pazopanib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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: OFP
    • 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
BA (Bioavailability) 22 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 3.106 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 3.899 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 45.604 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 12.134 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 2.480 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 11.110 % High 1
herg hERG pIC50 5.325 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 10.990 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 48.195 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 0.860 % High 1
kinase-safety-class AAK1,ABL1,ABL2,ACVR1B,ACVR2A,ACVR2B,ACVRL1,AKT1,AKT2,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,BTK,CAMK2A,CAMK2B,CAMK2D,CAMK2G,CDK1,CDK14,CDK16,CDK19,CDK2,CDK3,CDK4,CDK5,CDK6,CDK7,CDK9,CHEK1,CLK2,CLK4,CSF1R,CSK,DDR1,DYRK1B,EGFR,EIF2AK3,EPHA2,EPHB1,EPHB3,EPHB4,ERBB2,ERBB4,FGFR1,FGFR4,FLT1,FLT3,FLT4,FYN,GAK,GRK1,GRK2,GSK3A,GSK3B,HASPIN,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,MAPK14,MAPK3,MAPK7,MAPK8,MAPK9,MARK1,MARK2,MARK4,MELK,MET,MINK1,MST1R,MTOR,NTRK1,NTRK2,NTRK3,NUAK1,PAK1,PAK2,PAK4,PAK5,PDGFRB,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CD,PIK3CG,PRKAA1,PRKAA2,PRKACA,PRKCD,PRKCI,PRKCZ,PTK2,PTK6,RET,RIPK3,ROCK1,ROCK2,SGK1,SIK2,SIK3,SRC,STK10,STK11,STK16,STK33,STK4,SYK,TBK1,TEK,TGFBR1,TNIK,TNK1,TTK,TYRO3,ULK1,ULK2,YES1,ZAP70 157
kinase-selectivity-class AAK1,ABL2,ACVR1B,ACVR2A,ACVR2B,ACVRL1,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,BTK,CAMK2A,CAMK2B,CAMK2D,CDK1,CDK16,CDK2,CDK4,CDK6,CDK7,CDK9,CLK2,CLK4,CSF1R,CSK,DDR1,DYRK1B,EGFR,EPHA2,EPHB3,EPHB4,ERBB2,ERBB4,FGFR1,FGFR4,FLT1,FLT3,FLT4,FYN,GAK,GRK2,GSK3A,GSK3B,IKBKB,INSR,IRAK1,IRAK3,IRAK4,JAK1,JAK2,JAK3,KDR,KIT,LCK,LRRK2,LYN,MAP2K1,MAP2K3,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K21,MAP3K7,MAP3K9,MAP4K1,MAP4K3,MAP4K5,MAPK1,MAPK10,MAPK12,MAPK7,MAPK8,MARK1,MARK4,MET,MINK1,MST1R,NTRK1,NTRK3,NUAK1,PAK1,PAK4,PDGFRB,PDK1,PDK4,PIK3CA,PIK3CD,PIK3CG,PRKAA1,PRKCD,PRKCI,PRKCZ,PTK2,RET,RIPK3,SIK2,SIK3,SRC,STK10,STK11,STK16,STK33,SYK,TEK,TGFBR1,TNIK,TNK1,TYRO3,ULK1,ULK2,YES1,ZAP70 118
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 16.788 High 1
mh-clint Mouse hepatocyte intrinsic clearance 41.783 High 1
mppb Mouse plasma protein binding (% unbound) 2.080 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 25.003 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 4.410 % High 1
rh-clint Rat hepatocyte intrinsic clearance 43.551 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 24.530 % High 1
rppb Rat plasma protein binding (% unbound) 1.010 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 1 uM High 1

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 854.25 21.95 396 14731 106474 90506846
Hair colour changes 536.31 21.95 123 15004 3371 90609949
Death 522.83 21.95 500 14627 456051 90157269
Diarrhoea 424.96 21.95 640 14487 938550 89674770
Disease progression 244.40 21.95 205 14922 156410 90456910
Hypertension 213.94 21.95 318 14809 457214 90156106
Nausea 176.87 21.95 492 14635 1109824 89503496
Hepatic function abnormal 153.88 21.95 96 15031 46192 90567128
Fatigue 142.64 21.95 468 14659 1153555 89459765
Palmar-plantar erythrodysaesthesia syndrome 132.42 21.95 73 15054 27950 90585370
Decreased appetite 128.26 21.95 227 14900 376313 90237007
Metastases to lung 120.26 21.95 57 15070 15934 90597386
Product use in unapproved indication 120.06 21.95 207 14920 336029 90277291
Desmoplastic small round cell tumour 114.74 21.95 19 15108 81 90613239
Alanine aminotransferase increased 100.64 21.95 111 15016 118227 90495093
Blood bilirubin increased 93.79 21.95 69 15058 43401 90569919
Aspartate aminotransferase increased 86.56 21.95 96 15031 102841 90510479
Hypothyroidism 85.70 21.95 71 15056 53056 90560264
Metastases to liver 83.93 21.95 55 15072 28752 90584568
Metastases to peritoneum 79.99 21.95 29 15098 4126 90609194
Vomiting 75.65 21.95 295 14832 787998 89825322
Blood pressure increased 74.99 21.95 125 15002 197092 90416228
Posterior reversible encephalopathy syndrome 70.86 21.95 45 15082 22294 90591026
Jaundice 66.52 21.95 50 15077 32467 90580853
Dysgeusia 66.16 21.95 61 15066 52499 90560821
Pneumothorax 61.77 21.95 39 15088 19128 90594192
Ascites 59.29 21.95 55 15072 47685 90565635
Transaminases increased 56.45 21.95 48 15079 37144 90576176
Drug hypersensitivity 56.21 21.95 6 15121 463603 90149717
Hepatotoxicity 55.37 21.95 52 15075 45790 90567530
Proteinuria 54.85 21.95 39 15088 23252 90590068
Dehydration 54.49 21.95 108 15019 194339 90418981
Joint swelling 52.91 21.95 10 15117 503290 90110030
Neoplasm progression 52.84 21.95 50 15077 44436 90568884
Metastases to central nervous system 49.89 21.95 33 15094 17509 90595811
Hypertensive crisis 49.48 21.95 33 15094 17751 90595569
Arthropathy 49.20 21.95 3 15124 366239 90247081
Metastases to lymph nodes 48.56 21.95 28 15099 11661 90601659
Condition aggravated 47.54 21.95 20 15107 595525 90017795
Metastases to pancreas 47.03 21.95 11 15116 328 90612992
Blood thyroid stimulating hormone increased 43.64 21.95 24 15103 9131 90604189
Platelet count decreased 43.18 21.95 80 15047 136889 90476431
Ageusia 42.73 21.95 29 15098 16047 90597273
Sinusitis 42.71 21.95 4 15123 343084 90270236
Hypersensitivity 41.89 21.95 12 15115 454665 90158655
Pleural effusion 41.21 21.95 70 15057 111921 90501399
Cell death 39.66 21.95 16 15111 3039 90610281
Left ventricular dysfunction 37.90 21.95 26 15101 14643 90598677
Treatment failure 36.64 21.95 4 15123 303924 90309396
Wound 36.50 21.95 4 15123 302976 90310344
Thrombocytopenia 36.27 21.95 96 15031 208629 90404691
Ejection fraction decreased 36.03 21.95 32 15095 26221 90587099
Therapeutic product effect decreased 35.18 21.95 3 15124 277568 90335752
Weight increased 35.02 21.95 13 15114 417914 90195406
Peripheral artery haematoma 34.11 21.95 6 15121 39 90613281
Pericarditis 34.02 21.95 3 15124 270148 90343172
Glossodynia 32.52 21.95 7 15120 321772 90291548
Cardiac failure 32.08 21.95 62 15065 109434 90503886
Intestinal transit time abnormal 30.97 21.95 6 15121 70 90613250
Musculoskeletal stiffness 30.90 21.95 6 15121 296526 90316794
Hyperthyroidism 30.62 21.95 25 15102 18285 90595035
Cardiac failure acute 30.48 21.95 21 15106 11908 90601412
Asthenia 30.47 21.95 172 14955 533579 90079741
Neurofibrosarcoma 30.45 21.95 7 15120 193 90613127
Hepatocellular injury 29.62 21.95 30 15097 28928 90584392
Cardiomyopathy 28.47 21.95 25 15102 20181 90593139
Tumour pain 28.40 21.95 11 15116 1876 90611444
Pulmonary embolism 27.80 21.95 65 15062 130755 90482565
Urticaria 27.44 21.95 9 15118 312725 90300595
Anaemia 27.37 21.95 124 15003 352678 90260642
Tumour lysis syndrome 27.01 21.95 19 15108 11133 90602187
Swelling 26.27 21.95 19 15108 419039 90194281
Gamma-glutamyltransferase increased 26.19 21.95 32 15095 37920 90575400
Cholestasis 25.69 21.95 31 15096 36268 90577052
Abdominal pain 25.59 21.95 132 14995 395589 90217731
Asthma 25.01 21.95 5 15122 242155 90371165
Nasopharyngitis 24.82 21.95 19 15108 407085 90206235
Amylase increased 24.32 21.95 15 15112 7057 90606263
Concomitant disease aggravated 24.19 21.95 18 15109 11500 90601820
Nephrotic syndrome 23.81 21.95 15 15112 7324 90605996
Tumour rupture 23.74 21.95 6 15121 249 90613071
Therapy cessation 22.45 21.95 29 15098 36332 90576988
Discomfort 22.19 21.95 9 15118 274326 90338994

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 932.55 19.04 217 21016 1985 42598117
Malignant neoplasm progression 821.72 19.04 565 20668 107835 42492267
Diarrhoea 602.38 19.04 923 20310 459926 42140176
Death 374.26 19.04 760 20473 470425 42129677
Decreased appetite 287.28 19.04 413 20820 192724 42407378
Metastases to lung 245.74 19.04 118 21115 11306 42588796
Fatigue 242.18 19.04 611 20622 435030 42165072
Disease progression 205.65 19.04 302 20931 143354 42456748
Palmar-plantar erythrodysaesthesia syndrome 200.66 19.04 126 21107 20456 42579646
Nausea 188.04 19.04 525 20708 396274 42203828
Hypertension 185.90 19.04 313 20920 166891 42433211
Dysgeusia 125.74 19.04 117 21116 34072 42566030
Pneumothorax 93.23 19.04 84 21149 23459 42576643
Metastases to bone 86.08 19.04 66 21167 14743 42585359
Off label use 79.08 19.04 123 21110 638212 41961890
Neoplasm progression 76.67 19.04 83 21150 28917 42571185
Hypothyroidism 74.82 19.04 86 21147 31998 42568104
Metastases to central nervous system 73.36 19.04 52 21181 10303 42589799
Jaundice 67.99 19.04 85 21148 34504 42565598
Blood pressure increased 67.89 19.04 154 21079 101774 42498328
Hepatic enzyme increased 67.81 19.04 98 21135 45686 42554416
Proteinuria 66.46 19.04 69 21164 22914 42577188
Hepatic function abnormal 64.47 19.04 102 21131 51465 42548637
Ageusia 61.55 19.04 49 21184 11556 42588546
Vomiting 60.03 19.04 294 20939 289429 42310673
Alanine aminotransferase increased 59.34 19.04 134 21099 88272 42511830
Blood thyroid stimulating hormone increased 58.17 19.04 35 21198 5257 42594845
Product use in unapproved indication 57.46 19.04 212 21021 184244 42415858
Weight decreased 57.42 19.04 230 21003 207718 42392384
Soft tissue sarcoma 57.25 19.04 13 21220 105 42599997
Blood bilirubin increased 54.79 19.04 85 21148 42167 42557935
Metastatic renal cell carcinoma 54.57 19.04 25 21208 2149 42597953
Metastases to liver 54.52 19.04 53 21180 16273 42583829
Tumour pain 49.16 19.04 20 21213 1287 42598815
Nephrotic syndrome 46.63 19.04 37 21196 8681 42591421
Therapy cessation 46.29 19.04 54 21179 20396 42579706
Hepatotoxicity 44.97 19.04 59 21174 25108 42574994
Skin depigmentation 43.57 19.04 14 21219 454 42599648
Condition aggravated 42.98 19.04 40 21193 260714 42339388
Stomatitis 42.71 19.04 84 21149 50245 42549857
Pneumothorax spontaneous 42.61 19.04 16 21217 830 42599272
Asthenia 42.02 19.04 261 20972 280532 42319570
Abdominal pain upper 40.40 19.04 111 21122 82498 42517604
Hypotension 38.50 19.04 43 21190 257588 42342514
Synovial sarcoma metastatic 37.92 19.04 7 21226 16 42600086
Metastases to lymph nodes 37.66 19.04 28 21205 5970 42594132
Skin hypopigmentation 37.23 19.04 12 21221 393 42599709
Aspartate aminotransferase increased 34.14 19.04 100 21133 77063 42523039
Activated partial thromboplastin time abnormal 33.79 19.04 9 21224 148 42599954
Toxicity to various agents 33.40 19.04 39 21194 229097 42371005
Renal cancer metastatic 33.28 19.04 12 21221 555 42599547
Osteonecrosis of jaw 33.01 19.04 44 21189 19005 42581097
Pulmonary necrosis 32.85 19.04 11 21222 407 42599695
Osteoma 32.52 19.04 8 21225 94 42600008
Polycystic liver disease 32.14 19.04 8 21225 99 42600003
COVID-19 32.09 19.04 9 21224 115939 42484163
Fall 32.00 19.04 42 21191 234478 42365624
Splenic necrosis 30.91 19.04 8 21225 117 42599985
Renal cell carcinoma 30.77 19.04 24 21209 5493 42594609
Pleural effusion 30.46 19.04 112 21121 97054 42503048
Taste disorder 30.14 19.04 31 21202 10176 42589926
Renal cancer 29.93 19.04 28 21205 8196 42591906
Splenic cyst 29.90 19.04 8 21225 134 42599968
Haemoglobin urine present 29.46 19.04 8 21225 142 42599960
Liver disorder 28.72 19.04 62 21171 39582 42560520
Metastases to adrenals 28.69 19.04 13 21220 1089 42599013
Blood alkaline phosphatase increased 28.41 19.04 56 21177 33541 42566561
Metastases to soft tissue 28.01 19.04 10 21223 449 42599653
Overdose 27.62 19.04 9 21224 105255 42494847
Neoplasm recurrence 27.34 19.04 17 21216 2707 42597395
Liver function test increased 26.99 19.04 41 21192 19957 42580145
Somnolence 26.50 19.04 19 21214 141086 42459016
Impaired healing 25.96 19.04 37 21196 17016 42583086
Metastasis 25.23 19.04 20 21213 4685 42595417
Drug hypersensitivity 25.21 19.04 9 21224 99380 42500722
Second primary malignancy 24.59 19.04 27 21206 9548 42590554
Urinary sediment present 24.45 19.04 8 21225 275 42599827
Malignant pleural effusion 24.29 19.04 14 21219 1941 42598161
Faeces pale 23.99 19.04 13 21220 1601 42598501
Gamma-glutamyltransferase increased 23.74 19.04 51 21182 32446 42567656
Metastases to spine 23.07 19.04 16 21217 3061 42597041
Drug interaction 23.05 19.04 63 21170 266936 42333166
Sepsis 23.02 19.04 40 21193 199294 42400808
Lordosis 22.76 19.04 8 21225 343 42599759
Eyelash discolouration 22.76 19.04 4 21229 6 42600096
Splenic lesion 22.65 19.04 8 21225 348 42599754
Dysphonia 22.35 19.04 46 21187 28404 42571698
Oxygen saturation decreased 22.12 19.04 3 21230 64684 42535418
Renal cancer recurrent 21.84 19.04 5 21228 42 42600060
Intestinal perforation 21.80 19.04 27 21206 10847 42589255
Intentional product use issue 20.97 19.04 5 21228 71828 42528274
Glossodynia 20.88 19.04 17 21216 4135 42595967
Intentional product misuse 20.87 19.04 3 21230 61897 42538205
Red blood cell abnormality 20.86 19.04 8 21225 440 42599662
Product dose omission issue 20.67 19.04 28 21205 154337 42445765
Eye colour change 20.45 19.04 7 21226 277 42599825
Pulmonary mass 20.07 19.04 32 21201 16233 42583869
Malignant connective tissue neoplasm 19.82 19.04 3 21230 0 42600102
Abdominal discomfort 19.71 19.04 82 21151 75173 42524929
Tremor 19.61 19.04 12 21221 96917 42503185

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 1350.66 19.54 715 26352 173852 110388380
Hair colour changes 823.17 19.54 198 26869 4503 110557729
Death 702.28 19.54 856 26211 698013 109864219
Diarrhoea 533.33 19.54 975 26092 1138530 109423702
Disease progression 439.88 19.54 409 26658 243625 110318607
Metastases to lung 321.95 19.54 142 26925 22921 110539311
Hypertension 292.26 19.54 479 26588 509605 110052627
Decreased appetite 268.64 19.54 444 26623 475402 110086830
Palmar-plantar erythrodysaesthesia syndrome 263.29 19.54 149 26918 40876 110521356
Hepatic function abnormal 188.76 19.54 164 26903 89131 110473101
Fatigue 187.32 19.54 686 26381 1215272 109346960
Nausea 170.33 19.54 673 26394 1235017 109327215
Blood bilirubin increased 139.69 19.54 129 26938 75843 110486389
Pneumothorax 136.80 19.54 93 26974 35192 110527040
Hypothyroidism 130.58 19.54 122 26945 72777 110489455
Metastases to liver 127.14 19.54 89 26978 35297 110526935
Jaundice 125.55 19.54 109 26958 59127 110503105
Neoplasm progression 125.23 19.54 113 26954 64482 110497750
Alanine aminotransferase increased 123.38 19.54 186 26881 183587 110378645
Proteinuria 115.11 19.54 88 26979 39930 110522302
Desmoplastic small round cell tumour 110.84 19.54 20 27047 98 110562134
Metastases to central nervous system 102.65 19.54 66 27001 22751 110539481
Aspartate aminotransferase increased 94.95 19.54 153 26914 159783 110402449
Metastases to lymph nodes 94.79 19.54 54 27013 14978 110547254
Hepatotoxicity 90.96 19.54 94 26973 63306 110498926
Metastases to bone 90.25 19.54 69 26998 31303 110530929
Dysgeusia 86.71 19.54 96 26971 69889 110492343
Product use in unapproved indication 85.48 19.54 272 26795 447105 110115127
Metastases to peritoneum 82.99 19.54 36 27031 5574 110556658
Blood thyroid stimulating hormone increased 82.46 19.54 46 27021 12255 110549977
Drug hypersensitivity 82.29 19.54 8 27059 454082 110108150
Blood pressure increased 80.36 19.54 188 26879 258185 110304047
Infusion related reaction 80.13 19.54 3 27064 381159 110181073
Metastatic renal cell carcinoma 76.09 19.54 27 27040 2453 110559779
Therapy cessation 74.46 19.54 72 26995 44785 110517447
Vomiting 71.00 19.54 422 26645 910253 109651979
Condition aggravated 66.16 19.54 50 27017 734786 109827446
Pleural effusion 65.00 19.54 138 26929 177571 110384661
Joint swelling 63.88 19.54 15 27052 442830 110119402
Dehydration 59.89 19.54 177 26890 279334 110282898
Nephrotic syndrome 59.73 19.54 39 27028 13792 110548440
Ageusia 58.25 19.54 44 27023 19601 110542631
Platelet count decreased 54.27 19.54 151 26916 230292 110331940
Hypertensive crisis 53.96 19.54 46 27021 24326 110537906
Hyperthyroidism 52.43 19.54 49 27018 29212 110533020
Wheezing 50.43 19.54 3 27064 255227 110307005
Urticaria 49.69 19.54 9 27058 318848 110243384
Asthenia 48.98 19.54 312 26755 688687 109873545
Osteonecrosis of jaw 47.99 19.54 59 27008 47958 110514274
Off label use 44.37 19.54 203 26864 1499982 109062250
Soft tissue sarcoma 44.11 19.54 11 27056 291 110561941
Tumour pain 43.76 19.54 19 27048 2948 110559284
Transaminases increased 43.68 19.54 65 27002 63325 110498907
Musculoskeletal stiffness 43.38 19.54 8 27059 279814 110282418
Posterior reversible encephalopathy syndrome 42.88 19.54 47 27020 33814 110528418
Sinusitis 42.86 19.54 10 27057 296678 110265554
Hypersensitivity 42.44 19.54 23 27044 403975 110158257
Metastasis 42.42 19.54 26 27041 8241 110553991
Nasopharyngitis 42.09 19.54 22 27045 394339 110167893
Asthma 41.38 19.54 6 27061 250285 110311947
Ascites 41.00 19.54 78 26989 92730 110469502
Blood alkaline phosphatase increased 40.89 19.54 67 27000 70868 110491364
Fall 40.55 19.54 53 27014 603429 109958803
Ejection fraction decreased 40.48 19.54 50 27017 40830 110521402
Disseminated intravascular coagulation 40.09 19.54 50 27017 41236 110520996
Therapeutic product effect decreased 40.06 19.54 6 27061 244310 110317922
Weight increased 39.74 19.54 27 27040 419617 110142615
Hyperbilirubinaemia 39.58 19.54 43 27024 30628 110531604
Pulmonary mass 39.17 19.54 47 27020 37254 110524978
Thrombocytopenia 39.04 19.54 179 26888 348706 110213526
Pneumothorax spontaneous 38.22 19.54 15 27052 1802 110560430
Renal cancer 38.21 19.54 29 27038 13005 110549227
Wound 37.88 19.54 6 27061 234431 110327801
Osteoma 37.09 19.54 8 27059 109 110562123
Amylase increased 37.03 19.54 28 27039 12491 110549741
Weight decreased 37.02 19.54 218 26849 467839 110094393
Renal cell carcinoma 36.91 19.54 23 27044 7507 110554725
Metastases to adrenals 36.44 19.54 14 27053 1589 110560643
Pulmonary necrosis 36.31 19.54 11 27056 607 110561625
Renal impairment 36.28 19.54 115 26952 188330 110373902
Overdose 35.56 19.54 7 27060 233787 110328445
Neurofibrosarcoma 35.36 19.54 9 27058 259 110561973
Pericarditis 34.53 19.54 6 27061 219108 110343124
Skin hypopigmentation 34.16 19.54 13 27054 1438 110560794
COVID-19 33.96 19.54 9 27058 245051 110317181
Polycystic liver disease 33.57 19.54 8 27059 174 110562058
Lower respiratory tract infection 33.55 19.54 9 27058 243097 110319135
Neoplasm recurrence 33.53 19.54 19 27048 5213 110557019
Retro-orbital neoplasm 33.35 19.54 7 27060 83 110562149
Splenic necrosis 33.02 19.54 8 27059 187 110562045
Liver function test abnormal 33.02 19.54 60 27007 68890 110493342
Cardiac failure 32.97 19.54 111 26956 187515 110374717
Gamma-glutamyltransferase increased 32.79 19.54 56 27011 61253 110500979
Activated partial thromboplastin time abnormal 32.29 19.54 9 27058 369 110561863
Arthralgia 31.88 19.54 92 26975 779540 109782692
Metastases to soft tissue 30.58 19.54 10 27057 709 110561523
Left ventricular dysfunction 30.43 19.54 33 27034 23460 110538772
Treatment failure 30.27 19.54 15 27052 277219 110285013
Sleep disorder 30.10 19.54 6 27061 198638 110363594
Peripheral swelling 29.75 19.54 33 27034 404001 110158231
Splenic cyst 29.74 19.54 8 27059 287 110561945
Synovial sarcoma metastatic 29.41 19.54 5 27062 16 110562216
Malignant pleural effusion 29.34 19.54 16 27051 4077 110558155
Intentional product use issue 29.27 19.54 12 27055 247894 110314338
Depression 29.26 19.54 21 27046 317314 110244918
Blood creatinine increased 28.50 19.54 104 26963 182785 110379447
Hepatic mass 28.47 19.54 14 27053 2884 110559348
Cholestasis 28.21 19.54 54 27013 64464 110497768
Metastases to spine 27.92 19.54 17 27050 5326 110556906
Tumour necrosis 27.67 19.54 13 27054 2423 110559809
Recall phenomenon 27.53 19.54 11 27056 1385 110560847
Hepatic lesion 27.37 19.54 20 27047 8473 110553759
Polycythaemia 26.85 19.54 14 27053 3261 110558971
Intestinal transit time abnormal 26.52 19.54 6 27061 103 110562129
Intestinal perforation 26.39 19.54 29 27038 20915 110541317
Second primary malignancy 26.28 19.54 27 27040 18041 110544191
Loss of personal independence in daily activities 26.23 19.54 3 27064 150017 110412215
Renal cancer recurrent 26.20 19.54 6 27061 109 110562123
Lordosis 26.00 19.54 8 27059 465 110561767
Hepatic failure 25.82 19.54 54 27013 68685 110493547
Renal cancer metastatic 25.71 19.54 9 27058 785 110561447
Mobility decreased 25.68 19.54 13 27054 237409 110324823
Peripheral artery haematoma 25.66 19.54 6 27061 120 110562112
Mucosal inflammation 25.63 19.54 66 27001 96075 110466157
Lipase increased 25.54 19.54 27 27040 18645 110543587
Metastases to pelvis 25.09 19.54 9 27058 843 110561389
Skin depigmentation 24.83 19.54 10 27057 1286 110560946
Osteoarthritis 24.75 19.54 7 27060 182616 110379616
Migraine 24.36 19.54 6 27061 171646 110390586
Hepatocellular injury 24.16 19.54 44 27023 50598 110511634
Thyroid function test abnormal 23.69 19.54 13 27054 3354 110558878
Splenic lesion 23.69 19.54 8 27059 627 110561605
Pruritus 23.48 19.54 69 26998 581491 109980741
Blood cholesterol increased 23.39 19.54 8 27059 184777 110377455
Swelling 23.37 19.54 31 27036 351010 110211222
Abdominal pain 23.19 19.54 209 26858 512780 110049452
Prostatic specific antigen abnormal 23.16 19.54 8 27059 671 110561561
Chromaturia 22.99 19.54 32 27035 29328 110532904
Discomfort 22.86 19.54 12 27055 214695 110347537
Glossodynia 22.78 19.54 13 27054 221991 110340241
Metastases to pancreas 22.43 19.54 8 27059 737 110561495
Synovial sarcoma 22.04 19.54 5 27062 87 110562145
Malignant connective tissue neoplasm 21.95 19.54 3 27064 0 110562232
Sarcoma metastatic 21.77 19.54 5 27062 92 110562140
Muscle mass 21.69 19.54 7 27060 476 110561756
Bronchitis 21.31 19.54 6 27061 157026 110405206
Red blood cell abnormality 21.06 19.54 8 27059 880 110561352
Faeces pale 21 19.54 12 27055 3345 110558887
Haemoglobin urine present 20.69 19.54 8 27059 924 110561308
Cardiotoxicity 20.63 19.54 23 27044 16858 110545374
Hypotension 20.53 19.54 63 27004 523786 110038446
Anxiety 20.50 19.54 33 27034 345045 110217187
Metastases to pleura 20.37 19.54 10 27057 2053 110560179
Intentional product misuse 20.16 19.54 4 27063 132900 110429332
Haemoptysis 20.08 19.54 50 27017 71304 110490928
Insomnia 20.02 19.54 36 27031 360554 110201678
Cardiac ventricular scarring 19.87 19.54 3 27064 3 110562229

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:22587 antiviral agent
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:38637 tyrosine kinase inhibitor
CHEBI has role CHEBI:50926 angiogenesis modulating agent
CHEBI has role CHEBI:65207 vascular endothelial growth factor receptor antagonist
CHEBI has role CHEBI:50748 antipsoriatic
CHEBI has role CHEBI:66981 ophthalmology drug

Related Drugs by ATC class:

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avapritinibcabozantinibcapivasertibentrectinibgilteritiniblarotrectiniblenvatinibmidostaurinnintedanibpexidartinibpralsetinibquizartinib show all 21 →

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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 400MG BASE PAZOPANIB HYDROCHLORIDE TORRENT A219922 Sept. 4, 2025 RX TABLET ORAL May 6, 2026 COMPETITIVE GENERIC THERAPY

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
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/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
Carbonic anhydrase 2 Enzyme Ki 7.49 CHEMBL
Carbonic anhydrase 1 Enzyme Ki 7.92 CHEMBL
Acetylcholinesterase Enzyme IC50 6.03 CHEMBL
Carbonic anhydrase 9 Enzyme Ki 8.04 CHEMBL
Carbonic anhydrase 12 Enzyme Ki 9.05 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
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
372454 MMSL
d07499 MMSL
013302 NDDF
013303 NDDF
443763005 SNOMEDCT_US
443764004 SNOMEDCT_US
735169009 SNOMEDCT_US
7RN5DR86CK INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
VOTRIENT HUMAN PRESCRIPTION DRUG LABEL 1 0078-1077 TABLET, FILM COATED 200 mg ORAL NDA 33 sections
Pazopanib HUMAN PRESCRIPTION DRUG LABEL 1 0480-4184 TABLET, FILM COATED 200 mg ORAL ANDA 28 sections
pazopanib HUMAN PRESCRIPTION DRUG LABEL 1 13668-735 TABLET, FILM COATED 400 mg ORAL ANDA 26 sections
Pazopanib HUMAN PRESCRIPTION DRUG LABEL 1 42291-939 TABLET, FILM COATED 200 mg ORAL ANDA 28 sections
Pazopanib HUMAN PRESCRIPTION DRUG LABEL 1 51407-872 TABLET 200 mg ORAL ANDA 27 sections
Pazopanib Human Prescription Drug Label 1 59651-582 TABLET, FILM COATED 200 mg ORAL ANDA 28 sections
Pazopanib HUMAN PRESCRIPTION DRUG LABEL 1 60505-4779 TABLET 200 mg ORAL ANDA 27 sections
Pazopanib HUMAN PRESCRIPTION DRUG LABEL 1 63304-116 TABLET, FILM COATED 200 mg ORAL ANDA 30 sections
pazopanib HUMAN PRESCRIPTION DRUG LABEL 1 82293-022 TABLET, FILM COATED 200 mg ORAL ANDA 33 sections