sunitinib ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 2544 557795-19-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • sunitinib
  • sunitinib malate
  • sutent
  • SU-011248
  • SU-010398
  • PHA-290940AD
An indole and pyrrole derivative that inhibits VEGFR-2 and PDGFR BETA RECEPTOR TYROSINE KINASES. It is used as an antineoplastic agent for the treatment of GASTROINTESTINAL STROMAL TUMORS, and for treatment of advanced or metastatic RENAL CELL CARCINOMA.
  • Molecular weight: 398.48
  • Formula: C22H27FN4O2
  • CLOGP: 3
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 3
  • TPSA: 77.23
  • ALOGS: -4.11
  • ROTB: 7

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
33 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 25 mg/mL 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) 1.34 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 54.50 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 2.132 High 0.86
caco2-efflux Caco-2 efflux ratio (BA/AB) 7.586 High 0.86
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 10.069 10^-6 cm/s High 0.86
dh-clint Dog hepatocyte intrinsic clearance 4.188 uL/min/10^6 cells High 0.86
dppb Dog plasma protein binding (% unbound) 18.190 % High 0.86
fcs-ppb Fetal calf serum protein binding (% unbound) 25.480 % High 0.86
herg hERG pIC50 5.400 pIC50 High 0.86
hh-clint Human hepatocyte intrinsic clearance 2.938 uL/min/10^6 cells High 0.86
hlm-clint Human liver microsomal intrinsic clearance 23.605 uL/min/mg protein High 0.86
hppb Human plasma protein binding (% unbound) 10.240 % High 0.86
kinase-safety-class AAK1,ABL1,ABL2,ACVR2A,ACVR2B,ACVRL1,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,BTK,CAMK1,CAMK2A,CAMK2B,CAMK2D,CAMK2G,CDK1,CDK14,CDK16,CDK19,CDK2,CDK3,CDK4,CDK5,CDK6,CDK7,CDK9,CHEK1,CHEK2,CHUK,CLK1,CLK2,CLK4,CSF1R,CSK,CSNK2A2,DDR1,DYRK1A,DYRK1B,DYRK2,DYRK3,EGFR,EIF2AK3,EPHA2,EPHB1,EPHB4,ERBB2,ERBB4,FGFR1,FGFR4,FLT1,FLT3,FLT4,FYN,GAK,GRK1,GRK2,GSK3A,GSK3B,HASPIN,HIPK2,IGF1R,IKBKB,INSR,IRAK1,IRAK3,IRAK4,ITK,JAK1,JAK2,JAK3,KDR,KIT,LCK,LRRK2,LYN,MAP2K1,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K19,MAP3K2,MAP3K21,MAP3K3,MAP3K7,MAP3K9,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK1,MAPK10,MAPK12,MAPK15,MAPK3,MAPK7,MAPK8,MAPK9,MARK1,MARK2,MARK3,MARK4,MELK,MET,MINK1,MKNK1,MKNK2,MST1R,MTOR,MYLK,NTRK1,NTRK2,NTRK3,NUAK1,PAK1,PAK2,PAK4,PAK5,PDGFRB,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PIM1,PIM2,PIM3,PLK1,PLK2,PLK3,PLK4,PRKAA1,PRKAA2,PRKACA,PRKCA,PRKCD,PRKCI,PRKCZ,PRKD1,PRKDC,PTK2,PTK6,RET,RIPK3,ROCK1,ROCK2,RPS6KA1,SGK1,SIK2,SIK3,SRC,STK10,STK16,STK17A,STK3,STK33,STK4,SYK,TBK1,TEK,TGFBR1,TNIK,TNK1,TTK,TYRO3,UHMK1,ULK1,ULK2,YES1,ZAP70 180
kinase-selectivity-class AAK1,ABL2,ACVR2A,ACVR2B,ALK,AURKA,AURKB,AURKC,AXL,BLK,BRAF,CAMK2A,CAMK2B,CAMK2D,CDK1,CDK16,CDK2,CDK3,CDK4,CDK6,CDK7,CDK9,CHEK1,CLK2,CLK4,CSF1R,CSK,DDR1,DYRK1B,DYRK3,EGFR,EIF2AK3,EPHA2,EPHB4,ERBB2,FGFR1,FGFR4,FLT1,FLT3,FLT4,FYN,GAK,GRK2,GSK3A,GSK3B,HIPK2,IGF1R,INSR,IRAK1,IRAK3,IRAK4,JAK1,JAK2,JAK3,KDR,KIT,LCK,LRRK2,LYN,MAP2K1,MAP2K3,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K19,MAP3K2,MAP3K21,MAP3K7,MAP3K9,MAP4K1,MAP4K3,MAP4K5,MAPK1,MAPK12,MAPK7,MARK1,MARK2,MARK3,MARK4,MELK,MET,MINK1,MKNK2,MST1R,MTOR,NTRK1,NTRK3,NUAK1,PAK2,PAK4,PDGFRB,PDK1,PDK4,PDPK1,PIK3CA,PIM3,PLK4,PRKAA1,PRKAA2,PRKCD,PRKCZ,PRKDC,PTK2,RET,RIPK3,ROCK1,SGK1,SIK2,SIK3,SRC,STK10,STK16,STK17A,STK33,STK4,SYK,TEK,TGFBR1,TNIK,TTK,TYRO3,ULK1,ULK2,YES1 126
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 6.109 High 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 13.740 High 0.86
mh-clint Mouse hepatocyte intrinsic clearance 47.534 High 0.86
mppb Mouse plasma protein binding (% unbound) 10.930 High 0.86
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 36.728 High 0.86
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 1 High 1
pppb Pig plasma protein binding (% unbound) 23.240 % High 0.86
rat-kpuu-brain Rat brain Kpuu 0.033 % High 1
rh-clint Rat hepatocyte intrinsic clearance 16.520 uL/min/10^6 cells High 0.86
rh-fuinc Rat hepatocyte fraction unbound in incubation 45.750 % High 0.86
rppb Rat plasma protein binding (% unbound) 11.370 % High 0.86
solubility-dd Solubility at pH 7.4 in DMSO 268.534 uM High 0.86

Approvals:

DateAgencyCompanyOrphan
July 19, 2006 EMA Pfizer Limited
Jan. 26, 2006 FDA CPPI CV

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
Disease progression 1277.52 20.91 745 30253 155870 90441579
Palmar-plantar erythrodysaesthesia syndrome 881.16 20.91 339 30659 27684 90569765
Neoplasm progression 805.64 20.91 363 30635 44123 90553326
Death 703.28 20.91 820 30178 455731 90141718
Dysgeusia 458.90 20.91 262 30736 52298 90545151
Oral pain 438.46 20.91 217 30781 32466 90564983
Hypothyroidism 429.71 20.91 252 30746 52875 90544574
Yellow skin 384.39 20.91 103 30895 2578 90594871
Diarrhoea 371.93 20.91 917 30081 938273 89659176
Thrombocytopenia 355.54 20.91 396 30602 208329 90389120
Platelet count decreased 273.74 20.91 283 30715 136686 90460763
Hair colour changes 270.28 20.91 83 30915 3411 90594038
Stomatitis 214.64 20.91 357 30641 274341 90323108
Fatigue 213.60 20.91 867 30131 1153156 89444293
Decreased appetite 194.85 20.91 410 30588 376130 90221319
Mucosal inflammation 172.38 20.91 149 30849 57476 90539973
Hypertension 161.33 20.91 429 30569 457103 90140346
Drug ineffective 161.05 20.91 143 30855 1384155 89213294
Dehydration 158.86 20.91 258 30740 194189 90403260
Asthenia 153.61 20.91 465 30533 533286 90064163
Nausea 144.49 20.91 753 30245 1109563 89487886
Ageusia 129.17 20.91 76 30922 16000 90581449
Blood pressure increased 128.74 20.91 237 30761 196980 90400469
Skin discolouration 125.31 20.91 111 30887 44204 90553245
Malignant neoplasm progression 120.50 20.91 165 30833 106705 90490744
Epistaxis 120.36 20.91 147 30851 84978 90512471
Rheumatoid arthritis 110.10 20.91 3 30995 362611 90234838
Pancreatic neuroendocrine tumour 108.86 20.91 28 30970 594 90596855
Vomiting 107.28 20.91 542 30456 787751 89809698
Arthropathy 104.40 20.91 5 30993 366237 90231212
Nephritic syndrome 99.75 20.91 24 30974 383 90597066
Oral discomfort 98.80 20.91 55 30943 10428 90587021
Drug hypersensitivity 97.47 20.91 20 30978 463589 90133860
Dry skin 93.32 20.91 132 30866 87941 90509508
Pleural effusion 93.27 20.91 150 30848 111841 90485608
Second primary malignancy 88.50 20.91 51 30947 10327 90587122
Hypersensitivity 81.51 20.91 27 30971 454650 90142799
Blood thyroid stimulating hormone increased 80.77 20.91 46 30952 9109 90588340
Ascites 80.04 20.91 90 30908 47650 90549799
Eyelid oedema 78.43 20.91 49 30949 11485 90585964
Bone marrow failure 78.00 20.91 74 30924 32147 90565302
Hyperkeratosis 75.44 20.91 40 30958 6888 90590561
Osteonecrosis of jaw 74.76 20.91 79 30919 39024 90558425
Joint swelling 71.17 20.91 42 30956 503258 90094191
Pancytopenia 70.32 20.91 138 30860 120125 90477324
Metastases to liver 69.43 20.91 66 30932 28741 90568708
Injection site hypersensitivity 68.60 20.91 28 30970 2659 90594790
Treatment failure 68.39 20.91 11 30987 303917 90293532
Arthralgia 66.84 20.91 102 30896 778420 89819029
Urticaria 66.71 20.91 13 30985 312721 90284728
Pericarditis 64.94 20.91 8 30990 270143 90327306
Discomfort 63.85 20.91 9 30989 274326 90323123
Swelling 63.55 20.91 32 30966 419026 90178423
Sinusitis 62.11 20.91 20 30978 343068 90254381
Face oedema 61.16 20.91 56 30942 23262 90574187
Mobility decreased 58.88 20.91 8 30990 250726 90346723
Asthma 58.62 20.91 7 30991 242153 90355296
Neutropenia 58.02 20.91 189 30809 224715 90372734
Skin exfoliation 57.93 20.91 92 30906 67821 90529628
Tongue discomfort 57.82 20.91 25 30973 2740 90594709
White blood cell count decreased 55.95 20.91 154 30844 166955 90430494
Renal cell carcinoma 55.88 20.91 27 30971 3824 90593625
Jaundice 55.69 20.91 62 30936 32455 90564994
Injury 55.23 20.91 3 30995 197346 90400103
Anaemia 54.52 20.91 252 30746 352550 90244899
Type 2 diabetes mellitus 54.17 20.91 4 30994 203240 90394209
Nasal discharge discolouration 53.85 20.91 24 30974 2829 90594620
Flatulence 51.38 20.91 67 30931 41300 90556149
Condition aggravated 51.08 20.91 78 30920 595467 90001982
Ingrowing nail 50.56 20.91 23 30975 2844 90594605
Muscle contractions involuntary 50.09 20.91 23 30975 2905 90594544
Wound 49.22 20.91 21 30977 302959 90294490
Musculoskeletal stiffness 49.06 20.91 20 30978 296512 90300937
Hyperaesthesia 47.70 20.91 35 30963 10667 90586782
Gingival bleeding 47.52 20.91 40 30958 14863 90582586
Infection 46.03 20.91 34 30964 362060 90235389
Off label use 42.83 20.91 213 30785 1102039 89495410
Thyroid disorder 41.44 20.91 40 30958 17745 90579704
Metastatic renal cell carcinoma 40.68 20.91 14 30984 827 90596622
Blood lactate dehydrogenase increased 40.27 20.91 47 30951 25885 90571564
Lower respiratory tract infection 39.71 20.91 18 30980 250641 90346808
Blood cholesterol increased 39.67 20.91 11 30987 208001 90389448
Dyspepsia 39.47 20.91 153 30845 198007 90399442
Neoplasm malignant 39.19 20.91 53 30945 33827 90563622
Proteinuria 39.18 20.91 44 30954 23247 90574202
Plantar erythema 39.11 20.91 10 30988 207 90597242
Liver injury 38.74 20.91 6 30992 170561 90426888
Disseminated intravascular coagulation 38.50 20.91 42 30956 21496 90575953
Gastrointestinal stromal tumour 37.43 20.91 15 30983 1358 90596091
Gingival pain 37.33 20.91 29 30969 9623 90587826
Psoriasis 36.43 20.91 4 30994 147750 90449699
Renal cancer metastatic 35.23 20.91 10 30988 311 90597138
Joint range of motion decreased 35.21 20.91 3 30995 135640 90461809
Metastases to central nervous system 34.52 20.91 36 30962 17506 90579943
Tumour haemorrhage 34.42 20.91 16 30982 2078 90595371
Therapeutic product effect incomplete 33.85 20.91 12 30986 193884 90403565
Generalised oedema 33.78 20.91 37 30961 19016 90578433
Chromaturia 33.57 20.91 37 30961 19150 90578299
Skin toxicity 32.10 20.91 23 30975 6756 90590693
Bursitis 31.37 20.91 4 30994 131650 90465799
Leukopenia 30.93 20.91 90 30908 100620 90496829
Nephrotic syndrome 30.47 20.91 23 30975 7316 90590133
Needle issue 29.97 20.91 30 30968 13904 90583545
Migraine 29.64 20.91 14 30984 190378 90407071
Hepatic enzyme increased 29.22 20.91 49 30949 360687 90236762
Hypogeusia 29.14 20.91 13 30985 1536 90595913
Sleep disorder 28.69 20.91 16 30982 198014 90399435
Metastases to lung 28.26 20.91 31 30967 15960 90581489
Metastases to bone 28.14 20.91 39 30959 25466 90571983
Weight decreased 27.52 20.91 223 30775 379687 90217762
Hepatic failure 27.46 20.91 49 30949 39679 90557770
Haemorrhage 27.36 20.91 68 30930 69301 90528148
Pain 27.01 20.91 215 30783 996126 89601323
Petechiae 26.93 20.91 30 30968 15711 90581738
Pruritus 26.92 20.91 95 30903 541430 90056019
Glossitis 26.32 20.91 16 30982 3571 90593878
Soft tissue sarcoma 26.31 20.91 7 30991 170 90597279
Posterior reversible encephalopathy syndrome 25.92 20.91 35 30963 22304 90575145
Eyelash discolouration 25.87 20.91 6 30992 81 90597368
Gastrointestinal disorder 25.64 20.91 30 30968 256657 90340792
Periorbital oedema 25.37 20.91 20 30978 6779 90590670
Weight increased 25.27 20.91 67 30931 417860 90179589
Tenderness 25.14 20.91 38 30960 26830 90570619
Oral mucosal blistering 25.05 20.91 20 30978 6904 90590545
Thyroid function test abnormal 24.76 20.91 16 30982 3973 90593476
Drug intolerance 24.67 20.91 75 30923 447516 90149933
Cardiac failure 24.67 20.91 88 30910 109408 90488041
Skin plaque 24.31 20.91 23 30975 9952 90587497
Lung infiltration 24.23 20.91 28 30970 15254 90582195
Body temperature decreased 24.18 20.91 35 30963 23781 90573668
Nasopharyngitis 24.06 20.91 66 30932 407038 90190411
Hypertensive crisis 23.96 20.91 30 30968 17754 90579695
Eating disorder 23.89 20.91 38 30960 28035 90569414
Constipation 23.89 20.91 171 30827 280224 90317225
Pain in extremity 23.77 20.91 247 30751 450282 90147167
Wound infection 23.58 20.91 4 30994 106398 90491051
Haematuria 22.76 20.91 42 30956 34895 90562554
Tongue disorder 22.66 20.91 23 30975 10837 90586612
COVID-19 22.56 20.91 15 30983 168828 90428621
Mouth ulceration 22.30 20.91 45 30953 39929 90557520
Hypophagia 21.91 20.91 42 30956 35895 90561554
Injection site induration 21.53 20.91 22 30976 10446 90587003
Therapy non-responder 21.36 20.91 10 30988 136694 90460755
Thyroiditis 21.14 20.91 14 30984 3623 90593826
Dysphagia 20.97 20.91 85 30913 112193 90485256
Adverse event 20.95 20.91 7 30991 117411 90480038

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
Disease progression 2103.88 15.87 1540 46734 142116 42430945
Neoplasm progression 1354.20 15.87 659 47615 28341 42544720
Palmar-plantar erythrodysaesthesia syndrome 1346.29 15.87 591 47683 19991 42553070
Death 881.22 15.87 1753 46521 469432 42103629
Dysgeusia 657.58 15.87 435 47839 33754 42539307
Osteonecrosis of jaw 491.05 15.87 292 47982 18757 42554304
Yellow skin 489.86 15.87 158 48116 2196 42570865
Diarrhoea 479.57 15.87 1368 46906 459481 42113580
Stomatitis 475.17 15.87 419 47855 49910 42523151
Fatigue 392.62 15.87 1230 47044 434411 42138650
Oral pain 382.92 15.87 215 48059 12381 42560680
Hair colour changes 370.87 15.87 126 48148 2076 42570985
Decreased appetite 328.36 15.87 694 47580 192443 42380618
Hypertension 325.94 15.87 636 47638 166568 42406493
Hypothyroidism 308.40 15.87 270 48004 31814 42541247
Ageusia 291.46 15.87 175 48099 11430 42561631
Glossodynia 273.56 15.87 120 48154 4032 42569029
Off label use 206.66 15.87 253 48021 638082 41934979
Drug ineffective 205.88 15.87 248 48026 629949 41943112
Asthenia 176.61 15.87 706 47568 280087 42292974
Platelet count decreased 172.38 15.87 441 47833 138140 42434921
Dyspepsia 158.26 15.87 214 48060 41138 42531923
Blood pressure increased 149.78 15.87 346 47928 101582 42471479
Mucosal inflammation 140.28 15.87 222 48052 49152 42523909
Nausea 138.93 15.87 844 47430 395955 42177106
Thrombocytopenia 124.67 15.87 485 47789 189794 42383267
Blister 121.88 15.87 153 48121 27337 42545724
Second primary malignancy 117.76 15.87 93 48181 9482 42563579
Febrile neutropenia 112.88 15.87 35 48239 185668 42387393
Drug interaction 108.76 15.87 86 48188 266913 42306148
COVID-19 103.96 15.87 7 48267 115941 42457120
Malignant neoplasm progression 103.07 15.87 313 47961 108087 42464974
Epistaxis 100.46 15.87 229 48045 66597 42506464
Dry skin 97.63 15.87 187 48087 48151 42524910
Renal cell carcinoma 95.87 15.87 66 48208 5451 42567610
Drug abuse 94.89 15.87 6 48268 104765 42468296
Completed suicide 92.14 15.87 4 48270 96461 42476600
Skin discolouration 89.00 15.87 114 48160 20776 42552285
Blood thyroid stimulating hormone increased 84.24 15.87 60 48214 5232 42567829
Oral discomfort 82.87 15.87 48 48226 2929 42570132
Pleural effusion 79.95 15.87 267 48007 96899 42476162
Exposed bone in jaw 73.66 15.87 36 48238 1553 42571508
Renal cancer metastatic 70.87 15.87 26 48248 541 42572520
Jaw fistula 69.46 15.87 16 48258 52 42573009
Dehydration 68.59 15.87 330 47944 141437 42431624
Vomiting 68.01 15.87 560 47714 289163 42283898
Hyperkeratosis 66.45 15.87 49 48225 4509 42568552
Gastrointestinal stromal tumour 65.72 15.87 30 48244 1108 42571953
Neoplasm malignant 65.57 15.87 103 48171 22640 42550421
Skin exfoliation 61.97 15.87 142 48132 41411 42531650
Cardiopulmonary failure 60.86 15.87 47 48227 4636 42568425
Inappropriate schedule of product administration 60.18 15.87 17 48257 95885 42477176
Overdose 58.47 15.87 23 48251 105241 42467820
Metastatic renal cell carcinoma 57.73 15.87 34 48240 2140 42570921
Condition aggravated 54.92 15.87 135 48139 260619 42312442
Acute kidney injury 53.13 15.87 225 48049 367112 42205949
Metastases to liver 52.80 15.87 78 48196 16248 42556813
Asthma 52.39 15.87 5 48269 62309 42510752
Bone marrow failure 51.47 15.87 115 48159 32978 42540083
Hypotension 49.22 15.87 140 48134 257491 42315570
Thyroid function test abnormal 48.72 15.87 21 48253 675 42572386
Pancreatic neuroendocrine tumour metastatic 48.69 15.87 14 48260 128 42572933
Tongue discomfort 48.18 15.87 21 48253 694 42572367
White blood cell count decreased 47.72 15.87 249 48025 110147 42462914
Aortic dissection 46.99 15.87 34 48240 3038 42570023
Fall 46.61 15.87 125 48149 234395 42338666
Proteinuria 46.48 15.87 89 48185 22894 42550167
Intentional product use issue 46.44 15.87 12 48262 71821 42501240
Intentional overdose 46.41 15.87 3 48271 51453 42521608
Oxygen saturation decreased 45.44 15.87 9 48265 64678 42508383
Hypogeusia 45.21 15.87 23 48251 1082 42571979
Impaired healing 43.41 15.87 73 48201 16980 42556081
Tachycardia 43.06 15.87 31 48243 101056 42472005
Drug hypersensitivity 42.97 15.87 30 48244 99359 42473702
Weight decreased 42.97 15.87 391 47883 207557 42365504
Suicidal ideation 42.87 15.87 3 48271 48158 42524903
Dry mouth 41.50 15.87 119 48155 39760 42533301
Oral mucosal blistering 41.30 15.87 29 48245 2472 42570589
Pain in extremity 41.27 15.87 302 47972 150302 42422759
Nephrotic syndrome 39.38 15.87 49 48225 8669 42564392
Tongue blistering 39.01 15.87 15 48259 357 42572704
Intentional product misuse 38.77 15.87 11 48263 61889 42511172
Jaundice 38.73 15.87 106 48168 34483 42538578
Hospitalisation 38.47 15.87 18 48256 74312 42498749
Urticaria 38.20 15.87 18 48256 74018 42499043
Mouth ulceration 38.01 15.87 64 48210 14899 42558162
Product dose omission issue 37.32 15.87 74 48200 154291 42418770
Disseminated intravascular coagulation 37.25 15.87 85 48189 24709 42548352
Therapeutic product effect incomplete 36.99 15.87 17 48257 70922 42502139
Wrong technique in product usage process 36.98 15.87 3 48271 42632 42530429
Drug reaction with eosinophilia and systemic symptoms 36.38 15.87 3 48271 42072 42530989
Atrial fibrillation 36.32 15.87 64 48210 139529 42433532
Metastases to lung 36.11 15.87 54 48220 11370 42561691
Aggression 35.94 15.87 4 48270 44159 42528902
Psoriasis 35.78 15.87 6 48268 48598 42524463
Salivary gland fistula 35.65 15.87 7 48267 7 42573054
Thyroid disorder 35.44 15.87 32 48242 3918 42569143
Blood creatinine increased 35.09 15.87 229 48045 109774 42463287
Pneumonia 34.98 15.87 308 47966 421841 42151220
Skin disorder 34.74 15.87 66 48208 16878 42556183
Suicide attempt 33.26 15.87 6 48268 46094 42526967
Periorbital oedema 32.79 15.87 33 48241 4624 42568437
Plasma cell myeloma 32.62 15.87 7 48267 47571 42525490
Wheezing 32.04 15.87 11 48263 54770 42518291
Abdominal discomfort 31.99 15.87 169 48105 75086 42497975
Ascites 31.87 15.87 138 48136 56540 42516521
Tumour necrosis 31.75 15.87 21 48253 1623 42571438
Tumour haemorrhage 31.72 15.87 29 48245 3609 42569452
Stress 31.37 15.87 6 48268 44206 42528855
Anal abscess 30.57 15.87 41 48233 7809 42565252
Acute respiratory failure 30.44 15.87 4 48270 38854 42534207
Pain in jaw 30.36 15.87 57 48217 14445 42558616
Flatulence 30.09 15.87 79 48195 25073 42547988
Metastases to bone 29.52 15.87 57 48217 14752 42558309
Rhabdomyolysis 29.39 15.87 27 48247 77992 42495069
Taste disorder 29.10 15.87 46 48228 10161 42562900
Anxiety 28.50 15.87 57 48217 118503 42454558
Gingival pain 28.07 15.87 41 48233 8453 42564608
Anaemia 27.91 15.87 459 47815 279819 42293242
Product use in unapproved indication 27.82 15.87 111 48163 184345 42388716
Abdominal pain 27.43 15.87 333 47941 190138 42382923
Periodontal disease 27.06 15.87 15 48259 841 42572220
Treatment noncompliance 26.96 15.87 5 48269 37667 42535394
Osteonecrosis 26.79 15.87 57 48217 15808 42557253
Metastases to gastrointestinal tract 26.50 15.87 8 48266 88 42572973
Glossitis 26.47 15.87 18 48256 1456 42571605
Malaise 26.38 15.87 361 47913 211795 42361266
Chronic obstructive pulmonary disease 26.04 15.87 20 48254 63094 42509967
Myxoedema 25.99 15.87 7 48267 49 42573012
Agitation 25.75 15.87 21 48253 64293 42508768
Constipation 25.70 15.87 289 47985 162002 42411059
Hypoxia 25.29 15.87 25 48249 69761 42503300
Skin toxicity 25.19 15.87 34 48240 6515 42566546
Gastrooesophageal reflux disease 24.83 15.87 109 48165 44914 42528147
Tumour compression 24.82 15.87 9 48265 181 42572880
Metastases to central nervous system 24.60 15.87 43 48231 10312 42562749
Anaphylactic reaction 24.29 15.87 9 48265 42734 42530327
Musculoskeletal stiffness 24.22 15.87 18 48256 57747 42515314
Gastrointestinal toxicity 24.08 15.87 26 48248 3953 42569108
Tooth avulsion 23.99 15.87 6 48268 30 42573031
Gingival bleeding 23.86 15.87 38 48236 8447 42564614
Septic shock 23.86 15.87 42 48232 91630 42481431
Delirium 23.84 15.87 15 48259 52504 42520557
Hypertensive crisis 23.76 15.87 42 48232 10164 42562897
Coronary artery disease 23.49 15.87 16 48258 53704 42519357
Cardiac arrest 23.43 15.87 56 48218 109264 42463797
Hyperhidrosis 23.08 15.87 42 48232 90470 42482591
Hyperaesthesia 23.05 15.87 31 48243 5921 42567140
Adverse drug reaction 22.80 15.87 7 48267 37427 42535634
Blood glucose decreased 22.76 15.87 50 48224 14169 42558892
Medication error 22.48 15.87 5 48269 33149 42539912
Sinusitis 22.17 15.87 13 48261 47279 42525782
Tumour rupture 22.17 15.87 10 48264 359 42572702
Upper respiratory tract infection 22.14 15.87 10 48264 42163 42530898
Performance status decreased 22.08 15.87 27 48247 4693 42568368
Lacrimation increased 21.91 15.87 44 48230 11714 42561347
Injection site pain 21.77 15.87 20 48254 57778 42515283
Blood bilirubin abnormal 21.75 15.87 13 48261 841 42572220
Dental fistula 21.58 15.87 7 48267 99 42572962
Drug ineffective for unapproved indication 21.21 15.87 13 48261 46150 42526911
Ejection fraction decreased 21.15 15.87 64 48210 22023 42551038
Treatment failure 20.95 15.87 24 48250 62600 42510461
Vogt-Koyanagi-Harada disease 20.74 15.87 8 48266 192 42572869
Face oedema 20.69 15.87 47 48227 13619 42559442
Haemoptysis 20.52 15.87 105 48169 46062 42526999
Incorrect dose administered 20.35 15.87 18 48256 52956 42520105
Skin fissures 20.22 15.87 38 48236 9638 42563423
Agranulocytosis 20.00 15.87 5 48269 30607 42542454
General physical health deterioration 19.87 15.87 260 48014 150986 42422075
Drug level increased 19.81 15.87 3 48271 26197 42546864
Anorectal discomfort 19.71 15.87 18 48256 2237 42570824
Pericardial effusion 19.39 15.87 75 48199 29200 42543861
Splenic artery aneurysm 19.23 15.87 5 48269 30 42573031
Blood lactate dehydrogenase increased 19.09 15.87 69 48205 26012 42547049
Skin ulcer 18.97 15.87 68 48206 25533 42547528
Hypersensitivity 18.97 15.87 33 48241 72337 42500724
Tremor 18.96 15.87 52 48222 96877 42476184
Unresponsive to stimuli 18.90 15.87 6 48268 31397 42541664
Pruritus 18.70 15.87 131 48143 188640 42384421
Prostate cancer 18.60 15.87 14 48260 44629 42528432
Eating disorder 18.43 15.87 37 48237 9848 42563213
Obstructive airways disorder 18.34 15.87 3 48271 24756 42548305
Diffuse uveal melanocytic proliferation 18.14 15.87 4 48270 10 42573051
Eyelid oedema 18.11 15.87 27 48247 5668 42567393
Gingival swelling 18.08 15.87 14 48260 1386 42571675
Chromaturia 17.89 15.87 49 48225 15940 42557121
Renal mass 17.53 15.87 16 48258 1986 42571075
Gingivitis 17.42 15.87 22 48252 3951 42569110
Therapy non-responder 17.25 15.87 21 48253 53338 42519723
Pulmonary hypertension 17.14 15.87 3 48271 23566 42549495
Appetite disorder 17.03 15.87 19 48255 2996 42570065
Soft tissue sarcoma 16.96 15.87 6 48268 112 42572949
Migraine 16.90 15.87 4 48270 25410 42547651
Restlessness 16.88 15.87 6 48268 29243 42543818
Angular cheilitis 16.88 15.87 7 48267 204 42572857
Dyskinesia 16.87 15.87 4 48270 25386 42547675
Neoplasm recurrence 16.84 15.87 18 48256 2706 42570355
Depression 16.78 15.87 67 48207 111296 42461765
Cholecystitis 16.78 15.87 42 48232 12946 42560115
Hyperchlorhydria 16.71 15.87 10 48264 648 42572413
Rash maculo-papular 16.63 15.87 11 48263 37492 42535569
Chest wall mass 16.58 15.87 6 48268 120 42572941
Gastric fistula 16.48 15.87 6 48268 122 42572939
Psoriatic arthropathy 16.46 15.87 4 48270 24963 42548098
Neoplasm of thymus 16.34 15.87 4 48270 18 42573043
Toxic epidermal necrolysis 16.30 15.87 5 48269 26745 42546316
Therapeutic response decreased 16.21 15.87 11 48263 37001 42536060
Cholecystitis acute 16.05 15.87 30 48244 7576 42565485
Cancer pain 16.03 15.87 20 48254 3547 42569514
Intestinal perforation 16.02 15.87 37 48237 10837 42562224

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
Disease progression 2744.74 17.15 1769 67074 242265 110278191
Palmar-plantar erythrodysaesthesia syndrome 2030.48 17.15 813 68030 40212 110480244
Neoplasm progression 1986.83 17.15 914 67929 63681 110456775
Death 1174.78 17.15 1779 67064 697090 109823366
Dysgeusia 1067.03 17.15 618 68225 69367 110451089
Diarrhoea 833.09 17.15 2036 66807 1137469 109382987
Oral pain 747.18 17.15 395 68448 37049 110483407
Yellow skin 741.01 17.15 215 68628 3887 110516569
Hypothyroidism 675.39 17.15 470 68373 72429 110448027
Hair colour changes 589.44 17.15 186 68657 4515 110515941
Fatigue 558.14 17.15 1838 67005 1214120 109306336
Decreased appetite 536.26 17.15 1016 67827 474830 110045626
Stomatitis 464.03 17.15 697 68146 269545 110250911
Platelet count decreased 463.85 17.15 641 68202 229802 110290654
Osteonecrosis of jaw 452.60 17.15 313 68530 47704 110472752
Ageusia 451.59 17.15 228 68615 19417 110501039
Thrombocytopenia 393.78 17.15 746 68097 348139 110172317
Hypertension 367.15 17.15 909 67934 509175 110011281
Asthenia 338.24 17.15 1068 67775 687931 109832525
Mucosal inflammation 293.78 17.15 330 68513 95811 110424645
Drug ineffective 267.38 17.15 334 68509 1520206 109000250
Blood pressure increased 234.50 17.15 505 68338 257868 110262588
Dry skin 223.11 17.15 304 68539 107349 110413107
Epistaxis 215.91 17.15 331 68512 130041 110390415
Nausea 204.49 17.15 1390 67453 1234300 109286156
Malignant neoplasm progression 202.41 17.15 378 68465 174189 110346267
Second primary malignancy 199.51 17.15 130 68713 17938 110502518
Pleural effusion 193.93 17.15 375 68468 177334 110343122
Dehydration 187.91 17.15 486 68357 279025 110241431
Skin discolouration 186.26 17.15 189 68654 48857 110471599
Drug hypersensitivity 181.42 17.15 32 68811 454058 110066398
Rheumatoid arthritis 171.37 17.15 3 68840 299610 110220846
Off label use 163.03 17.15 442 68401 1499743 109020713
Oral discomfort 146.41 17.15 90 68753 11221 110509235
Blood thyroid stimulating hormone increased 144.43 17.15 92 68751 12209 110508247
Bone marrow failure 144.20 17.15 179 68664 57669 110462787
Hyperkeratosis 139.04 17.15 81 68762 9158 110511298
Dyspepsia 131.29 17.15 335 68508 190630 110329826
Arthropathy 129.51 17.15 14 68829 287508 110232948
Completed suicide 129.00 17.15 5 68838 242376 110278080
Hypersensitivity 127.66 17.15 46 68797 403952 110116504
Skin exfoliation 126.42 17.15 209 68634 87442 110433014
Wheezing 118.67 17.15 11 68832 255219 110265237
Urticaria 117.84 17.15 27 68816 318830 110201626
Intentional product use issue 114.42 17.15 11 68832 247895 110272561
Vomiting 114.24 17.15 961 67882 909714 109610742
White blood cell count decreased 114.17 17.15 358 68485 229032 110291424
Asthma 113.20 17.15 12 68831 250279 110270177
Ascites 108.78 17.15 202 68641 92606 110427850
Anaemia 106.24 17.15 642 68201 546444 109974012
Psoriatic arthropathy 104.90 17.15 4 68839 196757 110323699
Metastases to liver 103.83 17.15 119 68724 35267 110485189
Sinusitis 102.18 17.15 29 68814 296659 110223797
Joint swelling 102.04 17.15 76 68767 442769 110077687
Tongue discomfort 98.51 17.15 44 68799 2844 110517612
Condition aggravated 97.54 17.15 194 68649 734642 109785814
Treatment failure 97.53 17.15 26 68817 277208 110243248
Disseminated intravascular coagulation 93.78 17.15 122 68721 41164 110479292
Pancreatic neuroendocrine tumour 93.21 17.15 31 68812 892 110519564
Renal cell carcinoma 92.61 17.15 58 68785 7472 110512984
Weight decreased 92.57 17.15 552 68291 467505 110052951
Proteinuria 92.07 17.15 119 68724 39899 110480557
Mobility decreased 92.02 17.15 18 68825 237404 110283052
Osteoarthritis 90.12 17.15 6 68837 182617 110337839
COVID-19 90.04 17.15 21 68822 245039 110275417
Eyelid oedema 89.49 17.15 75 68768 15187 110505269
Overdose 87.97 17.15 19 68824 233775 110286681
Drug abuse 87.04 17.15 6 68837 177405 110343051
Musculoskeletal stiffness 86.44 17.15 33 68810 279789 110240667
Pericarditis 86.22 17.15 16 68827 219098 110301358
Jaundice 85.07 17.15 141 68702 59095 110461361
Flatulence 84.29 17.15 131 68712 52018 110468438
Type 2 diabetes mellitus 84.10 17.15 7 68836 177225 110343231
Hypogeusia 83.27 17.15 36 68807 2151 110518305
Ill-defined disorder 80.93 17.15 4 68839 156849 110363607
Gastrointestinal stromal tumour 80.88 17.15 35 68808 2096 110518360
Arthralgia 80.36 17.15 235 68608 779397 109741059
Nephritic syndrome 80.22 17.15 24 68819 484 110519972
Injury 76.41 17.15 10 68833 177255 110343201
Drug interaction 76.27 17.15 121 68722 500062 110020394
Renal cancer metastatic 73.59 17.15 25 68818 769 110519687
Gingival pain 73.57 17.15 68 68775 15668 110504788
Aortic dissection 70.94 17.15 42 68801 4891 110515565
Nephrotic syndrome 69.03 17.15 62 68781 13769 110506687
Tumour haemorrhage 68.56 17.15 42 68801 5203 110515253
Lower respiratory tract infection 66.67 17.15 34 68809 243072 110277384
Jaw fistula 66.61 17.15 16 68827 132 110520324
Therapeutic product effect incomplete 66.48 17.15 28 68815 223777 110296679
Intentional overdose 66.42 17.15 4 68839 132497 110387959
Hyperaesthesia 65.70 17.15 62 68781 14665 110505791
Swelling 65.64 17.15 73 68770 350968 110169488
Muscle injury 65.61 17.15 6 68837 140801 110379655
Febrile neutropenia 64.76 17.15 61 68782 316706 110203750
Thyroid disorder 63.69 17.15 65 68778 16904 110503552
Migraine 62.47 17.15 15 68828 171637 110348819
Oral mucosal blistering 61.60 17.15 46 68797 7888 110512568
Gingival bleeding 60.37 17.15 68 68775 19771 110500685
Psoriasis 60.09 17.15 8 68835 139985 110380471
Thyroid function test abnormal 60.07 17.15 33 68810 3334 110517122
Face oedema 59.65 17.15 88 68755 33381 110487075
Discomfort 58.91 17.15 30 68813 214677 110305779
Blood creatinine increased 56.74 17.15 245 68598 182644 110337812
Constipation 56.58 17.15 399 68444 357387 110163069
Blood lactate dehydrogenase increased 56.38 17.15 100 68743 44234 110476222
Injection site hypersensitivity 54.79 17.15 28 68815 2443 110518013
Joint range of motion decreased 54.66 17.15 6 68837 121826 110398630
Wound 54.25 17.15 40 68803 234397 110286059
Periorbital oedema 53.48 17.15 47 68796 10145 110510311
Hepatic enzyme increased 53.39 17.15 73 68770 320819 110199637
Skin toxicity 53.32 17.15 50 68793 11733 110508723
Drug intolerance 52.40 17.15 109 68734 406403 110114053
Tumour necrosis 52.27 17.15 27 68816 2409 110518047
Exposed bone in jaw 51.05 17.15 31 68812 3780 110516676
Hypertensive crisis 50.71 17.15 69 68774 24303 110496153
Chromaturia 50.61 17.15 76 68767 29284 110491172
Pancreatic neuroendocrine tumour metastatic 50.36 17.15 14 68829 215 110520241
Metastases to central nervous system 49.61 17.15 66 68777 22751 110497705
Liver injury 49.41 17.15 16 68827 150397 110370059
Tongue blistering 48.99 17.15 24 68819 1913 110518543
Nasopharyngitis 48.95 17.15 108 68735 394253 110126203
Glossitis 48.74 17.15 32 68811 4469 110515987
Skin disorder 48.51 17.15 92 68751 42821 110477635
Pulmonary fibrosis 48.49 17.15 4 68839 102038 110418418
Anal abscess 48.14 17.15 47 68796 11591 110508865
Bursitis 47.97 17.15 11 68832 129907 110390549
Medication error 47.75 17.15 5 68838 105361 110415095
Pain in extremity 47.68 17.15 488 68355 486630 110033826
Metastases to bone 46.82 17.15 76 68767 31296 110489160
Fall 46.72 17.15 205 68638 603277 109917179
Therapy non-responder 44.64 17.15 21 68822 157286 110363170
Mouth ulceration 44.61 17.15 95 68748 48043 110472413
Pruritus 44.14 17.15 199 68644 581361 109939095
Blood cholesterol increased 43.43 17.15 31 68812 184754 110335702
Metastases to lung 43.07 17.15 62 68781 23001 110497455
Wrong technique in product usage process 42.70 17.15 3 68840 87345 110433111
Osteoporosis 42.59 17.15 3 68840 87149 110433307
Tachycardia 42.49 17.15 47 68796 226598 110293858
Ingrowing nail 42.33 17.15 26 68817 3236 110517220
Intentional product misuse 42.15 17.15 15 68828 132889 110387567
Blood glucose decreased 42.07 17.15 70 68773 29418 110491038
Suicide attempt 41.86 17.15 7 68836 103387 110417069
Oxygen saturation decreased 41.49 17.15 23 68820 156959 110363497
Performance status decreased 41.15 17.15 35 68808 7231 110513225
Metastatic renal cell carcinoma 40.68 17.15 23 68820 2457 110517999
Salivary gland fistula 39.83 17.15 7 68836 7 110520449
Haemoptysis 39.81 17.15 116 68727 71238 110449218
Anaphylactic reaction 39.64 17.15 11 68832 114289 110406167
Inappropriate schedule of product administration 39.54 17.15 41 68802 203596 110316860
Plantar erythema 37.76 17.15 12 68831 298 110520158
Nasal discharge discolouration 37.72 17.15 24 68819 3177 110517279
Eating disorder 37.19 17.15 68 68775 30790 110489666
Suicidal ideation 36.64 17.15 7 68836 93930 110426526
Grip strength decreased 35.83 17.15 4 68839 80170 110440286
Leukopenia 35.67 17.15 185 68658 148606 110371850
Eyelash discolouration 35.31 17.15 9 68834 97 110520359
Upper respiratory tract infection 35.06 17.15 19 68824 131309 110389147
Product quality issue 34.18 17.15 4 68839 77295 110443161
Inflammation 34.14 17.15 42 68801 193196 110327260
Infection 33.82 17.15 114 68729 362086 110158370
Generalised oedema 33.69 17.15 65 68778 30639 110489817
Bronchitis 33.55 17.15 29 68814 157003 110363453
Arthritis 33.38 17.15 33 68810 167553 110352903
Red blood cell sedimentation rate increased 32.37 17.15 5 68838 78297 110442159
Feeding disorder 32.22 17.15 52 68791 21310 110499146
Neutropenia 31.84 17.15 365 68478 374255 110146201
Blister 31.59 17.15 246 68597 227130 110293326
Weight increased 31.57 17.15 144 68699 419500 110100956
Delirium 31.27 17.15 23 68820 135002 110385454
Cancer pain 31.15 17.15 29 68814 6743 110513713
Thrombotic microangiopathy 31.12 17.15 61 68782 29088 110491368
Haematemesis 30.98 17.15 94 68749 59014 110461442
Skin lesion 30.81 17.15 86 68757 51545 110468911
Hiccups 30.75 17.15 39 68804 12830 110507626
Lower limb fracture 30.72 17.15 5 68838 75343 110445113
Muscle contractions involuntary 30.62 17.15 24 68819 4420 110516036
Anxiety 30.61 17.15 111 68732 344967 110175489
Pericardial effusion 30.00 17.15 91 68752 57126 110463330
Hyperchlorhydria 29.97 17.15 18 68825 2151 110518305
Soft tissue sarcoma 29.93 17.15 10 68833 292 110520164
Drug-induced liver injury 29.74 17.15 19 68824 120048 110400408
Pneumonia 29.50 17.15 377 68466 876337 109644119
Pneumatosis intestinalis 29.01 17.15 31 68812 8498 110511958
Tumour rupture 28.91 17.15 12 68831 648 110519808
Gingival swelling 28.81 17.15 25 68818 5305 110515151
Wound infection 28.74 17.15 12 68831 96453 110424003
Hepatic cirrhosis 28.69 17.15 4 68839 67622 110452834
Chest discomfort 28.44 17.15 40 68803 173808 110346648
Hospitalisation 28.44 17.15 28 68815 142465 110377991
Haemorrhage 27.92 17.15 136 68707 106556 110413900
Anorectal discomfort 27.82 17.15 22 68821 4104 110516352
Mouth haemorrhage 27.77 17.15 38 68805 13450 110507006
Hepatic failure 27.70 17.15 100 68743 68639 110451817
Needle issue 27.69 17.15 44 68799 17796 110502660
Lip dry 27.42 17.15 14 68829 100069 110420387
Neoplasm malignant 27.42 17.15 67 68776 37076 110483380
Myxoedema 27.36 17.15 9 68834 250 110520206
Adverse event 27.25 17.15 17 68826 108792 110411664
Malaise 26.78 17.15 576 68267 671243 109849213
Renal failure 26.59 17.15 236 68607 226338 110294118
Dry mouth 26.50 17.15 214 68629 199734 110320722
Drug reaction with eosinophilia and systemic symptoms 26.49 17.15 9 68834 82086 110438370
Haematuria 26.34 17.15 112 68731 82893 110437563
Intestinal perforation 26.31 17.15 47 68796 20897 110499559
Gastrointestinal disorder 26.27 17.15 71 68772 241881 110278575
Depression 26.25 17.15 105 68738 317230 110203226
Cholecystitis 26.23 17.15 53 68790 25829 110494627
Incorrect dose administered 26.23 17.15 16 68827 103625 110416831
Hypoaesthesia 25.97 17.15 104 68739 314119 110206337
Periodontal disease 25.94 17.15 16 68827 2006 110518450
Sleep disorder 25.79 17.15 53 68790 198591 110321865
Gingival discomfort 25.13 17.15 10 68833 484 110519972
Tumour compression 24.71 17.15 8 68835 211 110520245
Cholecystitis acute 24.60 17.15 39 68804 15743 110504713
Drug ineffective for unapproved indication 24.49 17.15 17 68826 102821 110417635
General physical health deterioration 24.40 17.15 386 68457 424909 110095547
Thyroiditis 24.34 17.15 25 68818 6548 110513908
Aggression 23.98 17.15 4 68839 59206 110461250
Plasma cell myeloma 23.89 17.15 5 68838 62931 110457525
Gastrointestinal toxicity 23.86 17.15 32 68811 11116 110509340
Haematotoxicity 23.58 17.15 45 68798 21037 110499419
Chronic obstructive pulmonary disease 23.51 17.15 20 68823 109138 110411318
Pancytopenia 23.41 17.15 216 68627 209397 110311059
Peritonitis 23.20 17.15 58 68785 32549 110487907
Adverse drug reaction 23.15 17.15 19 68824 105540 110414916
Acute respiratory failure 23.01 17.15 9 68834 75251 110445205
Therapeutic response decreased 22.92 17.15 16 68827 96483 110423973
Hyperthyroidism 22.91 17.15 54 68789 29207 110491249
Road traffic accident 22.74 17.15 20 68823 107378 110413078
Skin ulcer 22.67 17.15 89 68754 63556 110456900
Abdominal pain 22.45 17.15 446 68397 512543 110007913
Accidental overdose 22.15 17.15 3 68840 51831 110468625
Blood bilirubin abnormal 22.12 17.15 14 68829 1836 110518620
Lacrimation increased 21.97 17.15 55 68788 30895 110489561
Tenderness 21.62 17.15 53 68790 29384 110491072
Neck pain 21.50 17.15 27 68816 123103 110397353
C-kit gene mutation 21.49 17.15 4 68839 7 110520449
Metastases to adrenals 21.37 17.15 13 68830 1590 110518866
Pain in jaw 21.09 17.15 75 68768 51102 110469354
Hyperhidrosis 21.06 17.15 54 68789 187244 110333212
Appetite disorder 20.84 17.15 28 68815 9741 110510715
Dysphonia 20.74 17.15 98 68745 75831 110444625
Stress 20.68 17.15 21 68822 105327 110415129
Dysphagia 20.68 17.15 165 68678 153435 110367021
Tooth avulsion 20.64 17.15 6 68837 109 110520347
Oral disorder 20.58 17.15 31 68812 11972 110508484
Unresponsive to stimuli 20.57 17.15 7 68836 63783 110456673
Clear cell sarcoma of soft tissue 20.53 17.15 4 68839 10 110520446
Ejection fraction decreased 20.48 17.15 64 68779 40816 110479640
Loss of personal independence in daily activities 20.36 17.15 39 68804 149981 110370475
Treatment noncompliance 20.31 17.15 10 68833 72980 110447476
Diffuse uveal melanocytic proliferation 20.25 17.15 4 68839 11 110520445
Cerebral haemorrhage 20.10 17.15 87 68756 64881 110455575
Skin fissures 20.09 17.15 46 68797 24412 110496044
Product dose omission issue 19.92 17.15 118 68725 321664 110198792
Neoplasm recurrence 19.56 17.15 20 68823 5212 110515244
Agitation 19.52 17.15 25 68818 113026 110407430
Cardiac failure 19.29 17.15 190 68653 187436 110333020
Heart rate increased 18.99 17.15 38 68805 143796 110376660
Hypertriglyceridaemia 18.71 17.15 35 68808 16119 110504337
Renal cancer 18.67 17.15 31 68812 13003 110507453
Hypervolaemia 18.63 17.15 4 68839 49456 110471000
Haemoglobin decreased 18.35 17.15 236 68607 248491 110271965
Cardiac arrest 18.30 17.15 62 68781 196691 110323765
Foot deformity 18.10 17.15 4 68839 48476 110471980
Night sweats 18.03 17.15 35 68808 133948 110386508
Hypoalbuminaemia 18.02 17.15 49 68794 28925 110491531
Injection site swelling 17.91 17.15 8 68835 61782 110458674
Tongue disorder 17.85 17.15 32 68811 14266 110506190
Headache 17.80 17.15 416 68427 881961 109638495
Dyskinesia 17.75 17.15 5 68838 51441 110469015
Blastic plasmacytoid dendritic cell neoplasia 17.74 17.15 5 68838 81 110520375
Atrial fibrillation 17.73 17.15 78 68765 229564 110290892
Drug level increased 17.69 17.15 4 68839 47715 110472741
Hypotension 17.68 17.15 225 68618 523624 109996832
Hepatic pain 17.66 17.15 18 68825 4672 110515784
Renal mass 17.56 17.15 16 68827 3619 110516837
Acute kidney injury 17.55 17.15 284 68559 635146 109885310
Neoplasm of thymus 17.49 17.15 4 68839 26 110520430
Pneumothorax 17.46 17.15 55 68788 35230 110485226
Hypoglycaemia 17.46 17.15 128 68715 115976 110404480
Therapy change 17.40 17.15 26 68817 9971 110510485
Hepatic function abnormal 17.39 17.15 105 68738 89190 110431266

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EX01 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Other protein kinase inhibitors
FDA MoA N0000175076 Protein Kinase Inhibitors
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D006131 Growth Inhibitors
MeSH PA D006133 Growth Substances
MeSH PA D020533 Angiogenesis Inhibitors
MeSH PA D047428 Protein Kinase Inhibitors
FDA EPC N0000175605 Kinase Inhibitor
CHEBI has role CHEBI:22587 antiviral agent
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:48422 angiogenesis inhibitor
CHEBI has role CHEBI:50846 immunomodulator
CHEBI has role CHEBI:62434 EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor
CHEBI has role CHEBI:63726 neuroprotective agent
CHEBI has role CHEBI:65207 vascular endothelial growth factor receptor antagonist
CHEBI has role CHEBI:231911 renoprotective agent

Related Drugs by ATC class:

L01EX Other protein kinase inhibitors 21 drugs

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

DiseaseRelationSNOMED_IDDOID
Gastrointestinal stromal tumor indication 420120006 DOID:9253
Renal cell carcinoma indication 702391001 DOID:4450
Pancreatic Neuroendocrine Tumor indication 717919005
Acute hemorrhage contraindication 8573003
Hyperkalemia contraindication 14140009
Hyperbilirubinemia contraindication 14783006 DOID:2741
Torsades de pointes contraindication 31722008
Hyperthyroidism contraindication 34486009 DOID:7998
Hypothyroidism contraindication 40930008 DOID:1459
Hypokalemia contraindication 43339004
Bradycardia contraindication 48867003
Hepatic failure contraindication 59927004
Hemoptysis contraindication 66857006
Hypermagnesemia contraindication 66978005
Pancreatitis contraindication 75694006 DOID:4989
Heart failure contraindication 84114007 DOID:6000
Left heart failure contraindication 85232009
Prolonged QT interval contraindication 111975006
Seizure disorder contraindication 128613002
Hypomagnesemia contraindication 190855004
Decompensated cardiac failure contraindication 195111005
Disease of liver contraindication 235856003 DOID:409
Drug-induced hepatitis contraindication 235876009
Anemia contraindication 271737000 DOID:2355
Pregnancy, function contraindication 289908002
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Thromboembolic disorder contraindication 371039008
Adrenal cortical hypofunction contraindication 386584007 DOID:10493
Surgical procedure contraindication 387713003
Breastfeeding (mother) contraindication 413712001
Congenital long QT syndrome contraindication 442917000
Hypertensive urgency contraindication 443482000
Posterior reversible encephalopathy syndrome contraindication 450886002




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.52 acidic
pKa2 11.68 acidic
pKa3 12.32 acidic
pKa4 9.32 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 9.68 CHEMBL CHEMBL
Platelet-derived growth factor receptor beta Kinase INHIBITOR Kd 10.12 CHEMBL CHEMBL
Receptor-type tyrosine-protein kinase FLT3 Kinase INHIBITOR Kd 9.66 CHEMBL CHEMBL
Vascular endothelial growth factor receptor 2 Kinase INHIBITOR Kd 9.70 CHEMBL CHEMBL
Vascular endothelial growth factor receptor 3 Kinase INHIBITOR Ki 7.77 CHEMBL CHEMBL
Macrophage colony-stimulating factor 1 receptor Kinase INHIBITOR Kd 8.70 CHEMBL CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret Kinase INHIBITOR IC50 8.80 IUPHAR DRUG LABEL
Vascular endothelial growth factor receptor 1 Kinase INHIBITOR IC50 7.23 SCIENTIFIC LITERATURE DRUG LABEL
Platelet-derived growth factor receptor alpha Kinase INHIBITOR IC50 6.96 SCIENTIFIC LITERATURE DRUG LABEL
Tyrosine-protein kinase Lck Kinase Kd 6.64 CHEMBL
Tyrosine-protein kinase Yes Kinase Kd 6.92 CHEMBL
Tyrosine-protein kinase Fyn Kinase Kd 6.28 CHEMBL
Ribosomal protein S6 kinase alpha-3 Kinase Kd 7.26 CHEMBL
Phosphorylase b kinase gamma catalytic chain, liver/testis isoform Kinase Kd 8.23 CHEMBL
Insulin-like growth factor 1 receptor Kinase Kd 5.59 CHEMBL
Myosin light chain kinase, smooth muscle Kinase Kd 7.64 CHEMBL
Insulin receptor Kinase AGONIST Kd 6.74 CHEMBL
Death-associated protein kinase 3 Kinase Kd 7.66 CHEMBL
Calcium/calmodulin-dependent protein kinase type 1 Kinase Kd 6.01 CHEMBL
Fibroblast growth factor receptor 3 Kinase Kd 6.54 CHEMBL
Rho-associated protein kinase 1 Kinase Kd 6.34 CHEMBL
Focal adhesion kinase 1 Kinase Kd 6.36 CHEMBL
Tyrosine-protein kinase HCK Kinase Kd 6.06 CHEMBL
Tyrosine-protein kinase JAK1 Kinase Kd 8.05 CHEMBL
Mitogen-activated protein kinase 10 Kinase Kd 5.37 CHEMBL
Death-associated protein kinase 2 Kinase Kd 6.82 CHEMBL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform Kinase IC50 4.92 CHEMBL
High affinity nerve growth factor receptor Kinase Kd 7 CHEMBL
Tyrosine-protein kinase JAK2 Kinase Kd 6.39 CHEMBL
Rho-associated protein kinase 2 Kinase Kd 6.85 CHEMBL
Protein kinase C alpha type Kinase Kd 5.22 CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit delta Kinase Kd 6.38 CHEMBL
Myosin light chain kinase 2, skeletal/cardiac muscle Kinase Kd 7.31 CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit gamma Kinase Kd 6.36 CHEMBL
AP2-associated protein kinase 1 Kinase Kd 7.96 CHEMBL
Serine/threonine-protein kinase MARK2 Kinase Kd 6.51 CHEMBL
Hepatocyte growth factor receptor Kinase Kd 5.92 CHEMBL
Tyrosine-protein kinase Lyn Kinase Kd 6.57 CHEMBL
Serine/threonine-protein kinase Nek2 Kinase Kd 6.30 CHEMBL
Serine/threonine-protein kinase D3 Kinase Kd 6.55 CHEMBL
Ribosomal protein S6 kinase alpha-2 Kinase Kd 7.77 CHEMBL
5'-AMP-activated protein kinase catalytic subunit alpha-1 Kinase Kd 7.72 CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit beta Kinase Kd 5.85 CHEMBL
Fibroblast growth factor receptor 1 Kinase Kd 6.28 CHEMBL
Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform Kinase Kd 8.26 CHEMBL
Cyclin-dependent-like kinase 5 Kinase Kd 5.16 CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit alpha Kinase Kd 7.10 CHEMBL
Serine/threonine-protein kinase 17B Kinase Kd 6.96 CHEMBL
Serine/threonine-protein kinase 10 Kinase Kd 7.72 CHEMBL
Tyrosine-protein kinase Fer Kinase Kd 5.96 CHEMBL
Serine/threonine-protein kinase PLK4 Kinase Kd 6.72 CHEMBL
Aurora kinase C Kinase Kd 6.66 CHEMBL
Serine/threonine-protein kinase 16 Kinase Kd 6.60 CHEMBL
Dual specificity protein kinase TTK Kinase Kd 7.20 CHEMBL
Abelson tyrosine-protein kinase 2 Kinase Kd 6 CHEMBL
Ephrin type-A receptor 5 Kinase Kd 5.92 CHEMBL
Fibroblast growth factor receptor 2 Kinase Kd 6.28 CHEMBL
Serine/threonine-protein kinase N1 Kinase Kd 6.15 CHEMBL
Protein kinase C theta type Kinase Kd 5.37 CHEMBL
Serine/threonine-protein kinase 17A Kinase Kd 9 CHEMBL
Ephrin type-A receptor 6 Kinase Kd 6.02 CHEMBL
TRAF2 and NCK-interacting protein kinase Kinase Kd 7.60 CHEMBL
Casein kinase I isoform epsilon Kinase Kd 7.89 CHEMBL
Tyrosine-protein kinase Fgr Kinase Kd 6.57 CHEMBL
Aurora kinase A Kinase Kd 5.77 CHEMBL
ALK tyrosine kinase receptor Kinase Kd 6.77 CHEMBL
Ephrin type-A receptor 3 Kinase Kd 5.68 CHEMBL
BMP-2-inducible protein kinase Kinase Kd 8.26 CHEMBL
Serine/threonine-protein kinase pim-2 Kinase Kd 5.30 CHEMBL
Tyrosine-protein kinase FRK Kinase Kd 6.28 CHEMBL
Dual specificity protein kinase CLK1 Kinase Kd 7.66 CHEMBL
Dual specificity protein kinase CLK2 Kinase Kd 7.70 CHEMBL
Serine/threonine-protein kinase 38-like Kinase Kd 6.01 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 5 Kinase Kd 7.39 CHEMBL
Mitogen-activated protein kinase kinase kinase 4 Kinase Kd 5.48 CHEMBL
Cyclin-G-associated kinase Kinase Kd 7.70 CHEMBL
Ephrin type-B receptor 1 Kinase Kd 6.32 CHEMBL
Calcium/calmodulin-dependent protein kinase type 1D Kinase Kd 6.29 CHEMBL
Cyclin-dependent kinase 16 Kinase Kd 6.89 CHEMBL
Serine/threonine-protein kinase 4 Kinase Kd 7.72 CHEMBL
Activated CDC42 kinase 1 Kinase Kd 5.66 CHEMBL
Ribosomal protein S6 kinase alpha-5 Kinase Kd 7.77 CHEMBL
STE20-like serine/threonine-protein kinase Kinase Kd 7.25 CHEMBL
Dual specificity protein kinase CLK4 Kinase Kd 7.54 CHEMBL
MAP kinase-interacting serine/threonine-protein kinase 2 Kinase Kd 5.24 CHEMBL
Mitogen-activated protein kinase 9 Kinase Kd 5.62 CHEMBL
Calcium/calmodulin-dependent protein kinase kinase 2 Kinase Kd 5.82 CHEMBL
MAP/microtubule affinity-regulating kinase 3 Kinase Kd 6.39 CHEMBL
Calcium/calmodulin-dependent protein kinase kinase 1 Kinase Kd 6.38 CHEMBL
Calcium/calmodulin-dependent protein kinase type 1G Kinase Kd 6.36 CHEMBL
Epithelial discoidin domain-containing receptor 1 Kinase Kd 5.70 CHEMBL
Solute carrier family 22 member 1 Transporter IC50 5.21 CHEMBL
Testis-specific serine/threonine-protein kinase 1 Kinase Kd 5.20 CHEMBL
3-phosphoinositide-dependent protein kinase 1 Kinase Kd 5.46 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 1 Kinase Kd 6.89 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 2 Kinase Kd 6.96 CHEMBL
Tyrosine-protein kinase ITK/TSK Kinase Kd 7.89 CHEMBL
Protein-tyrosine kinase 6 Kinase Kd 5.34 CHEMBL
Tyrosine-protein kinase BTK Kinase Kd 5.68 CHEMBL
Tyrosine-protein kinase receptor UFO Kinase Kd 8.05 CHEMBL
BDNF/NT-3 growth factors receptor Kinase Kd 6.23 CHEMBL
Tyrosine-protein kinase receptor TYRO3 Kinase Kd 7.31 CHEMBL
Cyclin-dependent kinase 7 Kinase Kd 6.48 CHEMBL
Serine/threonine-protein kinase D1 Kinase Kd 6.51 CHEMBL
Ribosomal protein S6 kinase beta-1 Kinase Kd 7.32 CHEMBL
Serine/threonine-protein kinase N2 Kinase Kd 5.89 CHEMBL
RAC-beta serine/threonine-protein kinase Kinase Kd 5.57 CHEMBL
Serine/threonine-protein kinase DCLK3 Kinase Kd 6.96 CHEMBL
Serine/threonine-protein kinase 3 Kinase Kd 7.25 CHEMBL
Ribosomal protein S6 kinase alpha-6 Kinase Kd 5.62 CHEMBL
NUAK family SNF1-like kinase 2 Kinase Kd 6.82 CHEMBL
Non-receptor tyrosine-protein kinase TNK1 Kinase Kd 6.17 CHEMBL
Non-receptor tyrosine-protein kinase TYK2 Kinase Kd 6.44 CHEMBL
Serine/threonine-protein kinase Chk1 Kinase Kd 6.52 CHEMBL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Kinase IC50 4.96 CHEMBL
Ankyrin repeat and protein kinase domain-containing protein 1 Kinase Kd 6.51 CHEMBL
Serine/threonine-protein kinase PAK 3 Kinase Kd 7.80 CHEMBL
Cyclin-dependent kinase 17 Kinase Kd 5.92 CHEMBL
Cyclin-dependent kinase 18 Kinase Kd 5.77 CHEMBL
Cyclin-dependent kinase 14 Kinase Kd 6.57 CHEMBL
Phosphatidylinositol 4-phosphate 5-kinase type-1 alpha Kinase Kd 5.27 CHEMBL
Phosphatidylinositol 5-phosphate 4-kinase type-2 beta Kinase Kd 7.41 CHEMBL
Myosin light chain kinase family member 4 Kinase Kd 7.82 CHEMBL
Wee1-like protein kinase Kinase Kd 5.96 CHEMBL
Serine/threonine-protein kinase 25 Kinase Kd 6.54 CHEMBL
Protein-tyrosine kinase 2-beta Kinase Kd 7.09 CHEMBL
Serine/threonine-protein kinase RIO1 Kinase Kd 7.46 CHEMBL
Casein kinase I isoform alpha-like Kinase Kd 6.26 CHEMBL
Casein kinase I isoform delta Kinase Kd 7.82 CHEMBL
Casein kinase I isoform gamma-2 Kinase Kd 6.96 CHEMBL
Casein kinase I isoform gamma-3 Kinase Kd 6.62 CHEMBL
Tyrosine-protein kinase receptor Tie-1 Kinase Kd 5.41 CHEMBL
Serine/threonine-protein kinase tousled-like 1 Kinase Kd 6.13 CHEMBL
Serine/threonine-protein kinase tousled-like 2 Kinase Kd 6.48 CHEMBL
NT-3 growth factor receptor Kinase Kd 5.29 CHEMBL
Casein kinase II subunit alpha Kinase Kd 7.09 CHEMBL
Casein kinase II subunit alpha' Kinase Kd 6.80 CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 1B Kinase Kd 5.64 CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit epsilon Kinase Kd 6.21 CHEMBL
Serine/threonine-protein kinase STK11 Kinase Kd 7.42 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 3 Kinase Kd 5.77 CHEMBL
Maternal embryonic leucine zipper kinase Kinase Kd 6.46 CHEMBL
MAP kinase-interacting serine/threonine-protein kinase 1 Kinase Kd 5.41 CHEMBL
Serine/threonine-protein kinase 26 Kinase Kd 6.47 CHEMBL
Serine/threonine-protein kinase Nek7 Kinase Kd 5.39 CHEMBL
Eukaryotic translation initiation factor 2-alpha kinase 4 Kinase Kd 6.74 CHEMBL
Insulin receptor-related protein Kinase Kd 6.37 CHEMBL
Interleukin-1 receptor-associated kinase 3 Kinase Kd 6.03 CHEMBL
Serine/threonine-protein kinase RIO3 Kinase Kd 5.42 CHEMBL
Serine/threonine-protein kinase SIK2 Kinase Kd 6.24 CHEMBL
SRSF protein kinase 1 Kinase Kd 6.60 CHEMBL
SRSF protein kinase 2 Kinase Kd 6.72 CHEMBL
Serine/threonine-protein kinase 33 Kinase Kd 7.77 CHEMBL
5'-AMP-activated protein kinase catalytic subunit alpha-2 Kinase Kd 7.05 CHEMBL
Discoidin domain-containing receptor 2 Kinase Kd 5.54 CHEMBL
Serine/threonine-protein kinase LATS1 Kinase Kd 6.20 CHEMBL
Serine/threonine-protein kinase LATS2 Kinase Kd 6.34 CHEMBL
Leukocyte tyrosine kinase receptor Kinase Kd 5.74 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 1 Kinase Kd 7.80 CHEMBL
Serine/threonine-protein kinase PAK 6 Kinase Kd 5.62 CHEMBL
Serine/threonine-protein kinase PAK 7 Kinase Kd 6.19 CHEMBL
NUAK family SNF1-like kinase 1 Kinase Kd 7.32 CHEMBL
Serine/threonine-protein kinase pim-3 Kinase Kd 5.62 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 3 Kinase Kd 6.74 CHEMBL
Aurora kinase B Kinase Kd 6.42 CHEMBL
Tyrosine-protein kinase Blk Kinase Kd 7.19 CHEMBL
Bone morphogenetic protein receptor type-2 Kinase Kd 6.24 CHEMBL
Serine/threonine-protein kinase BRSK1 Kinase Kd 5.46 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 4 Kinase Kd 6.85 CHEMBL
Serine/threonine-protein kinase MARK1 Kinase Kd 5.92 CHEMBL
MAP/microtubule affinity-regulating kinase 4 Kinase Kd 5.44 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 4 Kinase Kd 6.15 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 6 Kinase Kd 5.28 CHEMBL
Tyrosine-protein kinase Mer Kinase Kd 7.59 CHEMBL
Calcium/calmodulin-dependent protein kinase type IV Kinase Kd 6.05 CHEMBL
Mitogen-activated protein kinase kinase kinase 9 Kinase Kd 5.47 CHEMBL
Mitogen-activated protein kinase kinase kinase 11 Kinase Kd 5.89 CHEMBL
Serine/threonine-protein kinase 24 Kinase Kd 7.20 CHEMBL
Muscle, skeletal receptor tyrosine-protein kinase Kinase Kd 6.31 CHEMBL
Citron Rho-interacting kinase Kinase Kd 5.41 CHEMBL
Casein kinase I isoform gamma-1 Kinase Kd 6.03 CHEMBL
Death-associated protein kinase 1 Kinase Kd 6.92 CHEMBL
Serine/threonine-protein kinase DCLK1 Kinase Kd 6.43 CHEMBL
Serine/threonine-protein kinase DCLK2 Kinase Kd 5.57 CHEMBL
Myosin-IIIa Kinase Kd 5.51 CHEMBL
Myosin-IIIb Kinase Kd 5.35 CHEMBL
Serine/threonine-protein kinase PAK 4 Kinase Kd 5.64 CHEMBL
Serine/threonine-protein kinase BRSK2 Kinase Kd 5.96 CHEMBL
Cyclin-dependent kinase 3 Kinase Kd 5.99 CHEMBL
Serine/threonine-protein kinase SIK1 Kinase Kd 5.49 CHEMBL
Mitogen-activated protein kinase 7 Kinase Kd 5 CHEMBL
Serine/threonine-protein kinase D2 Kinase Kd 6.42 CHEMBL
Interferon-induced, double-stranded RNA-activated protein kinase Kinase Kd 6.17 CHEMBL
Receptor-interacting serine/threonine-protein kinase 1 Kinase Kd 6.43 CHEMBL
Tyrosine-protein kinase Fes/Fps Kinase Kd 6.02 CHEMBL
Fibroblast growth factor receptor 4 Kinase Kd 5.68 CHEMBL
Ribosomal protein S6 kinase alpha-1 Kinase Kd 7.02 CHEMBL
Ribosomal protein S6 kinase alpha-4 Kinase Kd 7.02 CHEMBL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Kinase IC50 4.89 CHEMBL
Casein kinase I isoform alpha Kinase Kd 7 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 2 Kinase Kd 7.48 CHEMBL
Misshapen-like kinase 1 Kinase Kd 7.54 CHEMBL
Serine/threonine-protein kinase TBK1 Kinase Kd 6.92 CHEMBL
Interleukin-1 receptor-associated kinase 4 Kinase Kd 7.18 CHEMBL
Cyclin-dependent kinase 4 Kinase Kd 5.70 CHEMBL
Cyclin-dependent kinase-like 2 Kinase Kd 5.96 CHEMBL
Serine/threonine-protein kinase Chk2 Kinase Kd 8.15 CHEMBL
Protein delta homolog 1 Membrane other Kd 7 CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 1A Kinase Kd 6.70 CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 2 Kinase Kd 6.17 CHEMBL
Ephrin type-B receptor 6 Kinase Kd 6.07 CHEMBL
Serine/threonine-protein kinase/endoribonuclease IRE1 Kinase Kd 6.22 CHEMBL
Rhodopsin kinase Kinase Kd 6.54 CHEMBL
G protein-coupled receptor kinase 4 Kinase Kd 6.85 CHEMBL
G protein-coupled receptor kinase 7 Kinase Kd 6.74 CHEMBL
Homeodomain-interacting protein kinase 2 Kinase Kd 7.51 CHEMBL
Homeodomain-interacting protein kinase 3 Kinase Kd 7.39 CHEMBL
Homeodomain-interacting protein kinase 4 Kinase Kd 6.80 CHEMBL
Hormonally up-regulated neu tumor-associated kinase Kinase Kd 6.30 CHEMBL
Serine/threonine-protein kinase ICK Kinase Kd 6.33 CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit alpha Kinase Kd 6.28 CHEMBL
Interleukin-1 receptor-associated kinase 1 Kinase Kd 7.85 CHEMBL
Mitogen-activated protein kinase kinase kinase 13 Kinase Kd 7.02 CHEMBL
Mitogen-activated protein kinase kinase kinase 2 Kinase Kd 7.24 CHEMBL
Mitogen-activated protein kinase kinase kinase 3 Kinase Kd 6.66 CHEMBL
Microtubule-associated serine/threonine-protein kinase 1 Kinase Kd 6.70 CHEMBL
Serine/threonine-protein kinase 38 Kinase Kd 6.39 CHEMBL
Serine/threonine-protein kinase NIM1 Kinase Kd 6.07 CHEMBL
Serine/threonine-protein kinase OSR1 Kinase Kd 6.28 CHEMBL
U4/U6 small nuclear ribonucleoprotein Prp4 Nuclear other Kd 6.41 CHEMBL
Serine/threonine-protein kinase RIO2 Kinase Kd 7.31 CHEMBL
SRSF protein kinase 3 Kinase Kd 7.23 CHEMBL
STE20/SPS1-related proline-alanine-rich protein kinase Kinase Kd 6.85 CHEMBL
Mitogen-activated protein kinase kinase kinase 7 Kinase Kd 7.03 CHEMBL
Serine/threonine-protein kinase TAO1 Kinase Kd 6.05 CHEMBL
Serine/threonine-protein kinase TAO3 Kinase Kd 6.68 CHEMBL
Serine/threonine-protein kinase ULK1 Kinase Kd 7.64 CHEMBL
Serine/threonine-protein kinase ULK2 Kinase Kd 7.89 CHEMBL
Serine/threonine-protein kinase ULK3 Kinase Kd 7.38 CHEMBL
Epidermal growth factor receptor Kinase Kd 6.07 CHEMBL
Homeodomain-interacting protein kinase 1 Kinase Kd 7.26 CHEMBL
Mitogen-activated protein kinase kinase kinase 15 Kinase Kd 5.89 CHEMBL
Serine/threonine-protein kinase PLK2 Kinase Kd 5.33 CHEMBL
Receptor-interacting serine/threonine-protein kinase 4 Kinase Kd 5.68 CHEMBL
Uncharacterized serine/threonine-protein kinase SBK3 Kinase Kd 5.72 CHEMBL
Serine/threonine-protein kinase 35 Kinase Kd 5.89 CHEMBL
Tankyrase-2 Enzyme Kd 5.05 CHEMBL
Megakaryocyte-associated tyrosine-protein kinase Kinase Kd 5.11 CHEMBL
Bone morphogenetic protein receptor type-1B Kinase Kd 5.62 CHEMBL
Serine/threonine-protein kinase SBK1 Kinase Kd 6.70 CHEMBL
Serine/threonine-protein kinase PRP4 homolog Kinase Kd 6.41 CHEMBL
Mitogen-activated protein kinase kinase kinase 12 Kinase Kd 7 CHEMBL
Serine/threonine-protein kinase Sgk3 Kinase Kd 6.66 CHEMBL
SNF-related serine/threonine-protein kinase Kinase Kd 6.19 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 5 Kinase Kd 7.34 CHEMBL
Myosin light chain kinase 3 Kinase Kd 7.64 CHEMBL
Leucine-rich repeat serine/threonine-protein kinase 2 Kinase Kd 7.12 CHEMBL
Dual serine/threonine and tyrosine protein kinase Kinase Kd 5.89 CHEMBL
Bromodomain-containing protein 9 Nuclear other Kd 4.77 CHEMBL
Mitotic checkpoint serine/threonine-protein kinase BUB1 Kinase Kd 5.46 CHEMBL
TFIIH basal transcription factor complex helicase XPD subunit Enzyme Kd 5.91 CHEMBL
G protein-coupled receptor kinase 6 Kinase Kd 5.79 CHEMBL
5'-AMP-activated protein kinase subunit gamma-1 Kinase Kd 5.94 CHEMBL
Uncharacterized protein FLJ45252 Unclassified Kd 6.37 CHEMBL
5'-AMP-activated protein kinase subunit gamma-2 Kinase Kd 5.76 CHEMBL
G protein-coupled receptor kinase 5 Kinase IC50 6.08 CHEMBL
Ephrin type-A receptor 7 Kinase Kd 5.62 SCIENTIFIC LITERATURE
Ephrin type-B receptor 4 Kinase Kd 5.51 SCIENTIFIC LITERATURE
Mitogen-activated protein kinase kinase kinase 19 Kinase Kd 7.77 CHEMBL
Tyrosine-protein kinase JAK3 Kinase Kd 5.92 CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 6.30 CHEMBL
ATP-binding cassette sub-family G member 2 Transporter IC50 5.52 CHEMBL
Acetylcholinesterase Enzyme IC50 5.23 CHEMBL
Ribosyldihydronicotinamide dehydrogenase [quinone] Enzyme Kd 5.40 CHEMBL
Tyrosine-protein kinase ABL1 Kinase Kd 7.26 CHEMBL
Pyridoxal kinase Kinase Kd 5.22 CHEMBL
Proto-oncogene tyrosine-protein kinase Src Kinase Kd 5.68 CHEMBL
Serine/threonine-protein kinase 3 Kinase Kd 6.80 CHEMBL
Serine/threonine-protein kinase ULK3 Kinase Kd 6.96 CHEMBL
Proto-oncogene tyrosine-protein kinase Src Kinase IC50 6.26 CHEMBL
Myosin light chain kinase, smooth muscle Kinase Kd 7.64 CHEMBL
Calcium-dependent protein kinase 1 Kinase Kd 5.89 CHEMBL
Vascular endothelial growth factor receptor 2 Kinase IC50 7.14 CHEMBL
Serine/threonine-protein kinase PknB Kinase Kd 7.06 CHEMBL
Macrophage colony-stimulating factor 1 receptor Kinase IC50 8.39 CHEMBL

External reference:

IDSource
4025079 VUID
N0000175350 NUI
D06402 KEGG_DRUG
341031-54-7 SECONDARY_CAS_RN
4025079 VANDF
4025080 VANDF
C1176020 UMLSCUI
CHEBI:38940 CHEBI
B49 PDB_CHEM_ID
CHEMBL535 ChEMBL_ID
CHEMBL1567 ChEMBL_ID
D000077210 MESH_DESCRIPTOR_UI
DB01268 DRUGBANK_ID
5329102 PUBCHEM_CID
5713 IUPHAR_LIGAND_ID
8646 INN_ID
V99T50803M UNII
357977 RXNORM
20930 MMSL
21012 MMSL
349534 MMSL
75586 MMSL
d05717 MMSL
011192 NDDF
011193 NDDF
421192001 SNOMEDCT_US
421448007 SNOMEDCT_US
426455008 SNOMEDCT_US
V99T50803M INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
SUTENT HUMAN PRESCRIPTION DRUG LABEL 1 0069-0550 CAPSULE 12.50 mg ORAL NDA 33 sections
SUTENT HUMAN PRESCRIPTION DRUG LABEL 1 0069-0770 CAPSULE 25 mg ORAL NDA 33 sections
SUTENT HUMAN PRESCRIPTION DRUG LABEL 1 0069-0830 CAPSULE 37.50 mg ORAL NDA 33 sections
SUTENT HUMAN PRESCRIPTION DRUG LABEL 1 0069-0980 CAPSULE 50 mg ORAL NDA 33 sections
Sunitinib Malate HUMAN PRESCRIPTION DRUG LABEL 1 0093-8199 CAPSULE 12.50 mg ORAL ANDA 30 sections
Sunitinib Malate HUMAN PRESCRIPTION DRUG LABEL 1 0093-8224 CAPSULE 25 mg ORAL ANDA 30 sections
Sunitinib Malate HUMAN PRESCRIPTION DRUG LABEL 1 0093-8229 CAPSULE 37.50 mg ORAL ANDA 30 sections
Sunitinib Malate HUMAN PRESCRIPTION DRUG LABEL 1 0093-8231 CAPSULE 50 mg ORAL ANDA 30 sections
Sunitinib Malate HUMAN PRESCRIPTION DRUG LABEL 1 0378-6678 CAPSULE 12.50 mg ORAL ANDA 30 sections
Sunitinib Malate HUMAN PRESCRIPTION DRUG LABEL 1 0378-6679 CAPSULE 25 mg ORAL ANDA 30 sections
Sunitinib Malate HUMAN PRESCRIPTION DRUG LABEL 1 0378-6680 CAPSULE 50 mg ORAL ANDA 30 sections
Sunitinib Malate HUMAN PRESCRIPTION DRUG LABEL 1 0378-6681 CAPSULE 37.50 mg ORAL ANDA 30 sections
Sunitinib malate HUMAN PRESCRIPTION DRUG LABEL 1 16714-676 CAPSULE 12.50 mg ORAL ANDA 28 sections
Sunitinib malate HUMAN PRESCRIPTION DRUG LABEL 1 16714-677 CAPSULE 25 mg ORAL ANDA 28 sections
Sunitinib malate HUMAN PRESCRIPTION DRUG LABEL 1 16714-678 CAPSULE 37.50 mg ORAL ANDA 28 sections
Sunitinib malate HUMAN PRESCRIPTION DRUG LABEL 1 16714-679 CAPSULE 50 mg ORAL ANDA 28 sections
Sunitinib Malate HUMAN PRESCRIPTION DRUG LABEL 1 42291-901 CAPSULE 12.50 mg ORAL ANDA 31 sections
Sunitinib Malate HUMAN PRESCRIPTION DRUG LABEL 1 42291-902 CAPSULE 25 mg ORAL ANDA 31 sections
Sunitinib Malate HUMAN PRESCRIPTION DRUG LABEL 1 42291-903 CAPSULE 37.50 mg ORAL ANDA 31 sections
Sunitinib Malate HUMAN PRESCRIPTION DRUG LABEL 1 42291-904 CAPSULE 50 mg ORAL ANDA 31 sections
SUNITINIB MALATE HUMAN PRESCRIPTION DRUG LABEL 1 43598-045 CAPSULE 12.50 mg ORAL ANDA 28 sections
SUNITINIB MALATE HUMAN PRESCRIPTION DRUG LABEL 1 43598-046 CAPSULE 25 mg ORAL ANDA 28 sections
SUNITINIB MALATE HUMAN PRESCRIPTION DRUG LABEL 1 43598-047 CAPSULE 37.50 mg ORAL ANDA 28 sections
SUNITINIB MALATE HUMAN PRESCRIPTION DRUG LABEL 1 43598-048 CAPSULE 50 mg ORAL ANDA 28 sections
SUNITINIB MALATE Human Prescription Drug Label 1 59651-464 CAPSULE 12.50 mg ORAL ANDA 28 sections
SUNITINIB MALATE Human Prescription Drug Label 1 59651-465 CAPSULE 25 mg ORAL ANDA 28 sections
SUNITINIB MALATE Human Prescription Drug Label 1 59651-466 CAPSULE 37.50 mg ORAL ANDA 28 sections
SUNITINIB MALATE Human Prescription Drug Label 1 59651-467 CAPSULE 50 mg ORAL ANDA 28 sections
Sunitinib malate HUMAN PRESCRIPTION DRUG LABEL 1 63304-091 CAPSULE 12.50 mg ORAL ANDA 28 sections
Sunitinib malate HUMAN PRESCRIPTION DRUG LABEL 1 63304-092 CAPSULE 25 mg ORAL ANDA 28 sections