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:

None

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
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
Nausea 905.67 27.31 522 5259 111667 2240637
Death 862.10 27.31 454 5327 81014 2271290
Diarrhoea 700.72 27.31 400 5381 83164 2269140
Chronic myeloid leukaemia 643.81 27.31 119 5662 467 2351837
Rash 638.73 27.31 336 5445 59222 2293082
Malignant neoplasm progression 616.49 27.31 208 5573 11920 2340384
Vomiting 605.00 27.31 345 5436 71257 2281047
Neoplasm malignant 582.73 27.31 163 5618 4930 2347374
Gastrointestinal stromal tumour 573.28 27.31 97 5684 192 2352112
Anaemia 549.59 27.31 256 5525 34536 2317768
Blast crisis in myelogenous leukaemia 545.07 27.31 85 5696 68 2352236
Drug resistance 505.72 27.31 127 5654 2497 2349807
Oedema peripheral 473.81 27.31 206 5575 23557 2328747
Pleural effusion 464.81 27.31 167 5614 11501 2340803
Muscle spasms 452.93 27.31 194 5587 21372 2330932
Fatigue 420.32 27.31 292 5489 84581 2267723
Periorbital oedema 400.90 27.31 88 5693 930 2351374
Dyspnoea 378.01 27.31 266 5515 78467 2273837
Pyrexia 376.10 27.31 230 5551 53478 2298826
Fluid retention 365.81 27.31 123 5658 6923 2345381
Second primary malignancy 363.23 27.31 81 5700 925 2351379
Pancytopenia 342.72 27.31 133 5648 11319 2340985
Oedema 328.52 27.31 125 5656 10078 2342226
Haemoglobin decreased 321.40 27.31 145 5636 18006 2334298
Thrombocytopenia 320.38 27.31 147 5634 18984 2333320
Exposure during pregnancy 284.65 27.31 148 5633 25071 2327233
Eye swelling 281.63 27.31 90 5691 4300 2348004
Gene mutation identification test positive 279.90 27.31 43 5738 27 2352277
Drug intolerance 276.22 27.31 120 5661 13597 2338707
Disease progression 275.61 27.31 128 5653 16967 2335337
White blood cell count decreased 267.90 27.31 128 5653 18080 2334224
Neutropenia 261.99 27.31 133 5648 21415 2330889
Drug ineffective 233.52 27.31 224 5557 101400 2250904
Asthenia 227.48 27.31 160 5621 46766 2305538
Cytogenetic analysis abnormal 226.18 27.31 38 5743 70 2352234
Leukaemia recurrent 224.88 27.31 43 5738 209 2352095
Abdominal pain 221.52 27.31 140 5641 34234 2318070
Bone marrow failure 220.74 27.31 80 5701 5606 2346698
Malaise 216.35 27.31 166 5615 55419 2296885
Chromosome analysis abnormal 215.83 27.31 34 5747 31 2352273
Platelet count decreased 196.08 27.31 99 5682 15714 2336590
Pneumonia 191.20 27.31 147 5634 49149 2303155
Swelling face 177.79 27.31 79 5702 9414 2342890
Blood creatinine increased 176.17 27.31 81 5700 10452 2341852
Metastases to liver 175.06 27.31 57 5724 2884 2349420
Ascites 173.99 27.31 67 5714 5553 2346751
Eyelid oedema 173.10 27.31 55 5726 2571 2349733
Pericardial effusion 172.89 27.31 61 5720 3948 2348356
Neoplasm progression 171.19 27.31 63 5718 4605 2347699
Generalised oedema 169.49 27.31 53 5728 2350 2349954
Leukopenia 169.24 27.31 78 5703 10118 2342186
Normal newborn 168.56 27.31 46 5735 1254 2351050
Abdominal pain upper 167.64 27.31 100 5681 22000 2330304
Headache 159.98 27.31 164 5617 80015 2272289
Face oedema 158.61 27.31 57 5724 3891 2348413
Acute lymphocytic leukaemia recurrent 155.20 27.31 31 5750 196 2352108
Myalgia 155.00 27.31 97 5684 23236 2329068
White blood cell count increased 152.37 27.31 65 5716 7013 2345291
Hepatotoxicity 150.21 27.31 53 5728 3428 2348876
Aspartate aminotransferase increased 147.65 27.31 76 5705 12536 2339768
Pruritus 145.87 27.31 119 5662 43221 2309083
Alanine aminotransferase increased 145.61 27.31 78 5703 13954 2338350
Decreased appetite 143.10 27.31 100 5681 28791 2323513
Gastric antral vascular ectasia 142.14 27.31 26 5755 94 2352210
Weight increased 138.69 27.31 89 5692 22248 2330056
Blister 135.29 27.31 59 5722 6712 2345592
Therapeutic response decreased 135.06 27.31 60 5721 7135 2345169
Weight decreased 128.48 27.31 93 5688 28278 2324026
Bone pain 125.26 27.31 61 5720 8935 2343369
Haematocrit decreased 124.83 27.31 49 5732 4269 2348035
General physical health deterioration 120.35 27.31 69 5712 14070 2338234
Jaundice 119.89 27.31 51 5730 5457 2346847
Blood alkaline phosphatase increased 117.78 27.31 53 5728 6492 2345812
Pain in extremity 116.85 27.31 104 5677 42436 2309868
Cough 115.68 27.31 93 5688 33024 2319280
Alopecia 115.56 27.31 79 5702 21922 2330382
Surgery 113.07 27.31 49 5732 5486 2346818
Blood lactate dehydrogenase increased 109.44 27.31 42 5739 3442 2348862
Maternal exposure during pregnancy 109.32 27.31 66 5715 14797 2337507
Sepsis 108.16 27.31 71 5710 18417 2333887
Red blood cell count decreased 108.00 27.31 44 5737 4222 2348082
Arthralgia 107.89 27.31 111 5670 54174 2298130
Platelet count increased 107.82 27.31 37 5744 2200 2350104
Splenomegaly 104.31 27.31 33 5748 1518 2350786
Right ventricular failure 103.37 27.31 36 5745 2237 2350067
Philadelphia chromosome positive 102.74 27.31 17 5764 27 2352277
Leukocytosis 101.31 27.31 40 5741 3536 2348768
Therapy non-responder 101.07 27.31 51 5730 8053 2344251
Dehydration 100.67 27.31 73 5708 22222 2330082
Abdominal distension 99.95 27.31 55 5726 10356 2341948
Breast cancer 99.05 27.31 53 5728 9442 2342862
Gastrointestinal haemorrhage 98.68 27.31 58 5723 12377 2339927
Swelling 98.58 27.31 64 5717 16286 2336018
Abortion spontaneous 97.05 27.31 59 5722 13386 2338918
Pain 95.91 27.31 111 5670 61746 2290558
Abdominal discomfort 94.76 27.31 64 5717 17392 2334912
Treatment failure 94.52 27.31 47 5734 7192 2345112
Respiratory failure 94.16 27.31 58 5723 13470 2338834
Graft versus host disease 92.79 27.31 27 5754 932 2351372
Dry skin 92.24 27.31 45 5736 6607 2345697
Chronic graft versus host disease 90.59 27.31 22 5759 371 2351933
Conjunctival haemorrhage 90.11 27.31 24 5757 594 2351710
Growth retardation 89.06 27.31 20 5761 235 2352069
Haematotoxicity 87.56 27.31 27 5754 1140 2351164
Blood bilirubin increased 85.83 27.31 40 5741 5305 2346999
Acute lymphocytic leukaemia 85.77 27.31 22 5759 468 2351836
Renal failure 85.65 27.31 60 5721 17289 2335015
Cardiac failure congestive 84.92 27.31 58 5723 16043 2336261
Recurrent cancer 83.57 27.31 20 5761 316 2351988
Eye haemorrhage 83.43 27.31 27 5754 1336 2350968
Pseudoporphyria 82.93 27.31 15 5766 50 2352254
Metastases to peritoneum 82.30 27.31 21 5760 437 2351867
Hepatitis 82.30 27.31 41 5740 6296 2346008
Exposure via body fluid 82.00 27.31 19 5762 259 2352045
Thrombocytosis 80.49 27.31 24 5757 903 2351401
Drug interaction 79.37 27.31 71 5710 29092 2323212
Febrile neutropenia 79.15 27.31 48 5733 10834 2341470
Neoplasm recurrence 78.90 27.31 20 5761 405 2351899
Ejection fraction decreased 78.17 27.31 31 5750 2770 2349534
Lacrimation increased 77.86 27.31 31 5750 2799 2349505
Erythema 75.98 27.31 65 5716 25094 2327210
Product use in unapproved indication 75.33 27.31 47 5734 11153 2341151
Gamma-glutamyltransferase increased 75.23 27.31 37 5744 5525 2346779
Chronic myeloid leukaemia transformation 74.22 27.31 13 5768 34 2352270
Gastrooesophageal reflux disease 73.65 27.31 43 5738 9052 2343252
Lung infiltration 73.62 27.31 28 5753 2236 2350068
Chest pain 73.60 27.31 67 5714 28070 2324234
Liver function test abnormal 73.05 27.31 40 5741 7450 2344854
Hepatic failure 71.49 27.31 36 5745 5653 2346651
Interstitial lung disease 71.48 27.31 40 5741 7772 2344532
Septic shock 69.70 27.31 38 5743 7016 2345288
Constipation 69.65 27.31 58 5723 21571 2330733
Renal impairment 69.51 27.31 43 5738 10049 2342255
Cardiotoxicity 69.45 27.31 23 5758 1224 2351080
Drug level increased 67.98 27.31 28 5753 2759 2349545
Caesarean section 66.94 27.31 31 5750 4050 2348254
Neutrophil count decreased 66.62 27.31 36 5745 6531 2345773
Gastrointestinal disorder 66.56 27.31 40 5741 8877 2343427
Visual impairment 65.91 27.31 44 5737 11711 2340593
Infection 65.76 27.31 52 5729 17977 2334327
Acute myeloid leukaemia 65.33 27.31 27 5754 2683 2349621
Skin exfoliation 65.11 27.31 34 5747 5756 2346548
Blood urea increased 64.20 27.31 29 5752 3576 2348728
Blood creatine phosphokinase increased 63.07 27.31 32 5749 5104 2347200
Disseminated intravascular coagulation 63.02 27.31 28 5753 3322 2348982
C-reactive protein increased 62.64 27.31 34 5747 6221 2346083
Mucosal inflammation 62.55 27.31 32 5749 5192 2347112
Cardiac failure 62.40 27.31 43 5738 12051 2340253
Acute kidney injury 62.13 27.31 61 5720 28061 2324243
Eye oedema 61.73 27.31 16 5765 355 2351949
Cerebrovascular accident 60.61 27.31 52 5729 20134 2332170
Transaminases increased 60.50 27.31 30 5751 4557 2347747
Joint swelling 60.24 27.31 48 5733 16771 2335533
Lung disorder 60.09 27.31 33 5748 6179 2346125
Myelodysplastic syndrome 60.00 27.31 25 5756 2535 2349769
Gait disturbance 59.55 27.31 54 5727 22491 2329813
Chills 59.18 27.31 46 5735 15506 2336798
Abortion induced 59.17 27.31 27 5754 3409 2348895
Liver disorder 59.10 27.31 33 5748 6381 2345923
Depression 58.41 27.31 59 5722 28073 2324231
Leukaemia 58.04 27.31 18 5763 774 2351530
Left ventricular dysfunction 57.76 27.31 20 5761 1220 2351084
Eosinophilia 56.43 27.31 25 5756 2945 2349359
Bone marrow transplant 56.04 27.31 13 5768 178 2352126
Pulmonary oedema 54.86 27.31 33 5748 7330 2344974
Hypoaesthesia 54.52 27.31 49 5732 20166 2332138
Computerised tomogram abnormal 54.07 27.31 15 5766 434 2351870
Cytogenetic abnormality 53.43 27.31 12 5769 141 2352163
Dyspepsia 53.15 27.31 36 5745 9808 2342496
Dizziness 53.14 27.31 81 5700 58584 2293720
Neuropathy peripheral 52.83 27.31 38 5743 11394 2340910
Atelectasis 52.23 27.31 21 5760 1944 2350360
Hepatic necrosis 52.07 27.31 18 5763 1092 2351212
Tumour excision 51.84 27.31 11 5770 97 2352207
Chronic myeloid leukaemia recurrent 51.82 27.31 9 5772 22 2352282
Hypersensitivity 51.77 27.31 51 5730 23542 2328762
Premature labour 50.82 27.31 21 5760 2085 2350219
Peripheral swelling 50.12 27.31 44 5737 17553 2334751
Acute graft versus host disease 49.73 27.31 15 5766 587 2351717
Papilloedema 49.44 27.31 16 5765 791 2351513
Flatulence 49.24 27.31 26 5755 4499 2347805
Back pain 49.23 27.31 57 5724 31602 2320702
Blood test abnormal 49.05 27.31 18 5763 1300 2351004
Ocular hyperaemia 49.00 27.31 25 5756 4031 2348273
Respiratory distress 48.92 27.31 27 5754 5102 2347202
Exposure via father 48.88 27.31 12 5769 212 2352092
Multiple organ dysfunction syndrome 48.69 27.31 31 5750 7610 2344694
Palpitations 48.59 27.31 42 5739 16414 2335890
Blast cells present 48.44 27.31 10 5771 76 2352228
Premature baby 48.41 27.31 23 5758 3181 2349123
Musculoskeletal pain 47.76 27.31 35 5746 10795 2341509
Hepatomegaly 46.93 27.31 19 5762 1790 2350514
Hypoxia 46.63 27.31 28 5753 6199 2346105
Dyspnoea exertional 46.17 27.31 27 5754 5693 2346611
Hypokalaemia 46.01 27.31 34 5747 10620 2341684
Ankle brachial index decreased 45.79 27.31 7 5774 4 2352300
Pulse waveform abnormal 45.79 27.31 7 5774 4 2352300
Pneumatosis intestinalis 45.79 27.31 13 5768 410 2351894
Rash erythematous 45.08 27.31 27 5754 5949 2346355
Hepatic function abnormal 44.60 27.31 27 5754 6065 2346239
Insomnia 44.46 27.31 49 5732 25738 2326566
Toxicity to various agents 44.40 27.31 55 5726 32699 2319605
Metastases to lung 44.28 27.31 18 5763 1713 2350591
Chloroma 44.25 27.31 9 5772 63 2352241
Neoplasm 43.98 27.31 16 5765 1127 2351177
Myelofibrosis 43.98 27.31 12 5769 326 2351978
Condition aggravated 43.83 27.31 54 5727 31925 2320379
Carotid intima-media thickness increased 43.62 27.31 7 5774 8 2352296
Myocardial infarction 43.38 27.31 42 5739 18971 2333333
Colitis 43.06 27.31 25 5756 5201 2347103
Subdural haematoma 42.97 27.31 19 5762 2227 2350077
Blindness 42.84 27.31 22 5759 3596 2348708
Stem cell transplant 42.52 27.31 12 5769 370 2351934
Bronchopulmonary aspergillosis 42.19 27.31 15 5766 989 2351315
Morphoea 42.15 27.31 9 5772 82 2352222
Aspiration pleural cavity 42.08 27.31 10 5771 153 2352151
Tumour necrosis 40.66 27.31 10 5771 178 2352126
Cardiac output decreased 40.60 27.31 10 5771 179 2352125
Skin fragility 40.45 27.31 9 5772 101 2352203
Feeling abnormal 39.25 27.31 44 5737 23537 2328767
Eye pain 39.25 27.31 23 5758 4868 2347436
Urine odour abnormal 38.87 27.31 13 5768 713 2351591
Tumour haemorrhage 38.86 27.31 11 5770 343 2351961
Blood blister 38.68 27.31 11 5770 349 2351955
Hypothyroidism 38.53 27.31 22 5759 4435 2347869
Lymphadenopathy 38.51 27.31 24 5757 5674 2346630
Bronchitis 38.46 27.31 34 5747 13680 2338624
Vision blurred 38.44 27.31 35 5746 14633 2337671
Hypoacusis 38.17 27.31 20 5761 3405 2348899
Glaucoma 37.76 27.31 17 5764 2078 2350226
Tumour lysis syndrome 37.50 27.31 14 5767 1061 2351243
Skin disorder 37.08 27.31 20 5761 3611 2348693
Blood albumin decreased 36.98 27.31 16 5765 1779 2350525
Acute hepatic failure 36.98 27.31 18 5763 2624 2349680
Dysphagia 36.41 27.31 32 5749 12773 2339531
Atrial fibrillation 36.36 27.31 33 5748 13735 2338569
Photophobia 36.32 27.31 17 5764 2272 2350032
Blood uric acid increased 36.04 27.31 12 5769 649 2351655
Gene mutation 35.94 27.31 9 5772 173 2352131
Renal disorder 35.73 27.31 21 5760 4467 2347837
Exposure via partner 35.69 27.31 8 5773 93 2352211
Gastric cancer 35.62 27.31 12 5769 673 2351631
Blood glucose increased 35.52 27.31 31 5750 12259 2340045
Aplasia 35.40 27.31 11 5770 476 2351828
Hepatic enzyme increased 35.13 27.31 28 5753 9774 2342530
Cytopenia 34.68 27.31 13 5768 996 2351308
Mitral valve incompetence 34.57 27.31 17 5764 2533 2349771
Fall 34.37 27.31 59 5722 47040 2305264
Dialysis 34.09 27.31 16 5765 2151 2350153
Parosmia 33.72 27.31 12 5769 793 2351511
Uterine cancer 33.45 27.31 12 5769 812 2351492
Product substitution issue 33.37 27.31 21 5760 5048 2347256
Peripheral arterial occlusive disease 33.34 27.31 11 5770 578 2351726
Gastrectomy 33.32 27.31 8 5773 128 2352176
Dermatitis bullous 32.94 27.31 14 5767 1490 2350814
Thrombosis 32.51 27.31 26 5755 9118 2343186
Coagulopathy 32.46 27.31 17 5764 2892 2349412
Contusion 32.46 27.31 30 5751 12780 2339524
Muscular weakness 32.27 27.31 32 5749 14865 2337439
Haemorrhage 32.21 27.31 28 5753 11011 2341293
Dysgeusia 32.11 27.31 25 5756 8434 2343870
Lichen planus 31.89 27.31 10 5771 446 2351858
Cardiac disorder 31.59 27.31 24 5757 7809 2344495
Chordoma 31.50 27.31 5 5776 5 2352299
Paraesthesia 31.38 27.31 38 5743 22050 2330254
Drug eruption 30.64 27.31 17 5764 3242 2349062
Blast cell crisis 30.44 27.31 6 5775 35 2352269
Gastric haemorrhage 30.36 27.31 12 5769 1061 2351243
Memory impairment 30.32 27.31 29 5752 12894 2339410
Haematochezia 30.09 27.31 20 5761 5275 2347029
Visual acuity reduced 30.08 27.31 20 5761 5278 2347026
Blood potassium decreased 30.06 27.31 20 5761 5285 2347019
Lichenoid keratosis 29.93 27.31 9 5772 348 2351956
Skin lesion 29.87 27.31 18 5763 4007 2348297
Disease recurrence 29.73 27.31 17 5764 3434 2348870
Tachycardia 29.69 27.31 32 5749 16377 2335927
Urine output decreased 29.54 27.31 13 5768 1506 2350798
Somnolence 29.52 27.31 38 5743 23447 2328857
Trisomy 8 29.48 27.31 5 5776 10 2352294
Electrocardiogram QT prolonged 29.45 27.31 23 5758 7791 2344513
Rash maculo-papular 28.96 27.31 18 5763 4234 2348070
Blood sodium decreased 28.68 27.31 16 5765 3084 2349220
Anxiety 28.61 27.31 42 5739 29317 2322987
Blood iron decreased 28.45 27.31 12 5769 1253 2351051
Feeling cold 28.44 27.31 16 5765 3134 2349170
Diabetes mellitus 28.12 27.31 22 5759 7473 2344831
Ileus 28.02 27.31 14 5767 2158 2350146
Slit-lamp tests abnormal 27.97 27.31 4 5777 0 2352304
Odynophagia 27.96 27.31 11 5770 961 2351343
Hepatic enzyme abnormal 27.91 27.31 10 5771 674 2351630
Hypertension 27.91 27.31 40 5741 27321 2324983
Graft versus host disease in skin 27.71 27.31 8 5773 268 2352036
Polyneuropathy 27.68 27.31 13 5768 1750 2350554
Swollen tongue 27.54 27.31 19 5762 5324 2346980
Squamous cell carcinoma 27.42 27.31 12 5769 1371 2350933
Bone marrow oedema 27.41 27.31 7 5774 146 2352158

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 1242.39 26.96 716 5512 86727 1653826
Neoplasm malignant 893.28 26.96 249 5979 4090 1736463
Chronic myeloid leukaemia 847.17 26.96 169 6059 529 1740024
Drug resistance 826.07 26.96 220 6008 3010 1737543
Malignant neoplasm progression 812.69 26.96 308 5920 13850 1726703
Blast crisis in myelogenous leukaemia 681.55 26.96 118 6110 108 1740445
Gastrointestinal stromal tumour 671.82 26.96 127 6101 269 1740284
Pleural effusion 527.31 26.96 211 6017 10899 1729654
Nausea 485.68 26.96 328 5900 50868 1689685
Diarrhoea 398.95 26.96 297 5931 53555 1686998
Pyrexia 377.51 26.96 271 5957 46129 1694424
Haemoglobin decreased 376.67 26.96 190 6038 16924 1723629
Anaemia 375.59 26.96 228 6000 29229 1711324
Second primary malignancy 327.19 26.96 84 6144 975 1739578
Muscle spasms 315.34 26.96 149 6079 11472 1729081
Dyspnoea 312.83 26.96 254 5974 51805 1688748
Fatigue 307.68 26.96 249 5979 50532 1690021
Vomiting 300.06 26.96 219 6009 38096 1702457
Disease progression 289.64 26.96 160 6068 17103 1723450
Oedema peripheral 285.47 26.96 153 6075 15397 1725156
Thrombocytopenia 279.34 26.96 168 6060 21081 1719472
Neoplasm progression 276.01 26.96 95 6133 3172 1737381
Rash 269.00 26.96 206 6022 38487 1702066
Metastases to liver 268.11 26.96 85 6143 2182 1738371
Abdominal pain 259.62 26.96 161 6067 21329 1719224
Drug intolerance 258.97 26.96 107 6121 5955 1734598
Platelet count decreased 257.63 26.96 146 6082 16377 1724176
Drug ineffective 254.62 26.96 247 5981 63554 1676999
Leukaemia recurrent 254.41 26.96 54 6174 245 1740308
Pancytopenia 246.19 26.96 125 6103 11232 1729321
Ascites 243.34 26.96 100 6128 5486 1735067
Blood creatinine increased 219.34 26.96 124 6104 13822 1726731
Therapeutic response decreased 217.79 26.96 92 6136 5408 1735145
Chromosome analysis abnormal 210.94 26.96 36 6192 27 1740526
Periorbital oedema 201.37 26.96 53 6175 681 1739872
Asthenia 196.59 26.96 164 6064 34506 1706047
White blood cell count increased 195.72 26.96 93 6135 7219 1733334
Prostate cancer 195.25 26.96 81 6147 4545 1736008
Oedema 190.96 26.96 90 6138 6858 1733695
Fluid retention 189.28 26.96 75 6153 3734 1736819
Pneumonia 185.87 26.96 180 6048 46002 1694551
White blood cell count decreased 169.91 26.96 103 6125 13046 1727507
Splenomegaly 168.72 26.96 59 6169 2061 1738492
Gene mutation identification test positive 168.46 26.96 31 6197 52 1740501
Neutropenia 164.48 26.96 114 6114 18146 1722407
Treatment failure 155.65 26.96 68 6160 4333 1736220
Arthralgia 154.01 26.96 121 6107 23323 1717230
Bone marrow failure 150.99 26.96 70 6158 5130 1735423
Myalgia 146.24 26.96 100 6128 15558 1724995
Surgery 144.38 26.96 57 6171 2806 1737747
Acute lymphocytic leukaemia recurrent 144.13 26.96 34 6194 268 1740285
Malaise 143.30 26.96 128 6100 29437 1711116
Neoplasm recurrence 143.11 26.96 36 6192 381 1740172
Decreased appetite 139.34 26.96 115 6113 23756 1716797
Cytogenetic analysis abnormal 138.00 26.96 26 6202 53 1740500
Sepsis 135.58 26.96 104 6124 19334 1721219
Haematocrit decreased 131.80 26.96 60 6168 4213 1736340
Pain in extremity 129.18 26.96 99 6129 18373 1722180
Bone pain 128.87 26.96 55 6173 3307 1737246
Cardiac failure 123.61 26.96 83 6145 12519 1728034
Pain 116.55 26.96 109 6119 26548 1714005
Face oedema 115.99 26.96 46 6182 2290 1738263
General physical health deterioration 115.88 26.96 81 6147 13037 1727516
Graft versus host disease 115.07 26.96 41 6187 1512 1739041
Philadelphia chromosome positive 115.00 26.96 20 6208 19 1740534
Product use in unapproved indication 114.43 26.96 71 6157 9351 1731202
Red blood cell count decreased 114.43 26.96 52 6176 3634 1736919
Gene mutation 113.65 26.96 25 6203 138 1740415
Therapy non-responder 112.80 26.96 61 6167 6205 1734348
Pericardial effusion 112.15 26.96 50 6178 3340 1737213
Respiratory failure 108.56 26.96 81 6147 14424 1726129
Blood lactate dehydrogenase increased 108.29 26.96 50 6178 3625 1736928
Pruritus 107.38 26.96 98 6130 23124 1717429
Weight decreased 105.16 26.96 96 6132 22657 1717896
Acquired gene mutation 103.85 26.96 24 6204 171 1740382
Ejection fraction decreased 103.81 26.96 42 6186 2203 1738350
Blast cell count increased 103.60 26.96 24 6204 173 1740380
Blood alkaline phosphatase increased 103.16 26.96 54 6174 5141 1735412
Renal failure 101.47 26.96 89 6139 19928 1720625
Chronic myeloid leukaemia recurrent 97.14 26.96 18 6210 32 1740521
Chronic myeloid leukaemia transformation 92.99 26.96 18 6210 45 1740508
Abdominal distension 92.27 26.96 54 6174 6390 1734163
Abdominal discomfort 91.85 26.96 61 6167 9020 1731533
Cough 88.66 26.96 81 6147 19116 1721437
Abdominal pain upper 88.05 26.96 64 6164 10937 1729616
Chronic graft versus host disease 87.46 26.96 26 6202 532 1740021
Eyelid oedema 87.29 26.96 32 6196 1281 1739272
Blast cell crisis 86.32 26.96 17 6211 48 1740505
Recurrent cancer 86.25 26.96 22 6206 247 1740306
Alanine aminotransferase increased 86.15 26.96 66 6162 12212 1728341
Myelofibrosis 86.14 26.96 24 6204 386 1740167
Multiple organ dysfunction syndrome 86.10 26.96 59 6169 9183 1731370
Interstitial lung disease 85.87 26.96 60 6168 9636 1730917
Metastases to peritoneum 85.71 26.96 23 6205 319 1740234
Blood urea increased 85.14 26.96 46 6182 4665 1735888
Cytogenetic abnormality 84.35 26.96 21 6207 212 1740341
Aspartate aminotransferase increased 82.52 26.96 61 6167 10695 1729858
Generalised oedema 81.63 26.96 33 6195 1726 1738827
Colon cancer 79.78 26.96 33 6195 1831 1738722
Leukocytosis 79.60 26.96 40 6188 3493 1737060
Stem cell transplant 78.62 26.96 23 6205 444 1740109
Renal impairment 77.32 26.96 62 6166 12252 1728301
Cardiomyopathy 76.58 26.96 36 6192 2716 1737837
Acute myeloid leukaemia 76.15 26.96 37 6191 3004 1737549
Blood bilirubin increased 75.86 26.96 47 6181 6163 1734390
Lymphadenopathy 73.86 26.96 40 6188 4074 1736479
Gastric antral vascular ectasia 71.18 26.96 15 6213 65 1740488
Chest pain 71.15 26.96 73 6155 19841 1720712
Headache 70.91 26.96 95 6133 34281 1706272
Gastric cancer 70.41 26.96 26 6202 1062 1739491
Blindness 69.95 26.96 34 6194 2762 1737791
Infection 68.74 26.96 58 6170 12302 1728251
Eye swelling 68.48 26.96 30 6198 1919 1738634
Dehydration 67.22 26.96 67 6161 17591 1722962
Bone marrow necrosis 66.37 26.96 14 6214 61 1740492
Dyspnoea exertional 65.22 26.96 37 6191 4124 1736429
Blood creatine phosphokinase increased 65.17 26.96 49 6179 8807 1731746
Skin lesion 65.05 26.96 33 6195 2939 1737614
Cardiac failure congestive 63.84 26.96 61 6167 15209 1725344
Swelling face 62.66 26.96 37 6191 4446 1736107
Weight increased 62.54 26.96 53 6175 11304 1729249
Swelling 61.23 26.96 43 6185 6953 1733600
Platelet count increased 60.37 26.96 26 6202 1595 1738958
Gastrointestinal haemorrhage 59.65 26.96 57 6171 14210 1726343
Gait disturbance 59.48 26.96 54 6174 12616 1727937
Chloroma 56.56 26.96 13 6215 90 1740463
Dizziness 56.13 26.96 85 6143 34276 1706277
Bone marrow transplant 55.56 26.96 15 6213 213 1740340
Multiple-drug resistance 55.42 26.96 16 6212 294 1740259
Muscular weakness 54.73 26.96 47 6181 10202 1730351
Skin exfoliation 54.55 26.96 34 6194 4501 1736052
Septic shock 53.38 26.96 42 6186 8067 1732486
Tumour haemorrhage 53.37 26.96 18 6210 561 1739992
Pseudoporphyria 53.27 26.96 12 6216 75 1740478
Atrial fibrillation 53.23 26.96 55 6173 15056 1725497
Lung disorder 53.20 26.96 35 6193 5084 1735469
Palpitations 53.02 26.96 39 6189 6775 1733778
Drug interaction 51.18 26.96 73 6155 27885 1712668
Exposure via father 51.03 26.96 12 6216 93 1740460
Dysphagia 51.01 26.96 45 6183 10123 1730430
Hypoxia 50.66 26.96 36 6192 5927 1734626
Back pain 50.63 26.96 56 6172 16557 1723996
Erythema 50.62 26.96 52 6176 14136 1726417
Blast cells present 50.11 26.96 11 6217 60 1740493
Hepatotoxicity 49.88 26.96 28 6200 3056 1737497
Hepatomegaly 49.84 26.96 23 6205 1662 1738891
Myocardial infarction 49.81 26.96 71 6157 27103 1713450
Hypoalbuminaemia 49.75 26.96 22 6206 1438 1739115
Subdural haematoma 49.53 26.96 29 6199 3428 1737125
Cerebral haemorrhage 49.00 26.96 36 6192 6241 1734312
Tumour lysis syndrome 48.99 26.96 23 6205 1728 1738825
Acute respiratory distress syndrome 48.81 26.96 29 6199 3522 1737031
Chordoma 48.78 26.96 8 6220 3 1740550
C-reactive protein increased 48.78 26.96 35 6193 5850 1734703
Peripheral swelling 47.60 26.96 39 6189 7932 1732621
Desmoid tumour 47.54 26.96 9 6219 19 1740534
Pulmonary oedema 47.46 26.96 36 6192 6550 1734003
Eosinophil count increased 47.38 26.96 21 6207 1380 1739173
Hepatitis 46.98 26.96 32 6196 4923 1735630
Lung neoplasm malignant 46.42 26.96 27 6201 3152 1737401
Hepatic failure 46.41 26.96 34 6194 5869 1734684
Gastrectomy 46.36 26.96 11 6217 89 1740464
Haemorrhage 46.33 26.96 42 6186 9787 1730766
Pneumonitis 46.20 26.96 29 6199 3886 1736667
Chronic kidney disease 46.04 26.96 30 6198 4287 1736266
Condition aggravated 45.92 26.96 60 6168 21090 1719463
Jaundice 45.60 26.96 34 6194 6028 1734525
Cardiomegaly 45.55 26.96 24 6204 2310 1738243
Metastases to lung 45.55 26.96 21 6207 1514 1739039
Acute kidney injury 45.50 26.96 78 6150 34866 1705687
Tumour excision 45.03 26.96 10 6218 58 1740495
Hepatic lesion 44.18 26.96 15 6213 477 1740076
Visual acuity reduced 43.88 26.96 28 6200 3860 1736693
Myocardial ischaemia 43.68 26.96 26 6202 3167 1737386
Leukopenia 43.47 26.96 38 6190 8442 1732111
Melaena 43.21 26.96 31 6197 5179 1735374
Growth retardation 43.17 26.96 15 6213 512 1740041
Myelodysplastic syndrome 42.97 26.96 26 6202 3263 1737290
Metastases to lymph nodes 42.78 26.96 17 6211 849 1739704
Bone marrow oedema 42.60 26.96 11 6217 130 1740423
Tumour necrosis 42.27 26.96 12 6216 207 1740346
Haematotoxicity 41.12 26.96 17 6211 941 1739612
Disseminated intravascular coagulation 40.72 26.96 26 6202 3588 1736965
Visual impairment 40.47 26.96 32 6196 6186 1734367
Depression 40.45 26.96 50 6178 16619 1723934
Marrow hyperplasia 40.00 26.96 11 6217 168 1740385
Dyspepsia 39.83 26.96 29 6199 4956 1735597
Metastasis 39.83 26.96 16 6212 822 1739731
Constipation 39.67 26.96 47 6181 14953 1725600
Scleroderma 39.40 26.96 12 6216 267 1740286
Cerebrovascular accident 39.26 26.96 51 6177 17815 1722738
Gamma-glutamyltransferase increased 39.25 26.96 29 6199 5069 1735484
Complications of transplant surgery 39.22 26.96 10 6218 112 1740441
Transaminases increased 38.81 26.96 26 6202 3891 1736662
Gastrointestinal disorder 38.80 26.96 28 6200 4720 1735833
Lung infiltration 38.76 26.96 21 6207 2138 1738415
Post embolisation syndrome 38.71 26.96 7 6221 10 1740543
Myositis 38.61 26.96 19 6209 1584 1738969
Rash erythematous 38.52 26.96 26 6202 3939 1736614
Concomitant disease aggravated 37.96 26.96 15 6213 738 1739815
Rales 37.86 26.96 16 6212 936 1739617
Blood blister 37.67 26.96 12 6216 311 1740242
Gastrooesophageal reflux disease 37.05 26.96 27 6201 4620 1735933
Neutrophil count decreased 36.82 26.96 30 6198 6051 1734502
Confusional state 36.63 26.96 54 6174 21224 1719329
Hepatic enzyme increased 36.63 26.96 31 6197 6590 1733963
Bone marrow disorder 36.56 26.96 12 6216 343 1740210
Gastritis 36.55 26.96 23 6205 3094 1737459
Cardiac disorder 36.50 26.96 33 6195 7658 1732895
Ileus 36.31 26.96 21 6207 2425 1738128
Chest expansion decreased 36.30 26.96 7 6221 17 1740536
Acute graft versus host disease 36.25 26.96 15 6213 832 1739721
Tuberculosis 35.88 26.96 19 6209 1847 1738706
Vision blurred 35.83 26.96 34 6194 8389 1732164
Disease recurrence 35.25 26.96 21 6207 2561 1737992
Lung adenocarcinoma 35.10 26.96 14 6214 706 1739847
Hyperbilirubinaemia 34.92 26.96 20 6208 2267 1738286
Hepatitis B 34.90 26.96 17 6211 1386 1739167
Cytopenia 34.80 26.96 15 6213 921 1739632
Pneumothorax 34.30 26.96 21 6207 2691 1737862
Bladder cancer 34.15 26.96 19 6209 2037 1738516
Metastases to heart 34.02 26.96 8 6220 62 1740491
Drug level increased 33.84 26.96 21 6207 2756 1737797
Leukaemia 33.70 26.96 14 6214 784 1739769
Amylase increased 33.66 26.96 16 6212 1236 1739317
Hypokalaemia 33.54 26.96 29 6199 6345 1734208
Fall 33.12 26.96 59 6169 27155 1713398
Haematuria 33.08 26.96 31 6197 7529 1733024
Product substitution issue 33.00 26.96 22 6206 3264 1737289
Clonal evolution 32.62 26.96 6 6222 10 1740543
Protein total decreased 32.54 26.96 13 6215 658 1739895
Pancreatitis 32.47 26.96 30 6198 7157 1733396
Osteomyelitis 32.21 26.96 19 6209 2276 1738277
Conjunctival haemorrhage 32.08 26.96 12 6216 508 1740045
Pigmentation disorder 32.03 26.96 12 6216 510 1740043
Left ventricular failure 32.01 26.96 13 6215 687 1739866
Joint swelling 31.61 26.96 28 6200 6325 1734228
Eosinophilia 31.59 26.96 22 6206 3505 1737048
Hypertension 31.53 26.96 48 6180 19400 1721153
Diabetes mellitus 31.52 26.96 29 6199 6879 1733674
Cholestasis 30.83 26.96 22 6206 3643 1736910
Graft versus host disease in skin 30.58 26.96 11 6217 416 1740137
Blood uric acid increased 30.55 26.96 14 6214 995 1739558
Chills 29.87 26.96 36 6192 11651 1728902
Biopsy bone marrow abnormal 29.80 26.96 8 6220 111 1740442
Thrombocytosis 29.79 26.96 12 6216 621 1739932
Lipase increased 29.72 26.96 16 6212 1608 1738945
Febrile neutropenia 29.70 26.96 35 6193 11065 1729488
Mitral valve incompetence 29.70 26.96 17 6211 1925 1738628
Neoplasm 29.64 26.96 13 6215 833 1739720
Hyperkeratosis 29.59 26.96 12 6216 632 1739921
Central nervous system leukaemia 29.57 26.96 7 6221 56 1740497
Blood albumin decreased 29.50 26.96 16 6212 1632 1738921
Chest X-ray abnormal 29.42 26.96 12 6216 641 1739912
Haemoptysis 29.40 26.96 24 6204 4852 1735701
Hepatic function abnormal 29.03 26.96 28 6200 7046 1733507
Productive cough 28.93 26.96 21 6207 3570 1736983
Metastases to bone 28.70 26.96 16 6212 1722 1738831
Dysgeusia 28.66 26.96 24 6204 5025 1735528
Aspiration pleural cavity 28.63 26.96 8 6220 130 1740423
Venoocclusive liver disease 28.42 26.96 13 6215 920 1739633
Pleural fibrosis 28.37 26.96 9 6219 230 1740323
Liver disorder 28.36 26.96 25 6203 5611 1734942
Concomitant disease progression 28.23 26.96 11 6217 521 1740032
Chest discomfort 28.19 26.96 28 6200 7303 1733250
Renal cell carcinoma 27.99 26.96 15 6213 1493 1739060
Acute lymphocytic leukaemia 27.68 26.96 11 6217 549 1740004
Intra-abdominal haemorrhage 27.63 26.96 10 6218 385 1740168
Eating disorder 27.57 26.96 14 6214 1248 1739305
Bronchopulmonary aspergillosis 27.46 26.96 15 6213 1551 1739002
Inflammation 27.40 26.96 20 6208 3430 1737123
Haematemesis 27.35 26.96 22 6206 4355 1736198
Nephrectomy 27.31 26.96 8 6220 155 1740398
Acute myeloid leukaemia recurrent 27.29 26.96 9 6219 261 1740292
Optic neuritis 27.28 26.96 12 6216 774 1739779
Dilatation ventricular 27.25 26.96 11 6217 572 1739981
Haematochezia 27.08 26.96 23 6205 4909 1735644

Pharmacologic Action:

SourceCodeDescription
ATC L01XE01 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Protein kinase inhibitors
FDA EPC N0000175605 Kinase Inhibitor
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D047428 Protein Kinase Inhibitors
CHEBI has role CHEBI:35610 antineoplastic agent

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
Myelodysplastic/ Myeloproliferative Diseases associated with Platelet-derived Growth Factor Receptor indication
Philadelphia Chromosome Positive Chronic Myelocytic Leukemia indication
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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 100MG BASE **Federal Register determination that product was not discontinued or withdrawn for safety or efficacy reasons** GLEEVEC NOVARTIS N021335 May 10, 2001 DISCN CAPSULE ORAL 6958335 Dec. 19, 2021 GLEEVEC IS ALSO INDICATED FOR THE TREATMENT OF PATIENTS WITH KIT (CD117) POSITIVE UNRESECTABLE AND/OR METASTATIC MALIGNANT GASTROINTESTINAL STROMAL TUMORS (GIST)
EQ 50MG BASE **Federal Register determination that product was not discontinued or withdrawn for safety or efficacy reasons** GLEEVEC NOVARTIS N021335 May 10, 2001 DISCN CAPSULE ORAL 6958335 Dec. 19, 2021 GLEEVEC IS ALSO INDICATED FOR THE TREATMENT OF PATIENTS WITH KIT (CD117) POSITIVE UNRESECTABLE AND/OR METASTATIC MALIGNANT GASTROINTESTINAL STROMAL TUMORS (GIST)
EQ 100MG BASE GLEEVEC NOVARTIS N021588 April 18, 2003 RX TABLET ORAL 6958335 Dec. 19, 2021 GLEEVEC IS ALSO INDICATED FOR THE TREATMENT OF PATIENTS WITH KIT (CD117) POSITIVE UNRESECTABLE AND/OR METASTATIC MALIGNANT GASTROINTESTINAL STROMAL TUMORS (GIST)
EQ 100MG BASE GLEEVEC NOVARTIS N021588 April 18, 2003 RX TABLET ORAL 6958335 Dec. 19, 2021 TREATMENT OF GASTROINTESTINAL STROMAL TUMORS (GIST)
EQ 400MG BASE GLEEVEC NOVARTIS N021588 April 18, 2003 RX TABLET ORAL 6958335 Dec. 19, 2021 GLEEVEC IS ALSO INDICATED FOR THE TREATMENT OF PATIENTS WITH KIT (CD117) POSITIVE UNRESECTABLE AND/OR METASTATIC MALIGNANT GASTROINTESTINAL STROMAL TUMORS (GIST)
EQ 400MG BASE GLEEVEC NOVARTIS N021588 April 18, 2003 RX TABLET ORAL 6958335 Dec. 19, 2021 TREATMENT OF GASTROINTESTINAL STROMAL TUMORS (GIST)

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 100MG BASE GLEEVEC NOVARTIS N021588 April 18, 2003 RX TABLET ORAL Jan. 25, 2020 TREATMENT OF PEDIATRIC PATIENTS WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA (PH+ ALL) IN COMBINATION WITH CHEMOTHERAPY, APPROVED UNDER NDA #21588/S-037
EQ 400MG BASE GLEEVEC NOVARTIS N021588 April 18, 2003 RX TABLET ORAL Jan. 25, 2020 TREATMENT OF PEDIATRIC PATIENTS WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA (PH+ ALL) IN COMBINATION WITH CHEMOTHERAPY, APPROVED UNDER NDA #21588/S-037

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

External reference:

IDSource
D000068877 MESH_DESCRIPTOR_UI
4021257 VUID
N0000148698 NUI
C0935989 UMLSCUI
D01441 KEGG_DRUG
391634008 SNOMEDCT_US
d04758 MMSL
282388 RXNORM
4021257 VANDF
414460008 SNOMEDCT_US
009151 NDDF
8A1O1M485B UNII
220127-57-1 SECONDARY_CAS_RN
8031 INN_ID
CHEMBL941 ChEMBL_ID
DB00619 DRUGBANK_ID
CHEMBL1642 ChEMBL_ID
CHEBI:45783 CHEBI
5291 PUBCHEM_CID
5687 IUPHAR_LIGAND_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 0054-0248 TABLET, FILM COATED 100 mg ORAL ANDA 18 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 0054-0249 TABLET, FILM COATED 400 mg ORAL ANDA 18 sections
Gleevec HUMAN PRESCRIPTION DRUG LABEL 1 0078-0401 TABLET 100 mg ORAL NDA 17 sections
Gleevec HUMAN PRESCRIPTION DRUG LABEL 1 0078-0649 TABLET 400 mg ORAL NDA 17 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 0093-7629 TABLET, FILM COATED 100 mg ORAL ANDA 18 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 0093-7630 TABLET, FILM COATED 400 mg ORAL ANDA 18 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 0378-2245 TABLET, FILM COATED 100 mg ORAL ANDA 17 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 0378-2246 TABLET, FILM COATED 400 mg ORAL ANDA 17 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 0904-6621 TABLET, FILM COATED 400 mg ORAL ANDA 18 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 0904-6901 TABLET, FILM COATED 100 mg ORAL ANDA 18 sections
imatinib mesylate HUMAN PRESCRIPTION DRUG LABEL 1 16714-704 TABLET, FILM COATED 100 mg ORAL ANDA 18 sections
imatinib mesylate HUMAN PRESCRIPTION DRUG LABEL 1 16714-705 TABLET, FILM COATED 400 mg ORAL ANDA 18 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 42292-043 TABLET, FILM COATED 100 mg ORAL ANDA 17 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 42292-044 TABLET, FILM COATED 400 mg ORAL ANDA 17 sections
Imatinib HUMAN PRESCRIPTION DRUG LABEL 1 43598-344 TABLET 100 mg ORAL ANDA 18 sections
Imatinib HUMAN PRESCRIPTION DRUG LABEL 1 43598-345 TABLET 400 mg ORAL ANDA 18 sections
imatinib mesylate HUMAN PRESCRIPTION DRUG LABEL 1 47335-472 TABLET, FILM COATED 100 mg ORAL ANDA 18 sections
imatinib mesylate HUMAN PRESCRIPTION DRUG LABEL 1 47335-475 TABLET, FILM COATED 400 mg ORAL ANDA 18 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 50268-426 TABLET, FILM COATED 100 mg ORAL ANDA 19 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 50268-427 TABLET, FILM COATED 400 mg ORAL ANDA 19 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 51407-269 TABLET, FILM COATED 100 mg ORAL ANDA 17 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 51407-270 TABLET, FILM COATED 400 mg ORAL ANDA 17 sections
IMATINIB MESYLATE HUMAN PRESCRIPTION DRUG LABEL 1 51991-376 TABLET, COATED 100 mg ORAL ANDA 18 sections
IMATINIB MESYLATE HUMAN PRESCRIPTION DRUG LABEL 1 51991-377 TABLET, COATED 400 mg ORAL ANDA 18 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 59923-723 TABLET, COATED 100 mg ORAL ANDA 17 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 59923-724 TABLET, COATED 400 mg ORAL ANDA 17 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 60429-925 TABLET, FILM COATED 100 mg ORAL ANDA 18 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 60429-926 TABLET, FILM COATED 400 mg ORAL ANDA 18 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 60505-2900 TABLET, FILM COATED 100 mg ORAL ANDA 18 sections
Imatinib Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 60505-2901 TABLET, FILM COATED 400 mg ORAL ANDA 18 sections