrent 71.29 15.38 35 33738 5752 110549774
Amylase increased 69.80 15.38 45 33728 12474 110543052
Chronic myeloid leukaemia 68.52 15.38 31 33742 4242 110551284
Pancytopenia 67.22 15.38 177 33596 209436 110346090
Hyperbilirubinaemia 66.49 15.38 63 33710 30608 110524918
Bone marrow failure 66.27 15.38 85 33688 57763 110497763
Hypotension 66.15 15.38 39 33734 523810 110031716
Haemoglobin decreased 65.97 15.38 196 33577 248531 110306995
Cerebral artery stenosis 65.87 15.38 20 33753 887 110554639
Hyperglycaemia 64.92 15.38 103 33670 84987 110470539
Cerebrovascular accident 63.21 15.38 158 33615 181126 110374400
Peripheral artery occlusion 62.72 15.38 26 33747 2879 110552647
Drug hypersensitivity 61.41 15.38 31 33742 454059 110101467
Haematotoxicity 61.02 15.38 51 33722 21031 110534495
Concomitant disease progression 60.47 15.38 27 33746 3583 110551943
Confusional state 59.01 15.38 35 33738 468645 110086881
Concomitant disease aggravated 58.92 15.38 45 33728 16319 110539207
Blast cell crisis 58.63 15.38 13 33760 160 110555366
Arterial stenosis 58.23 15.38 21 33752 1598 110553928
Gamma-glutamyltransferase increased 56.42 15.38 81 33692 61228 110494298
Cytopenia 56.21 15.38 57 33716 30059 110525467
Arthropathy 56.17 15.38 10 33763 287512 110268014
Acute kidney injury 56.04 15.38 67 33706 635363 109920163
Amaurosis fugax 53.67 15.38 22 33751 2368 110553158
Pruritus 52.40 15.38 330 33443 581230 109974296
Platelet count increased 51.27 15.38 51 33722 26283 110529243
Peripheral ischaemia 50.23 15.38 35 33738 11023 110544503
Glossodynia 49.82 15.38 5 33768 221999 110333527
Wheezing 49.59 15.38 9 33764 255221 110300305
Therapeutic response decreased 49.30 15.38 98 33675 96401 110459125
Gene mutation 49.11 15.38 23 33750 3406 110552120
Atrial fibrillation 49.04 15.38 168 33605 229474 110326052
Psoriatic arthropathy 48.15 15.38 3 33770 196758 110358768
Anaemia 47.15 15.38 307 33466 546779 110008747
Chest pain 46.08 15.38 232 33541 376143 110179383
Leukocytosis 45.03 15.38 68 33705 53760 110501766
Acquired gene mutation 44.22 15.38 20 33753 2734 110552792
Toxicity to various agents 43.06 15.38 50 33723 480505 110075021
Mobility decreased 42.75 15.38 10 33763 237412 110318114
Therapeutic response delayed 42.50 15.38 16 33757 1374 110554152
Cardiac failure 42.47 15.38 140 33633 187486 110368040
Overdose 41.80 15.38 10 33763 233784 110321742
Hypersensitivity 40.73 15.38 38 33735 403960 110151566
Sinusitis 40.46 15.38 20 33753 296668 110258858
Thrombocytosis 40.44 15.38 30 33743 10414 110545112
Lower respiratory tract infection 40.43 15.38 12 33761 243094 110312432
Angina unstable 39.97 15.38 36 33737 16396 110539130
Loss of therapeutic response 39.58 15.38 18 33755 2492 110553034
Abdominal pain 39.48 15.38 280 33493 512709 110042817
Leukaemia recurrent 38.76 15.38 19 33754 3112 110552414
Musculoskeletal stiffness 37.95 15.38 19 33754 279803 110275723
Diabetes mellitus 37.15 15.38 89 33684 99292 110456234
Exposure during pregnancy 36.97 15.38 4 33769 167420 110388106
Hepatic function abnormal 36.70 15.38 83 33690 89212 110466314
Ill-defined disorder 36.62 15.38 3 33770 156850 110398676
Intentional product use issue 36.48 15.38 15 33758 247891 110307635
Angiopathy 35.89 15.38 26 33747 8704 110546822
Stomatitis 35.68 15.38 19 33754 270223 110285303
Asthma 35.47 15.38 16 33757 250275 110305251
Abdominal pain upper 35.13 15.38 204 33569 348907 110206619
Keratosis pilaris 34.93 15.38 8 33765 115 110555411
Alanine aminotransferase increased 34.57 15.38 129 33644 183644 110371882
Infarction 34.56 15.38 21 33752 5248 110550278
Hepatotoxicity 33.11 15.38 65 33708 63335 110492191
Arterial occlusive disease 32.33 15.38 31 33742 15277 110540249
Acne 31.89 15.38 45 33728 33475 110522051
Palpitations 31.83 15.38 114 33659 159098 110396428
Discomfort 31.57 15.38 13 33760 214694 110340832
Blood lactate dehydrogenase increased 31.54 15.38 52 33721 44282 110511244
White blood cell count decreased 31.35 15.38 146 33627 229244 110326282
Gangrene 30.62 15.38 31 33742 16310 110539216
Wound 30.20 15.38 17 33756 234420 110321106
Clonal evolution 29.23 15.38 8 33765 244 110555282
Karyotype analysis abnormal 28.97 15.38 6 33767 52 110555474
Helicobacter infection 28.43 15.38 10 33763 181867 110373659
Product use issue 28.36 15.38 32 33741 311663 110243863
Coronary artery occlusion 27.89 15.38 29 33744 15743 110539783
Myelofibrosis 27.62 15.38 15 33758 3036 110552490
Ischaemic stroke 27.49 15.38 47 33726 41216 110514310
Transformation to acute myeloid leukaemia 27.47 15.38 12 33761 1511 110554015
Xanthelasma 27.42 15.38 7 33766 162 110555364
Generalised oedema 27.42 15.38 40 33733 30664 110524862
Intentional product misuse 27.34 15.38 4 33769 132900 110422626
Chylothorax 27.19 15.38 11 33762 1145 110554381
Blood creatine phosphokinase increased 26.83 15.38 65 33708 73012 110482514
Central nervous system leukaemia 26.37 15.38 9 33764 582 110554944
Labelled drug-food interaction medication error 25.91 15.38 7 33766 203 110555323
Dyslipidaemia 25.83 15.38 28 33745 15937 110539589
Delirium 25.71 15.38 5 33768 135020 110420506
Cytogenetic response 25.61 15.38 4 33769 4 110555522
Ocular discomfort 25.43 15.38 21 33752 8512 110547014
Pancreatic toxicity 25.31 15.38 6 33767 101 110555425
Hyponatraemia 24.99 15.38 18 33755 217635 110337891
Vertebral artery stenosis 24.87 15.38 7 33766 237 110555289
Arterial thrombosis 24.58 15.38 14 33759 3105 110552421
Swelling 24.08 15.38 44 33729 350997 110204529
Oxygen saturation decreased 23.91 15.38 9 33764 156973 110398553
Osteoarthritis 23.87 15.38 13 33760 182610 110372916
Basophilia 23.78 15.38 5 33768 47 110555479
Urticaria 23.67 15.38 38 33735 318819 110236707
Transient ischaemic attack 23.59 15.38 57 33716 63925 110491601
Blast cell count increased 23.51 15.38 11 33762 1626 110553900
Pulmonary hypertension 23.44 15.38 52 33721 55168 110500358
Acoustic neuroma 23.04 15.38 7 33766 311 110555215
Impaired healing 22.94 15.38 16 33757 196701 110358825
Pancreatic enzymes increased 22.93 15.38 11 33762 1718 110553808
Chronic myeloid leukaemia (in remission) 22.84 15.38 4 33769 12 110555514
Injury 22.62 15.38 13 33760 177252 110378274
Irritable bowel syndrome 22.48 15.38 11 33762 164204 110391322
Basophil count increased 22.45 15.38 11 33762 1799 110553727
Pain in extremity 21.79 15.38 236 33537 486882 110068644
Haemolytic transfusion reaction 21.75 15.38 4 33769 17 110555509
Skin toxicity 21.44 15.38 22 33751 11761 110543765
Peripheral artery thrombosis 21.29 15.38 14 33759 4010 110551516
Dry mouth 21.10 15.38 18 33755 199930 110355596
Exposure via father 20.83 15.38 5 33768 89 110555437
Cardiovascular disorder 20.83 15.38 30 33743 22730 110532796
Product use in unapproved indication 20.56 15.38 69 33704 447308 110108218
Aspartate aminotransferase increased 20.54 15.38 100 33673 159836 110395690
Vascular stenosis 20.37 15.38 8 33765 770 110554756
Oedematous pancreatitis 20.36 15.38 10 33763 1644 110553882
Blood bilirubin unconjugated increased 20.32 15.38 9 33764 1172 110554354
Necrosis 20.22 15.38 21 33752 11385 110544141
Vertebral artery occlusion 19.90 15.38 7 33766 495 110555031
Chloroma 19.70 15.38 8 33765 840 110554686
Remission not achieved 19.57 15.38 7 33766 520 110555006
Chromosome analysis abnormal 19.49 15.38 6 33767 279 110555247
Myopathy toxic 19.32 15.38 9 33764 1316 110554210
Suicide attempt 19.32 15.38 4 33769 103390 110452136
Pyrexia 19.32 15.38 383 33390 897882 109657644
Pleurisy 19.16 15.38 21 33752 12095 110543431
Neoplasm progression 19.12 15.38 53 33720 64542 110490984
Folliculitis 19.07 15.38 14 33759 167639 110387887
Moyamoya disease 18.96 15.38 5 33768 132 110555394
Dry skin 18.94 15.38 74 33699 107579 110447947
Jaundice 18.94 15.38 50 33723 59186 110496340
Skin disorder 18.88 15.38 41 33732 42872 110512654
Myeloproliferative neoplasm 18.82 15.38 9 33764 1396 110554130
Urinary tract disorder 18.72 15.38 15 33758 5829 110549697
Pancreatitis acute 18.39 15.38 50 33723 60224 110495302
Obesity 18.11 15.38 6 33767 113345 110442181
Adverse drug reaction 17.93 15.38 5 33768 105554 110449972
Therapy non-responder 17.85 15.38 95 33678 157212 110398314
Liver injury 17.84 15.38 12 33761 150401 110405125
Cerebrovascular stenosis 17.78 15.38 5 33768 169 110555357
Fall 17.61 15.38 110 33663 603372 109952154
Skin sensitisation 17.57 15.38 8 33765 1111 110554415
Muscle spasms 17.53 15.38 145 33628 278012 110277514
Renal artery stenosis 17.41 15.38 12 33761 3714 110551812
Diplopia 17.27 15.38 39 33734 41855 110513671
Therapeutic product effect incomplete 17.25 15.38 26 33747 223779 110331747
Drug ineffective for unapproved indication 17.23 15.38 5 33768 102833 110452693
Extremity necrosis 17.19 15.38 12 33761 3790 110551736
Splenitis 17.13 15.38 3 33770 9 110555517
Blood alkaline phosphatase increased 17.00 15.38 54 33719 70881 110484645
Psoriasis 16.84 15.38 11 33762 139982 110415544
Suicidal ideation 16.82 15.38 4 33769 93933 110461593
Acute lymphocytic leukaemia 16.79 15.38 14 33759 5751 110549775
Myelodysplastic syndrome 16.70 15.38 36 33737 37448 110518078
Graft versus host disease in eye 16.67 15.38 6 33767 454 110555072
General physical health deterioration 16.67 15.38 70 33703 425225 110130301
Vaginal odour 16.58 15.38 6 33767 461 110555065
Paternal exposure during pregnancy 16.46 15.38 5 33768 222 110555304
Vertebral artery hypoplasia 16.46 15.38 3 33770 12 110555514
Supraventricular extrasystoles 16.39 15.38 16 33757 8057 110547469
Agitation 16.37 15.38 7 33766 113044 110442482
Musculoskeletal toxicity 16.31 15.38 5 33768 229 110555297
Peripheral venous disease 16.25 15.38 3 33770 84114 110471412
Tremor 16.06 15.38 23 33750 202209 110353317
Recurrent cancer 15.94 15.38 11 33762 3412 110552114
Dyslalia 15.88 15.38 8 33765 1389 110554137
Red blood cell count decreased 15.63 15.38 50 33723 65873 110489653
Peripheral swelling 15.52 15.38 67 33706 403967 110151559
Therapy cessation 15.51 15.38 39 33734 44818 110510708

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EA03 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
BCR-ABL tyrosine kinase inhibitors
FDA MoA N0000020009 Bcr-Abl Tyrosine Kinase Inhibitors
MeSH PA D000092004 Tyrosine Kinase Inhibitors
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D047428 Protein Kinase Inhibitors
FDA EPC N0000175605 Kinase Inhibitor
FDA MoA N0000182137 Cytochrome P450 2D6 Inhibitors
FDA MoA N0000185503 P-Glycoprotein Inhibitors
FDA MoA N0000187062 Cytochrome P450 2C8 Inhibitors
FDA MoA N0000187063 Cytochrome P450 2C8 Inducers
FDA MoA N0000187064 Cytochrome P450 2B6 Inducers
FDA MoA N0000191272 UGT1A1 Inhibitors
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:35674 antihypertensive agent
CHEBI has role CHEBI:38637 tyrosine kinase inhibitor
CHEBI has role CHEBI:48407 antiparkinson drug
CHEBI has role CHEBI:149553 anticoronaviral agent

Related Drugs by ATC class:

L01EA BCR-ABL tyrosine kinase inhibitors 5 drugs
asciminibbosutinibdasatinibimatinibponatinib

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

DiseaseRelationSNOMED_IDDOID
Chronic phase chronic myeloid leukemia indication 413847001
Philadelphia Chromosome Positive Chronic Myelocytic Leukemia indication
Chronic Myelocytic Leukemia Accelerated Phase indication
Hypophosphatemia contraindication 4996001
Hypocalcemia contraindication 5291005
Hypercholesterolemia contraindication 13644009
Hyperkalemia contraindication 14140009
Hyperbilirubinemia contraindication 14783006 DOID:2741
Torsades de pointes contraindication 31722008
Hypertensive disorder contraindication 38341003 DOID:10763
Hypokalemia contraindication 43339004
Gastrectomy contraindication 53442002
Diabetes mellitus contraindication 73211009 DOID:9351
Pancreatitis contraindication 75694006 DOID:4989
Hyperglycemia contraindication 80394007 DOID:4195
Hyponatremia contraindication 89627008
Prolonged QT interval contraindication 111975006
Liver function tests abnormal contraindication 166603001
Hypomagnesemia contraindication 190855004
Disease of liver contraindication 235856003 DOID:409
Anemia contraindication 271737000 DOID:2355
Pregnancy, function contraindication 289908002
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Neutropenic disorder contraindication 303011007 DOID:1227
Breastfeeding (mother) contraindication 413712001
Congenital long QT syndrome contraindication 442917000
Elevated Serum Lipase contraindication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.89 acidic
pKa2 6.03 Basic
pKa3 3.97 Basic
pKa4 2.2 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 50MG BASE TASIGNA NOVARTIS N022068 March 22, 2018 RX CAPSULE ORAL 8389537 July 18, 2026 TREATMENT OF PHILADELPHIA CHROMOSOME POSITIVE CHRONIC MYELOID LEUKEMIA (PH+CML)
EQ 50MG BASE TASIGNA NOVARTIS N022068 March 22, 2018 RX CAPSULE ORAL 8415363 July 18, 2026 TREATMENT OF NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME POSITIVE CHRONIC MYELOID LEUKEMIA (PH + CML)
EQ 50MG BASE TASIGNA NOVARTIS N022068 March 22, 2018 RX CAPSULE ORAL 8415363 July 18, 2026 TREATMENT OF PHILADELPHIA CHROMOSOME POSITIVE CHRONIC MYELOID LEUKEMIA (PH+CML)
EQ 50MG BASE TASIGNA NOVARTIS N022068 March 22, 2018 RX CAPSULE ORAL 9061029 April 7, 2032 TREATMENT OF PHILADELPHIA CHROMOSOME POSITIVE CHRONIC MYELOID LEUKEMIA (PH+CML)
EQ 50MG BASE TASIGNA NOVARTIS N022068 March 22, 2018 RX CAPSULE ORAL 9061029 April 7, 2032 TREATMENT OF PHILADELPHIA CHROMOSOME POSITIVE CHRONIC MYELOID LEUKEMIA (PH+CML) BY ADMINISTERING NILOTINIB DISPERSED IN A FRUIT PREPARATION
60MG CAVHANZA FLEX PHARMA N217379 May 29, 2026 RX TABLET, ORALLY DISINTEGRATING ORAL 11389450 Jan. 29, 2041 USE OF NILOTINIB FOR TREATMENT OF ADULT PATIENTS WITH CHRONIC PHASE AND ACCELERATED PHASE PH+ CHRONIC MYELOID LEUKEMIA RESISTANT TO OR INTOLERANT TO PRIOR THERAPY THAT INCLUDED IMATINIB, WHEN ADMINISTERED WITH FOOD OR IN FED STATE
60MG CAVHANZA FLEX PHARMA N217379 May 29, 2026 RX TABLET, ORALLY DISINTEGRATING ORAL 11389450 Jan. 29, 2041 USE OF NILOTINIB FOR TREATMENT OF ADULT PATIENTS WITH NEWLY DIAGNOSED PH+ CHRONIC MYELOID LEUKEMIA IN CHRONIC PHASE, WHEN ADMINISTERED WITH FOOD OR IN FED STATE
60MG CAVHANZA FLEX PHARMA N217379 May 29, 2026 RX TABLET, ORALLY DISINTEGRATING ORAL 12016861 Jan. 29, 2041 USE OF 120 MG NILOTINIB TWICE DAILY FOR TREATMENT OF ADULT PATIENTS WITH NEWLY DIAGNOSED PH+ CHRONIC MYELOID LEUKEMIA IN CHRONIC PHASE
60MG CAVHANZA FLEX PHARMA N217379 May 29, 2026 RX TABLET, ORALLY DISINTEGRATING ORAL 12016861 Jan. 29, 2041 USE OF 160 MG NILOTINIB TWICE DAILY FOR TREATMENT OF ADULT PATIENTS WITH CHRONIC PHASE AND ACCELERATED PHASE PH+ CHRONIC MYELOID LEUKEMIA RESISTANT TO OR INTOLERANT TO PRIOR THERAPY THAT INCLUDED IMATINIB
80MG CAVHANZA FLEX PHARMA N217379 May 29, 2026 RX TABLET, ORALLY DISINTEGRATING ORAL 11389450 Jan. 29, 2041 USE OF NILOTINIB FOR TREATMENT OF ADULT PATIENTS WITH CHRONIC PHASE AND ACCELERATED PHASE PH+ CHRONIC MYELOID LEUKEMIA RESISTANT TO OR INTOLERANT TO PRIOR THERAPY THAT INCLUDED IMATINIB, WHEN ADMINISTERED WITH FOOD OR IN FED STATE
80MG CAVHANZA FLEX PHARMA N217379 May 29, 2026 RX TABLET, ORALLY DISINTEGRATING ORAL 11389450 Jan. 29, 2041 USE OF NILOTINIB FOR TREATMENT OF ADULT PATIENTS WITH NEWLY DIAGNOSED PH+ CHRONIC MYELOID LEUKEMIA IN CHRONIC PHASE, WHEN ADMINISTERED WITH FOOD OR IN FED STATE
80MG CAVHANZA FLEX PHARMA N217379 May 29, 2026 RX TABLET, ORALLY DISINTEGRATING ORAL 12016861 Jan. 29, 2041 USE OF 120 MG NILOTINIB TWICE DAILY FOR TREATMENT OF ADULT PATIENTS WITH NEWLY DIAGNOSED PH+ CHRONIC MYELOID LEUKEMIA IN CHRONIC PHASE
80MG CAVHANZA FLEX PHARMA N217379 May 29, 2026 RX TABLET, ORALLY DISINTEGRATING ORAL 12016861 Jan. 29, 2041 USE OF 160 MG NILOTINIB TWICE DAILY FOR TREATMENT OF ADULT PATIENTS WITH CHRONIC PHASE AND ACCELERATED PHASE PH+ CHRONIC MYELOID LEUKEMIA RESISTANT TO OR INTOLERANT TO PRIOR THERAPY THAT INCLUDED IMATINIB

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 50MG BASE TASIGNA NOVARTIS N022068 March 22, 2018 RX CAPSULE ORAL Sept. 23, 2028 TREATMENT OF PEDIATRIC PATIENTS GREATER THAN OR EQUAL TO 1 YEAR OF AGE WITH ACCELERATED PHASE PHILADELPHIA CHROMOSOME POSITIVE CHRONIC MYELOID LEUKEMIA (PH+ CML) WITH RESISTANCE OR INTOLERANCE TO PRIOR TYROSINE-KINASE INHIBITOR (TKI) THERAPY
EQ 50MG BASE TASIGNA NOVARTIS N022068 March 22, 2018 RX CAPSULE ORAL March 23, 2029 PEDIATRIC EXCLUSIVITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Tyrosine-protein kinase ABL1 Kinase INHIBITOR Kd 8.44 CHEMBL CHEMBL
Mitogen-activated protein kinase 14 Kinase Kd 6.34 CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 6.35 CHEMBL
Carbonic anhydrase 2 Enzyme Ki 8.39 CHEMBL
ATP-binding cassette sub-family G member 2 Transporter IC50 5.60 CHEMBL
Carbonic anhydrase 1 Enzyme Ki 7.53 CHEMBL
Carbonic anhydrase 4 Enzyme Ki 6.35 CHEMBL
Ribosyldihydronicotinamide dehydrogenase [quinone] Enzyme IC50 6.42 CHEMBL
Carbonic anhydrase 9 Enzyme Ki 7.38 CHEMBL
Carbonic anhydrase 12 Enzyme Ki 6.52 CHEMBL
Platelet-derived growth factor receptor beta Kinase Kd 7.80 CHEMBL
Mast/stem cell growth factor receptor Kit Kinase Kd 7.77 CHEMBL
Carbonic anhydrase 5A, mitochondrial Enzyme Ki 5.26 CHEMBL
Carbonic anhydrase 5B, mitochondrial Enzyme Ki 4.83 CHEMBL
Carbonic anhydrase 7 Enzyme Ki 7 CHEMBL
Proto-oncogene tyrosine-protein kinase Src Kinase Kd 5.72 CHEMBL
Tyrosine-protein kinase Lck Kinase Kd 7.33 CHEMBL
Tyrosine-protein kinase Yes Kinase Kd 5.96 CHEMBL
Tyrosine-protein kinase Fyn Kinase Kd 5.80 CHEMBL
Ephrin type-A receptor 2 Kinase Kd 6.64 CHEMBL
RAF proto-oncogene serine/threonine-protein kinase Kinase Kd 5.41 CHEMBL
Serine/threonine-protein kinase B-raf Kinase Kd 6.24 CHEMBL
Receptor-type tyrosine-protein kinase FLT3 Kinase Kd 4.40 CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret Kinase Kd 6.06 CHEMBL
Macrophage colony-stimulating factor 1 receptor Kinase Kd 7.35 CHEMBL
Platelet-derived growth factor receptor alpha Kinase Kd 7.13 CHEMBL
Phosphorylase b kinase gamma catalytic chain, liver/testis isoform Kinase Kd 6.48 CHEMBL
Insulin receptor Kinase Ki 5.39 PDSP
Mitogen-activated protein kinase 8 Kinase Kd 6.35 CHEMBL
Tyrosine-protein kinase HCK Kinase Kd 6.41 CHEMBL
Carbonic anhydrase 3 Enzyme Ki 6.35 CHEMBL
Carbonic anhydrase 6 Enzyme Ki 6.34 CHEMBL
Mitogen-activated protein kinase 10 Kinase Kd 5.70 CHEMBL
Tyrosine-protein kinase JAK2 Kinase Ki 5.07 PDSP
Tyrosine-protein kinase CSK Kinase Kd 5.62 CHEMBL
Angiopoietin-1 receptor Kinase Kd 6 CHEMBL
Ephrin type-A receptor 8 Kinase Kd 7.43 CHEMBL
Tyrosine-protein kinase Lyn Kinase Kd 7 CHEMBL
Cytoplasmic tyrosine-protein kinase BMX Kinase Ki 5.32 PDSP
Carbonic anhydrase 14 Enzyme Ki 6.65 CHEMBL
Fibroblast growth factor receptor 1 Kinase Ki 5.10 PDSP
Serine/threonine-protein kinase 10 Kinase Kd 5.17 CHEMBL
Abelson tyrosine-protein kinase 2 Kinase Kd 7.59 CHEMBL
Mitogen-activated protein kinase 11 Kinase Kd 7.44 CHEMBL
Ephrin type-A receptor 5 Kinase Kd 5.72 CHEMBL
Ephrin type-A receptor 4 Kinase Kd 6.48 CHEMBL
Fibroblast growth factor receptor 2 Kinase Ki 5.14 PDSP
Ephrin type-A receptor 6 Kinase Kd 6.19 CHEMBL
Tyrosine-protein kinase Fgr Kinase Kd 6.49 CHEMBL
Ephrin type-A receptor 3 Kinase Kd 6.96 CHEMBL
Dual specificity protein kinase CLK1 Kinase Kd 5.68 CHEMBL
Ephrin type-B receptor 1 Kinase Kd 5.89 CHEMBL
Dual specificity protein kinase CLK4 Kinase Kd 5.15 CHEMBL
Mitogen-activated protein kinase 9 Kinase Kd 5.24 CHEMBL
Epithelial discoidin domain-containing receptor 1 Kinase Kd 8.96 CHEMBL
Ephrin type-B receptor 4 Kinase Kd 6.14 CHEMBL
BDNF/NT-3 growth factors receptor Kinase Kd 6.31 CHEMBL
Ephrin type-B receptor 2 Kinase Kd 6.19 CHEMBL
Mitogen-activated protein kinase kinase kinase MLT Kinase Kd 7.96 CHEMBL
Tyrosine-protein kinase receptor Tie-1 Kinase Kd 6 CHEMBL
NT-3 growth factor receptor Kinase Kd 6.22 CHEMBL
Serine/threonine-protein kinase TNNI3K Kinase Kd 6.44 CHEMBL
Discoidin domain-containing receptor 2 Kinase Kd 8.22 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 1 Kinase Kd 6.05 CHEMBL
Tyrosine-protein kinase Blk Kinase Kd 6.30 CHEMBL
Serine/threonine-protein kinase MRCK beta Kinase Kd 6.04 CHEMBL
Ephrin type-A receptor 1 Kinase Kd 6.23 CHEMBL
Ephrin type-B receptor 3 Kinase Kd 6 CHEMBL
Ephrin type-B receptor 6 Kinase Kd 6.30 CHEMBL
Serine/threonine-protein kinase TAO1 Kinase Kd 5.33 CHEMBL
Serine/threonine-protein kinase TAO3 Kinase Kd 5.77 CHEMBL
Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma Kinase Kd 5.06 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 5 Kinase Kd 6.72 CHEMBL
Bcr/Abl fusion protein Kinase IC50 9.48 CHEMBL
Ferrochelatase, mitochondrial Enzyme Kd 5.38 CHEMBL
Receptor-interacting serine/threonine-protein kinase 3 Kinase Kd 5.89 CHEMBL
Integrin-linked protein kinase Kinase Kd 7.70 CHEMBL
Tyrosine-protein kinase FRK Kinase Kd 7.07 CHEMBL
Carbonic anhydrase 13 Enzyme Ki 5.33 CHEMBL
Carbonic anhydrase 15 Enzyme Ki 7.10 CHEMBL
Calcium-dependent protein kinase 1 Kinase Kd 6.10 CHEMBL
Macrophage colony-stimulating factor 1 receptor Kinase IC50 6.27 CHEMBL

External reference:

IDSource
4026964 VUID
N0000176124 NUI
D06413 KEGG_DRUG
4026964 VANDF
C1721377 UMLSCUI
CHEBI:52172 CHEBI
NIL PDB_CHEM_ID
CHEMBL255863 ChEMBL_ID
CHEMBL1201740 ChEMBL_ID
DB04868 DRUGBANK_ID
C498826 MESH_SUPPLEMENTAL_RECORD_UI
5697 IUPHAR_LIGAND_ID
8654 INN_ID
923288-90-8 SECONDARY_CAS_RN
F41401512X UNII
644241 PUBCHEM_CID
2701416 RXNORM
127956 MMSL
24733 MMSL
395040 MMSL
d07057 MMSL
012401 NDDF
427941004 SNOMEDCT_US
428468009 SNOMEDCT_US
438943005 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Tasigna HUMAN PRESCRIPTION DRUG LABEL 1 0078-0526 CAPSULE 200 mg ORAL NDA 32 sections
Tasigna HUMAN PRESCRIPTION DRUG LABEL 1 0078-0592 CAPSULE 150 mg ORAL NDA 32 sections
Tasigna HUMAN PRESCRIPTION DRUG LABEL 1 0078-0951 CAPSULE 50 mg ORAL NDA 32 sections
nilotinib HUMAN PRESCRIPTION DRUG LABEL 1 13668-710 CAPSULE 150 mg ORAL ANDA 26 sections
nilotinib HUMAN PRESCRIPTION DRUG LABEL 1 13668-711 CAPSULE 200 mg ORAL ANDA 26 sections
DANZITEN Human Prescription Drug Label 1 24338-154 TABLET 71 mg ORAL NDA 27 sections
DANZITEN Human Prescription Drug Label 1 24338-155 TABLET 95 mg ORAL NDA 27 sections
Nilotinib HUMAN PRESCRIPTION DRUG LABEL 1 31722-779 CAPSULE 150 mg ORAL ANDA 28 sections
Nilotinib HUMAN PRESCRIPTION DRUG LABEL 1 31722-780 CAPSULE 200 mg ORAL ANDA 28 sections
Nilotinib HUMAN PRESCRIPTION DRUG LABEL 1 43598-055 CAPSULE 50 mg ORAL ANDA 31 sections
Nilotinib HUMAN PRESCRIPTION DRUG LABEL 1 43598-455 CAPSULE 150 mg ORAL ANDA 31 sections
Nilotinib HUMAN PRESCRIPTION DRUG LABEL 1 43598-456 CAPSULE 200 mg ORAL ANDA 31 sections
Nilotinib HUMAN PRESCRIPTION DRUG LABEL 1 60505-3801 CAPSULE 150 mg ORAL ANDA 26 sections
Nilotinib HUMAN PRESCRIPTION DRUG LABEL 1 60505-3802 CAPSULE 200 mg ORAL ANDA 26 sections
Nilotinib HUMAN PRESCRIPTION DRUG LABEL 1 60505-3803 CAPSULE 50 mg ORAL ANDA 26 sections
Nilotinib HUMAN PRESCRIPTION DRUG LABEL 1 69097-030 CAPSULE 50 mg ORAL NDA 32 sections
Nilotinib HUMAN PRESCRIPTION DRUG LABEL 1 69097-031 CAPSULE 150 mg ORAL NDA 32 sections
Nilotinib HUMAN PRESCRIPTION DRUG LABEL 1 69097-032 CAPSULE 200 mg ORAL NDA 32 sections
CAVHANZA HUMAN PRESCRIPTION DRUG LABEL 1 70709-191 TABLET, ORALLY DISINTEGRATING 60 mg ORAL NDA 32 sections
CAVHANZA HUMAN PRESCRIPTION DRUG LABEL 1 70709-192 TABLET, ORALLY DISINTEGRATING 80 mg ORAL NDA 32 sections
nilotinib Human Prescription Drug Label 1 72205-237 CAPSULE 50 mg ORAL ANDA 25 sections
nilotinib Human Prescription Drug Label 1 72205-238 CAPSULE 150 mg ORAL ANDA 25 sections
nilotinib Human Prescription Drug Label 1 72205-239 CAPSULE 200 mg ORAL ANDA 25 sections
nilotinib HUMAN PRESCRIPTION DRUG LABEL 1 73190-033 CAPSULE 150 mg ORAL ANDA 25 sections
nilotinib HUMAN PRESCRIPTION DRUG LABEL 1 73190-034 CAPSULE 200 mg ORAL ANDA 25 sections
Nilotinib HUMAN PRESCRIPTION DRUG LABEL 1 76282-788 CAPSULE 50 mg ORAL NDA 32 sections
Nilotinib HUMAN PRESCRIPTION DRUG LABEL 1 76282-789 CAPSULE 150 mg ORAL NDA 32 sections
Nilotinib HUMAN PRESCRIPTION DRUG LABEL 1 76282-790 CAPSULE 200 mg ORAL NDA 32 sections