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

Stem definitionDrug idCAS RN
angiogenesis inhibitors 4118 444731-52-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • GW786034B
  • pazopanib
  • votrient
  • GW 786034
  • pazopanib hydrochloride
  • pazopanib HCl
Pazopanib is a multi-tyrosine kinase inhibitor of vascular endothelial growth factor receptor (VEGFR)-1, VEGFR-2, VEGFR-3, platelet-derived growth factor receptor (PDGFR)-α and -β, fibroblast growth factor receptor (FGFR)-1 and -3, cytokine receptor (Kit), interleukin-2 receptor-inducible T-cell kinase (Itk), leukocyte-specific protein tyrosine kinase (Lck), and transmembrane glycoprotein receptor tyrosine kinase (c-Fms). In vitro, pazopanib inhibited ligand-induced autophosphorylation of VEGFR-2, Kit, and PDGFR-β receptors. In vivo, pazopanib inhibited VEGF-induced VEGFR-2 phosphorylation in mouse lungs, angiogenesis in a mouse model, and the growth of some human tumor xenografts in mice.
  • Molecular weight: 437.52
  • Formula: C21H23N7O2S
  • CLOGP: 3.50
  • LIPINSKI: 0
  • HAC: 9
  • HDO: 2
  • TPSA: 119.03
  • ALOGS: -4
  • ROTB: 5
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.80 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Hosey CM, Chan R, Benet LZ
Vd (Volume of distribution) 0.16 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 0.06 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.01 % Lombardo F, Berellini G, Obach RS
S (Water solubility) 0.00 mg/mL Bocci G, Oprea TI, Benet LZ

Approvals:

DateAgencyCompanyOrphan
June 14, 2010 EMA
Oct. 19, 2009 FDA NOVARTIS PHARMS CORP

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
Malignant neoplasm progression 775.09 22.04 362 12471 81759 63394430
Hair colour changes 484.57 22.04 115 12718 3012 63473177
Death 451.73 22.04 460 12373 373921 63102268
Diarrhoea 382.10 22.04 583 12250 714783 62761406
Hypertension 244.83 22.04 291 12542 279012 63197177
Nausea 155.72 22.04 449 12384 854022 62622167
Disease progression 150.77 22.04 153 12680 122605 63353584
Product use in unapproved indication 150.59 22.04 183 12650 178897 63297292
Decreased appetite 135.73 22.04 207 12626 250845 63225344
Fatigue 125.87 22.04 428 12405 887600 62588589
Hepatic function abnormal 124.17 22.04 83 12750 37059 63439130
Palmar-plantar erythrodysaesthesia syndrome 105.95 22.04 63 12770 22952 63453237
Desmoplastic small round cell tumour 105.02 22.04 18 12815 78 63476111
Metastases to lung 103.91 22.04 51 12782 12699 63463490
Metastases to peritoneum 83.65 22.04 30 12803 3412 63472777
Metastases to liver 72.26 22.04 50 12783 23589 63452600
Hypothyroidism 67.11 22.04 61 12772 42571 63433618
Vomiting 62.92 22.04 251 12582 559366 62916823
Jaundice 58.50 22.04 48 12785 29203 63446986
Blood bilirubin increased 58.17 22.04 53 12780 37087 63439102
Alanine aminotransferase increased 57.91 22.04 87 12746 103683 63372506
Blood pressure increased 57.46 22.04 111 12722 161951 63314238
Aspartate aminotransferase increased 55.16 22.04 79 12754 90198 63385991
Dysgeusia 55.01 22.04 57 12776 46653 63429536
Metastases to lymph nodes 52.97 22.04 28 12805 8130 63468059
Posterior reversible encephalopathy syndrome 51.39 22.04 36 12797 17309 63458880
Drug hypersensitivity 50.82 22.04 3 12830 310684 63165505
Transaminases increased 49.59 22.04 45 12788 31322 63444867
Metastases to pancreas 46.42 22.04 11 12822 285 63475904
Proteinuria 45.98 22.04 35 12798 19110 63457079
Ascites 44.92 22.04 48 12785 40680 63435509
Blood thyroid stimulating hormone increased 41.98 22.04 23 12810 7171 63469018
Pneumothorax 41.88 22.04 31 12802 16230 63459959
Ageusia 41.86 22.04 29 12804 13699 63462490
Hepatotoxicity 41.46 22.04 44 12789 36997 63439192
Metastases to central nervous system 40.70 22.04 28 12805 13077 63463112
Condition aggravated 39.46 22.04 16 12817 402201 63073988
Hypertensive crisis 39.05 22.04 29 12804 15257 63460932
Joint swelling 37.45 22.04 10 12823 327656 63148533
Neoplasm progression 36.81 22.04 41 12792 36387 63439802
Hypersensitivity 35.26 22.04 8 12825 292677 63183512
Peripheral artery haematoma 32.96 22.04 6 12827 39 63476150
Sinusitis 32.13 22.04 4 12829 226649 63249540
Asthenia 30.84 22.04 156 12677 383448 63092741
Neurofibrosarcoma 30.50 22.04 7 12826 157 63476032
Intestinal transit time abnormal 29.82 22.04 6 12827 70 63476119
Treatment failure 29.50 22.04 3 12830 199040 63277149
Cell death 29.24 22.04 13 12820 2588 63473601
Hyperthyroidism 29.16 22.04 24 12809 14649 63461540
Platelet count decreased 28.96 22.04 69 12764 116053 63360136
Pleural effusion 27.25 22.04 59 12774 93151 63383038
Left ventricular dysfunction 26.79 22.04 21 12812 11967 63464222
Tumour pain 25.68 22.04 10 12823 1427 63474762
Nephrotic syndrome 24.96 22.04 15 12818 5561 63470628
Concomitant disease aggravated 24.89 22.04 18 12815 9094 63467095
Thrombocytopenia 24.81 22.04 77 12756 151080 63325109
Amylase increased 23.18 22.04 15 12818 6330 63469859
Liver disorder 23.07 22.04 40 12793 53647 63422542
Weight increased 23.02 22.04 12 12821 260780 63215409
Dehydration 22.85 22.04 82 12751 173272 63302917
Wound 22.84 22.04 3 12830 163260 63312929
Cardiac failure 22.25 22.04 53 12780 89089 63387100

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
Hair colour changes 878.86 18.36 204 18802 1673 34936252
Malignant neoplasm progression 771.76 18.36 519 18487 87527 34850398
Diarrhoea 595.11 18.36 879 18127 389033 34548892
Death 368.70 18.36 720 18286 397329 34540596
Decreased appetite 274.18 18.36 391 18615 166001 34771924
Fatigue 229.93 18.36 572 18434 370081 34567844
Metastases to lung 212.55 18.36 103 18903 9217 34928708
Hypertension 203.22 18.36 306 18700 136137 34801788
Palmar-plantar erythrodysaesthesia syndrome 180.69 18.36 113 18893 16682 34921243
Nausea 168.20 18.36 483 18523 339425 34598500
Disease progression 154.52 18.36 238 18768 107839 34830086
Dysgeusia 138.56 18.36 115 18891 26382 34911543
Hypothyroidism 87.61 18.36 80 18926 20822 34917103
Pneumothorax 79.87 18.36 73 18933 19019 34918906
Product use in unapproved indication 78.13 18.36 187 18819 117312 34820613
Metastases to bone 75.45 18.36 58 18948 11912 34926013
Off label use 68.08 18.36 77 18929 419447 34518478
Blood pressure increased 65.99 18.36 147 18859 87955 34849970
Hepatic enzyme increased 65.68 18.36 93 18913 38987 34898938
Metastases to central nervous system 63.51 18.36 45 18961 8160 34929765
Proteinuria 62.32 18.36 63 18943 18579 34919346
Soft tissue sarcoma 61.64 18.36 13 18993 64 34937861
Weight decreased 61.57 18.36 223 18783 176078 34761847
Jaundice 59.79 18.36 80 18926 31802 34906123
Ageusia 58.60 18.36 47 18959 10261 34927664
Blood thyroid stimulating hormone increased 57.05 18.36 33 18973 4222 34933703
Hepatic function abnormal 52.74 18.36 90 18916 44273 34893652
Vomiting 50.91 18.36 267 18739 247354 34690571
Metastases to liver 49.03 18.36 48 18958 13615 34924310
Metastatic renal cell carcinoma 47.63 18.36 23 18983 2038 34935887
Therapy cessation 47.18 18.36 52 18954 16921 34921004
Blood bilirubin increased 45.92 18.36 78 18928 38218 34899707
Tumour pain 43.93 18.36 18 18988 1079 34936846
Alanine aminotransferase increased 43.65 18.36 119 18887 80696 34857229
Hypotension 42.43 18.36 35 18971 221614 34716311
Nephrotic syndrome 40.87 18.36 33 18973 7270 34930655
Neoplasm progression 39.95 18.36 56 18950 23244 34914681
Skin depigmentation 39.30 18.36 13 18993 423 34937502
Metastases to lymph nodes 39.08 18.36 27 18979 4701 34933224
Abdominal pain upper 38.33 18.36 105 18901 71385 34866540
Synovial sarcoma metastatic 37.31 18.36 7 18999 16 34937909
Stomatitis 36.46 18.36 75 18931 42439 34895486
Hepatotoxicity 34.42 18.36 50 18956 21435 34916490
Liver function test increased 34.37 18.36 41 18965 14524 34923401
Taste disorder 33.16 18.36 29 18977 7126 34930799
Activated partial thromboplastin time abnormal 33.13 18.36 9 18997 146 34937779
Pulmonary necrosis 33.05 18.36 11 18995 365 34937560
Renal cancer metastatic 32.98 18.36 12 18994 521 34937404
Condition aggravated 32.45 18.36 34 18972 192162 34745763
Fall 31.95 18.36 38 18968 202847 34735078
Osteoma 31.16 18.36 8 18998 103 34937822
Polycystic liver disease 31.09 18.36 8 18998 104 34937821
Toxicity to various agents 31.05 18.36 38 18968 200324 34737601
Osteonecrosis of jaw 30.67 18.36 43 18963 17846 34920079
Splenic necrosis 30.28 18.36 8 18998 116 34937809
Febrile neutropenia 29.55 18.36 19 18987 136830 34801095
Haemoglobin urine present 29.55 18.36 8 18998 128 34937797
Splenic cyst 29.43 18.36 8 18998 130 34937795
Asthenia 28.98 18.36 230 18776 245021 34692904
Neoplasm recurrence 28.98 18.36 17 18989 2232 34935693
Renal cell carcinoma 28.65 18.36 23 18983 5025 34932900
Liver disorder 28.04 18.36 58 18948 32939 34904986
Metastases to soft tissue 27.66 18.36 10 18996 426 34937499
Renal cancer 27.42 18.36 27 18979 7708 34930217
Aspartate aminotransferase increased 27.29 18.36 90 18916 67693 34870232
Drug interaction 27.15 18.36 51 18955 225895 34712030
Skin hypopigmentation 27.09 18.36 9 18997 297 34937628
Overdose 26.97 18.36 8 18998 91051 34846874
Metastases to adrenals 25.54 18.36 12 18994 1000 34936925
Sepsis 25.36 18.36 32 18974 166529 34771396
Dysphonia 24.62 18.36 45 18961 23338 34914587
Blood alkaline phosphatase increased 24.41 18.36 53 18953 31122 34906803
Splenic lesion 24.22 18.36 8 18998 259 34937666
Pleural effusion 24.14 18.36 98 18908 81448 34856477
Drug hypersensitivity 23.99 18.36 7 18999 80522 34857403
Urinary sediment present 23.55 18.36 8 18998 283 34937642
Second primary malignancy 23.38 18.36 25 18981 7861 34930064
Abdominal discomfort 22.80 18.36 78 18928 59757 34878168
Eyelash discolouration 22.41 18.36 4 19002 6 34937919
Intestinal perforation 22.19 18.36 26 18980 9034 34928891
Somnolence 21.91 18.36 17 18989 111099 34826826
Lordosis 21.88 18.36 8 18998 352 34937573
Faeces pale 21.83 18.36 12 18994 1391 34936534
Glossodynia 21.33 18.36 17 18989 3676 34934249
Red blood cell abnormality 20.98 18.36 8 18998 396 34937529
COVID-19 20.90 18.36 8 18998 77542 34860383
Pneumonia 20.89 18.36 114 18892 362513 34575412
Tremor 19.92 18.36 10 18996 82577 34855348
Malignant connective tissue neoplasm 19.55 18.36 3 19003 0 34937925
Oxygen saturation decreased 19.45 18.36 3 19003 53815 34884110
Impaired healing 19.39 18.36 32 18974 15302 34922623
Pulmonary mass 19.34 18.36 29 18977 12783 34925142
Disseminated intravascular coagulation 19.30 18.36 39 18967 21777 34916148
Recurrent cancer 19.24 18.36 11 18995 1376 34936549
Hyperthyroidism 19.01 18.36 26 18980 10540 34927385
Blood bilirubin abnormal 19.01 18.36 9 18997 763 34937162
Gamma-glutamyltransferase increased 18.80 18.36 46 18960 29185 34908740

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
Malignant neoplasm progression 1193.58 17.84 648 23233 135342 79585165
Hair colour changes 748.90 17.84 187 23694 4045 79716462
Death 631.45 17.84 808 23073 565706 79154801
Diarrhoea 505.11 17.84 922 22959 879567 78840940
Hypertension 344.82 17.84 458 23423 330534 79389973
Disease progression 279.72 17.84 309 23572 184053 79536454
Metastases to lung 275.72 17.84 126 23755 18037 79702470
Decreased appetite 269.77 17.84 415 23466 342003 79378504
Palmar-plantar erythrodysaesthesia syndrome 219.85 17.84 132 23749 33002 79687505
Fatigue 174.74 17.84 641 23240 929086 78791421
Hepatic function abnormal 158.98 17.84 149 23732 72958 79647549
Nausea 148.89 17.84 622 23259 956574 78763933
Hypothyroidism 118.15 17.84 109 23772 52283 79668224
Metastases to liver 110.39 17.84 81 23800 28233 79692274
Pneumothorax 110.37 17.84 81 23800 28242 79692265
Jaundice 105.09 17.84 103 23778 53246 79667261
Product use in unapproved indication 104.42 17.84 231 23650 250128 79470379
Proteinuria 100.47 17.84 81 23800 32421 79688086
Metastases to lymph nodes 100.40 17.84 53 23828 10344 79710163
Blood bilirubin increased 98.44 17.84 110 23771 66122 79654385
Desmoplastic small round cell tumour 95.34 17.84 18 23863 93 79720414
Metastases to central nervous system 87.78 17.84 57 23824 16318 79704189
Alanine aminotransferase increased 82.93 17.84 163 23718 162407 79558100
Metastases to peritoneum 78.07 17.84 34 23847 4338 79716169
Dysgeusia 76.58 17.84 90 23791 57087 79663420
Blood thyroid stimulating hormone increased 75.78 17.84 43 23838 9665 79710842
Hepatotoxicity 72.40 17.84 83 23798 51269 79669238
Drug hypersensitivity 70.24 17.84 5 23876 298911 79421596
Therapy cessation 67.48 17.84 69 23812 37493 79683014
Metastases to bone 67.39 17.84 57 23824 24370 79696137
Aspartate aminotransferase increased 65.89 17.84 135 23746 138506 79582001
Metastatic renal cell carcinoma 64.92 17.84 25 23856 2330 79718177
Neoplasm progression 63.71 17.84 78 23803 51604 79668903
Blood pressure increased 63.49 17.84 172 23709 211188 79509319
Vomiting 61.91 17.84 375 23506 665453 79055054
Condition aggravated 56.12 17.84 41 23840 501083 79219424
Ageusia 54.70 17.84 43 23838 16589 79703918
Nephrotic syndrome 52.89 17.84 36 23845 11138 79709369
Hyperthyroidism 47.72 17.84 45 23836 22164 79698343
Hypertensive crisis 46.39 17.84 43 23838 20727 79699780
Soft tissue sarcoma 45.93 17.84 11 23870 198 79720309
Joint swelling 45.28 17.84 15 23866 288631 79431876
Fall 44.83 17.84 48 23833 487581 79232926
Tumour pain 44.73 17.84 19 23862 2280 79718227
Pleural effusion 43.37 17.84 118 23763 145144 79575363
Asthenia 42.36 17.84 280 23601 511409 79209098
Weight decreased 41.51 17.84 213 23668 354985 79365522
Off label use 38.57 17.84 141 23740 907074 78813433
Platelet count decreased 38.49 17.84 137 23744 194527 79525980
Transaminases increased 38.13 17.84 61 23820 51682 79668825
Osteonecrosis of jaw 36.11 17.84 54 23827 43172 79677335
Pulmonary mass 36.07 17.84 44 23837 28990 79691517
Overdose 35.90 17.84 6 23875 184200 79536307
Pulmonary necrosis 35.79 17.84 11 23870 519 79719988
Osteoma 35.55 17.84 8 23873 108 79720399
Hypotension 35.50 17.84 48 23833 440269 79280238
Retro-orbital neoplasm 35.26 17.84 7 23874 49 79720458
Therapeutic product effect decreased 35.09 17.84 4 23877 163859 79556648
Renal cancer 34.69 17.84 29 23852 12197 79708310
Neoplasm recurrence 33.79 17.84 19 23862 4195 79716312
Liver disorder 33.76 17.84 70 23811 72347 79648160
Disseminated intravascular coagulation 33.17 17.84 47 23834 35795 79684712
Ejection fraction decreased 32.98 17.84 46 23835 34531 79685976
Polycystic liver disease 32.37 17.84 8 23873 165 79720342
Splenic necrosis 32.10 17.84 8 23873 171 79720336
Hyperbilirubinaemia 31.83 17.84 38 23843 24480 79696027
Activated partial thromboplastin time abnormal 31.28 17.84 9 23872 337 79720170
COVID-19 31.03 17.84 5 23876 157669 79562838
Sinusitis 30.92 17.84 10 23871 195491 79525016
Renal cell carcinoma 30.68 17.84 21 23860 6557 79713950
Neurofibrosarcoma 30.32 17.84 8 23873 216 79720291
Metastases to soft tissue 30.23 17.84 10 23871 599 79719908
Urticaria 30.14 17.84 9 23872 185192 79535315
Hypersensitivity 29.90 17.84 21 23860 262218 79458289
Metastasis 29.82 17.84 21 23860 6859 79713648
Posterior reversible encephalopathy syndrome 29.72 17.84 38 23843 26243 79694264
Liver function test increased 29.45 17.84 47 23834 39726 79680781
Musculoskeletal stiffness 29.41 17.84 8 23873 175000 79545507
Splenic cyst 29.02 17.84 8 23873 256 79720251
Synovial sarcoma metastatic 28.40 17.84 5 23876 16 79720491
Ascites 28.40 17.84 67 23814 75495 79645012
Weight increased 28.12 17.84 25 23856 277361 79443146
Hepatic mass 28.01 17.84 14 23867 2437 79718070
Blood alkaline phosphatase increased 27.89 17.84 60 23821 63604 79656903
Intestinal transit time abnormal 27.47 17.84 6 23875 70 79720437
Renal impairment 26.97 17.84 106 23775 157677 79562830
Nasopharyngitis 26.81 17.84 22 23859 253859 79466648
Cardiac failure 26.44 17.84 104 23777 154738 79565769
Drug-induced liver injury 26.35 17.84 60 23821 66057 79654450
Arthralgia 26.16 17.84 86 23795 571717 79148790
Hepatic enzyme increased 26.00 17.84 116 23765 182494 79538013
Polycythaemia 25.97 17.84 13 23868 2271 79718236
Skin hypopigmentation 25.43 17.84 10 23871 985 79719522
Hepatic lesion 25.08 17.84 19 23862 6940 79713567
Tumour necrosis 25.03 17.84 12 23869 1910 79718597
Lordosis 24.79 17.84 8 23873 443 79720064
Thyroid function test abnormal 24.78 17.84 14 23867 3120 79717387
Renal cancer metastatic 24.67 17.84 9 23872 722 79719785
Prostatic specific antigen abnormal 24.62 17.84 8 23873 453 79720054
Gamma-glutamyltransferase increased 24.49 17.84 52 23829 54628 79665879
Peripheral artery haematoma 24.22 17.84 6 23875 125 79720382
Depression 23.88 17.84 18 23863 216772 79503735
Second primary malignancy 23.33 17.84 25 23856 14325 79706182
Treatment failure 23.20 17.84 11 23870 170475 79550032
Asthma 23.03 17.84 6 23875 135089 79585418
Thrombocytopenia 23.01 17.84 147 23734 265112 79455395
Splenic lesion 22.84 17.84 8 23873 570 79719937
Metastases to pancreas 22.81 17.84 8 23873 572 79719935
Mucosal inflammation 22.14 17.84 61 23820 75519 79644988
Bronchitis 21.90 17.84 6 23875 130638 79589869
Malignant connective tissue neoplasm 21.34 17.84 3 23878 0 79720507
Dehydration 21.19 17.84 137 23744 248050 79472457
Skin depigmentation 21.02 17.84 9 23872 1101 79719406
Intestinal perforation 20.98 17.84 26 23855 17400 79703107
Amylase increased 20.87 17.84 21 23860 11188 79709319
Loss of personal independence in daily activities 20.76 17.84 3 23878 102577 79617930
Red blood cell abnormality 20.69 17.84 8 23873 754 79719753
Metastases to spine 20.63 17.84 14 23867 4310 79716197
Muscle mass 20.58 17.84 7 23874 457 79720050
Left ventricular dysfunction 20.34 17.84 27 23854 19334 79701173
Renal cancer recurrent 20.33 17.84 5 23876 101 79720406
Metastases to adrenals 19.46 17.84 9 23872 1321 79719186
Cardiac ventricular scarring 19.26 17.84 3 23878 3 79720504
Anxiety 19.10 17.84 28 23853 248484 79472023
Pericarditis 19.01 17.84 4 23877 104232 79616275
Intentional product use issue 18.95 17.84 11 23870 152101 79568406
Haemoglobin urine present 18.94 17.84 8 23873 947 79719560
Tremor 18.88 17.84 14 23867 170069 79550438
Neoplasm 18.68 17.84 18 23863 9098 79711409
Blood bilirubin abnormal 18.63 17.84 9 23872 1456 79719051
Stomatitis 18.50 17.84 90 23791 146667 79573840
Wound 18.26 17.84 6 23875 116173 79604334
Peripheral swelling 18.26 17.84 33 23848 269584 79450923
Metastases to pelvis 18.15 17.84 7 23874 655 79719852

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EX03 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Other protein kinase inhibitors
FDA MoA N0000175076 Protein Kinase Inhibitors
FDA EPC N0000175605 Kinase Inhibitor
FDA MoA N0000182137 Cytochrome P450 2D6 Inhibitors
FDA MoA N0000182141 Cytochrome P450 3A4 Inhibitors
FDA MoA N0000187062 Cytochrome P450 2C8 Inhibitors
CHEBI has role CHEBI:35610 antineoplastic agents
CHEBI has role CHEBI:38637 tyrosine kinase inhibitors
CHEBI has role CHEBI:65207 vascular endothelial growth factor receptor inhibitors

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

DiseaseRelationSNOMED_IDDOID
Sarcoma of soft tissue indication 424952003
Renal cell carcinoma indication 702391001 DOID:4450
Hypocalcemia contraindication 5291005
Acute hemorrhage contraindication 8573003
Hyperbilirubinemia contraindication 14783006 DOID:2741
Myocardial infarction contraindication 22298006 DOID:5844
Proteinuria contraindication 29738008 DOID:576
Torsades de pointes contraindication 31722008
Gastrointestinal fistula contraindication 37831005
Hypertensive disorder contraindication 38341003 DOID:10763
Hypothyroidism contraindication 40930008 DOID:1459
Hypokalemia contraindication 43339004
Gastrointestinal perforation contraindication 51875005
Hepatic failure contraindication 59927004
Diarrhea contraindication 62315008
Gastrointestinal hemorrhage contraindication 74474003
Pancreatitis contraindication 75694006 DOID:4989
Prolonged QT interval contraindication 111975006
Liver function tests abnormal contraindication 166603001
Hypomagnesemia contraindication 190855004
Angina pectoris contraindication 194828000
Drug-induced hepatitis contraindication 235876009
Impaired wound healing contraindication 271618001
Cerebral hemorrhage contraindication 274100004
Pregnancy, function contraindication 289908002
Thromboembolic disorder contraindication 371039008
Surgical procedure contraindication 387713003
Cardiovascular event risk contraindication 395112001
UGT1A1*28 polymorphism contraindication 430235005
Congenital long QT syndrome contraindication 442917000
Hypertensive urgency contraindication 443482000
Acute Thromboembolic Stroke contraindication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.3 acidic
pKa2 5.69 Basic
pKa3 1.23 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
Vascular endothelial growth factor receptor 2 Kinase INHIBITOR Kd 7.85 CHEMBL CHEMBL
Vascular endothelial growth factor receptor 3 Kinase INHIBITOR Kd 7.57 CHEMBL CHEMBL
Macrophage colony-stimulating factor 1 receptor Kinase INHIBITOR Kd 8.10 CHEMBL CHEMBL
Platelet-derived growth factor receptor alpha Kinase INHIBITOR Kd 8.31 CHEMBL CHEMBL
Tyrosine-protein kinase ITK/TSK Kinase INHIBITOR CHEMBL CHEMBL
Mast/stem cell growth factor receptor Kit Kinase INHIBITOR Kd 8.74 CHEMBL CHEMBL
Platelet-derived growth factor receptor beta Kinase INHIBITOR Kd 8.70 CHEMBL CHEMBL
Fibroblast growth factor receptor 3 Kinase INHIBITOR Kd 6.21 CHEMBL CHEMBL
Tyrosine-protein kinase Lck Kinase INHIBITOR Kd 5.92 CHEMBL CHEMBL
Vascular endothelial growth factor receptor 1 Kinase INHIBITOR Kd 7.85 CHEMBL CHEMBL
Fibroblast growth factor receptor 1 Kinase INHIBITOR Kd 6 CHEMBL CHEMBL
Calcium/calmodulin-dependent protein kinase type 1 Kinase Kd 5.68 CHEMBL
Mitogen-activated protein kinase 8 Kinase Kd 5.70 CHEMBL
Tyrosine-protein kinase HCK Kinase Kd 5.24 CHEMBL
Mitogen-activated protein kinase 10 Kinase Kd 5.72 CHEMBL
Tyrosine-protein kinase JAK2 Kinase Kd 5.77 CHEMBL
Tyrosine-protein kinase SYK Kinase Kd 5.33 CHEMBL
Myosin light chain kinase 2, skeletal/cardiac muscle Kinase Kd 5.70 CHEMBL
Angiopoietin-1 receptor Kinase Kd 5.48 CHEMBL
AP2-associated protein kinase 1 Kinase Kd 5.54 CHEMBL
Hepatocyte growth factor receptor Kinase Kd 5.70 CHEMBL
Tyrosine-protein kinase Lyn Kinase Kd 6.05 CHEMBL
Serine/threonine-protein kinase Nek2 Kinase Kd 6.01 CHEMBL
LIM domain kinase 1 Kinase Kd 6.14 CHEMBL
Serine/threonine-protein kinase 10 Kinase Kd 7.08 CHEMBL
Tyrosine-protein kinase Fer Kinase Kd 5.57 CHEMBL
Serine/threonine-protein kinase PLK4 Kinase Kd 6.54 CHEMBL
Aurora kinase C Kinase Kd 6.12 CHEMBL
Serine/threonine-protein kinase 16 Kinase Kd 6.44 CHEMBL
Dual specificity protein kinase TTK Kinase Kd 6.82 CHEMBL
Abelson tyrosine-protein kinase 2 Kinase Kd 5.52 CHEMBL
Fibroblast growth factor receptor 2 Kinase Kd 6.68 CHEMBL
TRAF2 and NCK-interacting protein kinase Kinase Kd 6.51 CHEMBL
Tyrosine-protein kinase Fgr Kinase Kd 5.80 CHEMBL
Aurora kinase A Kinase Kd 5.15 CHEMBL
ALK tyrosine kinase receptor Kinase Kd 5.66 CHEMBL
Serine/threonine-protein kinase 36 Kinase Kd 6.33 CHEMBL
BMP-2-inducible protein kinase Kinase Kd 5.06 CHEMBL
Tyrosine-protein kinase FRK Kinase Kd 6.12 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 5 Kinase Kd 5.52 CHEMBL
Cyclin-G-associated kinase Kinase Kd 6.70 CHEMBL
Receptor-interacting serine/threonine-protein kinase 2 Kinase Kd 6.24 CHEMBL
Cyclin-dependent kinase 16 Kinase Kd 5.92 CHEMBL
STE20-like serine/threonine-protein kinase Kinase Kd 6.62 CHEMBL
MAP/microtubule affinity-regulating kinase 3 Kinase Kd 5.40 CHEMBL
Calcium/calmodulin-dependent protein kinase type 1G Kinase Kd 5.43 CHEMBL
Epithelial discoidin domain-containing receptor 1 Kinase Kd 7.24 CHEMBL
TGF-beta receptor type-2 Kinase Kd 5.52 CHEMBL
Protein-tyrosine kinase 6 Kinase Kd 5.64 CHEMBL
Non-receptor tyrosine-protein kinase TNK1 Kinase Kd 6.01 CHEMBL
Non-receptor tyrosine-protein kinase TYK2 Kinase Kd 5.47 CHEMBL
Tyrosine-protein kinase receptor Tie-1 Kinase Kd 6.15 CHEMBL
Tyrosine-protein kinase TXK Kinase Kd 5.59 CHEMBL
LIM domain kinase 2 Kinase Kd 6.41 CHEMBL
Serine/threonine-protein kinase NLK Kinase Kd 5.36 CHEMBL
Interleukin-1 receptor-associated kinase 3 Kinase Kd 6.10 CHEMBL
Serine/threonine-protein kinase SIK2 Kinase Kd 5.14 CHEMBL
Activin receptor type-2B Kinase Kd 5.62 CHEMBL
Discoidin domain-containing receptor 2 Kinase Kd 7.01 CHEMBL
Leukocyte tyrosine kinase receptor Kinase Kd 5.17 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 1 Kinase Kd 6.12 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 3 Kinase Kd 5.80 CHEMBL
Tyrosine-protein kinase Blk Kinase Kd 5.59 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 4 Kinase Kd 5.66 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 4 Kinase Kd 6.23 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 6 Kinase Kd 5.39 CHEMBL
Tyrosine-protein kinase Mer Kinase Kd 5.48 CHEMBL
Cyclin-dependent kinase 11B Kinase Kd 5.68 CHEMBL
Cyclin-dependent kinase 11A Kinase Kd 5.89 CHEMBL
Mitogen-activated protein kinase kinase kinase 9 Kinase Kd 6.54 CHEMBL
Mitogen-activated protein kinase kinase kinase 10 Kinase Kd 5.68 CHEMBL
Mitogen-activated protein kinase kinase kinase 11 Kinase Kd 6.13 CHEMBL
Serine/threonine-protein kinase Nek5 Kinase Kd 5.14 CHEMBL
Serine/threonine-protein kinase SIK1 Kinase Kd 5.66 CHEMBL
Tyrosine-protein kinase Srms Kinase Kd 5.60 CHEMBL
Interferon-induced, double-stranded RNA-activated protein kinase Kinase Kd 5.72 CHEMBL
Receptor-interacting serine/threonine-protein kinase 1 Kinase Kd 6.59 CHEMBL
Tyrosine-protein kinase Fes/Fps Kinase Kd 5.85 CHEMBL
Fibroblast growth factor receptor 4 Kinase Kd 5.55 CHEMBL
Proto-oncogene tyrosine-protein kinase ROS Kinase Kd 6.04 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 2 Kinase Kd 5.57 CHEMBL
Ephrin type-B receptor 6 Kinase Kd 7.09 CHEMBL
Interleukin-1 receptor-associated kinase 1 Kinase Kd 5.23 CHEMBL
Mitogen-activated protein kinase kinase kinase 2 Kinase Kd 6.54 CHEMBL
Serine/threonine-protein kinase RIO2 Kinase Kd 6.21 CHEMBL
Serine/threonine-protein kinase TAO1 Kinase Kd 6.62 CHEMBL
Serine/threonine-protein kinase TAO3 Kinase Kd 7.35 CHEMBL
Mitogen-activated protein kinase kinase kinase 19 Kinase Kd 6.03 CHEMBL
Mitogen-activated protein kinase kinase kinase 1 Kinase Kd 5.54 CHEMBL
Phosphatidylinositol 4-kinase beta Kinase Kd 6.02 CHEMBL
Bone morphogenetic protein receptor type-1B Kinase Kd 6 CHEMBL
Phosphatidylinositol 4-phosphate 5-kinase type-1 gamma Kinase Kd 5.72 CHEMBL
Serine/threonine-protein kinase TAO2 Kinase Kd 5.74 CHEMBL
Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma Kinase Kd 6.55 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 5 Kinase Kd 6.32 CHEMBL
Receptor-interacting serine/threonine-protein kinase 3 Kinase Kd 5.73 CHEMBL
Tyrosine-protein kinase JAK3 Kinase Kd 5.16 CHEMBL
Uncharacterized aarF domain-containing protein kinase 1 Kinase Kd 4.79 CHEMBL
Acetylcholinesterase Enzyme IC50 6.03 CHEMBL
Carbonic anhydrase 9 Enzyme Ki 8.04 CHEMBL
Tyrosine-protein kinase ABL1 Kinase Kd 6.42 CHEMBL
Proto-oncogene tyrosine-protein kinase Src Kinase Kd 5.55 CHEMBL
Tyrosine-protein kinase Yes Kinase Kd 5.30 CHEMBL
Tyrosine-protein kinase Fyn Kinase Kd 5.57 CHEMBL
RAF proto-oncogene serine/threonine-protein kinase Kinase Kd 6.05 CHEMBL
Serine/threonine-protein kinase B-raf Kinase Kd 6.37 CHEMBL
Receptor-type tyrosine-protein kinase FLT3 Kinase Kd 6.13 CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret Kinase Kd 6.57 CHEMBL
Calcium-dependent protein kinase 1 Kinase Kd 6.43 CHEMBL

External reference:

IDSource
4029464 VUID
N0000180309 NUI
D05380 KEGG_DRUG
635702-64-6 SECONDARY_CAS_RN
4029464 VANDF
C1831796 UMLSCUI
CHEBI:71219 CHEBI
CHEMBL477772 ChEMBL_ID
CHEMBL1201733 ChEMBL_ID
DB06589 DRUGBANK_ID
C516667 MESH_SUPPLEMENTAL_RECORD_UI
5698 IUPHAR_LIGAND_ID
8681 INN_ID
7RN5DR86CK UNII
10113978 PUBCHEM_CID
714438 RXNORM
168598 MMSL
26797 MMSL
d07499 MMSL
013302 NDDF
013303 NDDF
443763005 SNOMEDCT_US
443764004 SNOMEDCT_US
735169009 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
VOTRIENT HUMAN PRESCRIPTION DRUG LABEL 1 0078-0670 TABLET, FILM COATED 200 mg ORAL NDA 33 sections
VOTRIENT HUMAN PRESCRIPTION DRUG LABEL 1 0078-0670 TABLET, FILM COATED 200 mg ORAL NDA 33 sections
VOTRIENT HUMAN PRESCRIPTION DRUG LABEL 1 0078-0670 TABLET, FILM COATED 200 mg ORAL NDA 33 sections
VOTRIENT HUMAN PRESCRIPTION DRUG LABEL 1 0078-1077 TABLET, FILM COATED 200 mg ORAL NDA 33 sections
VOTRIENT HUMAN PRESCRIPTION DRUG LABEL 1 0078-1077 TABLET, FILM COATED 200 mg ORAL NDA 33 sections
VOTRIENT HUMAN PRESCRIPTION DRUG LABEL 1 0078-1077 TABLET, FILM COATED 200 mg ORAL NDA 33 sections