sorafenib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
Raf (Rapidely Accelerated Fibrosarcoma) kinase inhibitors 2459 284461-73-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • BAY 43-9006
  • BAY 545-9085
  • BAY-545-9085
  • sorafenib tosilate
  • sorafenib
  • nexavar
  • sorafenib tosylate
Sorafenib is a kinase inhibitor that decreases tumor cell proliferation in vitro. Sorafenib was shown to inhibit multiple intracellular (c-CRAF, BRAF and mutant BRAF) and cell surface kinases (KIT, FLT-3, RET, RET/PTC, VEGFR-1, VEGFR-2, VEGFR-3, and PDGFR-beta). Several of these kinases are thought to be involved in tumor cell signaling, angiogenesis and apoptosis. Sorafenib inhibited tumor growth of HCC, RCC, and DTC human tumor xenografts in immunocompromised mice. Reductions in tumor angiogenesis were seen in models of HCC and RCC upon sorafenib treatment, and increases in tumor apoptosis were observed in models of hepatocellular carcinoma, renal cell carcinoma, and differentiated thyroid carcinoma.
  • Molecular weight: 464.83
  • Formula: C21H16ClF3N4O3
  • CLOGP: 5.16
  • LIPINSKI: 1
  • HAC: 7
  • HDO: 3
  • TPSA: 92.35
  • ALOGS: -5.43
  • ROTB: 6
  • 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 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 12.29 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 39 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 4.999 High 0.83
caco2-efflux Caco-2 efflux ratio (BA/AB) 2.037 High 0.83
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 5.902 10^-6 cm/s High 0.83
dh-clint Dog hepatocyte intrinsic clearance 2.344 uL/min/10^6 cells High 0.83
dppb Dog plasma protein binding (% unbound) 0.130 % High 0.83
fcs-ppb Fetal calf serum protein binding (% unbound) 0.190 % High 0.83
herg hERG pIC50 4.839 pIC50 High 0.83
hh-clint Human hepatocyte intrinsic clearance 4.721 uL/min/10^6 cells High 0.83
hlm-clint Human liver microsomal intrinsic clearance 3.214 uL/min/mg protein High 0.83
hppb Human plasma protein binding (% unbound) 0.260 % High 0.83
kinase-safety-class ABL1,ABL2,ACVR2A,ACVR2B,ACVRL1,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,CAMK2B,CAMK2D,CDK1,CDK16,CDK19,CDK5,CDK7,CDK9,CHEK1,CSF1R,CSK,DDR1,DYRK1B,EGFR,EIF2AK3,EPHA2,EPHB1,EPHB3,EPHB4,ERBB2,ERBB4,FGFR1,FLT1,FLT3,FLT4,FYN,GAK,GRK2,IKBKB,INSR,IRAK1,ITK,JAK1,JAK2,KDR,KIT,LCK,LYN,MAP2K1,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K2,MAP3K21,MAP3K7,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK10,MAPK11,MAPK12,MAPK14,MAPK7,MAPK8,MAPK9,MAPKAPK2,MARK4,MELK,MET,MINK1,MST1R,MTOR,NTRK1,NTRK2,NTRK3,PAK4,PDGFRB,PDK1,PDK2,PDK4,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PRKCD,PRKDC,PTK6,RET,RIPK3,SIK2,SIK3,SRC,STK10,STK33,SYK,TEK,TNIK,TTK,TYRO3,ULK1,ULK2,YES1 108
kinase-selectivity-class ABL2,ACVR2B,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,CAMK2D,CDK9,CSF1R,CSK,DDR1,EGFR,EIF2AK3,EPHA2,EPHB4,ERBB2,ERBB4,FGFR1,FLT1,FLT3,FLT4,FYN,JAK1,KDR,KIT,LCK,LYN,MAP2K1,MAP2K6,MAP3K11,MAP3K21,MAP4K1,MAP4K3,MAPK14,MAPK7,MARK4,MELK,MET,MINK1,MKNK1,MKNK2,MST1R,MTOR,NTRK3,PDGFRB,PDK4,PIK3CA,PRKCD,PRKDC,RET,RIPK1,RIPK3,SIK2,SIK3,SRC,STK10,STK33,SYK,TEK,TNIK,TYRO3,ULK1,YES1 67
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 7.145 High 0.83
mh-clint Mouse hepatocyte intrinsic clearance 17.378 High 0.83
mppb Mouse plasma protein binding (% unbound) 0.110 High 0.83
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 6.067 High 0.83
pfas-class PFAS structural alert (1 = True, 0 = False) 1
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 1 High 1
pppb Pig plasma protein binding (% unbound) 0.300 % High 0.83
rat-kpuu-brain Rat brain Kpuu 0.366 % High 1
rh-clint Rat hepatocyte intrinsic clearance 4.236 uL/min/10^6 cells High 0.83
rh-fuinc Rat hepatocyte fraction unbound in incubation 0.560 % High 0.83
rppb Rat plasma protein binding (% unbound) 0.130 % High 0.83
solubility-dd Solubility at pH 7.4 in DMSO 0.432 uM High 0.83

Approvals:

DateAgencyCompanyOrphan
Dec. 20, 2005 FDA BAYER HLTHCARE
July 19, 2006 EMA BAYER AG

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
Palmar-plantar erythrodysaesthesia syndrome 1723.73 20.41 478 15360 27545 90585064
Diarrhoea 245.50 20.41 518 15320 938672 89673937
Hepatic function abnormal 236.79 20.41 129 15709 46159 90566450
Hepatic cancer 235.13 20.41 69 15769 4812 90607797
Hepatic encephalopathy 192.43 20.41 77 15761 13695 90598914
Decreased appetite 157.36 20.41 255 15583 376285 90236324
Metastases to lung 148.79 20.41 67 15771 15924 90596685
Ascites 127.87 20.41 88 15750 47652 90564957
Off label use 124.85 20.41 448 15390 1101804 89510805
Rash 122.95 20.41 360 15478 795740 89816869
Hyperkeratosis 122.60 20.41 46 15792 6882 90605727
Hepatocellular carcinoma 102.48 20.41 31 15807 2397 90610212
Skin exfoliation 96.36 20.41 86 15752 67827 90544782
Alpha 1 foetoprotein increased 95.55 20.41 18 15820 170 90612439
Hypertension 93.69 20.41 230 15608 457302 90155307
Amylase increased 93.46 20.41 38 15800 7034 90605575
Hepatic failure 80.78 20.41 62 15776 39666 90572943
Lipase increased 77.00 20.41 38 15800 11073 90601536
Erythema multiforme 70.63 20.41 37 15801 12209 90600400
Pain of skin 69.08 20.41 40 15798 16042 90596567
Dry skin 69.04 20.41 81 15757 87992 90524617
Death 67.79 20.41 204 15634 456347 90156262
Pneumonia adenoviral 66.99 20.41 14 15824 233 90612376
Drug ineffective 65.68 20.41 88 15750 1384210 89228399
Blister 62.83 20.41 138 15700 254860 90357749
Erythema 59.83 20.41 127 15711 229119 90383490
Platelet count decreased 58.67 20.41 94 15744 136875 90475734
Adenoviral hepatitis 58.57 20.41 14 15824 438 90612171
Ammonia increased 56.47 20.41 24 15814 4962 90607647
Blood bilirubin increased 55.68 20.41 52 15786 43418 90569191
Alopecia 55.37 20.41 201 15637 494870 90117739
Drug hypersensitivity 54.67 20.41 8 15830 463601 90149008
Skin toxicity 52.44 20.41 25 15813 6754 90605855
Arthropathy 51.94 20.41 3 15835 366239 90246370
Rheumatoid arthritis 51.33 20.41 3 15835 362611 90249998
Condition aggravated 49.68 20.41 21 15817 595524 90017085
Hypophosphataemia 48.50 20.41 31 15807 14823 90597786
Mucosal inflammation 46.82 20.41 54 15784 57571 90555038
Blood pressure increased 43.28 20.41 102 15736 197115 90415494
Product use in unapproved indication 41.39 20.41 141 15697 336095 90276514
Weight increased 41.33 20.41 11 15827 417916 90194693
Joint swelling 39.99 20.41 19 15819 503281 90109328
Swelling 39.65 20.41 12 15826 419046 90193563
Tumour necrosis 38.92 20.41 12 15826 989 90611620
Sinusitis 38.01 20.41 7 15831 343081 90269528
Oral pain 37.87 20.41 37 15801 32646 90579963
Abdominal pain 36.29 20.41 151 15687 395570 90217039
Protein induced by vitamin K absence or antagonist II increased 35.91 20.41 5 15833 3 90612606
Metastases to bone 35.56 20.41 32 15806 25473 90587136
Food refusal 35.13 20.41 10 15828 625 90611984
Pain in extremity 34.57 20.41 163 15675 450366 90162243
Stomatitis 34.50 20.41 116 15722 274582 90338027
Nasopharyngitis 34.49 20.41 14 15824 407090 90205519
Treatment failure 34.10 20.41 6 15832 303922 90308687
Weight decreased 34.07 20.41 144 15694 379766 90232843
Wound 33.95 20.41 6 15832 302974 90309635
Pyrexia 33.23 20.41 213 15625 660272 89952337
Catabolic state 32.85 20.41 6 15832 47 90612562
Jaundice 32.53 20.41 34 15804 32483 90580126
Malignant neoplasm progression 32.34 20.41 63 15775 106807 90505802
Renal cell carcinoma 32.24 20.41 15 15823 3836 90608773
Pancreatic enzymes increased 32.02 20.41 10 15828 860 90611749
Hypersensitivity 31.98 20.41 20 15818 454657 90157952
Discomfort 31.70 20.41 5 15833 274330 90338279
Asthma 31.43 20.41 3 15835 242157 90370452
Disease progression 31.14 20.41 78 15760 156537 90456072
Metastases to adrenals 30.87 20.41 10 15828 968 90611641
Dehydration 30.77 20.41 89 15749 194358 90418251
Acute myeloid leukaemia recurrent 30.46 20.41 12 15826 2045 90610564
Hyperammonaemia 30.20 20.41 17 15821 6458 90606151
Plantar erythema 29.57 20.41 7 15831 210 90612399
Herpes simplex viraemia 29.42 20.41 8 15830 422 90612187
Pleural effusion 29.12 20.41 62 15776 111929 90500680
Haemoptysis 28.37 20.41 32 15806 33288 90579321
Metastasis 28.32 20.41 16 15822 6121 90606488
Febrile neutropenia 27.52 20.41 75 15763 158274 90454335
Adenovirus infection 26.75 20.41 14 15824 4608 90608001
Hospitalisation 26.73 20.41 65 15773 128035 90484574
Liver carcinoma ruptured 25.93 20.41 5 15833 54 90612555
Blood cholesterol increased 25.90 20.41 3 15835 208009 90404600
Bone marrow failure 25.84 20.41 30 15808 32191 90580418
Asthenia 25.50 20.41 170 15668 533581 90079028
Musculoskeletal stiffness 25.42 20.41 10 15828 296522 90316087
Skin lesion 25.41 20.41 32 15806 37333 90575276
Dysphonia 25.23 20.41 42 15796 63042 90549567
Aspartate aminotransferase increased 24.50 20.41 55 15783 102882 90509727
Pain 24.29 20.41 91 15747 996250 89616359
Metastatic renal cell carcinoma 24.13 20.41 8 15830 833 90611776
Varices oesophageal 23.46 20.41 12 15826 3767 90608842
Tumour haemorrhage 23.45 20.41 10 15828 2084 90610525
Migraine 23.08 20.41 3 15835 190389 90422220
Arthralgia 22.47 20.41 66 15772 778456 89834153
Gastrointestinal haemorrhage 22.35 20.41 49 15789 90199 90522410
Fatigue 22.35 20.41 303 15535 1153720 89458889
Hypocalcaemia 22.26 20.41 32 15806 42336 90570273
Wheezing 22.17 20.41 7 15831 238073 90374536
Coma hepatic 21.80 20.41 7 15831 659 90611950
Vomiting 21.44 20.41 221 15617 788072 89824537
Palmoplantar keratoderma 21.38 20.41 11 15827 3496 90609113
Tumour thrombosis 20.76 20.41 4 15834 43 90612566
Metastases to central nervous system 20.58 20.41 20 15818 17522 90595087

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
Palmar-plantar erythrodysaesthesia syndrome 3855.79 16.81 1201 36858 19381 42563895
Hepatic cancer 864.43 16.81 314 37745 8166 42575110
Hepatic function abnormal 667.93 16.81 469 37590 51098 42532178
Hepatic encephalopathy 651.32 16.81 310 37749 16132 42567144
Diarrhoea 645.84 16.81 1324 36735 459525 42123751
Ascites 485.38 16.81 403 37656 56275 42527001
Decreased appetite 476.73 16.81 714 37345 192423 42390853
Hypertension 414.95 16.81 620 37439 166584 42416692
Metastases to lung 399.89 16.81 198 37861 11226 42572050
Hepatic failure 379.28 16.81 296 37763 37804 42545472
Alpha 1 foetoprotein increased 323.52 16.81 84 37975 658 42582618
Alopecia 307.79 16.81 235 37824 29041 42554235
Blister 270.08 16.81 212 37847 27278 42555998
Dysphonia 240.55 16.81 201 37858 28249 42555027
Rash 182.53 16.81 602 37457 276352 42306924
Amylase increased 170.62 16.81 94 37965 6635 42576641
Acute myeloid leukaemia recurrent 166.29 16.81 75 37984 3437 42579839
Blood bilirubin increased 165.00 16.81 196 37863 42056 42541220
Ammonia increased 151.93 16.81 77 37982 4582 42578694
Hepatocellular carcinoma 143.27 16.81 90 37969 8104 42575172
Liver carcinoma ruptured 137.97 16.81 35 38024 247 42583029
Jaundice 137.59 16.81 162 37897 34427 42548849
Skin toxicity 127.40 16.81 77 37982 6472 42576804
Drug ineffective 121.33 16.81 238 37821 629959 41953317
Metastases to lymph nodes 117.91 16.81 71 37988 5927 42577349
Hyperkeratosis 116.45 16.81 64 37995 4494 42578782
Oesophageal varices haemorrhage 115.83 16.81 59 38000 3548 42579728
Stomatitis 114.95 16.81 180 37879 50149 42533127
Lipase increased 106.98 16.81 83 37976 10483 42572793
Fatigue 103.33 16.81 703 37356 434938 42148338
Toxicity to various agents 101.33 16.81 39 38020 229097 42354179
Liver disorder 99.28 16.81 148 37911 39496 42543780
Metastases to bone 90.19 16.81 87 37972 14722 42568554
Drug interaction 89.34 16.81 65 37994 266934 42316342
Tumour rupture 83.56 16.81 25 38034 344 42582932
Skin exfoliation 83.15 16.81 140 37919 41413 42541863
Acute kidney injury 81.04 16.81 127 37932 367210 42216066
Renal cell carcinoma 80.25 16.81 54 38005 5463 42577813
Portal vein thrombosis 79.61 16.81 50 38009 4499 42578777
Metastases to peritoneum 78.46 16.81 40 38019 2409 42580867
COVID-19 77.80 16.81 7 38052 115941 42467335
Overdose 74.43 16.81 5 38054 105259 42478017
Asthenia 74.17 16.81 466 37593 280327 42302949
Abdominal pain 71.64 16.81 348 37711 190123 42393153
Abdominal pain upper 70.48 16.81 197 37862 82412 42500864
Metastases to adrenals 70.11 16.81 29 38030 1073 42582203
Aspartate aminotransferase increased 69.79 16.81 188 37871 76975 42506301
Condition aggravated 68.76 16.81 79 37980 260675 42322601
Platelet count decreased 67.85 16.81 274 37785 138307 42444969
Completed suicide 66.99 16.81 5 38054 96460 42486816
Hepatic lesion 65.40 16.81 44 38015 4450 42578826
Erythema multiforme 65.30 16.81 61 37998 9916 42573360
Hepatorenal syndrome 61.89 16.81 36 38023 2818 42580458
Blood pressure increased 61.03 16.81 215 37844 101713 42481563
Weight decreased 58.54 16.81 351 37708 207597 42375679
Metastatic renal cell carcinoma 56.84 16.81 31 38028 2143 42581133
Coma hepatic 54.97 16.81 19 38040 424 42582852
Drug hypersensitivity 54.86 16.81 11 38048 99378 42483898
Protein induced by vitamin K absence or antagonist II increased 54.25 16.81 12 38047 42 42583234
Bone marrow failure 52.75 16.81 101 37958 32992 42550284
Pain of skin 50.20 16.81 48 38011 8032 42575244
Inappropriate schedule of product administration 50.13 16.81 12 38047 95890 42487386
Dry skin 50.11 16.81 124 37935 48214 42535062
Gait inability 49.80 16.81 80 37979 22753 42560523
Tumour thrombosis 49.77 16.81 15 38044 212 42583064
Pain in extremity 49.46 16.81 265 37794 150339 42432937
Fall 48.89 16.81 84 37975 234436 42348840
Malignant neoplasm progression 48.06 16.81 208 37851 108192 42475084
Metastases to central nervous system 47.07 16.81 52 38007 10303 42572973
Metastases to spine 46.88 16.81 31 38028 3046 42580230
Pyrexia 45.82 16.81 545 37514 393497 42189779
Pancreatic enzymes increased 45.42 16.81 20 38039 865 42582411
Metastases to liver 43.82 16.81 63 37996 16263 42567013
Hypophosphataemia 43.80 16.81 72 37987 20873 42562403
Nephrotic syndrome 43.52 16.81 46 38013 8672 42574604
Hypotension 42.90 16.81 105 37954 257526 42325750
Cerebral infarction 42.34 16.81 89 37970 31080 42552196
Metastasis 41.31 16.81 34 38025 4671 42578605
Pneumonia 39.36 16.81 219 37840 421930 42161346
Intentional product misuse 38.29 16.81 5 38054 61895 42521381
Weight increased 37.74 16.81 25 38034 107958 42475318
Therapeutic product effect incomplete 36.82 16.81 9 38050 70930 42512346
Tumour marker increased 36.73 16.81 17 38042 827 42582449
Alanine aminotransferase increased 36.43 16.81 166 37893 88240 42495036
Hepatic rupture 36.05 16.81 9 38050 59 42583217
Gastric ulcer 35.81 16.81 61 37998 18201 42565075
Liver abscess 35.67 16.81 32 38027 4938 42578338
Tumour haemorrhage 33.43 16.81 27 38032 3611 42579665
Product dose omission issue 33.33 16.81 54 38005 154311 42428965
Haematemesis 32.92 16.81 79 37980 30120 42553156
Neutropenia 32.61 16.81 82 37977 199349 42383927
Graft versus host disease in skin 32.45 16.81 31 38028 5181 42578095
Keratoacanthoma 32.27 16.81 16 38043 908 42582368
Asthma 32.16 16.81 8 38051 62306 42520970
Intentional product use issue 32.07 16.81 12 38047 71821 42511455
Death 31.99 16.81 594 37465 470591 42112685
Reactive perforating collagenosis 31.98 16.81 6 38053 6 42583270
Epistaxis 31.75 16.81 131 37928 66695 42516581
Cardiac arrest 31.12 16.81 31 38028 109289 42473987
Anxiety 31.10 16.81 36 38023 118524 42464752
Oral lichenoid reaction 30.21 16.81 9 38050 122 42583154
Skin fissures 29.95 16.81 40 38019 9636 42573640
Malaise 29.87 16.81 305 37754 211851 42371425
Lactic acidosis 29.63 16.81 3 38056 45258 42538018
Erythema 29.50 16.81 182 37877 108611 42474665
Hyperamylasaemia 28.57 16.81 13 38046 608 42582668
Wheezing 28.33 16.81 7 38052 54774 42528502
Bradycardia 28.27 16.81 21 38038 85463 42497813
Hepatic cancer metastatic 28.16 16.81 14 38045 799 42582477
Cancer pain 27.66 16.81 24 38035 3543 42579733
General physical health deterioration 27.63 16.81 230 37829 151016 42432260
Coronary artery disease 27.52 16.81 7 38052 53713 42529563
Chronic obstructive pulmonary disease 27.41 16.81 11 38048 63103 42520173
Suicidal ideation 27.27 16.81 5 38054 48156 42535120
Product administered to patient of inappropriate age 27.17 16.81 27 38032 4734 42578542
Proteinuria 27.09 16.81 62 37997 22921 42560355
Septal panniculitis 26.71 16.81 7 38052 57 42583219
Prostate cancer 26.68 16.81 4 38055 44639 42538637
Hyperammonaemia 26.65 16.81 34 38025 7832 42575444
Stress 26.34 16.81 4 38055 44208 42539068
Depression 25.91 16.81 37 38022 111326 42471950
Haemobilia 25.55 16.81 11 38048 450 42582826
Plantar erythema 25.52 16.81 7 38052 69 42583207
Incorrect dose administered 25.11 16.81 8 38051 52966 42530310
Parathyroid tumour malignant 24.83 16.81 7 38052 77 42583199
Gingival bleeding 24.63 16.81 34 38025 8451 42574825
Drug reaction with eosinophilia and systemic symptoms 24.63 16.81 4 38055 42071 42541205
Therapeutic product effect decreased 24.61 16.81 3 38056 39147 42544129
Sinusitis 24.54 16.81 6 38053 47286 42535990
Glossodynia 24.54 16.81 24 38035 4128 42579148
Melaena 24.26 16.81 83 37976 38663 42544613
Morphoea 24.19 16.81 9 38050 250 42583026
Hepatic cirrhosis 24.17 16.81 54 38005 19648 42563628
Lower respiratory tract infection 23.93 16.81 4 38055 41202 42542074
Agitation 23.69 16.81 14 38045 64300 42518976
Hypersensitivity 23.64 16.81 18 38041 72352 42510924
Varices oesophageal 23.53 16.81 24 38035 4341 42578935
Tachycardia 23.11 16.81 34 38025 101053 42482223
Gastric antral vascular ectasia 23.01 16.81 10 38049 419 42582857
Varicose vein ruptured 22.90 16.81 7 38052 104 42583172
Cytomegalovirus infection reactivation 22.79 16.81 38 38021 11140 42572136
Febrile neutropenia 22.79 16.81 87 37972 185616 42397660
Abdominal distension 22.67 16.81 125 37934 71610 42511666
Nasopharyngitis 22.57 16.81 25 38034 83971 42499305
Neuropathy peripheral 22.57 16.81 35 38024 101818 42481458
Neoplasm 22.55 16.81 28 38031 6277 42576999
Prothrombin level increased 22.14 16.81 8 38051 204 42583072
Hyperhidrosis 22.14 16.81 29 38030 90483 42492793
Genital rash 22.13 16.81 12 38047 820 42582456
Poikiloderma 21.91 16.81 9 38050 327 42582949
Faeces discoloured 21.28 16.81 47 38012 16967 42566309
Oxygen saturation decreased 21.25 16.81 16 38043 64671 42518605
Influenza 20.91 16.81 15 38044 62160 42521116
Skin ulcer 20.78 16.81 60 37999 25541 42557735
Hospitalisation 20.55 16.81 125 37934 74205 42509071
Graft versus host disease in lung 20.49 16.81 11 38048 737 42582539
Hepatic infarction 20.26 16.81 8 38051 262 42583014
Hepatic artery thrombosis 20.14 16.81 8 38051 266 42583010
Rhabdomyolysis 20.12 16.81 24 38035 77995 42505281
Metastases to heart 20.09 16.81 7 38052 160 42583116
Blood lactate dehydrogenase increased 20.09 16.81 60 37999 26021 42557255
Septic shock 19.84 16.81 32 38027 91640 42491636
Joint swelling 19.68 16.81 19 38040 68003 42515273
Gastrointestinal perforation 19.48 16.81 22 38037 4464 42578812
Somnolence 19.38 16.81 63 37996 141042 42442234
Food refusal 18.80 16.81 8 38051 318 42582958
Lymphadenopathy 18.76 16.81 69 37990 33296 42549980
Therapeutic response decreased 18.62 16.81 5 38054 37007 42546269
Aortic dissection 18.61 16.81 18 38041 3054 42580222
Oropharyngeal blistering 18.46 16.81 7 38052 205 42583071
Tumour embolism 18.41 16.81 6 38053 111 42583165
Glossitis 18.09 16.81 13 38046 1461 42581815
Metastases to gallbladder 18.07 16.81 3 38056 0 42583276
Thyroid atrophy 18.07 16.81 3 38056 0 42583276
Encephalopathy 18.05 16.81 79 37980 41254 42542022
Dehydration 17.68 16.81 199 37860 141568 42441708
Medication error 17.61 16.81 4 38055 33150 42550126
Wrong technique in product usage process 17.60 16.81 8 38051 42627 42540649
Thyroid cancer metastatic 17.49 16.81 5 38054 58 42583218
Upper respiratory tract infection 17.28 16.81 8 38051 42165 42541111
Arthritis 17.20 16.81 8 38051 42057 42541219
Albumin urine present 17.15 16.81 8 38051 396 42582880
Hepatic pain 17.14 16.81 13 38046 1587 42581689
Sleep disorder 16.98 16.81 11 38048 48084 42535192
Electrocardiogram QT prolonged 16.88 16.81 11 38048 47934 42535342
Dysphagia 16.86 16.81 117 37942 72602 42510674
Tumour necrosis 16.82 16.81 13 38046 1631 42581645

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
Palmar-plantar erythrodysaesthesia syndrome 5399.72 17.17 1558 48058 39467 110500216
Hepatic cancer 1075.12 17.17 334 49282 10822 110528861
Hepatic function abnormal 943.94 17.17 554 49062 88741 110450942
Hepatic encephalopathy 865.28 17.17 362 49254 27894 110511789
Diarrhoea 834.28 17.17 1672 47944 1137833 109401850
Ascites 650.14 17.17 444 49172 92364 110447319
Decreased appetite 604.51 17.17 894 48722 474952 110064731
Metastases to lung 553.93 17.17 249 49367 22814 110516869
Hepatic failure 476.82 17.17 327 49289 68412 110471271
Alpha 1 foetoprotein increased 433.64 17.17 96 49520 768 110538915
Hypertension 409.63 17.17 781 48835 509303 110030380
Hepatocellular carcinoma 280.39 17.17 120 49496 9760 110529923
Amylase increased 262.39 17.17 123 49493 12396 110527287
Blood bilirubin increased 232.19 17.17 224 49392 75748 110463935
Hyperkeratosis 228.95 17.17 102 49514 9137 110530546
Rash 227.30 17.17 845 48771 820119 109719564
Acute myeloid leukaemia recurrent 224.00 17.17 85 49531 5054 110534629
Dysphonia 221.06 17.17 218 49398 75711 110463972
Lipase increased 199.99 17.17 117 49499 18555 110521128
Jaundice 198.85 17.17 184 49432 59052 110480631
Ammonia increased 191.45 17.17 87 49529 8163 110531520
Skin toxicity 187.69 17.17 96 49520 11687 110527996
Skin exfoliation 179.75 17.17 209 49407 87442 110452241
Platelet count decreased 167.52 17.17 339 49277 230104 110309579
Liver carcinoma ruptured 161.93 17.17 36 49580 294 110539389
Infusion related reaction 156.17 17.17 3 49613 381159 110158524
Death 154.36 17.17 671 48945 698198 109841485
Drug hypersensitivity 149.96 17.17 15 49601 454075 110085608
Drug ineffective 148.29 17.17 287 49329 1520253 109019430
Oesophageal varices haemorrhage 146.73 17.17 62 49554 4883 110534800
Blister 126.02 17.17 300 49316 227076 110312607
Renal cell carcinoma 124.74 17.17 63 49553 7467 110532216
Erythema multiforme 117.74 17.17 88 49528 21009 110518674
Dry skin 117.36 17.17 189 49427 107464 110432219
Condition aggravated 117.04 17.17 95 49521 734741 109804942
Rheumatoid arthritis 116.54 17.17 4 49612 299609 110240074
Alopecia 115.49 17.17 393 49223 364360 110175323
Metastases to bone 112.19 17.17 101 49515 31271 110508412
Weight increased 111.07 17.17 26 49590 419618 110120065
Metastases to lymph nodes 110.05 17.17 74 49542 14958 110524725
Malignant neoplasm progression 109.60 17.17 242 49374 174325 110365358
Bone marrow failure 108.76 17.17 132 49484 57716 110481967
Joint swelling 106.72 17.17 33 49583 442812 110096871
Portal vein thrombosis 105.20 17.17 55 49561 7003 110532680
Asthenia 103.26 17.17 593 49023 688406 109851277
Pain of skin 101.76 17.17 79 49537 19950 110519733
Metastases to adrenals 101.71 17.17 35 49581 1568 110538115
Aspartate aminotransferase increased 99.58 17.17 221 49395 159715 110379968
Weight decreased 98.99 17.17 444 49172 467613 110072070
Fatigue 96.37 17.17 898 48718 1215060 109324623
Hypophosphataemia 96.02 17.17 95 49521 33087 110506596
Blood pressure increased 95.86 17.17 294 49322 258079 110281604
Tumour rupture 95.15 17.17 27 49589 633 110539050
Sinusitis 94.83 17.17 11 49605 296677 110243006
Pyrexia 94.34 17.17 707 48909 897558 109642125
Hypersensitivity 93.99 17.17 32 49584 403966 110135717
Nasopharyngitis 93.91 17.17 30 49586 394331 110145352
Off label use 93.74 17.17 1055 48561 1499130 109040553
Therapeutic product effect decreased 92.48 17.17 4 49612 244312 110295371
Lower respiratory tract infection 91.96 17.17 4 49612 243102 110296581
Completed suicide 88.46 17.17 5 49611 242376 110297307
Abdominal pain 85.77 17.17 455 49161 512534 110027149
Protein induced by vitamin K absence or antagonist II increased 85.45 17.17 16 49600 47 110539636
Metastases to peritoneum 84.43 17.17 44 49572 5566 110534117
Hepatic lesion 82.55 17.17 50 49566 8443 110531240
Overdose 79.04 17.17 7 49609 233787 110305896
Asthma 78.21 17.17 10 49606 250281 110289402
Pericarditis 75.61 17.17 6 49610 219108 110320575
Wheezing 75.55 17.17 12 49604 255218 110284465
Psoriatic arthropathy 75.21 17.17 3 49613 196758 110342925
Toxicity to various agents 74.10 17.17 64 49552 480491 110059192
COVID-19 73.72 17.17 11 49605 245049 110294634
Pancreatic enzymes increased 73.20 17.17 28 49588 1701 110537982
Cerebral infarction 70.64 17.17 101 49515 51737 110487946
Tumour thrombosis 68.56 17.17 18 49598 312 110539371
Stomatitis 67.63 17.17 270 49346 269972 110269711
Wound 67.22 17.17 12 49604 234425 110305258
Metastases to liver 66.92 17.17 81 49535 35305 110504378
Metastases to spine 66.67 17.17 37 49579 5306 110534377
Arthralgia 66.59 17.17 158 49458 779474 109760209
Coma hepatic 66.33 17.17 23 49593 1054 110538629
Hepatorenal syndrome 66.17 17.17 35 49581 4562 110535121
Metastasis 66.09 17.17 43 49573 8224 110531459
Swelling 65.61 17.17 38 49578 351003 110188680
Liver disorder 65.48 17.17 175 49441 142068 110397615
Injury 63.63 17.17 4 49612 177261 110362422
Metastases to central nervous system 63.57 17.17 64 49552 22753 110516930
Intentional product use issue 62.38 17.17 17 49599 247889 110291794
Inappropriate schedule of product administration 61.57 17.17 9 49607 203628 110336055
Duodenal ulcer perforation 60.94 17.17 5 49611 177695 110361988
Therapeutic product effect incomplete 60.91 17.17 13 49603 223792 110315891
Type 2 diabetes mellitus 60.74 17.17 5 49611 177227 110362456
Fall 60.15 17.17 112 49504 603370 109936313
Pleural effusion 59.26 17.17 195 49421 177514 110362169
Liver abscess 58.82 17.17 39 49577 7700 110531983
Musculoskeletal stiffness 58.70 17.17 26 49590 279796 110259887
Nephrotic syndrome 58.48 17.17 49 49567 13782 110525901
Dehydration 58.12 17.17 264 49352 279247 110260436
Alanine aminotransferase increased 57.17 17.17 197 49419 183576 110356107
Tumour haemorrhage 56.51 17.17 33 49583 5212 110534471
Hospitalisation 55.48 17.17 165 49451 142328 110397355
Discomfort 55.40 17.17 14 49602 214693 110324990
Osteoarthritis 55.38 17.17 8 49608 182615 110357068
Erythema 55.28 17.17 268 49348 291179 110248504
Hyperammonaemia 54.68 17.17 47 49569 13685 110525998
Epistaxis 54.64 17.17 155 49461 130217 110409466
Proteinuria 54.56 17.17 78 49538 39940 110499743
Metastatic renal cell carcinoma 53.92 17.17 25 49591 2455 110537228
Pain in extremity 53.55 17.17 388 49228 486730 110052953
Blood cholesterol increased 51.81 17.17 10 49606 184775 110354908
Varices oesophageal 51.57 17.17 35 49581 7180 110532503
Tumour necrosis 51.24 17.17 24 49592 2412 110537271
Migraine 50.94 17.17 8 49608 171644 110368039
Treatment failure 49.02 17.17 32 49584 277202 110262481
Anxiety 48.42 17.17 50 49566 345028 110194655
Sleep disorder 47.45 17.17 15 49601 198629 110341054
Blood lactate dehydrogenase increased 47.15 17.17 77 49539 44257 110495426
Drug interaction 46.21 17.17 97 49519 500086 110039597
Plantar erythema 46.13 17.17 13 49603 297 110539386
Food refusal 46.09 17.17 17 49599 933 110538750
Product administered to patient of inappropriate age 45.91 17.17 34 49582 8002 110531681
Cancer pain 44.05 17.17 31 49585 6741 110532942
Urticaria 43.83 17.17 47 49569 318810 110220873
Disease progression 43.83 17.17 221 49395 243813 110295870
Pain 43.55 17.17 251 49365 954704 109584979
Gastric ulcer 43.48 17.17 70 49546 39757 110499926
Arthritis 43.09 17.17 11 49605 167575 110372108
Haematemesis 42.92 17.17 87 49529 59021 110480662
Ill-defined disorder 42.90 17.17 9 49607 156844 110382839
Melaena 41.63 17.17 94 49522 68663 110471020
Pneumonia adenoviral 40.71 17.17 14 49602 626 110539057
Graft versus host disease 40.47 17.17 46 49570 18760 110520923
Gingival bleeding 40.12 17.17 47 49569 19792 110519891
Hepatic rupture 40.01 17.17 10 49606 141 110539542
Hypotension 38.70 17.17 114 49502 523735 110015948
Gastrointestinal disorder 37.52 17.17 32 49584 241920 110297763
Upper respiratory tract infection 37.04 17.17 7 49609 131321 110408362
Skin fissures 36.82 17.17 50 49566 24408 110515275
Graft versus host disease in skin 36.47 17.17 30 49586 8224 110531459
Dysphagia 36.43 17.17 151 49465 153449 110386234
Haemoptysis 36.12 17.17 91 49525 71263 110468420
Reactive perforating collagenosis 36.10 17.17 6 49610 6 110539677
Depression 36.10 17.17 54 49562 317281 110222402
Folliculitis 36.07 17.17 15 49601 167638 110372045
Keratoacanthoma 35.92 17.17 16 49600 1432 110538251
Intentional product misuse 35.59 17.17 8 49608 132896 110406787
Gastric antral vascular ectasia 35.49 17.17 15 49601 1182 110538501
Gastrointestinal haemorrhage 34.87 17.17 157 49459 165361 110374322
Hepatic cancer metastatic 34.85 17.17 14 49602 969 110538714
Oral pain 34.48 17.17 61 49555 37383 110502300
Adenoviral hepatitis 34.46 17.17 14 49602 998 110538685
Road traffic accident 34.25 17.17 4 49612 107394 110432289
Abdominal distension 33.88 17.17 162 49454 174941 110364742
Thrombocytopenia 33.86 17.17 270 49346 348615 110191068
Medication error 33.41 17.17 4 49612 105362 110434321
Cytomegalovirus infection reactivation 33.10 17.17 41 49575 18292 110521391
Oral lichenoid reaction 33.02 17.17 9 49607 181 110539502
Gastrointestinal perforation 32.74 17.17 27 49589 7429 110532254
Oropharyngeal blistering 32.22 17.17 13 49603 910 110538773
Night sweats 32.20 17.17 10 49606 133973 110405710
Blood albumin decreased 32.11 17.17 50 49566 27602 110512081
Pulmonary fibrosis 32.05 17.17 4 49612 102038 110437645
Inflammation 31.91 17.17 24 49592 193214 110346469
Palmoplantar keratoderma 31.24 17.17 23 49593 5364 110534319
Skin ulcer 31.00 17.17 80 49536 63565 110476118
Sciatica 30.59 17.17 3 49613 92396 110447287
Cholangitis 30.25 17.17 37 49579 16298 110523385
Fluid intake reduced 30.05 17.17 25 49591 6961 110532722
Lymphadenopathy 29.82 17.17 79 49537 63756 110475927
Mucosal inflammation 29.82 17.17 103 49513 96038 110443645
Faeces discoloured 29.59 17.17 54 49562 33894 110505789
Hyperbilirubinaemia 29.59 17.17 51 49565 30620 110509063
Catabolic state 29.53 17.17 7 49609 78 110539605
Parathyroid tumour malignant 29.30 17.17 8 49608 162 110539521
Stress 28.90 17.17 6 49610 105342 110434341
Neoplasm 28.89 17.17 30 49586 11057 110528626
Abdominal discomfort 28.86 17.17 86 49530 393772 110145911
Product use in unapproved indication 28.73 17.17 317 49299 447060 110092623
Hyperamylasaemia 28.72 17.17 13 49603 1208 110538475
Lymphadenopathy mediastinal 28.66 17.17 22 49594 5462 110534221
Bronchitis 27.92 17.17 18 49598 157014 110382669
Glossitis 27.88 17.17 20 49596 4481 110535202
Hypocalcaemia 26.68 17.17 77 49539 65289 110474394
Anaphylactic reaction 26.64 17.17 9 49607 114291 110425392
Illness 26.35 17.17 3 49613 82168 110457515
Contusion 26.25 17.17 40 49576 233321 110306362
Aortic dissection 26.24 17.17 20 49596 4913 110534770
Anaemia 26.23 17.17 367 49249 546719 109992964
Encephalopathy 26.16 17.17 88 49528 80967 110458716
Nasal congestion 26.14 17.17 6 49610 98276 110441407
Lactic acidosis 26.06 17.17 5 49611 92806 110446877
Osteoporosis 25.99 17.17 4 49612 87148 110452535
Memory impairment 25.99 17.17 30 49586 196914 110342769
Tumour marker increased 25.79 17.17 20 49596 5040 110534643
Hepatic enzyme increased 25.78 17.17 67 49549 320825 110218858
Gamma-glutamyltransferase increased 25.78 17.17 73 49543 61236 110478447
Liver injury 25.72 17.17 18 49598 150395 110389288
Septal panniculitis 25.63 17.17 7 49609 142 110539541
Tumour lysis syndrome 25.60 17.17 48 49568 30753 110508930
Haemobilia 25.60 17.17 10 49606 643 110539040
Headache 25.50 17.17 263 49353 882114 109657569
Influenza 25.45 17.17 23 49593 169078 110370605
Oxygen saturation decreased 25.28 17.17 20 49596 156962 110382721
Hypercholesterolaemia 25.28 17.17 5 49611 90832 110448851
Hypoalbuminaemia 25.14 17.17 46 49570 28928 110510755
Graft versus host disease in lung 25.07 17.17 12 49604 1266 110538417
Hepatic pain 24.92 17.17 19 49597 4671 110535012
Lip dry 24.91 17.17 7 49609 100076 110439607
Poikiloderma 24.59 17.17 9 49607 483 110539200
Hypophagia 24.45 17.17 65 49551 52561 110487122
Skin lesion 24.22 17.17 64 49552 51567 110488116
Thyroid cancer metastatic 24.20 17.17 7 49609 176 110539507
Renal cell carcinoma stage IV 24.12 17.17 6 49610 83 110539600
Blood sodium decreased 23.88 17.17 53 49563 38266 110501417
Hiccups 23.59 17.17 29 49587 12840 110526843
Grip strength decreased 23.20 17.17 4 49612 80170 110459513
Mobility decreased 22.78 17.17 45 49571 237377 110302306
Metastases to abdominal cavity 22.74 17.17 10 49606 868 110538815
Pneumonia 22.67 17.17 268 49348 876446 109663237
Morphoea 22.60 17.17 9 49607 609 110539074
Suicidal ideation 22.59 17.17 7 49609 93930 110445753
Feeding disorder 22.57 17.17 37 49579 21325 110518358
Rhinorrhoea 22.38 17.17 9 49607 102657 110437026
Acute kidney injury 21.97 17.17 181 49435 635249 109904434
Metastases to heart 21.96 17.17 8 49608 424 110539259
Gastrointestinal toxicity 21.86 17.17 26 49590 11122 110528561
Pancytopenia 21.86 17.17 165 49451 209448 110330235
Joint range of motion decreased 21.61 17.17 14 49602 121818 110417865
Alpha 1 foetoprotein abnormal 21.49 17.17 5 49611 51 110539632
Bradycardia 21.27 17.17 23 49593 155494 110384189
Psoriasis 21.11 17.17 19 49597 139974 110399709
Gastrooesophageal reflux disease 21.07 17.17 30 49586 179946 110359737
Product dose omission issue 20.96 17.17 74 49542 321708 110217975
Hypoaesthesia 20.65 17.17 72 49544 314151 110225532
Infection 20.58 17.17 88 49528 362112 110177571
Abdominal pain upper 20.43 17.17 243 49373 348868 110190815
Tumour pain 20.28 17.17 14 49602 2953 110536730
Varicose vein ruptured 20.23 17.17 6 49610 165 110539518
Disseminated intravascular coagulation 20.21 17.17 52 49564 41234 110498449
Therapeutic response decreased 20.17 17.17 9 49607 96490 110443193
Wound infection 20.16 17.17 9 49607 96456 110443227
Chronic obstructive pulmonary disease 20.11 17.17 12 49604 109146 110430537
Colitis ulcerative 20.03 17.17 5 49611 77358 110462325
Metastases to pleura 19.67 17.17 12 49604 2051 110537632
Incorrect dose administered 19.66 17.17 11 49605 103630 110436053
Large intestine perforation 19.21 17.17 30 49586 16599 110523084
Cataract 18.98 17.17 6 49610 79479 110460204
Incorrect route of product administration 18.97 17.17 3 49613 64058 110475625
Genital rash 18.75 17.17 10 49606 1325 110538358
Herpes simplex viraemia 18.56 17.17 8 49608 661 110539022
Hyperhidrosis 18.40 17.17 35 49581 187263 110352420
Duodenal ulcer 18.24 17.17 32 49584 19482 110520201
Bleeding varicose vein 18.07 17.17 8 49608 705 110538978
Scrotal ulcer 18.02 17.17 7 49609 443 110539240
Hypoglycaemia 17.99 17.17 101 49515 116003 110423680
Tongue blistering 17.79 17.17 11 49605 1926 110537757
Graft versus host disease in liver 17.72 17.17 12 49604 2453 110537230
Albumin urine present 17.66 17.17 8 49608 745 110538938
General physical health deterioration 17.51 17.17 278 49338 425017 110114666
Tumour embolism 17.22 17.17 6 49610 279 110539404

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EX02 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 D047428 Protein Kinase Inhibitors
FDA EPC N0000175605 Kinase Inhibitor
CHEBI has role CHEBI:35526 hypoglycemic agent
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:35674 antihypertensive agent
CHEBI has role CHEBI:38637 tyrosine kinase inhibitor
CHEBI has role CHEBI:48422 angiogenesis inhibitor
CHEBI has role CHEBI:50249 anticoagulant
CHEBI has role CHEBI:50925 EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor
CHEBI has role CHEBI:149553 anticoronaviral agent
CHEBI has role CHEBI:173085 ferroptosis inducer
CHEBI has role CHEBI:231911 renoprotective agent
CHEBI has role CHEBI:22587 antiviral agent

Related Drugs by ATC class:

L01EX Other protein kinase inhibitors 21 drugs
avapritinibcabozantinibcapivasertibentrectinibgilteritiniblarotrectiniblenvatinibmidostaurinnintedanibpazopanibpexidartinibpralsetinib show all 21 →

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

DiseaseRelationSNOMED_IDDOID
Liver cell carcinoma indication 109841003 DOID:684
Carcinoma of thyroid indication 448216007
Renal cell carcinoma indication 702391001 DOID:4450
Hypophosphatemia contraindication 4996001
Acute hemorrhage contraindication 8573003
Myocardial infarction contraindication 22298006 DOID:5844
Depressive disorder contraindication 35489007
Hypertensive disorder contraindication 38341003 DOID:10763
Gastrointestinal perforation contraindication 51875005
Hepatic failure contraindication 59927004
Blood coagulation disorder contraindication 64779008 DOID:1247
Pancreatitis contraindication 75694006 DOID:4989
Angina pectoris contraindication 194828000
Impaired wound healing contraindication 271618001
Anemia contraindication 271737000 DOID:2355
Pregnancy, function contraindication 289908002
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Neutropenic disorder contraindication 303011007 DOID:1227
Surgical procedure contraindication 387713003
Acute coronary syndrome contraindication 394659003
Breastfeeding (mother) contraindication 413712001
Disorder of coronary artery contraindication 414024009
Myocardial ischemia contraindication 414795007 DOID:3393




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.84 acidic
pKa2 11.97 acidic
pKa3 12.61 acidic
pKa4 2.76 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 200MG BASE NEXAVAR BAYER HLTHCARE N021923 Dec. 20, 2005 RX TABLET ORAL 8877933 Dec. 24, 2027 TREATMENT OF UNRESECTABLE HEPATOCELLULAR CARCINOMA, ADVANCED RENAL CELL CARCINOMA, OR DIFFERENTIATED THYROID CARCINOMA.
EQ 200MG BASE NEXAVAR BAYER HLTHCARE N021923 Dec. 20, 2005 RX TABLET ORAL 9737488 Sept. 10, 2028 TREATMENT OF ADVANCED RENAL CELL CARCINOMA
EQ 200MG BASE NEXAVAR BAYER HLTHCARE N021923 Dec. 20, 2005 RX TABLET ORAL 9737488 Sept. 10, 2028 TREATMENT OF LOCALLY RECURRENT OR METASTATIC, PROGRESSIVE, DIFFERENTIATED THYROID CARCINOMA REFRACTORY TO RADIOACTIVE IODINE TREATMENT
EQ 200MG BASE NEXAVAR BAYER HLTHCARE N021923 Dec. 20, 2005 RX TABLET ORAL 9737488 Sept. 10, 2028 TREATMENT OF UNRESECTABLE HEPATOCELLULAR CARCINOMA

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Platelet-derived growth factor receptor beta Kinase INHIBITOR Kd 7.43 CHEMBL CHEMBL
Mast/stem cell growth factor receptor Kit Kinase INHIBITOR Kd 7.80 CHEMBL CHEMBL
RAF proto-oncogene serine/threonine-protein kinase Kinase INHIBITOR Ki 8.22 CHEMBL CHEMBL
Receptor-type tyrosine-protein kinase FLT3 Kinase INHIBITOR Kd 8.35 CHEMBL CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret Kinase INHIBITOR Kd 8.13 CHEMBL CHEMBL
Vascular endothelial growth factor receptor 1 Kinase INHIBITOR Kd 7.51 CHEMBL CHEMBL
Vascular endothelial growth factor receptor 2 Kinase INHIBITOR Ki 10.68 CHEMBL CHEMBL
Vascular endothelial growth factor receptor 3 Kinase INHIBITOR Kd 7.80 CHEMBL CHEMBL
Serine/threonine-protein kinase B-raf Kinase INHIBITOR Ki 7.66 CHEMBL CHEMBL
5-hydroxytryptamine receptor 5A GPCR Ki 5.48 CHEMBL
Carbonic anhydrase 9 Enzyme Ki 5.09 CHEMBL
Tyrosine-protein kinase ABL1 Kinase Kd 6.89 CHEMBL
Epidermal growth factor receptor Kinase IC50 8.53 CHEMBL
Carbonic anhydrase 7 Enzyme Ki 5.09 CHEMBL
Proto-oncogene tyrosine-protein kinase Src Kinase IC50 6.41 CHEMBL
Tyrosine-protein kinase Lck Kinase Kd 5.57 CHEMBL
Tyrosine-protein kinase Fyn Kinase Kd 5.08 CHEMBL
Ephrin type-A receptor 2 Kinase Kd 5.70 CHEMBL
Macrophage colony-stimulating factor 1 receptor Kinase Kd 7.55 CHEMBL
Platelet-derived growth factor receptor alpha Kinase Kd 7.21 CHEMBL
Receptor tyrosine-protein kinase erbB-2 Kinase IC50 6.88 CHEMBL
Cyclin-dependent kinase 2 Kinase Kd 5.06 CHEMBL
Insulin receptor Kinase AGONIST IC50 5.28 CHEMBL
Fibroblast growth factor receptor 3 Kinase Kd 5.38 CHEMBL
Tyrosine-protein kinase HCK Kinase Kd 5.07 CHEMBL
High affinity nerve growth factor receptor Kinase Kd 5.44 CHEMBL
Myosin light chain kinase 2, skeletal/cardiac muscle Kinase Kd 5.89 CHEMBL
Tyrosine-protein kinase CSK Kinase Kd 5.54 CHEMBL
Angiopoietin-1 receptor Kinase Kd 5.68 CHEMBL
Ephrin type-A receptor 8 Kinase Kd 6.02 CHEMBL
Hepatocyte growth factor receptor Kinase IC50 5.24 CHEMBL
Tyrosine-protein kinase Lyn Kinase Kd 5.52 CHEMBL
LIM domain kinase 1 Kinase Kd 5.80 CHEMBL
Fibroblast growth factor receptor 1 Kinase Kd 5.60 CHEMBL
Cyclin-dependent-like kinase 5 Kinase Kd 5.21 CHEMBL
Serine/threonine-protein kinase 10 Kinase Kd 6.85 CHEMBL
Serine/threonine-protein kinase PLK4 Kinase Kd 5.47 CHEMBL
Aurora kinase C Kinase Kd 6.68 CHEMBL
Dual specificity protein kinase TTK Kinase Kd 5.46 CHEMBL
Abelson tyrosine-protein kinase 2 Kinase Kd 5.89 CHEMBL
Mitogen-activated protein kinase 11 Kinase Kd 6.70 CHEMBL
Ephrin type-A receptor 5 Kinase Kd 6.44 CHEMBL
Ephrin type-A receptor 4 Kinase Kd 5.89 CHEMBL
Fibroblast growth factor receptor 2 Kinase Kd 5.57 CHEMBL
Mitogen-activated protein kinase 3 Kinase IC50 7.74 CHEMBL
Ephrin type-A receptor 6 Kinase Kd 6.62 CHEMBL
TRAF2 and NCK-interacting protein kinase Kinase Kd 5.10 CHEMBL
Mitogen-activated protein kinase 12 Kinase Kd 5.12 CHEMBL
Tyrosine-protein kinase Fgr Kinase Kd 5.11 CHEMBL
Aurora kinase A Kinase IC50 5.42 CHEMBL
Serine/threonine-protein kinase 36 Kinase Kd 5.42 CHEMBL
Ephrin type-A receptor 3 Kinase Kd 5.72 CHEMBL
Mitogen-activated protein kinase 14 Kinase Kd 6.59 CHEMBL
Tyrosine-protein kinase FRK Kinase Kd 6.36 CHEMBL
Dual specificity protein kinase CLK1 Kinase Kd 5.12 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 5 Kinase Kd 5.80 CHEMBL
Glycogen synthase kinase-3 beta Kinase IC50 5.08 CHEMBL
Receptor-interacting serine/threonine-protein kinase 2 Kinase Kd 5.89 CHEMBL
Ephrin type-B receptor 1 Kinase Kd 5.77 CHEMBL
Ephrin type-A receptor 7 Kinase Kd 6.17 CHEMBL
STE20-like serine/threonine-protein kinase Kinase Kd 6 CHEMBL
MAP kinase-interacting serine/threonine-protein kinase 2 Kinase Kd 6.89 CHEMBL
Mitogen-activated protein kinase 9 Kinase Kd 5.44 CHEMBL
Epithelial discoidin domain-containing receptor 1 Kinase Kd 8.82 CHEMBL
Ephrin type-B receptor 4 Kinase Kd 5.74 CHEMBL
Cyclin-dependent kinase 15 Kinase Kd 5.54 CHEMBL
Bifunctional epoxide hydrolase 2 Enzyme IC50 7.92 CHEMBL
TGF-beta receptor type-2 Kinase Kd 5.16 CHEMBL
Mitogen-activated protein kinase 1 Kinase IC50 6.96 CHEMBL
Cyclin-dependent kinase 6 Kinase IC50 6.89 CHEMBL
Tyrosine-protein kinase receptor UFO Kinase Kd 5.35 CHEMBL
BDNF/NT-3 growth factors receptor Kinase Kd 5.68 CHEMBL
Ephrin type-B receptor 2 Kinase Kd 5.72 CHEMBL
Cyclin-dependent kinase 7 Kinase Kd 6.85 CHEMBL
Ribosomal protein S6 kinase alpha-6 Kinase Kd 5.12 CHEMBL
Non-receptor tyrosine-protein kinase TNK1 Kinase Kd 5.64 CHEMBL
Mitogen-activated protein kinase 13 Kinase Kd 5.18 CHEMBL
Cyclin-dependent kinase 17 Kinase Kd 5.80 CHEMBL
Cyclin-dependent kinase 14 Kinase Kd 5.54 CHEMBL
Mitogen-activated protein kinase kinase kinase MLT Kinase Kd 8.20 CHEMBL
Tyrosine-protein kinase receptor Tie-1 Kinase Kd 7.17 CHEMBL
NT-3 growth factor receptor Kinase Kd 6.22 CHEMBL
LIM domain kinase 2 Kinase Kd 5.02 CHEMBL
MAP kinase-interacting serine/threonine-protein kinase 1 Kinase Kd 6.64 CHEMBL
Serine/threonine-protein kinase NLK Kinase Kd 6.19 CHEMBL
Serine/threonine-protein kinase 33 Kinase Kd 5.62 CHEMBL
Serine/threonine-protein kinase TNNI3K Kinase Kd 6.55 CHEMBL
Discoidin domain-containing receptor 2 Kinase Kd 8.18 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 1 Kinase Kd 5.32 CHEMBL
Aurora kinase B Kinase Kd 6.36 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 4 Kinase Kd 5.32 CHEMBL
Tyrosine-protein kinase Mer Kinase Kd 5.44 CHEMBL
Cyclin-dependent kinase 19 Kinase Kd 6.60 CHEMBL
Cyclin-dependent kinase 8 Kinase Kd 6.51 CHEMBL
Muscle, skeletal receptor tyrosine-protein kinase Kinase Kd 6.89 CHEMBL
Citron Rho-interacting kinase Kinase Kd 5.21 CHEMBL
Myosin-IIIb Kinase Kd 5.15 CHEMBL
Cyclin-dependent kinase 3 Kinase Kd 5.42 CHEMBL
Tyrosine-protein kinase Srms Kinase Kd 5.01 CHEMBL
Ephrin type-A receptor 1 Kinase Kd 5.51 CHEMBL
Mitogen-activated protein kinase 15 Kinase Kd 7.34 CHEMBL
Receptor-interacting serine/threonine-protein kinase 1 Kinase IC50 5.82 CHEMBL
Casein kinase I isoform alpha Kinase IC50 6.60 CHEMBL
Cyclin-dependent kinase-like 2 Kinase Kd 6.89 CHEMBL
Cyclin-dependent kinase-like 3 Kinase Kd 6.31 CHEMBL
Ephrin type-B receptor 6 Kinase Kd 6.62 CHEMBL
Homeodomain-interacting protein kinase 2 Kinase Kd 5.77 CHEMBL
Homeodomain-interacting protein kinase 3 Kinase Kd 6.41 CHEMBL
Homeodomain-interacting protein kinase 4 Kinase Kd 8.57 CHEMBL
Mitogen-activated protein kinase kinase kinase 7 Kinase Kd 6.16 CHEMBL
Serine/threonine-protein kinase TAO1 Kinase Kd 6.27 CHEMBL
Serine/threonine-protein kinase TAO3 Kinase Kd 5.57 CHEMBL
Mitogen-activated protein kinase kinase kinase 19 Kinase Kd 7 CHEMBL
Homeodomain-interacting protein kinase 1 Kinase Kd 5.96 CHEMBL
Mitogen-activated protein kinase kinase kinase 1 Kinase Kd 5.42 CHEMBL
Serine/threonine-protein kinase TAO2 Kinase Kd 6.27 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 5 Kinase Kd 6.72 CHEMBL
Myosin light chain kinase 3 Kinase Kd 5.02 CHEMBL
Phosphodiesterase 6D Enzyme Kd 5.91 CHEMBL
Serine/threonine-protein kinase A-Raf Kinase IC50 8.15 CHEMBL
Receptor-interacting serine/threonine-protein kinase 3 Kinase IC50 4.84 CHEMBL
RuvB-like 2 Enzyme Kd 4.66 CHEMBL
Tyrosine-protein kinase JAK3 Kinase Kd 5.14 CHEMBL
5-hydroxytryptamine receptor 1A GPCR Ki 5.93 CHEMBL
5-hydroxytryptamine receptor 2A GPCR Ki 5.71 CHEMBL
5-hydroxytryptamine receptor 2B GPCR Ki 7.25 CHEMBL
5-hydroxytryptamine receptor 2C GPCR Ki 6.38 CHEMBL
5-hydroxytryptamine receptor 6 GPCR Ki 5.21 CHEMBL
5-hydroxytryptamine receptor 7 GPCR Ki 5.15 CHEMBL
ATP-binding cassette sub-family G member 2 Transporter IC50 5.51 CHEMBL
Tyrosine-protein kinase ABL1 Kinase IC50 6.65 CHEMBL
Calcium-dependent protein kinase 1 Kinase Kd 6.66 CHEMBL
Vascular endothelial growth factor receptor 2 Kinase IC50 7.82 CHEMBL
Vascular endothelial growth factor receptor 2 Kinase IC50 5.59 CHEMBL
Purine nucleoside phosphorylase Enzyme IC50 7.90 CHEMBL
Vascular endothelial growth factor receptor 3 Kinase INHIBITOR IC50 7.70 IUPHAR
Platelet-derived growth factor receptor beta Kinase INHIBITOR IC50 7.24 IUPHAR
Serine/threonine-protein kinase B-raf Kinase IC50 6.89 CHEMBL
Epidermal growth factor receptor Kinase IC50 5.46 CHEMBL

External reference:

IDSource
4025077 VUID
N0000175349 NUI
D06272 KEGG_DRUG
4025077 VANDF
C1516119 UMLSCUI
CHEBI:50924 CHEBI
BAX PDB_CHEM_ID
CHEMBL1336 ChEMBL_ID
CHEMBL1200485 ChEMBL_ID
D000077157 MESH_DESCRIPTOR_UI
DB00398 DRUGBANK_ID
5711 IUPHAR_LIGAND_ID
8234 INN_ID
475207-59-1 SECONDARY_CAS_RN
9ZOQ3TZI87 UNII
216239 PUBCHEM_CID
495881 RXNORM
20792 MMSL
348700 MMSL
40110 MMSL
73580 MMSL
d05691 MMSL
011160 NDDF
011161 NDDF
420681006 SNOMEDCT_US
422042001 SNOMEDCT_US
432886002 SNOMEDCT_US
9ZOQ3TZI87 INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Sorafenib Tosylate HUMAN PRESCRIPTION DRUG LABEL 1 0378-1201 TABLET, FILM COATED 200 mg ORAL ANDA 28 sections
Sorafenib HUMAN PRESCRIPTION DRUG LABEL 1 0480-5425 TABLET, FILM COATED 200 mg ORAL ANDA 27 sections
Sorafenib HUMAN PRESCRIPTION DRUG LABEL 1 13668-682 TABLET, FILM COATED 200 mg ORAL ANDA 27 sections
sorafenib HUMAN PRESCRIPTION DRUG LABEL 1 24979-715 TABLET, FILM COATED 200 mg ORAL ANDA 18 sections
sorafenib HUMAN PRESCRIPTION DRUG LABEL 1 24979-715 TABLET, FILM COATED 200 mg ORAL ANDA 18 sections
sorafenib HUMAN PRESCRIPTION DRUG LABEL 1 43598-458 TABLET, FILM COATED 200 mg ORAL ANDA 25 sections
Nexavar HUMAN PRESCRIPTION DRUG LABEL 1 50419-488 TABLET, FILM COATED 200 mg ORAL NDA 28 sections
Nexavar HUMAN PRESCRIPTION DRUG LABEL 1 50419-489 TABLET, FILM COATED 200 mg ORAL NDA 28 sections
sorafenib HUMAN PRESCRIPTION DRUG LABEL 1 51407-760 TABLET, FILM COATED 200 mg ORAL ANDA 17 sections
sorafenib HUMAN PRESCRIPTION DRUG LABEL 1 51990-201 TABLET, FILM COATED 200 mg ORAL ANDA 18 sections