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

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 1423 152459-95-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • imatinib
  • gleevec
  • imatinib mesylate
  • imatinib mesilate
  • CGP-57-148B
  • CGP57148B
  • CGP-57148
  • CGP57148
  • STI-571
  • STI571
A tyrosine kinase inhibitor and ANTINEOPLASTIC AGENT that inhibits the BCR-ABL kinase created by chromosome rearrangements in CHRONIC MYELOID LEUKEMIA and ACUTE LYMPHOBLASTIC LEUKEMIA, as well as PDG-derived tyrosine kinases that are overexpressed in gastrointestinal stromal tumors.
  • Molecular weight: 493.62
  • Formula: C29H31N7O
  • CLOGP: 4.38
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 2
  • TPSA: 86.28
  • ALOGS: -4.53
  • ROTB: 7

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
0.40 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 1 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 5 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 20.26 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 98 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 3.90 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 3.30 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.05 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 22 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Nov. 7, 2001 EMA Novartis Europharm Limited
May 10, 2001 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
Death 1594.24 12.50 1622 38268 355610 52953566
Gastrointestinal stromal tumour 855.91 12.50 195 39695 1004 53308172
Chronic myeloid leukaemia 832.33 12.50 224 39666 2490 53306686
Blast crisis in myelogenous leukaemia 673.09 12.50 139 39751 403 53308773
Drug resistance 553.75 12.50 279 39611 19683 53289493
Cytogenetic analysis abnormal 543.91 12.50 124 39766 640 53308536
Malignant neoplasm progression 431.74 12.50 386 39504 71155 53238021
Second primary malignancy 424.20 12.50 170 39720 6962 53302214
Periorbital oedema 313.68 12.50 126 39764 5189 53303987
Gene mutation identification test positive 252.86 12.50 50 39840 107 53309069
Chronic myeloid leukaemia recurrent 227.53 12.50 49 39841 184 53308992
Neoplasm malignant 220.69 12.50 170 39720 25431 53283745
Philadelphia chromosome positive 219.66 12.50 51 39839 289 53308887
Rheumatoid arthritis 197.46 12.50 9 39881 314522 52994654
Muscle spasms 187.29 12.50 350 39540 134445 53174731
Chromosome analysis abnormal 183.75 12.50 38 39852 111 53309065
Pleural effusion 180.42 12.50 273 39617 88306 53220870
Leukaemia recurrent 174.85 12.50 58 39832 1369 53307807
Acute lymphocytic leukaemia recurrent 167.03 12.50 63 39827 2185 53306991
Chronic myeloid leukaemia transformation 166.37 12.50 35 39855 114 53309062
Oedema 162.67 12.50 237 39653 74109 53235067
Eyelid oedema 139.48 12.50 91 39799 10463 53298713
Gastric antral vascular ectasia 138.16 12.50 40 39850 590 53308586
Eye swelling 136.50 12.50 120 39770 21574 53287602
Bone marrow failure 113.62 12.50 126 39764 29989 53279187
Fluid retention 109.74 12.50 167 39723 54234 53254942
Nausea 108.20 12.50 946 38944 755145 52554031
Pancytopenia 103.11 12.50 217 39673 90711 53218465
Haematotoxicity 99.27 12.50 66 39824 7831 53301345
Face oedema 96.57 12.50 96 39794 20144 53289032
Conjunctival haemorrhage 94.76 12.50 47 39843 3197 53305979
Graft versus host disease 93.11 12.50 61 39829 7061 53302115
Drug hypersensitivity 93.01 12.50 41 39849 265201 53043975
Product substitution issue 92.35 12.50 84 39806 15782 53293394
Anaemia 91.35 12.50 429 39461 276289 53032887
Oedema peripheral 88.64 12.50 305 39585 170482 53138694
Arthropathy 85.64 12.50 5 39885 141448 53167728
Normal newborn 83.07 12.50 57 39833 7122 53302054
Gene mutation 81.20 12.50 32 39858 1251 53307925
Pseudoporphyria 80.50 12.50 20 39870 157 53309019
Completed suicide 80.38 12.50 6 39884 138195 53170981
Blast cell crisis 79.98 12.50 17 39873 59 53309117
Cytogenetic abnormality 78.06 12.50 25 39865 526 53308650
Generalised oedema 74.60 12.50 73 39817 15026 53294150
Thrombocytosis 73.83 12.50 48 39842 5484 53303692
Recurrent cancer 73.21 12.50 33 39857 1809 53307367
Metastases to liver 72.70 12.50 85 39805 21411 53287765
Growth retardation 70.54 12.50 28 39862 1116 53308060
Pain 69.50 12.50 218 39672 588180 52720996
Swelling face 68.96 12.50 140 39750 57028 53252148
Systemic lupus erythematosus 68.70 12.50 7 39883 125407 53183769
Acute lymphocytic leukaemia 67.74 12.50 36 39854 2829 53306347
Disease progression 67.45 12.50 198 39692 101722 53207454
Exposure via father 66.94 12.50 20 39870 331 53308845
Chronic graft versus host disease 66.43 12.50 37 39853 3191 53305985
Thrombocytopenia 65.29 12.50 240 39650 138487 53170689
Off label use 64.55 12.50 163 39727 472049 52837127
Rash 63.79 12.50 559 39331 445632 52863544
Pericardial effusion 62.58 12.50 89 39801 27189 53281987
Splenomegaly 62.18 12.50 56 39834 10383 53298793
Vomiting 62.10 12.50 605 39285 496534 52812642
Hepatotoxicity 61.08 12.50 89 39801 27791 53281385
Hypotension 58.76 12.50 62 39828 254014 53055162
Neoplasm recurrence 58.48 12.50 31 39859 2423 53306753
Therapeutic response decreased 57.97 12.50 117 39773 47452 53261724
Therapeutic product effect decreased 57.34 12.50 12 39878 125643 53183533
Bone pain 56.23 12.50 120 39770 50602 53258574
Neoplasm progression 54.95 12.50 88 39802 29831 53279345
Drug intolerance 54.65 12.50 300 39590 205193 53103983
Leukaemia 54.03 12.50 34 39856 3672 53305504
Diarrhoea 52.71 12.50 705 39185 624841 52684335
Polymerase chain reaction positive 51.98 12.50 12 39878 66 53309110
White blood cell count increased 51.95 12.50 110 39780 46135 53263041
Eye haemorrhage 49.07 12.50 43 39847 7691 53301485
Haemoglobin decreased 48.99 12.50 218 39672 137089 53172087
Confusional state 48.81 12.50 44 39846 194177 53114999
Fall 48.70 12.50 124 39766 358316 52950860
Therapy non-responder 48.56 12.50 111 39779 49009 53260167
Sinusitis 47.60 12.50 34 39856 168530 53140646
Exposure via body fluid 47.36 12.50 17 39873 511 53308665
Cardiac output decreased 46.58 12.50 20 39870 975 53308201
Lower respiratory tract infection 45.16 12.50 7 39883 90974 53218202
Glossodynia 44.90 12.50 10 39880 100281 53208895
Metastases to peritoneum 44.63 12.50 28 39862 3007 53306169
Platelet count increased 44.53 12.50 57 39833 15750 53293426
Eye oedema 44.43 12.50 22 39868 1491 53307685
Condition aggravated 44.16 12.50 98 39792 297036 53012140
Chordoma 43.40 12.50 7 39883 0 53309176
Neutropenia 43.37 12.50 234 39656 158951 53150225
Myalgia 43.22 12.50 206 39684 133285 53175891
Psoriasis 42.55 12.50 7 39883 87082 53222094
Joint swelling 41.27 12.50 70 39820 234568 53074608
Myelofibrosis 41.26 12.50 20 39870 1294 53307882
Urinary tract infection 40.00 12.50 74 39816 239829 53069347
Blast cells present 39.81 12.50 14 39876 396 53308780
Product use issue 39.60 12.50 28 39862 139556 53169620
Platelet count decreased 39.58 12.50 173 39717 107926 53201250
Exposure via partner 39.27 12.50 11 39879 143 53309033
Periorbital swelling 39.14 12.50 21 39869 1682 53307494
Overdose 38.75 12.50 16 39874 107720 53201456
Leukocytosis 37.77 12.50 67 39823 24667 53284509
Wound 37.39 12.50 11 39879 91546 53217630
Erythrocyanosis 37.20 12.50 6 39884 0 53309176
Asthma 36.35 12.50 18 39872 108954 53200222
Discomfort 36.29 12.50 13 39877 95459 53213717
Jaundice 36.26 12.50 74 39816 30239 53278937
Tumour excision 36.05 12.50 13 39877 396 53308780
Blast cell count increased 35.33 12.50 13 39877 420 53308756
Therapeutic response delayed 35.03 12.50 14 39876 568 53308608
Chloroma 34.96 12.50 11 39879 218 53308958
Peripheral arterial occlusive disease 33.49 12.50 26 39864 3928 53305248
Skin fragility 33.21 12.50 14 39876 652 53308524
Ascites 33.05 12.50 84 39806 39651 53269525
Bone marrow oedema 32.58 12.50 15 39875 864 53308312
Bone marrow transplant 32.06 12.50 14 39876 711 53308465
Acute graft versus host disease 31.48 12.50 26 39864 4291 53304885
Gastrointestinal toxicity 31.27 12.50 27 39863 4735 53304441
White blood cell count decreased 31.23 12.50 179 39711 124296 53184880
Pneumatosis intestinalis 31.23 12.50 20 39870 2226 53306950
Pulse waveform abnormal 31.23 12.50 8 39882 72 53309104
Loss of personal independence in daily activities 31.16 12.50 7 39883 69808 53239368
Ankle brachial index decreased 31.13 12.50 8 39882 73 53309103
Trisomy 8 31.00 12.50 5 39885 0 53309176
Blood lactate dehydrogenase increased 30.71 12.50 57 39833 21724 53287452
Carotid intima-media thickness increased 30.65 12.50 8 39882 78 53309098
Cardiotoxicity 30.07 12.50 32 39858 7267 53301909
Nasopharyngitis 29.71 12.50 62 39828 192233 53116943
Breast cancer 28.98 12.50 92 39798 49266 53259910
Toxic skin eruption 28.86 12.50 42 39848 13097 53296079
Right ventricular failure 28.83 12.50 48 39842 16795 53292381
Musculoskeletal stiffness 28.60 12.50 30 39860 123338 53185838
Typhoid fever 28.19 12.50 6 39884 21 53309155
Surgery 28.08 12.50 69 39821 31895 53277281
Intentional overdose 27.57 12.50 8 39882 67197 53241979
Acute kidney injury 27.14 12.50 98 39792 253770 53055406
Morphoea 26.83 12.50 10 39880 335 53308841
Left ventricular dysfunction 26.26 12.50 37 39853 11200 53297976
Aplasia 25.98 12.50 23 39867 4169 53305007
Chronic graft versus host disease in skin 25.92 12.50 12 39878 700 53308476
Anxiety 25.18 12.50 70 39820 196634 53112542
Dizziness 25.17 12.50 169 39721 372090 52937086
Tumour haemorrhage 24.90 12.50 15 39875 1499 53307677
Pubertal failure 24.89 12.50 5 39885 12 53309164
Slit-lamp tests abnormal 24.80 12.50 4 39886 0 53309176
Peritoneal lesion 24.80 12.50 4 39886 0 53309176
Hypersensitivity 24.78 12.50 78 39812 210587 53098589
Tumour necrosis 24.64 12.50 12 39878 784 53308392
Transdifferentiation of neoplasm 24.60 12.50 5 39885 13 53309163
Blood pressure increased 24.59 12.50 42 39848 140437 53168739
Cytopenia 24.16 12.50 32 39858 9138 53300038
Urine odour abnormal 24.07 12.50 25 39865 5521 53303655
Syncope 24.03 12.50 29 39861 111964 53197212
Pyrexia 24.02 12.50 429 39461 402764 52906412
Back pain 24.00 12.50 92 39798 234155 53075021
Hepatic necrosis 23.32 12.50 25 39865 5725 53303451
Abortion 23.24 12.50 17 39873 2349 53306827
Abortion spontaneous 23.02 12.50 82 39808 46553 53262623
Injury 22.97 12.50 5 39885 50966 53258210
Hallucination 22.85 12.50 6 39884 53832 53255344
Leukopenia 22.77 12.50 112 39778 73351 53235825
Somnolence 22.75 12.50 58 39832 167676 53141500
Intentional product use issue 22.67 12.50 13 39877 72481 53236695
Inappropriate schedule of product administration 22.61 12.50 14 39876 74864 53234312
Agitation 22.24 12.50 8 39882 58618 53250558
Papilloedema 22.13 12.50 20 39870 3723 53305453
Liver disorder 21.90 12.50 73 39817 40082 53269094
Therapy partial responder 21.89 12.50 25 39865 6138 53303038
Suicidal ideation 21.73 12.50 9 39881 60502 53248674
Arthritis 21.64 12.50 20 39870 87278 53221898
Insomnia 21.48 12.50 70 39820 187002 53122174
Hyponatraemia 21.37 12.50 30 39860 108577 53200599
Basophilia 21.14 12.50 4 39886 6 53309170
Pericarditis 20.93 12.50 11 39879 64395 53244781
Tremor 20.74 12.50 39 39851 125697 53183479
Chylothorax 20.51 12.50 8 39882 304 53308872
Intracardiac mass 20.50 12.50 5 39885 36 53309140
Anaphylactic reaction 20.42 12.50 9 39881 58317 53250859
Oral pigmentation 20.41 12.50 4 39886 8 53309168
Therapy interrupted 20.41 12.50 45 39845 19391 53289785
Hypertension 20.33 12.50 93 39797 225338 53083838
Gastric cancer 20.25 12.50 18 39872 3279 53305897
Flushing 20.23 12.50 14 39876 70586 53238590
Drug ineffective 20.16 12.50 462 39428 816783 52492393
Microangiopathy 19.92 12.50 11 39879 933 53308243
Blood test abnormal 19.83 12.50 33 39857 11544 53297632
Stem cell transplant 19.82 12.50 14 39876 1831 53307345
Computerised tomogram abnormal 19.65 12.50 15 39875 2211 53306965
Exposure during pregnancy 19.61 12.50 160 39730 124700 53184476
Neoplasm 19.50 12.50 24 39866 6372 53302804
Lacrimation increased 19.42 12.50 42 39848 17861 53291315
Urticaria 19.19 12.50 46 39844 135839 53173337
Obliterative bronchiolitis 19.13 12.50 14 39876 1936 53307240
Exophthalmos 18.83 12.50 12 39878 1324 53307852
Acute myeloid leukaemia 18.69 12.50 40 39850 16892 53292284
Aspiration pleural cavity 18.56 12.50 10 39880 808 53308368
Fibromyalgia 18.54 12.50 5 39885 44070 53265106
Product dose omission issue 18.52 12.50 77 39813 191543 53117633
Jaw operation 18.50 12.50 10 39880 813 53308363
Myelocytosis 18.37 12.50 4 39886 16 53309160
Mobility decreased 18.29 12.50 18 39872 76253 53232923
Cellulitis 18.15 12.50 18 39872 75971 53233205
Gastrointestinal angiectasia 17.85 12.50 5 39885 65 53309111
Disseminated intravascular coagulation 17.78 12.50 43 39847 19676 53289500
Eosinophilia 17.63 12.50 45 39845 21290 53287886
Dengue fever 17.59 12.50 9 39881 654 53308522
Influenza like illness 17.52 12.50 12 39878 60847 53248329
Loss of consciousness 17.48 12.50 37 39853 114175 53195001
Scleroderma-like reaction 17.19 12.50 5 39885 75 53309101
Therapy cessation 17.15 12.50 53 39837 27972 53281204
Pigmentation disorder 17.05 12.50 18 39872 4049 53305127
Headache 16.96 12.50 291 39599 536530 52772646
Hyperhidrosis 16.88 12.50 29 39861 96764 53212412
Hepatic failure 16.85 12.50 62 39828 35744 53273432
Hyperkalaemia 16.58 12.50 10 39880 54246 53254930
Ejection fraction decreased 16.54 12.50 42 39848 19806 53289370
Metastasis 16.48 12.50 19 39871 4712 53304464
Fibrin degradation products increased 16.45 12.50 6 39884 189 53308987
Acquired gene mutation 16.24 12.50 9 39881 768 53308408
Deep vein thrombosis 16.21 12.50 23 39867 82890 53226286
Lichen planus 16.19 12.50 13 39877 2061 53307115
Abortion induced 16.11 12.50 29 39861 10797 53298379
Swelling of eyelid 15.96 12.50 12 39878 1728 53307448
Dry skin 15.80 12.50 72 39818 45688 53263488
Blood blister 15.78 12.50 12 39878 1759 53307417
Knee arthroplasty 15.73 12.50 3 39887 33566 53275610
Tumour lysis syndrome 15.62 12.50 24 39866 7850 53301326
Aspartate aminotransferase increased 15.60 12.50 112 39778 83917 53225259
Philadelphia positive chronic myeloid leukaemia 15.52 12.50 4 39886 37 53309139
Central nervous system leukaemia 15.49 12.50 5 39885 108 53309068
Helicobacter infection 15.39 12.50 5 39885 39064 53270112
Lichenoid keratosis 15.21 12.50 11 39879 1494 53307682
Acute leukaemia 15.19 12.50 10 39880 1166 53308010
Pulmonary embolism 15.18 12.50 40 39850 114402 53194774
Acute myeloid leukaemia recurrent 15.15 12.50 11 39879 1502 53307674
Delirium 15.14 12.50 6 39884 41423 53267753
Hepatic mass 15.10 12.50 11 39879 1510 53307666
Ocular hyperaemia 15.03 12.50 43 39847 21748 53287428
Subdural haematoma evacuation 14.99 12.50 3 39887 7 53309169
Food interaction 14.86 12.50 8 39882 645 53308531
Type 2 diabetes mellitus 14.49 12.50 3 39887 31667 53277509
Impaired healing 14.44 12.50 16 39874 64189 53244987
Osteoarthritis 14.33 12.50 19 39871 70467 53238709
Irritability 14.02 12.50 3 39887 30950 53278226
Cystitis 13.89 12.50 9 39881 46979 53262197
Myeloid maturation arrest 13.78 12.50 3 39887 12 53309164
Dermatofibrosarcoma protuberans 13.78 12.50 3 39887 12 53309164
Blood bilirubin increased 13.69 12.50 58 39832 35672 53273504
Suicide attempt 13.63 12.50 14 39876 58154 53251022
Oncologic complication 13.58 12.50 5 39885 162 53309014
Primary adrenal insufficiency 13.57 12.50 4 39886 63 53309113
Cardiac failure 13.47 12.50 110 39780 85734 53223442
Adenocarcinoma gastric 13.46 12.50 7 39883 526 53308650
Growth failure 13.39 12.50 6 39884 324 53308852
Polyhydramnios 13.38 12.50 12 39878 2213 53306963
Bone metabolism disorder 13.34 12.50 6 39884 327 53308849
Gastrectomy 13.28 12.50 7 39883 541 53308635
Hepatic enzyme increased 13.28 12.50 49 39841 126146 53183030
Desmoid tumour 13.18 12.50 4 39886 70 53309106
Hepatomegaly 13.11 12.50 28 39862 11803 53297373
Leukaemic infiltration extramedullary 13.07 12.50 4 39886 72 53309104
Therapeutic product effect incomplete 13.01 12.50 31 39859 91753 53217423
Therapy responder 13.01 12.50 6 39884 347 53308829
Hepatic neoplasm 12.92 12.50 11 39879 1893 53307283
Drug level increased 12.85 12.50 39 39851 20382 53288794
Complications of transplant surgery 12.85 12.50 5 39885 189 53308987
Skin hypopigmentation 12.83 12.50 7 39883 580 53308596
Skull fractured base 12.82 12.50 4 39886 77 53309099
Red blood cell count decreased 12.78 12.50 57 39833 35846 53273330
Central nervous system neoplasm 12.77 12.50 3 39887 18 53309158
Blood alkaline phosphatase increased 12.77 12.50 63 39827 41299 53267877
Arthralgia 12.73 12.50 242 39648 439541 52869635
Balance disorder 12.70 12.50 22 39868 73185 53235991
Blood creatine phosphokinase increased 12.66 12.50 49 39841 28936 53280240
Myelodysplastic syndrome 12.60 12.50 34 39856 16626 53292550
Therapy change 12.56 12.50 18 39872 5534 53303642
Vaccination failure 12.53 12.50 5 39885 202 53308974
Seizure 12.53 12.50 52 39838 129457 53179719

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Death 2388.69 12.34 2694 40045 379823 32090964
Gastrointestinal stromal tumour 1153.30 12.34 281 42458 1029 32469758
Chronic myeloid leukaemia 1066.48 12.34 309 42430 2475 32468312
Drug resistance 825.31 12.34 460 42279 22505 32448282
Blast crisis in myelogenous leukaemia 729.57 12.34 167 42572 429 32470358
Second primary malignancy 607.41 12.34 256 42483 6685 32464102
Malignant neoplasm progression 491.14 12.34 559 42180 77937 32392850
Cytogenetic analysis abnormal 442.18 12.34 109 42630 423 32470364
Neoplasm malignant 376.18 12.34 260 42479 18625 32452162
Philadelphia chromosome positive 297.86 12.34 72 42667 252 32470535
Pleural effusion 224.28 12.34 385 42354 78607 32392180
Drug intolerance 211.71 12.34 294 42445 49941 32420846
Gene mutation 198.68 12.34 67 42672 919 32469868
Chromosome analysis abnormal 197.97 12.34 43 42696 78 32470709
Acute lymphocytic leukaemia recurrent 193.49 12.34 90 42649 2982 32467805
Periorbital oedema 157.82 12.34 82 42657 3466 32467321
Leukaemia recurrent 155.25 12.34 64 42675 1575 32469212
Chronic myeloid leukaemia transformation 154.22 12.34 38 42701 147 32470640
Metastases to liver 151.62 12.34 130 42609 12802 32457985
Chronic myeloid leukaemia recurrent 149.58 12.34 37 42702 146 32470641
Gene mutation identification test positive 130.76 12.34 34 42705 171 32470616
Therapeutic response decreased 114.06 12.34 155 42584 25765 32445022
Recurrent cancer 105.83 12.34 45 42694 1199 32469588
Oedema 105.01 12.34 202 42537 44945 32425842
Chronic graft versus host disease 102.40 12.34 67 42672 4373 32466414
White blood cell count increased 98.45 12.34 187 42552 41215 32429572
Blast cell crisis 98.08 12.34 23 42716 68 32470719
Eyelid oedema 96.35 12.34 69 42670 5220 32465567
Hypotension 93.40 12.34 88 42651 216022 32254765
Muscle spasms 91.24 12.34 250 42489 70168 32400619
Drug abuse 88.51 12.34 4 42735 80239 32390548
Acute lymphocytic leukaemia 88.32 12.34 56 42683 3462 32467325
Neoplasm recurrence 87.30 12.34 46 42693 2001 32468786
Completed suicide 81.96 12.34 12 42727 92505 32378282
Neoplasm progression 81.14 12.34 114 42625 19544 32451243
Blast cells present 79.21 12.34 29 42710 513 32470274
Acute kidney injury 77.84 12.34 169 42570 293299 32177488
Overdose 77.82 12.34 11 42728 87066 32383721
Polymerase chain reaction positive 76.69 12.34 20 42719 102 32470685
Gastric antral vascular ectasia 76.42 12.34 25 42714 310 32470477
Therapy non-responder 74.56 12.34 145 42594 32509 32438278
Desmoid tumour 74.18 12.34 19 42720 89 32470698
Splenomegaly 68.93 12.34 90 42649 14387 32456400
Chordoma 67.63 12.34 12 42727 0 32470787
Necrotising panniculitis 67.45 12.34 15 42724 32 32470755
Face oedema 66.93 12.34 80 42659 11695 32459092
Graft versus host disease 62.38 12.34 74 42665 10732 32460055
Clonal evolution 61.12 12.34 17 42722 115 32470672
Scleroderma 60.81 12.34 32 42707 1388 32469399
Fluid retention 59.51 12.34 117 42622 26433 32444354
Acquired gene mutation 58.86 12.34 30 42709 1217 32469570
Fall 58.82 12.34 105 42634 196096 32274691
Product substitution issue 57.84 12.34 70 42669 10366 32460421
Blast cell count increased 56.55 12.34 28 42711 1067 32469720
Metastases to peritoneum 56.02 12.34 32 42707 1634 32469153
Prostate cancer 55.75 12.34 116 42623 27290 32443497
Bradycardia 55.42 12.34 13 42726 71549 32399238
Central nervous system leukaemia 51.17 12.34 18 42721 282 32470505
Confusional state 51.10 12.34 68 42671 143047 32327740
Off label use 50.68 12.34 219 42520 306101 32164686
Cytogenetic abnormality 50.15 12.34 24 42715 848 32469939
Disease progression 48.98 12.34 235 42504 86627 32384160
Myelofibrosis 47.94 12.34 29 42710 1648 32469139
Bone pain 47.23 12.34 91 42648 20253 32450534
Treatment failure 46.71 12.34 135 42604 39028 32431759
Accident 45.40 12.34 40 42699 4082 32466705
Bone marrow necrosis 45.07 12.34 14 42725 145 32470642
Hyperkalaemia 44.45 12.34 18 42721 69732 32401055
Central nervous system neoplasm 44.09 12.34 12 42727 74 32470713
Endocarditis noninfective 43.99 12.34 13 42726 112 32470675
Pituitary apoplexy 43.31 12.34 10 42729 27 32470760
Exposure via father 42.72 12.34 13 42726 125 32470662
Haemoglobin decreased 42.47 12.34 286 42453 119385 32351402
Bone marrow failure 42.41 12.34 111 42628 30293 32440494
Typhoid fever 42.29 12.34 10 42729 31 32470756
Chronic graft versus host disease in skin 42.11 12.34 21 42718 813 32469974
Thrombocytopenia 41.55 12.34 335 42404 147964 32322823
Somnolence 40.52 12.34 46 42693 103751 32367036
Intentional overdose 40.25 12.34 4 42735 41597 32429190
Pulmonary embolism 39.79 12.34 31 42708 83628 32387159
Tumour haemorrhage 39.23 12.34 31 42708 2720 32468067
Surgery 39.10 12.34 64 42675 12535 32458252
Platelet count decreased 38.37 12.34 270 42469 114321 32356466
Ascites 38.17 12.34 128 42611 40063 32430724
Hallucination 37.98 12.34 11 42728 52608 32418179
Tumour rupture 36.65 12.34 13 42726 209 32470578
Toxicity to various agents 36.08 12.34 117 42622 177924 32292863
Loss of therapeutic response 35.09 12.34 13 42726 238 32470549
Tumour necrosis 34.53 12.34 21 42718 1205 32469582
Colon cancer 34.49 12.34 50 42689 8816 32461971
Generalised oedema 34.22 12.34 60 42679 12423 32458364
Syncope 34.03 12.34 41 42698 90083 32380704
Nausea 33.28 12.34 599 42140 320250 32150537
Gastrectomy 32.81 12.34 11 42728 148 32470639
Drug hypersensitivity 32.68 12.34 29 42710 73371 32397416
Gastric cancer 32.65 12.34 38 42701 5399 32465388
Seizure 32.51 12.34 54 42685 103800 32366987
Pneumonia 32.37 12.34 305 42434 354947 32115840
Delirium 32.17 12.34 9 42730 44037 32426750
Cardiac arrest 31.54 12.34 49 42690 96727 32374060
Pulmonary aplasia 31.39 12.34 6 42733 3 32470784
Tuberculosis 30.76 12.34 47 42692 8682 32462105
Rhabdomyolysis 30.64 12.34 26 42713 67239 32403548
Inappropriate schedule of product administration 30.56 12.34 11 42728 45814 32424973
Dizziness 30.40 12.34 157 42582 209461 32261326
Eye swelling 30.22 12.34 49 42690 9523 32461264
Growth retardation 30.11 12.34 22 42717 1717 32469070
Pericardial effusion 30.08 12.34 82 42657 22920 32447867
Pemphigus 30.06 12.34 20 42719 1342 32469445
Deep vein thrombosis 29.80 12.34 24 42715 63689 32407098
Tumour excision 29.79 12.34 10 42729 135 32470652
Oral pigmentation 29.66 12.34 6 42733 6 32470781
Psoriasis 29.22 12.34 12 42727 46111 32424676
Chloroma 29.14 12.34 14 42725 499 32470288
Anxiety 29.06 12.34 51 42688 95954 32374833
Tremor 28.59 12.34 39 42700 81238 32389549
Demyelination 28.57 12.34 26 42713 2768 32468019
Loss of CAR T-cell persistence 28.22 12.34 7 42732 28 32470759
Renal tuberculosis 28.18 12.34 5 42734 0 32470787
Graft versus host disease in eye 27.82 12.34 11 42728 242 32470545
Flushing 27.63 12.34 4 42735 31123 32439664
Stem cell transplant 27.34 12.34 23 42716 2204 32468583
Oedema peripheral 27.33 12.34 249 42490 113842 32356945
Drug interaction 27.02 12.34 172 42567 218013 32252774
Pseudoporphyria 27.01 12.34 11 42728 262 32470525
Metabolic acidosis 26.75 12.34 10 42729 40689 32430098
Drug clearance decreased 26.42 12.34 19 42720 1446 32469341
Malaria 26.41 12.34 11 42728 278 32470509
Hyperhidrosis 26.21 12.34 33 42706 71135 32399652
Blindness 26.03 12.34 55 42684 13071 32457716
Optic neuritis 26.02 12.34 27 42712 3375 32467412
Blood lactate dehydrogenase increased 25.83 12.34 75 42664 21730 32449057
Plasma cell myeloma 25.36 12.34 23 42716 57591 32413196
Therapeutic product effect decreased 25.29 12.34 5 42734 31012 32439775
Metamyelocyte count increased 25.15 12.34 12 42727 421 32470366
Blood pressure increased 25.07 12.34 41 42698 79313 32391474
International normalised ratio increased 24.83 12.34 17 42722 49018 32421769
Haematotoxicity 24.61 12.34 37 42702 6739 32464048
Chronic obstructive pulmonary disease 24.55 12.34 17 42722 48736 32422051
Bone marrow disorder 24.33 12.34 19 42720 1639 32469148
Rash 23.87 12.34 397 42342 208936 32261851
Agitation 23.85 12.34 24 42715 57212 32413575
Post embolisation syndrome 23.22 12.34 7 42732 65 32470722
Bone marrow transplant 22.80 12.34 15 42724 988 32469799
Bone neoplasm 22.76 12.34 10 42729 289 32470498
Right ventricular diastolic collapse 22.76 12.34 7 42732 70 32470717
Cardio-respiratory arrest 22.73 12.34 24 42715 55965 32414822
Epistaxis 22.61 12.34 24 42715 55831 32414956
Dehydration 22.61 12.34 90 42649 128868 32341919
Spleen palpable 22.54 12.34 4 42735 0 32470787
Acute aortic syndrome 22.54 12.34 4 42735 0 32470787
Philadelphia chromosome negative 22.54 12.34 4 42735 0 32470787
Anaphylactic reaction 22.34 12.34 6 42733 30166 32440621
Aggression 22.25 12.34 12 42727 39377 32431410
Large intestine infection 22.21 12.34 17 42722 1423 32469364
Graft versus host disease in lung 22.03 12.34 12 42727 558 32470229
Urticaria 21.58 12.34 28 42711 59586 32411201
B-cell small lymphocytic lymphoma 21.57 12.34 8 42731 147 32470640
Pancytopenia 21.27 12.34 198 42541 91037 32379750
Arterial disorder 21.26 12.34 16 42723 1306 32469481
Philadelphia positive chronic myeloid leukaemia 21.24 12.34 7 42732 89 32470698
Ocular myasthenia 21.19 12.34 9 42730 239 32470548
Dengue fever 21.02 12.34 9 42730 244 32470543
Therapy partial responder 20.94 12.34 29 42710 4901 32465886
Suicidal ideation 20.94 12.34 12 42727 38071 32432716
Drug dependence 20.89 12.34 3 42736 23481 32447306
Condition aggravated 20.66 12.34 120 42619 155541 32315246
Rectosigmoid cancer 20.40 12.34 8 42731 172 32470615
Neoplasm 20.39 12.34 27 42712 4374 32466413
Complications of transplant surgery 20.33 12.34 11 42728 505 32470282
Myelocyte count increased 19.93 12.34 10 42729 392 32470395
Suicide attempt 19.71 12.34 13 42726 38231 32432556
Transformation to acute myeloid leukaemia 19.65 12.34 12 42727 694 32470093
Bone marrow oedema 19.45 12.34 11 42728 551 32470236
Peripheral arterial occlusive disease 19.08 12.34 30 42709 5679 32465108
Intentional product misuse 18.92 12.34 12 42727 36039 32434748
Tachycardia 18.90 12.34 48 42691 79040 32391747
Pericardial excision 18.89 12.34 4 42735 6 32470781
Multiple-drug resistance 18.80 12.34 24 42715 3751 32467036
Diaphragmatic disorder 18.75 12.34 14 42725 1129 32469658
Cytopenia 18.62 12.34 41 42698 10023 32460764
Mental status changes 18.48 12.34 14 42725 38323 32432464
Wheezing 18.38 12.34 13 42726 36861 32433926
Chest expansion decreased 18.32 12.34 7 42732 140 32470647
Acoustic neuroma 18.23 12.34 7 42732 142 32470645
Hyponatraemia 17.98 12.34 45 42694 74468 32396319
Concomitant disease aggravated 17.92 12.34 29 42710 5624 32465163
Lactic acidosis 17.83 12.34 11 42728 33525 32437262
Leukaemia 17.77 12.34 24 42715 3962 32466825
Asthma 17.76 12.34 19 42720 44046 32426741
Medication error 17.62 12.34 4 42735 22531 32448256
Platelet count increased 17.61 12.34 38 42701 9163 32461624
Neuropathy peripheral 17.43 12.34 48 42691 76934 32393853
Hepatic calcification 17.41 12.34 9 42730 376 32470411
Acinetobacter sepsis 17.36 12.34 5 42734 39 32470748
Marrow hyperplasia 17.30 12.34 13 42726 1059 32469728
Therapy change 17.28 12.34 20 42719 2825 32467962
Gelatinous transformation of the bone marrow 17.27 12.34 4 42735 11 32470776
Vomiting 17.21 12.34 418 42321 235139 32235648
Encephalopathy 17.17 12.34 12 42727 34245 32436542
Atrial fibrillation 17.11 12.34 87 42652 116617 32354170
Stress 17.11 12.34 5 42734 23777 32447010
Myeloproliferative neoplasm 17.04 12.34 10 42729 537 32470250
Adrenomegaly 16.94 12.34 9 42730 398 32470389
Pseudomyxoma peritonei 16.91 12.34 3 42736 0 32470787
Janus kinase 2 mutation 16.91 12.34 3 42736 0 32470787
Hepatic embolisation 16.91 12.34 3 42736 0 32470787
Cytoreductive surgery 16.91 12.34 3 42736 0 32470787
Hydrocele operation 16.91 12.34 3 42736 0 32470787
Drug reaction with eosinophilia and systemic symptoms 16.79 12.34 11 42728 32474 32438313
Abscess drainage 16.79 12.34 8 42731 280 32470507
Paternal exposure during pregnancy 16.77 12.34 4 42735 13 32470774
Anaemia 16.69 12.34 398 42341 223226 32247561
Costal cartilage fracture 16.53 12.34 8 42731 290 32470497
Blood pressure decreased 16.50 12.34 26 42713 51054 32419733
Coma 16.49 12.34 19 42720 42593 32428194
Product dose omission issue 16.48 12.34 74 42665 102501 32368286
Constipation 16.46 12.34 98 42641 126275 32344512
Periorbital swelling 16.35 12.34 8 42731 297 32470490
Essential thrombocythaemia 16.26 12.34 5 42734 50 32470737
Biopsy bone marrow abnormal 16.23 12.34 8 42731 302 32470485
Lung neoplasm malignant 16.19 12.34 52 42687 15911 32454876
Intentional product use issue 16.14 12.34 19 42720 42192 32428595
Pigmentation disorder 15.93 12.34 17 42722 2195 32468592
Cellulitis 15.82 12.34 26 42713 50204 32420583
Insomnia 15.76 12.34 73 42666 100275 32370512
Growth failure 15.67 12.34 5 42734 57 32470730
Colitis 15.61 12.34 13 42726 33938 32436849
Trisomy 8 15.36 12.34 5 42734 61 32470726
Lactose intolerance 15.11 12.34 13 42726 1285 32469502
Thrombosis 15.05 12.34 23 42716 45731 32425056
Intestinal congestion 14.94 12.34 4 42735 23 32470764
Bladder cancer 14.87 12.34 38 42701 10218 32460569
Metastases to bladder 14.86 12.34 5 42734 68 32470719
Bence Jones proteinuria 14.83 12.34 3 42736 3 32470784
Metastases to heart 14.58 12.34 6 42733 147 32470640
Hypereosinophilic syndrome 14.53 12.34 7 42732 251 32470536
Parakeratosis 14.46 12.34 6 42733 150 32470637
Product prescribing error 14.45 12.34 4 42735 19713 32451074
Angioedema 14.24 12.34 16 42723 36273 32434514
Disease recurrence 14.23 12.34 50 42689 16014 32454773
Lacrimation increased 14.14 12.34 31 42708 7553 32463234
Hyperchromic anaemia 14.14 12.34 4 42735 29 32470758
Product use in unapproved indication 14.14 12.34 176 42563 87028 32383759
Unevaluable event 14.08 12.34 14 42725 33572 32437215
Loss of personal independence in daily activities 13.99 12.34 9 42730 26824 32443963
Aspiration bone marrow 13.62 12.34 3 42736 6 32470781
Clear cell sarcoma of soft tissue 13.62 12.34 3 42736 6 32470781
Gastric neoplasm 13.47 12.34 5 42734 92 32470695
Leukostasis syndrome 13.38 12.34 4 42735 36 32470751
Therapy responder 13.32 12.34 6 42733 184 32470603
Metastasis 13.32 12.34 20 42719 3637 32467150
Pneumonia aspiration 13.24 12.34 21 42718 41135 32429652
Oropharyngeal pain 13.22 12.34 13 42726 31339 32439448
Ejection fraction decreased 13.16 12.34 52 42687 17606 32453181
Bladder neoplasm surgery 13.09 12.34 4 42735 39 32470748
Blast cell proliferation 13.02 12.34 3 42736 8 32470779
Transitional cell carcinoma 13.00 12.34 15 42724 2112 32468675
Hypoglycaemia 12.99 12.34 33 42706 54349 32416438
Cancer surgery 12.88 12.34 8 42731 477 32470310
Hypertension 12.85 12.34 111 42628 131639 32339148
Orthostatic hypotension 12.84 12.34 9 42730 25641 32445146
Bone development abnormal 12.83 12.34 4 42735 42 32470745
Ventricular tachycardia 12.75 12.34 9 42730 25547 32445240
Chills 12.74 12.34 56 42683 78028 32392759
Musculoskeletal stiffness 12.66 12.34 20 42719 39244 32431543
Drug-induced liver injury 12.64 12.34 8 42731 24055 32446732
Laryngeal cancer stage III 12.52 12.34 3 42736 10 32470777
Breast oedema 12.52 12.34 3 42736 10 32470777
Hyperkeratosis 12.51 12.34 19 42720 3490 32467297
Erythropoiesis abnormal 12.48 12.34 6 42733 214 32470573
Conjunctival haemorrhage 12.44 12.34 17 42722 2838 32467949
Heart rate decreased 12.41 12.34 9 42730 25191 32445596
Skin neoplasm excision 12.35 12.34 7 42732 352 32470435

Pharmacologic Action:

SourceCodeDescription
ATC L01EA01 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
BCR-ABL tyrosine kinase inhibitors
FDA MoA N0000020009 Bcr-Abl Tyrosine Kinase Inhibitors
MeSH PA D000970 Antineoplastic Agents
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 N0000182141 Cytochrome P450 3A4 Inhibitors
CHEBI has role CHEBI:35610 cytostatic
CHEBI has role CHEBI:38637 protein tyrosine kinase inhibitor
CHEBI has role CHEBI:68495 Type I programmed cell-death inducer
CHEBI has role CHEBI:149553 anti-coronaviral agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Dermatofibrosarcoma protuberans indication 276799004
Systemic mast cell disease indication 397016004 DOID:349
Blastic phase chronic myeloid leukemia indication 413656006
Chronic eosinophilic leukemia indication 413836008
Chronic phase chronic myeloid leukemia indication 413847001
Gastrointestinal stromal tumor indication 420120006 DOID:9253
Idiopathic hypereosinophilic syndrome indication 423294001
Philadelphia chromosome-positive acute lymphoblastic leukemia indication 425688002
Philadelphia Chromosome Positive Chronic Myelocytic Leukemia indication 449108003
Myelodysplastic/myeloproliferative diseases with re-arrangements of the gene for platelet-derived growth factor receptor (PDGFR) indication 738527001
Chronic Myelocytic Leukemia Accelerated Phase indication
Heart valve disorder contraindication 368009 DOID:4079
Cerebral edema contraindication 2032001
Hypophosphatemia contraindication 4996001
Congenital heart disease contraindication 13213009
Hyperbilirubinemia contraindication 14783006 DOID:2741
Pulmonary edema contraindication 19242006 DOID:11396
Hypertensive disorder contraindication 38341003 DOID:10763
Body fluid retention contraindication 43498006
Chronic heart failure contraindication 48447003
Myocarditis contraindication 50920009 DOID:820
Gastrointestinal perforation contraindication 51875005
Hepatic failure contraindication 59927004
Diabetes mellitus contraindication 73211009 DOID:9351
Gastrointestinal hemorrhage contraindication 74474003
Left heart failure contraindication 85232009
Cardiogenic shock contraindication 89138009
Kidney disease contraindication 90708001 DOID:557
Bleeding contraindication 131148009
Liver function tests abnormal contraindication 166603001
Disease of liver contraindication 235856003 DOID:409
Edema contraindication 267038008
Anemia contraindication 271737000 DOID:2355
Pregnancy, function contraindication 289908002
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Neutropenic disorder contraindication 303011007 DOID:1227
Pericardial effusion contraindication 373945007 DOID:118
Purpuric disorder contraindication 387778001
Ascites contraindication 389026000
Breastfeeding (mother) contraindication 413712001
Disorder of coronary artery contraindication 414024009
Obesity contraindication 414916001 DOID:9970
Pleural Effusions contraindication
Chronic Heart Failure Following Myocardial Infarction contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.96 acidic
pKa2 8.49 Basic
pKa3 4.34 Basic
pKa4 3.73 Basic
pKa5 2.2 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Mast/stem cell growth factor receptor Kit Kinase INHIBITOR Kd 7.89 CHEMBL CHEMBL
Platelet-derived growth factor receptor beta Kinase INHIBITOR Kd 7.85 CHEMBL CHEMBL
Tyrosine-protein kinase ABL1 Kinase INHIBITOR Kd 8.96 CHEMBL CHEMBL
Histamine H2 receptor GPCR Ki 5.71 DRUG MATRIX
Carbonic anhydrase 2 Enzyme Ki 7.52 CHEMBL
Multidrug resistance-associated protein 1 Transporter WOMBAT-PK
ATP-binding cassette sub-family G member 2 Transporter IC50 5.47 CHEMBL
Carbonic anhydrase 1 Enzyme Ki 7.50 CHEMBL
Carbonic anhydrase 4 Enzyme Ki 5.34 CHEMBL
Ribosyldihydronicotinamide dehydrogenase [quinone] Enzyme IC50 6.40 CHEMBL
Carbonic anhydrase 9 Enzyme Ki 7.12 CHEMBL
Carbonic anhydrase 12 Enzyme Ki 6.01 CHEMBL
Epidermal growth factor receptor Kinase Kd 5.12 CHEMBL
Carbonic anhydrase 5A, mitochondrial Enzyme Ki 4.69 CHEMBL
Carbonic anhydrase 5B, mitochondrial Enzyme Ki 4.77 CHEMBL
Carbonic anhydrase 7 Enzyme Ki 6.96 CHEMBL
Proto-oncogene tyrosine-protein kinase Src Kinase Ki 4.51 CHEMBL
Tyrosine-protein kinase Lck Kinase Kd 7.40 CHEMBL
Tyrosine-protein kinase Fyn Kinase Kd 5.51 CHEMBL
RAF proto-oncogene serine/threonine-protein kinase Kinase Kd 5.77 CHEMBL
Serine/threonine-protein kinase B-raf Kinase Kd 5.48 CHEMBL
Receptor-type tyrosine-protein kinase FLT3 Kinase Kd 5.20 CHEMBL
Vascular endothelial growth factor receptor 2 Kinase IC50 4.59 CHEMBL
Macrophage colony-stimulating factor 1 receptor Kinase Kd 7.96 CHEMBL
Platelet-derived growth factor receptor alpha Kinase Kd 7.51 CHEMBL
Insulin receptor Kinase AGONIST Ki 5 PDSP
Thromboxane-A synthase Enzyme IC50 6.70 DRUG MATRIX
Mitogen-activated protein kinase 8 Kinase Kd 5.49 CHEMBL
Carbonic anhydrase 3 Enzyme Ki 6.28 CHEMBL
Carbonic anhydrase 6 Enzyme Ki 6.41 CHEMBL
Mitogen-activated protein kinase 10 Kinase Kd 5.51 CHEMBL
Tyrosine-protein kinase JAK2 Kinase Ki 5 PDSP
Tyrosine-protein kinase SYK Kinase IC50 5.30 CHEMBL
Ephrin type-A receptor 8 Kinase Kd 5.85 CHEMBL
Tyrosine-protein kinase Lyn Kinase Kd 6.05 CHEMBL
Cytoplasmic tyrosine-protein kinase BMX Kinase Ki 5 PDSP
Carbonic anhydrase 14 Enzyme Ki 6.33 CHEMBL
Fibroblast growth factor receptor 1 Kinase Ki 5 PDSP
Serine/threonine-protein kinase PLK4 Kinase Kd 5.11 CHEMBL
Abelson tyrosine-protein kinase 2 Kinase Kd 8.22 CHEMBL
Fibroblast growth factor receptor 2 Kinase Ki 5 PDSP
Serine/threonine-protein kinase 17A Kinase Kd 5.55 CHEMBL
Tyrosine-protein kinase Fgr Kinase Kd 5.62 CHEMBL
Mitogen-activated protein kinase 14 Kinase IC50 4.86 CHEMBL
Tyrosine-protein kinase FRK Kinase Kd 5.82 CHEMBL
Dual specificity protein kinase CLK1 Kinase Kd 5.35 CHEMBL
Cyclin-G-associated kinase Kinase Kd 6 CHEMBL
Ephrin type-B receptor 1 Kinase Ki 5 PDSP
Dual specificity protein kinase CLK4 Kinase Kd 5.68 CHEMBL
Mitogen-activated protein kinase 9 Kinase Kd 5.28 CHEMBL
Epithelial discoidin domain-containing receptor 1 Kinase Kd 9.15 CHEMBL
Ephrin type-B receptor 4 Kinase Ki 5 PDSP
Lysine--tRNA ligase Enzyme Ki 5.30 CHEMBL
Non-receptor tyrosine-protein kinase TYK2 Kinase Kd 5.06 CHEMBL
Mitogen-activated protein kinase kinase kinase MLT Kinase Kd 5.59 CHEMBL
Casein kinase II subunit alpha' Kinase Kd 5.42 CHEMBL
Maternal embryonic leucine zipper kinase Kinase Kd 5.72 CHEMBL
Serine/threonine-protein kinase TNNI3K Kinase Kd 5.37 CHEMBL
Discoidin domain-containing receptor 2 Kinase Kd 7.82 CHEMBL
Tyrosine-protein kinase Blk Kinase Kd 6.28 CHEMBL
Cyclin-dependent kinase 19 Kinase Kd 5.26 CHEMBL
Homeodomain-interacting protein kinase 4 Kinase Kd 6.02 CHEMBL
Interleukin-1 receptor-associated kinase 1 Kinase Kd 5.92 CHEMBL
Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma Kinase Kd 6.42 CHEMBL
Solute carrier family 22 member 2 Transporter IC50 5.38 CHEMBL
Multidrug and toxin extrusion protein 1 Transporter IC50 7.40 CHEMBL
Multidrug and toxin extrusion protein 2 Transporter IC50 6.46 CHEMBL
Solute carrier family 22 member 3 Transporter IC50 4.59 CHEMBL
Platelet-derived growth factor receptor Kinase IC50 7.30 CHEMBL
Tyrosine-protein kinase ABL Kinase IC50 7.40 CHEMBL
Bcr/Abl fusion protein Kinase Ki 7.85 CHEMBL
Multidrug resistance protein 1 Transporter IC50 5.14 CHEMBL
ATP-dependent RNA helicase DDX3X Enzyme Kd 6.36 CHEMBL
Sodium-dependent serotonin transporter Transporter Ki 6.13 DRUG MATRIX
5-hydroxytryptamine receptor 2A GPCR Ki 6.27 DRUG MATRIX
Carbonic anhydrase 13 Enzyme Ki 5.13 CHEMBL
Carbonic anhydrase 15 Enzyme Ki 7.11 CHEMBL
Proto-oncogene tyrosine-protein kinase Src Kinase IC50 5.56 CHEMBL
Tyrosine-protein kinase ABL1 Kinase IC50 7.97 CHEMBL
Platelet-derived growth factor receptor beta Kinase IC50 6.79 CHEMBL

External reference:

IDSource
4021257 VUID
N0000148698 NUI
D01441 KEGG_DRUG
220127-57-1 SECONDARY_CAS_RN
4021257 VANDF
4021258 VANDF
C0939537 UMLSCUI
CHEBI:45783 CHEBI
STI PDB_CHEM_ID
CHEMBL941 ChEMBL_ID
CHEMBL1642 ChEMBL_ID
D000068877 MESH_DESCRIPTOR_UI
DB00619 DRUGBANK_ID
5687 IUPHAR_LIGAND_ID
8031 INN_ID
BKJ8M8G5HI UNII
5291 PUBCHEM_CID
282386 RXNORM
16030 MMSL
238904 MMSL
41395 MMSL
d04758 MMSL
009151 NDDF
009152 NDDF
129558005 SNOMEDCT_US
391634008 SNOMEDCT_US
414460008 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 0054-0248 TABLET, FILM COATED 100 mg ORAL ANDA 26 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 0054-0249 TABLET, FILM COATED 400 mg ORAL ANDA 26 sections
Gleevec HUMAN PRESCRIPTION DRUG LABEL 1 0078-0401 TABLET 100 mg ORAL NDA 32 sections
Gleevec HUMAN PRESCRIPTION DRUG LABEL 1 0078-0649 TABLET 400 mg ORAL NDA 32 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 0093-7629 TABLET, FILM COATED 100 mg ORAL ANDA 28 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 0093-7630 TABLET, FILM COATED 400 mg ORAL ANDA 28 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 0378-2245 TABLET, FILM COATED 100 mg ORAL ANDA 28 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 0378-2246 TABLET, FILM COATED 400 mg ORAL ANDA 28 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 0904-6621 TABLET, FILM COATED 400 mg ORAL ANDA 26 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 0904-6901 TABLET, FILM COATED 100 mg ORAL ANDA 26 sections
imatinib mesylate Human Prescription Drug Label 1 16714-704 TABLET, FILM COATED 100 mg ORAL ANDA 29 sections
imatinib mesylate Human Prescription Drug Label 1 16714-705 TABLET, FILM COATED 400 mg ORAL ANDA 29 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 42292-043 TABLET, FILM COATED 100 mg ORAL ANDA 28 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 42292-044 TABLET, FILM COATED 400 mg ORAL ANDA 28 sections
Imatinib HUMAN PRESCRIPTION DRUG LABEL 1 43598-344 TABLET 100 mg ORAL ANDA 26 sections
Imatinib HUMAN PRESCRIPTION DRUG LABEL 1 43598-345 TABLET 400 mg ORAL ANDA 26 sections
imatinib mesylate Human Prescription Drug Label 1 47335-472 TABLET, FILM COATED 100 mg ORAL ANDA 28 sections
imatinib mesylate Human Prescription Drug Label 1 47335-475 TABLET, FILM COATED 400 mg ORAL ANDA 28 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 50268-426 TABLET, FILM COATED 100 mg ORAL ANDA 26 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 50268-427 TABLET, FILM COATED 400 mg ORAL ANDA 26 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 51407-269 TABLET, FILM COATED 100 mg ORAL ANDA 28 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 51407-270 TABLET, FILM COATED 400 mg ORAL ANDA 28 sections
IMATINIB MESYLATE HUMAN PRESCRIPTION DRUG LABEL 1 51991-376 TABLET, COATED 100 mg ORAL ANDA 33 sections
IMATINIB MESYLATE HUMAN PRESCRIPTION DRUG LABEL 1 51991-377 TABLET, COATED 400 mg ORAL ANDA 33 sections
Imatinib Mesylate Human Prescription Drug Label 1 59651-240 TABLET, FILM COATED 100 mg ORAL ANDA 28 sections
Imatinib Mesylate Human Prescription Drug Label 1 59651-241 TABLET, FILM COATED 400 mg ORAL ANDA 28 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 59923-723 TABLET, COATED 100 mg ORAL ANDA 32 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 59923-724 TABLET, COATED 400 mg ORAL ANDA 32 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 60505-2900 TABLET, FILM COATED 100 mg ORAL ANDA 26 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 60505-2901 TABLET, FILM COATED 400 mg ORAL ANDA 26 sections