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

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 4715 849217-68-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • cabozantinib malate
  • cabozantinib (S)-malate
  • cabozantinib
  • cometriq
  • XL184
  • cabozantinib S-malate
  • cabometyx
Cabozantinib inhibits the tyrosine kinase activity of MET, VEGFR-1, -2 and -3, AXL, RET, ROS1, TYRO3, MER, KIT, TRKB, FLT-3, and TIE-2. These receptor tyrosine kinases are involved in both normal cellular function and pathologic processes such as oncogenesis, metastasis, tumor angiogenesis, drug resistance, and maintenance of the tumor microenvironment.
  • Molecular weight: 501.51
  • Formula: C28H24FN3O5
  • CLOGP: 4.44
  • LIPINSKI: 1
  • HAC: 8
  • HDO: 2
  • TPSA: 98.78
  • ALOGS: -5.40
  • ROTB: 8
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
60 mg O

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 4.585 Moderate 0.76
caco2-efflux Caco-2 efflux ratio (BA/AB) 3.083 Moderate 0.76
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 11.508 10^-6 cm/s Moderate 0.76
dh-clint Dog hepatocyte intrinsic clearance 5.861 uL/min/10^6 cells Moderate 0.76
dppb Dog plasma protein binding (% unbound) 0.390 % Moderate 0.76
fcs-ppb Fetal calf serum protein binding (% unbound) 1.540 % Moderate 0.76
herg hERG pIC50 4.903 pIC50 Moderate 0.76
hh-clint Human hepatocyte intrinsic clearance 3.199 uL/min/10^6 cells Moderate 0.76
hlm-clint Human liver microsomal intrinsic clearance 8.185 uL/min/mg protein Moderate 0.76
hppb Human plasma protein binding (% unbound) 0.240 % Moderate 0.76
kinase-safety-class ABL1,ABL2,ACVR1B,ACVR2A,ACVR2B,ACVRL1,AKT1,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,BTK,CAMK2B,CAMK2D,CDK1,CDK7,CDK9,CSF1R,CSK,DDR1,EGFR,EIF2AK3,EPHA2,EPHB1,EPHB4,ERBB2,ERBB4,FGFR1,FLT1,FLT3,FLT4,FYN,GAK,GRK2,INSR,IRAK3,ITK,JAK1,JAK2,KDR,KIT,LCK,LYN,MAP2K1,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K21,MAP3K7,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK10,MAPK14,MAPK7,MARK4,MET,MINK1,MST1R,MTOR,NTRK1,NTRK2,PAK4,PDGFRB,PDK1,PDK2,PDK4,PIK3CA,PIK3CD,PIK3CG,PRKCD,PRKDC,PTK6,RET,RIPK3,SIK2,SIK3,SRC,STK10,STK33,SYK,TEK,TGFBR1,TNIK,TTK,TYRO3,ULK1,YES1 95
kinase-selectivity-class ABL2,ACVR2B,AKT1,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,CSF1R,CSK,DDR1,EGFR,EIF2AK3,EPHA2,EPHB3,EPHB4,ERBB2,ERBB4,FGFR1,FLT1,FLT3,FLT4,FYN,INSR,KDR,KIT,LCK,LYN,MAP2K1,MAP3K11,MAP3K21,MAP4K1,MAP4K3,MAPK11,MAPK14,MAPK7,MARK4,MET,MINK1,MST1R,NTRK1,NTRK3,PDGFRB,PDK4,PLK4,RET,RIPK3,SIK2,SRC,STK10,STK33,SYK,TEK,TGFBR1,TNIK,TTK,TYRO3,YES1 61
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 4.571 Moderate 0.76
mh-clint Mouse hepatocyte intrinsic clearance 19.409 Moderate 0.76
mppb Mouse plasma protein binding (% unbound) 0.190 Moderate 0.76
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 15.453 Moderate 0.76
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 1 High 1
pppb Pig plasma protein binding (% unbound) 0.550 % Moderate 0.76
rh-clint Rat hepatocyte intrinsic clearance 11.117 uL/min/10^6 cells Moderate 0.76
rh-fuinc Rat hepatocyte fraction unbound in incubation 2.250 % Moderate 0.76
rppb Rat plasma protein binding (% unbound) 0.230 % Moderate 0.76
solubility-dd Solubility at pH 7.4 in DMSO 1.791 uM Moderate 0.76

Approvals:

DateAgencyCompanyOrphan
March 25, 2020 PMDA Takeda Pharmaceutical Company Limited
March 21, 2014 EMA TMC Pharma Services Ltd
Nov. 29, 2012 FDA EXELIXIS

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 1591.59 23.47 452 15846 27571 90584578
Malignant neoplasm progression 1251.97 23.47 529 15769 106341 90505808
Off label use 691.09 23.47 910 15388 1101342 89510807
Diarrhoea 594.03 23.47 780 15518 938410 89673739
Hepatic function abnormal 429.40 23.47 195 16103 46093 90566056
Hypothyroidism 409.81 23.47 197 16101 52930 90559219
Decreased appetite 320.33 23.47 365 15933 376175 90235974
Hair colour changes 214.28 23.47 60 16238 3434 90608715
Hypertension 212.54 23.47 330 15968 457202 90154947
Inappropriate schedule of product administration 193.24 23.47 182 16116 149751 90462398
Stomatitis 166.49 23.47 225 16073 274473 90337676
Taste disorder 165.60 23.47 115 16183 61431 90550718
Proteinuria 157.39 23.47 79 16219 23212 90588937
Mucosal inflammation 141.87 23.47 102 16196 57523 90554626
Blood thyroid stimulating hormone increased 122.39 23.47 50 16248 9105 90603044
Fatigue 119.74 23.47 465 15833 1153558 89458591
Metastases to lung 101.49 23.47 52 16246 15939 90596210
Nausea 97.31 23.47 425 15873 1109891 89502258
Product prescribing issue 94.59 23.47 40 16258 7939 90604210
Blood pressure increased 89.42 23.47 141 16157 197076 90415073
Disease progression 76.60 23.47 116 16182 156499 90455650
Weight decreased 73.11 23.47 190 16108 379720 90232429
Dysgeusia 69.88 23.47 65 16233 52495 90559654
Oral pain 69.50 23.47 53 16245 32630 90579519
Hypersensitivity 69.04 23.47 3 16295 454674 90157475
Hyperthyroidism 68.27 23.47 42 16256 18268 90593881
Alanine aminotransferase increased 67.08 23.47 94 16204 118244 90493905
Hyperkeratosis 66.71 23.47 30 16268 6898 90605251
Drug ineffective 64.14 23.47 94 16204 1384204 89227945
Dysphonia 63.43 23.47 67 16231 63017 90549132
Death 63.32 23.47 203 16095 456348 90155801
Asthenia 58.10 23.47 219 16079 533532 90078617
Constipation 57.80 23.47 144 16154 280251 90331898
Nasopharyngitis 57.73 23.47 4 16294 407100 90205049
Malaise 56.96 23.47 232 16066 585754 90026395
Aspartate aminotransferase increased 54.26 23.47 79 16219 102858 90509291
Drug hypersensitivity 50.25 23.47 11 16287 463598 90148551
Rheumatoid arthritis 50.16 23.47 4 16294 362610 90249539
Pneumothorax 49.60 23.47 35 16263 19132 90593017
Infusion related reaction 49.19 23.47 8 16290 416772 90195377
Dry skin 48.47 23.47 69 16229 88004 90524145
Metastases to bone 46.97 23.47 38 16260 25467 90586682
Immune-mediated hepatic disorder 46.81 23.47 16 16282 1776 90610373
Skin toxicity 45.79 23.47 23 16275 6756 90605393
Swelling 45.30 23.47 10 16288 419048 90193101
Joint swelling 43.60 23.47 18 16280 503282 90108867
Metastases to liver 40.95 23.47 37 16261 28770 90583379
Condition aggravated 40.40 23.47 29 16269 595516 90016633
Treatment failure 40.28 23.47 4 16294 303924 90308225
Sinusitis 39.56 23.47 7 16291 343081 90269068
Genitourinary tract neoplasm 39.47 23.47 7 16291 44 90612105
Discomfort 38 23.47 3 16295 274332 90337817
Product use issue 37.45 23.47 7 16291 329912 90282237
Pericarditis 37.29 23.47 3 16295 270148 90342001
Abdominal discomfort 35.40 23.47 21 16277 477307 90134842
Stomatitis haemorrhagic 34.43 23.47 7 16291 98 90612051
Cancer pain 34.26 23.47 16 16282 4009 90608140
Metastases to central nervous system 34.14 23.47 27 16271 17515 90594634
Wound 33.19 23.47 7 16291 302973 90309176
Large intestine perforation 32.98 23.47 21 16277 9691 90602458
Thyroiditis 32.65 23.47 15 16283 3622 90608527
Metastases to spine 32.24 23.47 15 16283 3728 90608421
Hypertransaminasaemia 32.19 23.47 25 16273 15800 90596349
Liver disorder 31.21 23.47 68 16230 121201 90490948
Metastases to abdominal cavity 30.78 23.47 9 16289 601 90611548
Alpha 1 foetoprotein increased 30.37 23.47 7 16291 181 90611968
Osteonecrosis of jaw 29.85 23.47 36 16262 39067 90573082
Fall 29.46 23.47 26 16272 481784 90130365
Wheezing 29.38 23.47 4 16294 238076 90374073
Hyponatraemia 28.97 23.47 70 16228 133468 90478681
Immune-mediated enterocolitis 28.82 23.47 15 16283 4742 90607407
Oral mucosal blistering 28.69 23.47 17 16281 6907 90605242
Musculoskeletal stiffness 28.37 23.47 9 16289 296523 90315626
Pleural effusion 27.91 23.47 62 16236 111929 90500220
Metastases to spinal cord 27.33 23.47 7 16291 284 90611865
Liver function test increased 27.06 23.47 52 16246 84803 90527346
Pain 26.76 23.47 91 16207 996250 89615899
Fibromyalgia 26.59 23.47 3 16295 206266 90405883
Weight increased 26.22 23.47 22 16276 417905 90194244
Urticaria 25.76 23.47 12 16286 312722 90299427
Insomnia 25.67 23.47 14 16284 333460 90278689
Pelvic neoplasm 25.60 23.47 7 16291 366 90611783
Adrenal insufficiency 25.25 23.47 29 16269 29892 90582257
Mobility decreased 25.10 23.47 7 16291 250727 90361422
Ulcerative gastritis 25.08 23.47 5 16293 63 90612086
Osteoarthritis 24.84 23.47 3 16295 195727 90416422
Blood cholesterol increased 24.50 23.47 4 16294 208008 90404141
Gastrointestinal perforation 24.37 23.47 13 16285 4319 90607830
Skin ulcer 24.32 23.47 37 16261 50038 90562111
Infection 24.04 23.47 18 16280 362076 90250073
Embolism 23.81 23.47 17 16281 9464 90602685
Metastases to spleen 23.70 23.47 6 16292 232 90611917
Pulmonary embolism 23.63 23.47 64 16234 130756 90481393

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 3845.86 20.18 1196 36511 19386 42564242
Malignant neoplasm progression 2055.10 20.18 1243 36464 107157 42476471
Hepatic function abnormal 1271.09 20.18 703 37004 50864 42532764
Diarrhoea 1248.04 20.18 1761 35946 459088 42124540
Hypothyroidism 914.20 20.18 482 37225 31602 42552026
Taste disorder 782.25 20.18 306 37401 9901 42573727
Decreased appetite 771.67 20.18 899 36808 192238 42391390
Stomatitis 658.65 20.18 459 37248 49870 42533758
Proteinuria 628.09 20.18 336 37371 22647 42560981
Hypertension 568.54 20.18 718 36989 166486 42417142
Malaise 549.63 20.18 798 36909 211358 42372270
Off label use 432.26 20.18 1386 36321 636949 41946679
Inappropriate schedule of product administration 359.22 20.18 433 37274 95469 42488159
Hair colour changes 356.10 20.18 115 37592 2087 42581541
Dysphonia 295.75 20.18 226 37481 28224 42555404
Fatigue 253.11 20.18 901 36806 434740 42148888
Product prescribing issue 251.83 20.18 122 37585 6651 42576977
Liver disorder 228.75 20.18 225 37482 39419 42544209
Blister 177.42 20.18 166 37541 27324 42556304
Drug ineffective 161.58 20.18 193 37514 630004 41953624
Metastases to bone 150.22 20.18 116 37591 14693 42568935
Disease progression 147.92 20.18 365 37342 143291 42440337
Metastases to lung 141.71 20.18 101 37606 11323 42572305
Product selection error 124.32 20.18 28 37679 110 42583518
Blood pressure increased 122.26 20.18 275 37432 101653 42481975
Drug interaction 122.18 20.18 42 37665 266957 42316671
Blood thyroid stimulating hormone increased 121.38 20.18 69 37638 5223 42578405
Oral pain 117.68 20.18 94 37613 12502 42571126
Weight decreased 113.92 20.18 423 37284 207525 42376103
Dysgeusia 112.69 20.18 145 37562 34044 42549584
Skin ulcer 109.61 20.18 124 37583 25477 42558151
Adrenal insufficiency 108.33 20.18 107 37600 18817 42564811
Drug intolerance 107.83 20.18 227 37480 80197 42503431
Osteonecrosis of jaw 107.73 20.18 107 37600 18942 42564686
Skin toxicity 102.85 20.18 67 37640 6482 42577146
Product use in unapproved indication 91.54 20.18 25 37682 184431 42399197
Mucosal inflammation 88.99 20.18 158 37549 49216 42534412
Nausea 86.41 20.18 623 37084 396176 42187452
Hyperthyroidism 81.91 20.18 81 37626 14260 42569368
Skin disorder 77.55 20.18 85 37622 16859 42566769
Febrile neutropenia 75.39 20.18 35 37672 185668 42397960
Adverse drug reaction 71.62 20.18 123 37584 37311 42546317
Asthenia 69.96 20.18 456 37251 280337 42303291
Metastases to central nervous system 69.61 20.18 64 37643 10291 42573337
Ageusia 68.99 20.18 67 37640 11538 42572090
Drug hypersensitivity 68.69 20.18 5 37702 99384 42484244
Liver function test increased 67.74 20.18 86 37621 19912 42563716
Cancer pain 67.31 20.18 41 37666 3526 42580102
Impaired healing 66.94 20.18 79 37628 16974 42566654
Immune-mediated enterocolitis 65.40 20.18 48 37659 5629 42577999
Dry skin 64.23 20.18 136 37571 48202 42535426
Aspartate aminotransferase increased 61.02 20.18 178 37529 76985 42506643
Acute kidney injury 60.99 20.18 148 37559 367189 42216439
Immune-mediated hepatitis 60.22 20.18 39 37668 3735 42579893
Protein urine present 60.04 20.18 46 37661 5755 42577873
Glossodynia 59.20 20.18 40 37667 4112 42579516
Immune-mediated hepatic disorder 58.24 20.18 33 37674 2481 42581147
Nephrotic syndrome 56.89 20.18 53 37654 8665 42574963
Neutropenia 56.36 20.18 56 37651 199375 42384253
Hypotension 55.49 20.18 89 37618 257542 42326086
Bradycardia 54.49 20.18 6 37701 85478 42498150
Alanine aminotransferase increased 54.37 20.18 187 37520 88219 42495409
Thyroiditis 53.01 20.18 34 37673 3202 42580426
Pneumonia 52.84 20.18 194 37513 421955 42161673
Thyroid disorder 51.47 20.18 36 37671 3914 42579714
Overdose 50.82 20.18 15 37692 105249 42478379
Dry mouth 50.44 20.18 110 37597 39769 42543859
Multiple organ dysfunction syndrome 50.31 20.18 12 37695 97023 42486605
Condition aggravated 49.89 20.18 97 37610 260657 42322971
Interstitial lung disease 47.40 20.18 165 37542 78297 42505331
Product use issue 47.40 20.18 6 37701 76745 42506883
Adverse event 46.95 20.18 79 37628 23561 42560067
Hypertransaminasaemia 45.22 20.18 48 37659 9179 42574449
Weight increased 42.79 20.18 21 37686 107962 42475666
Hyperkeratosis 42.53 20.18 34 37673 4524 42579104
Dyspnoea 41.18 20.18 227 37480 442394 42141234
Urticaria 40.72 20.18 8 37699 74028 42509600
Fall 40.03 20.18 93 37614 234427 42349201
Gastrointestinal toxicity 39.97 20.18 31 37676 3948 42579680
Metastases to liver 39.92 20.18 60 37647 16266 42567362
Pulmonary embolism 39.89 20.18 210 37497 119402 42464226
Injection site pain 39.66 20.18 3 37704 57795 42525833
Sensitive skin 39.20 20.18 20 37687 1218 42582410
Alpha 1 foetoprotein increased 38.98 20.18 17 37690 725 42582903
Lipase increased 38.27 20.18 47 37660 10519 42573109
Cardiac failure congestive 38.15 20.18 14 37693 85588 42498040
Intentional product misuse 37.83 20.18 5 37702 61895 42521733
Immune-mediated lung disease 36.95 20.18 28 37679 3445 42580183
Amylase increased 36.57 20.18 37 37670 6692 42576936
Pancytopenia 34.47 20.18 32 37675 117711 42465917
Haemoglobin decreased 34.28 20.18 40 37667 132431 42451197
Depression 34.12 20.18 29 37678 111334 42472294
Agitation 33.24 20.18 8 37699 64306 42519322
Glossitis 33.21 20.18 19 37688 1455 42582173
Blood glucose increased 32.93 20.18 12 37695 73687 42509941
Cardiac arrest 32.85 20.18 29 37678 109291 42474337
Tremor 32.54 20.18 23 37684 96906 42486722
Musculoskeletal stiffness 32.28 20.18 6 37701 57759 42525869
Chronic obstructive pulmonary disease 30.44 20.18 9 37698 63105 42520523
Syncope 30.31 20.18 26 37681 99380 42484248
Hepatic encephalopathy 30.09 20.18 53 37654 16389 42567239
Suicide attempt 29.97 20.18 3 37704 46097 42537531
Somnolence 29.16 20.18 50 37657 141055 42442573
Leukopenia 28.91 20.18 15 37692 74731 42508897
Stress 28.43 20.18 3 37704 44209 42539419
Aggression 28.39 20.18 3 37704 44160 42539468
Tachycardia 27.82 20.18 29 37678 101058 42482570
Pneumothorax 27.58 20.18 63 37644 23480 42560148
Thyroid hormones increased 27.44 20.18 8 37699 101 42583527
Lactic acidosis 26.85 20.18 4 37703 45257 42538371
Diverticulitis intestinal perforated 26.69 20.18 10 37697 286 42583342
Drug reaction with eosinophilia and systemic symptoms 26.68 20.18 3 37704 42072 42541556
Renal cancer metastatic 26.60 20.18 12 37695 555 42583073
Anxiety 26.39 20.18 40 37667 118520 42465108
Loss of consciousness 25.98 20.18 26 37681 92328 42491300
Respiratory failure 25.93 20.18 46 37661 128086 42455542
Chills 25.87 20.18 27 37680 94039 42489589
Infection 25.73 20.18 37 37670 112031 42471597
Platelet count decreased 25.72 20.18 210 37497 138371 42445257
Productive cough 25.52 20.18 7 37700 51560 42532068
Tumour haemorrhage 25.46 20.18 23 37684 3615 42580013
Vomiting 25.36 20.18 378 37329 289345 42294283
Ascites 25.05 20.18 108 37599 56570 42527058
Oxygen saturation decreased 24.99 20.18 13 37694 64674 42518954
Hepatic enzyme increased 24.84 20.18 93 37614 45691 42537937
Incorrect dose administered 24.74 20.18 8 37699 52966 42530662
Angioedema 24.63 20.18 4 37703 42473 42541155
White blood cell count increased 24.52 20.18 5 37702 45082 42538546
Hypersensitivity 24.51 20.18 17 37690 72353 42511275
Metastatic renal cell carcinoma 24.18 20.18 18 37689 2156 42581472
Prostate cancer 24.18 20.18 5 37702 44638 42538990
Scrotal exfoliation 24.13 20.18 4 37703 0 42583628
Metastases to lymph nodes 23.89 20.18 28 37679 5970 42577658
Cardio-respiratory arrest 23.84 20.18 11 37696 58625 42525003
Rash 23.71 20.18 360 37347 276594 42307034
No adverse event 23.49 20.18 82 37625 38939 42544689
Insomnia 23.44 20.18 43 37664 118210 42465418
Metastases to abdominal cavity 23.34 20.18 9 37698 279 42583349
Diabetes mellitus 23.32 20.18 12 37695 60075 42523553
Oral discomfort 23.18 20.18 20 37687 2957 42580671
Skin exfoliation 23.04 20.18 85 37622 41468 42542160
Joint swelling 23.01 20.18 16 37691 68006 42515622
White blood cell count decreased 22.91 20.18 39 37668 110357 42473271
Swelling 22.78 20.18 10 37697 54875 42528753
Scrotal inflammation 22.76 20.18 5 37702 17 42583611
Metastases to spine 22.61 20.18 20 37687 3057 42580571
Flushing 22.60 20.18 3 37704 37025 42546603
Atrial fibrillation 22.49 20.18 57 37650 139536 42444092
Infusion related reaction 22.35 20.18 13 37694 60793 42522835
Genital rash 22.23 20.18 12 37695 820 42582808
Performance status decreased 22.15 20.18 24 37683 4696 42578932
Hypoproteinaemia 22.12 20.18 19 37688 2793 42580835
Pain 21.91 20.18 127 37580 244721 42338907
Rhabdomyolysis 21.90 20.18 22 37685 77997 42505631
Influenza 21.87 20.18 14 37693 62161 42521467
Metastases to adrenals 21.65 20.18 13 37694 1089 42582539
Headache 21.51 20.18 124 37583 239245 42344383
Scrotal erythema 21.25 20.18 6 37701 67 42583561
Seizure 21.19 20.18 47 37660 120514 42463114
Intestinal perforation 21.14 20.18 36 37671 10838 42572790
Tongue discomfort 21.05 20.18 11 37696 704 42582924
Constipation 20.65 20.18 227 37480 162064 42421564
Intentional product use issue 20.45 20.18 20 37687 71813 42511815
Coronary artery disease 20.45 20.18 11 37696 53709 42529919
Toxicity to various agents 20.42 20.18 119 37588 229017 42354611
Upper respiratory tract infection 20.36 20.18 6 37701 42167 42541461
Metastases to pancreas 20.20 20.18 9 37698 404 42583224

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 5040.76 20.22 1443 43272 39582 110505002
Malignant neoplasm progression 2129.01 20.22 1145 43570 173422 110371162
Hepatic function abnormal 1802.64 20.22 826 43889 88469 110456115
Diarrhoea 1576.88 20.22 2100 42615 1137405 109407179
Hypothyroidism 1360.44 20.22 639 44076 72260 110472324
Decreased appetite 941.12 20.22 1055 43660 474791 110069793
Proteinuria 796.17 20.22 367 44348 39651 110504933
Hypertension 687.43 20.22 933 43782 509151 110035433
Taste disorder 589.49 20.22 353 44362 65034 110479550
Malaise 455.44 20.22 901 43814 670918 109873666
Stomatitis 448.69 20.22 549 44166 269693 110274891
Hair colour changes 404.52 20.22 126 44589 4575 110540009
Disease progression 317.77 20.22 440 44275 243594 110300990
Inappropriate schedule of product administration 289.10 20.22 383 44332 203254 110341330
Dysphonia 286.78 20.22 241 44474 75688 110468896
Off label use 238.40 20.22 1213 43502 1498972 109045612
Metastases to lung 227.31 20.22 132 44583 22931 110521653
Fatigue 225.17 20.22 1028 43687 1214930 109329654
Blood thyroid stimulating hormone increased 217.27 20.22 104 44611 12197 110532387
Mucosal inflammation 207.56 20.22 224 44491 95917 110448667
Metastases to bone 199.48 20.22 136 44579 31236 110513348
Dysgeusia 181.59 20.22 180 44535 69805 110474779
Liver disorder 176.76 20.22 251 44464 141992 110402592
Drug ineffective 175.72 20.22 215 44500 1520325 109024259
Weight decreased 170.27 20.22 494 44221 467563 110077021
Hyperthyroidism 165.35 20.22 118 44597 29143 110515441
Blood pressure increased 155.76 20.22 331 44384 258042 110286542
Alanine aminotransferase increased 144.13 20.22 263 44452 183510 110361074
Adrenal insufficiency 140.63 20.22 125 44590 42265 110502319
Aspartate aminotransferase increased 139.74 20.22 240 44475 159696 110384888
Drug hypersensitivity 139.20 20.22 12 44703 454078 110090506
Product selection error 138.02 20.22 33 44682 428 110544156
Death 130.97 20.22 594 44121 698275 109846309
Osteonecrosis of jaw 123.61 20.22 123 44592 47894 110496690
Skin toxicity 112.29 20.22 66 44649 11717 110532867
Asthenia 111.18 20.22 561 44154 688438 109856146
Immune-mediated enterocolitis 110.28 20.22 62 44653 10123 110534461
Hypersensitivity 108.13 20.22 17 44698 403981 110140603
Oral pain 105.90 20.22 101 44614 37343 110507241
Interstitial lung disease 104.92 20.22 196 44519 139138 110405446
Joint swelling 101.24 20.22 27 44688 442818 110101766
Immune-mediated hepatic disorder 98.48 20.22 44 44671 4406 110540178
Immune-mediated hepatitis 98.43 20.22 50 44665 6661 110537923
Nausea 96.30 20.22 838 43877 1234852 109309732
Infusion related reaction 95.55 20.22 19 44696 381143 110163441
Treatment failure 94.89 20.22 4 44711 277230 110267354
Pneumothorax 93.81 20.22 92 44623 35193 110509391
Swelling 93.41 20.22 15 44700 351026 110193558
Arthropathy 92.61 20.22 6 44709 287516 110257068
Nasopharyngitis 92.13 20.22 23 44692 394338 110150246
Dry skin 91.96 20.22 160 44555 107493 110437091
Pulmonary embolism 91.29 20.22 240 44475 214234 110330350
Cancer pain 89.38 20.22 47 44668 6725 110537859
Product use issue 88.35 20.22 11 44704 311684 110232900
Platelet count decreased 88.22 20.22 248 44467 230195 110314389
Skin ulcer 87.53 20.22 118 44597 63527 110481057
Pain 86.63 20.22 159 44556 954796 109589788
Hyperkeratosis 86.07 20.22 51 44664 9188 110535396
Drug interaction 84.04 20.22 49 44666 500134 110044450
Rheumatoid arthritis 83.89 20.22 11 44704 299602 110244982
Product use in unapproved indication 83.83 20.22 38 44677 447339 110097245
Wheezing 83.17 20.22 5 44710 255225 110289359
Weight increased 82.85 20.22 33 44682 419611 110124973
Metastases to liver 80.82 20.22 85 44630 35301 110509283
Protein urine present 80.72 20.22 53 44662 11431 110533153
Condition aggravated 80.23 20.22 108 44607 734728 109809856
Metastases to central nervous system 79.10 20.22 69 44646 22748 110521836
Ascites 78.05 20.22 137 44578 92671 110451913
Product prescribing issue 77.94 20.22 54 44661 12718 110531866
Urticaria 77.62 20.22 17 44698 318840 110225744
Hypertransaminasaemia 73.52 20.22 68 44647 24187 110520397
Ageusia 73.38 20.22 62 44653 19583 110525001
Amylase increased 71.90 20.22 51 44664 12468 110532116
Thyroiditis 71.13 20.22 40 44675 6533 110538051
Musculoskeletal stiffness 70.00 20.22 14 44701 279808 110264776
Lipase increased 67.84 20.22 58 44657 18614 110525970
Constipation 67.45 20.22 305 44410 357481 110187103
Pleural effusion 65.79 20.22 189 44526 177520 110367064
Alpha 1 foetoprotein increased 65.38 20.22 21 44694 843 110543741
Nephrotic syndrome 62.96 20.22 49 44666 13782 110530802
Skin disorder 61.20 20.22 81 44634 42832 110501752
Injection site pain 59.46 20.22 3 44712 177919 110366665
Blood cholesterol increased 59.06 20.22 4 44711 184781 110359803
Discomfort 57.48 20.22 9 44706 214698 110329886
Fibromyalgia 56.74 20.22 3 44712 170906 110373678
Sinusitis 55.86 20.22 25 44690 296663 110247921
Osteoarthritis 55.43 20.22 5 44710 182618 110361966
Mobility decreased 55.12 20.22 14 44701 237408 110307176
Insomnia 54.19 20.22 40 44675 360550 110184034
Depression 53.38 20.22 31 44684 317304 110227280
Headache 51.94 20.22 183 44532 882194 109662390
Immune-mediated lung disease 51.31 20.22 30 44685 5273 110539311
Metastases to spine 51.10 20.22 30 44685 5313 110539271
Type 2 diabetes mellitus 50.83 20.22 6 44709 177226 110367358
Metastases to abdominal cavity 49.13 20.22 17 44698 861 110543723
Fall 49.01 20.22 107 44608 603375 109941209
Infection 48.46 20.22 45 44670 362155 110182429
Transaminases increased 47.47 20.22 89 44626 63301 110481283
Toxicity to various agents 47.12 20.22 76 44639 480479 110064105
Dehydration 46.60 20.22 230 44485 279281 110265303
Intentional product use issue 46.48 20.22 21 44694 247885 110296699
Hepatic encephalopathy 46.06 20.22 57 44658 28199 110516385
Liver function test increased 46.00 20.22 107 44608 88441 110456143
Ill-defined disorder 45.76 20.22 5 44710 156848 110387736
Anal abscess 44.02 20.22 37 44678 11601 110532983
Tumour pain 43.20 20.22 22 44693 2945 110541639
Thyroid disorder 42.80 20.22 43 44672 16926 110527658
Wound 42.20 20.22 21 44694 234416 110310168
Intentional product misuse 42.11 20.22 3 44712 132901 110411683
Blood bilirubin increased 41.90 20.22 94 44621 75878 110468706
Malignant pleural effusion 41.84 20.22 24 44691 4069 110540515
Tumour haemorrhage 41.29 20.22 26 44689 5219 110539365
Bursitis 40.97 20.22 3 44712 129915 110414669
Metastatic renal cell carcinoma 40.87 20.22 20 44695 2460 110542124
Sleep disorder 40.20 20.22 15 44700 198629 110345955
Large intestine perforation 39.86 20.22 41 44674 16588 110527996
Metastases to lymph nodes 39.59 20.22 39 44676 14993 110529591
Dermatitis acneiform 39.27 20.22 36 44679 12659 110531925
Gastrointestinal toxicity 39.22 20.22 34 44681 11114 110533470
Renal cancer metastatic 39.18 20.22 14 44701 780 110543804
Folliculitis 38.69 20.22 10 44705 167643 110376941
Arthritis 38.66 20.22 10 44705 167576 110377008
Bradycardia 38.42 20.22 8 44707 155509 110389075
Anxiety 38.31 20.22 50 44665 345028 110199556
Febrile neutropenia 38.23 20.22 43 44672 316724 110227860
Immune-mediated hypothyroidism 38.07 20.22 20 44695 2855 110541729
Arthralgia 38.06 20.22 174 44541 779458 109765126
Gastrointestinal perforation 37.43 20.22 28 44687 7428 110537156
Dyspnoea 37.02 20.22 279 44436 1106593 109437991
Lower respiratory tract infection 36.47 20.22 27 44688 243079 110301505
Overdose 36.33 20.22 25 44690 233769 110310815
No adverse event 35.94 20.22 87 44628 73752 110470832
Therapeutic product effect incomplete 34.69 20.22 24 44691 223781 110320803
Migraine 34.67 20.22 13 44702 171639 110372945
Radiotherapy 33.85 20.22 15 44700 1473 110543111
Performance status decreased 33.63 20.22 26 44689 7240 110537344
Sensitive skin 33.30 20.22 20 44695 3692 110540892
Hypocalcaemia 32.87 20.22 78 44637 65288 110479296
Hypoalbuminaemia 32.85 20.22 49 44666 28925 110515659
Hypopituitarism 32.66 20.22 21 44694 4369 110540215
Road traffic accident 32.43 20.22 3 44712 107395 110437189
Glossitis 32.19 20.22 21 44694 4480 110540104
Intestinal perforation 32.15 20.22 41 44674 20903 110523681
Bronchitis 31.53 20.22 12 44703 157020 110387564
Colitis 31.45 20.22 102 44613 102221 110442363
Genitourinary tract neoplasm 31.41 20.22 7 44708 65 110544519
Psoriasis 31.08 20.22 9 44706 139984 110404600
Liver injury 31.04 20.22 11 44704 150402 110394182
Suicide attempt 30.92 20.22 3 44712 103391 110441193
Renal cell carcinoma 30.69 20.22 25 44690 7505 110537079
Oxygen saturation decreased 29.89 20.22 13 44702 156969 110387615
Scrotal inflammation 29.69 20.22 5 44710 7 110544577
Metastases to adrenals 29.67 20.22 14 44701 1589 110542995
Inflammation 29.58 20.22 21 44694 193217 110351367
Depressed level of consciousness 29.39 20.22 5 44710 112273 110432311
Blood creatine phosphokinase increased 29.26 20.22 80 44635 72997 110471587
Chest discomfort 29.19 20.22 17 44698 173831 110370753
Stress 29.15 20.22 4 44711 105344 110439240
Hepatotoxicity 29.06 20.22 73 44642 63327 110481257
Contusion 28.90 20.22 31 44684 233330 110311254
Lung disorder 28.31 20.22 19 44696 180028 110364556
Diverticulitis intestinal perforated 28.16 20.22 10 44705 547 110544037
Gait inability 28.09 20.22 10 44705 136366 110408218
Productive cough 27.99 20.22 6 44709 114299 110430285
Cell death 27.41 20.22 21 44694 5770 110538814
Abdominal discomfort 27.11 20.22 76 44639 393782 110150802
Therapy non-responder 26.96 20.22 15 44700 157292 110387292
Metastases to spinal cord 26.92 20.22 8 44707 247 110544337
Embolism 26.78 20.22 33 44682 16256 110528328
Hypotension 26.68 20.22 115 44600 523734 110020850
Physical deconditioning 26.52 20.22 17 44698 3520 110541064
Upper respiratory tract infection 26.43 20.22 10 44705 131318 110413266
Influenza 26.38 20.22 18 44697 169083 110375501
Anal fistula 26.15 20.22 24 44691 8449 110536135
Neutropenia 25.99 20.22 72 44643 374548 110170036
Pancreatic enzymes increased 25.70 20.22 13 44702 1716 110542868
Agitation 25.59 20.22 7 44708 113044 110431540
Drug intolerance 25.42 20.22 82 44633 406430 110138154
Blood corticotrophin increased 25.35 20.22 8 44707 303 110544281
Musculoskeletal pain 25.35 20.22 22 44693 183001 110361583
Metastases to pancreas 25.33 20.22 10 44705 735 110543849
Pneumonitis 25.08 20.22 78 44637 76453 110468131
Medication error 24.86 20.22 6 44709 105360 110439224
Incorrect dose administered 24.26 20.22 6 44709 103635 110440949
Immune-mediated myocarditis 24.23 20.22 16 44699 3482 110541102
Eastern Cooperative Oncology Group performance status worsened 24.08 20.22 15 44700 2954 110541630
Skin exfoliation 23.96 20.22 84 44631 87567 110457017
White blood cell count increased 23.88 20.22 5 44710 96837 110447747
Thyroid hormones increased 23.77 20.22 9 44706 591 110543993
Acquired perforating dermatosis 23.59 20.22 4 44711 6 110544578
Loss of personal independence in daily activities 23.36 20.22 16 44699 150004 110394580
Bronchial injury 23.21 20.22 4 44711 7 110544577
Intracranial tumour haemorrhage 23.15 20.22 9 44706 635 110543949
Failure to thrive 23.12 20.22 28 44687 13546 110531038
Lip dry 23.03 20.22 6 44709 100077 110444507
Immune-mediated adrenal insuficiency 22.49 20.22 12 44703 1768 110542816
Lactic acidosis 22.46 20.22 5 44710 92806 110451778
Stomatitis haemorrhagic 22.44 20.22 7 44708 255 110544329
Paraesthesia 22.43 20.22 49 44666 276472 110268112
Cardiac failure congestive 22.34 20.22 17 44698 150983 110393601
Sciatica 22.32 20.22 5 44710 92394 110452190
Bleeding varicose vein 22.26 20.22 9 44706 704 110543880
Tongue discomfort 21.95 20.22 14 44701 2874 110541710
Wound infection 21.79 20.22 6 44709 96459 110448125
Chills 21.77 20.22 27 44688 190553 110354031
Hypercholesterolaemia 21.77 20.22 5 44710 90832 110453752
Tremor 21.72 20.22 30 44685 202202 110342382
Thrombophlebitis migrans 21.54 20.22 9 44706 765 110543819
Cholecystitis 21.48 20.22 38 44677 25844 110518740
Pelvic neoplasm 21.44 20.22 7 44708 296 110544288
Pneumonia 21.42 20.22 239 44476 876475 109668109
Multiple organ dysfunction syndrome 21.29 20.22 18 44697 151692 110392892
Lung abscess 21.19 20.22 17 44698 4995 110539589
KL-6 increased 21.13 20.22 7 44708 310 110544274
Haemoglobin decreased 21.07 20.22 43 44672 248684 110295900
Angular cheilitis 21.06 20.22 10 44705 1151 110543433
Peripheral swelling 20.99 20.22 88 44627 403946 110140638
Influenza like illness 20.92 20.22 5 44710 88407 110456177
Intestinal metastasis 20.90 20.22 8 44707 541 110544043
Chronic obstructive pulmonary disease 20.84 20.22 9 44706 109149 110435435
Metastases to pleura 20.83 20.22 12 44703 2051 110542533
C-reactive protein increased 20.83 20.22 35 44680 217884 110326700
Renal impairment 20.80 20.22 139 44576 188306 110356278
Angioedema 20.67 20.22 7 44708 98493 110446091
Scrotal dermatitis 20.44 20.22 3 44712 0 110544584
Pneumatosis intestinalis 20.39 20.22 21 44694 8508 110536076
Cardiac arrest 20.32 20.22 30 44685 196723 110347861

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EX07 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Other protein kinase inhibitors
FDA MoA N0000175076 Protein Kinase Inhibitors
FDA EPC N0000175605 Kinase Inhibitor
CHEBI has role CHEBI:22587 antiviral agent
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:38637 tyrosine kinase inhibitor
CHEBI has role CHEBI:50266 prodrug

Related Drugs by ATC class:

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

DiseaseRelationSNOMED_IDDOID
Liver cell carcinoma indication 109841003 DOID:684
Medullary thyroid carcinoma indication 255032005 DOID:3973
Renal cell carcinoma indication 702391001 DOID:4450
Metastatic renal cell carcinoma indication 702392008




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.15 acidic
pKa2 11.76 acidic
pKa3 4.95 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 20MG BASE COMETRIQ EXELIXIS N203756 Nov. 29, 2012 RX CAPSULE ORAL 11098015 Jan. 15, 2030 METHOD OF TREATING MEDULLARY THYROID CANCER
EQ 80MG BASE COMETRIQ EXELIXIS N203756 Nov. 29, 2012 RX CAPSULE ORAL 11098015 Jan. 15, 2030 METHOD OF TREATING MEDULLARY THYROID CANCER
EQ 20MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 11098015 Jan. 15, 2030 TREATMENT OF ADVANCED RENAL CELL CARCINOMA
EQ 20MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 11098015 Jan. 15, 2030 TREATMENT OF DIFFERENTIATED THYROID CANCER THAT HAS PROGRESSED FOLLOWING PRIOR VEGFR-TARGETED THERAPY
EQ 20MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 11098015 Jan. 15, 2030 TREATMENT OF PATIENTS WITH HEPATOCELLULAR CARCINOMA (HCC) WHO HAVE BEEN PREVIOUSLY TREATED WITH SORAFENIB
EQ 20MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 11098015 Jan. 15, 2030 TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC, WELL-DIFFERENTIATED EXTRA-PANCREATIC NEUROENDOCRINE TUMORS
EQ 20MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 11098015 Jan. 15, 2030 TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC, WELL-DIFFERENTIATED PANCREATIC NEUROENDOCRINE TUMORS
EQ 20MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 11098015 Jan. 15, 2030 TREATMENT OF RENAL CELL CARCINOMA
EQ 40MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 11098015 Jan. 15, 2030 TREATMENT OF ADVANCED RENAL CELL CARCINOMA
EQ 40MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 11098015 Jan. 15, 2030 TREATMENT OF DIFFERENTIATED THYROID CANCER THAT HAS PROGRESSED FOLLOWING PRIOR VEGFR-TARGETED THERAPY
EQ 40MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 11098015 Jan. 15, 2030 TREATMENT OF PATIENTS WITH HEPATOCELLULAR CARCINOMA (HCC) WHO HAVE BEEN PREVIOUSLY TREATED WITH SORAFENIB
EQ 40MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 11098015 Jan. 15, 2030 TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC, WELL-DIFFERENTIATED EXTRA-PANCREATIC NEUROENDOCRINE TUMORS
EQ 40MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 11098015 Jan. 15, 2030 TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC, WELL-DIFFERENTIATED PANCREATIC NEUROENDOCRINE TUMORS
EQ 40MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 11098015 Jan. 15, 2030 TREATMENT OF RENAL CELL CARCINOMA
EQ 60MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 11098015 Jan. 15, 2030 TREATMENT OF ADVANCED RENAL CELL CARCINOMA
EQ 60MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 11098015 Jan. 15, 2030 TREATMENT OF DIFFERENTIATED THYROID CANCER THAT HAS PROGRESSED FOLLOWING PRIOR VEGFR-TARGETED THERAPY
EQ 60MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 11098015 Jan. 15, 2030 TREATMENT OF PATIENTS WITH HEPATOCELLULAR CARCINOMA (HCC) WHO HAVE BEEN PREVIOUSLY TREATED WITH SORAFENIB
EQ 60MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 11098015 Jan. 15, 2030 TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC, WELL-DIFFERENTIATED EXTRA-PANCREATIC NEUROENDOCRINE TUMORS
EQ 60MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 11098015 Jan. 15, 2030 TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC, WELL-DIFFERENTIATED PANCREATIC NEUROENDOCRINE TUMORS
EQ 60MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 11098015 Jan. 15, 2030 TREATMENT OF RENAL CELL CARCINOMA
EQ 20MG BASE COMETRIQ EXELIXIS N203756 Nov. 29, 2012 RX CAPSULE ORAL 8877776 Oct. 8, 2030 METHOD OF TREATING MEDULLARY THYROID CANCER
EQ 80MG BASE COMETRIQ EXELIXIS N203756 Nov. 29, 2012 RX CAPSULE ORAL 8877776 Oct. 8, 2030 METHOD OF TREATING MEDULLARY THYROID CANCER
EQ 20MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 8877776 Oct. 8, 2030 TREATMENT OF DIFFERENTIATED THYROID CANCER THAT HAS PROGRESSED FOLLOWING PRIOR VEGFR-TARGETED THERAPY
EQ 40MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 8877776 Oct. 8, 2030 TREATMENT OF DIFFERENTIATED THYROID CANCER THAT HAS PROGRESSED FOLLOWING PRIOR VEGFR-TARGETED THERAPY
EQ 60MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 8877776 Oct. 8, 2030 TREATMENT OF DIFFERENTIATED THYROID CANCER THAT HAS PROGRESSED FOLLOWING PRIOR VEGFR-TARGETED THERAPY
EQ 20MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 10034873 July 18, 2031 TREATMENT OF PATIENTS WITH HEPATOCELLULAR CARCINOMA (HCC) WHO HAVE BEEN PREVIOUSLY TREATED WITH SORAFENIB
EQ 20MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 10039757 July 18, 2031 TREATMENT OF ADVANCED RENAL CELL CARCINOMA
EQ 40MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 10034873 July 18, 2031 TREATMENT OF PATIENTS WITH HEPATOCELLULAR CARCINOMA (HCC) WHO HAVE BEEN PREVIOUSLY TREATED WITH SORAFENIB
EQ 40MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 10039757 July 18, 2031 TREATMENT OF ADVANCED RENAL CELL CARCINOMA
EQ 60MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 10034873 July 18, 2031 TREATMENT OF PATIENTS WITH HEPATOCELLULAR CARCINOMA (HCC) WHO HAVE BEEN PREVIOUSLY TREATED WITH SORAFENIB
EQ 60MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 10039757 July 18, 2031 TREATMENT OF ADVANCED RENAL CELL CARCINOMA
EQ 20MG BASE COMETRIQ EXELIXIS N203756 Nov. 29, 2012 RX CAPSULE ORAL 12128039 Feb. 10, 2032 METHOD OF TREATING MEDULLARY THYROID CANCER
EQ 80MG BASE COMETRIQ EXELIXIS N203756 Nov. 29, 2012 RX CAPSULE ORAL 12128039 Feb. 10, 2032 METHOD OF TREATING MEDULLARY THYROID CANCER
EQ 20MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 12128039 Feb. 10, 2032 TREATMENT OF ADVANCED RENAL CELL CARCINOMA
EQ 20MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 12128039 Feb. 10, 2032 TREATMENT OF DIFFERENTIATED THYROID CANCER THAT HAS PROGRESSED FOLLOWING PRIOR VEGFR-TARGETED THERAPY
EQ 20MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 12128039 Feb. 10, 2032 TREATMENT OF PATIENTS WITH HEPATOCELLULAR CARCINOMA (HCC) WHO HAVE BEEN PREVIOUSLY TREATED WITH SORAFENIB
EQ 20MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 12128039 Feb. 10, 2032 TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC, WELL-DIFFERENTIATED EXTRA-PANCREATIC NEUROENDOCRINE TUMORS
EQ 20MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 12128039 Feb. 10, 2032 TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC, WELL-DIFFERENTIATED PANCREATIC NEUROENDOCRINE TUMORS
EQ 20MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 12128039 Feb. 10, 2032 TREATMENT OF RENAL CELL CARCINOMA
EQ 40MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 12128039 Feb. 10, 2032 TREATMENT OF ADVANCED RENAL CELL CARCINOMA
EQ 40MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 12128039 Feb. 10, 2032 TREATMENT OF DIFFERENTIATED THYROID CANCER THAT HAS PROGRESSED FOLLOWING PRIOR VEGFR-TARGETED THERAPY
EQ 40MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 12128039 Feb. 10, 2032 TREATMENT OF PATIENTS WITH HEPATOCELLULAR CARCINOMA (HCC) WHO HAVE BEEN PREVIOUSLY TREATED WITH SORAFENIB
EQ 40MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 12128039 Feb. 10, 2032 TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC, WELL-DIFFERENTIATED EXTRA-PANCREATIC NEUROENDOCRINE TUMORS
EQ 40MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 12128039 Feb. 10, 2032 TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC, WELL-DIFFERENTIATED PANCREATIC NEUROENDOCRINE TUMORS
EQ 40MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 12128039 Feb. 10, 2032 TREATMENT OF RENAL CELL CARCINOMA
EQ 60MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 12128039 Feb. 10, 2032 TREATMENT OF ADVANCED RENAL CELL CARCINOMA
EQ 60MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 12128039 Feb. 10, 2032 TREATMENT OF DIFFERENTIATED THYROID CANCER THAT HAS PROGRESSED FOLLOWING PRIOR VEGFR-TARGETED THERAPY
EQ 60MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 12128039 Feb. 10, 2032 TREATMENT OF PATIENTS WITH HEPATOCELLULAR CARCINOMA (HCC) WHO HAVE BEEN PREVIOUSLY TREATED WITH SORAFENIB
EQ 60MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 12128039 Feb. 10, 2032 TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC, WELL-DIFFERENTIATED EXTRA-PANCREATIC NEUROENDOCRINE TUMORS
EQ 60MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 12128039 Feb. 10, 2032 TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC, WELL-DIFFERENTIATED PANCREATIC NEUROENDOCRINE TUMORS
EQ 60MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 12128039 Feb. 10, 2032 TREATMENT OF RENAL CELL CARCINOMA

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 20MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL Jan. 14, 2026 INDICATED FOR TREATMENT OF PATIENTS WITH HEPATOCELLULAR CARCINOMA (HCC) WHO HAVE BEEN PREVIOUSLY TREATED WITH SORAFENIB
EQ 40MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL Jan. 14, 2026 INDICATED FOR TREATMENT OF PATIENTS WITH HEPATOCELLULAR CARCINOMA (HCC) WHO HAVE BEEN PREVIOUSLY TREATED WITH SORAFENIB
EQ 60MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL Jan. 14, 2026 INDICATED FOR TREATMENT OF PATIENTS WITH HEPATOCELLULAR CARCINOMA (HCC) WHO HAVE BEEN PREVIOUSLY TREATED WITH SORAFENIB
EQ 20MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL Sept. 17, 2028 THE TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH LOCALLY ADVANCED OR METASTATIC DIFFERENTIATED THYROID CANCER (DTC) THAT HAS PROGRESSED FOLLOWING PRIOR VEGFR-TARGETED THERAPY AND WHO ARE RADIOACTIVE IODINE-REFRACTORY OR INELIGIBLE
EQ 40MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL Sept. 17, 2028 THE TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH LOCALLY ADVANCED OR METASTATIC DIFFERENTIATED THYROID CANCER (DTC) THAT HAS PROGRESSED FOLLOWING PRIOR VEGFR-TARGETED THERAPY AND WHO ARE RADIOACTIVE IODINE-REFRACTORY OR INELIGIBLE
EQ 60MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL Sept. 17, 2028 THE TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH LOCALLY ADVANCED OR METASTATIC DIFFERENTIATED THYROID CANCER (DTC) THAT HAS PROGRESSED FOLLOWING PRIOR VEGFR-TARGETED THERAPY AND WHO ARE RADIOACTIVE IODINE-REFRACTORY OR INELIGIBLE
EQ 20MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL March 26, 2032 TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH PREVIOUSLY TREATED, UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC, WELL-DIFFERENTIATED PANCREATIC NEUROENDOCRINE TUMORS (PNET)
EQ 40MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL March 26, 2032 TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH PREVIOUSLY TREATED, UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC, WELL-DIFFERENTIATED PANCREATIC NEUROENDOCRINE TUMORS (PNET)
EQ 60MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL March 26, 2032 TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH PREVIOUSLY TREATED, UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC, WELL-DIFFERENTIATED PANCREATIC NEUROENDOCRINE TUMORS (PNET)

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Mast/stem cell growth factor receptor Kit Kinase INHIBITOR IC50 8.34 WOMBAT-PK DRUG LABEL
Receptor-type tyrosine-protein kinase FLT3 Kinase INHIBITOR IC50 7.95 WOMBAT-PK DRUG LABEL
Proto-oncogene tyrosine-protein kinase receptor Ret Kinase INHIBITOR IC50 8.28 WOMBAT-PK DRUG LABEL
Vascular endothelial growth factor receptor 2 Kinase INHIBITOR IC50 10.46 WOMBAT-PK DRUG LABEL
Angiopoietin-1 receptor Kinase INHIBITOR IC50 7.85 WOMBAT-PK DRUG LABEL
Hepatocyte growth factor receptor Kinase INHIBITOR IC50 8.89 WOMBAT-PK DRUG LABEL
Ephrin type-A receptor 2 Kinase Kd 6.13 CHEMBL
Vascular endothelial growth factor receptor 1 Kinase IC50 7.92 CHEMBL
Vascular endothelial growth factor receptor 3 Kinase IC50 8.22 CHEMBL
Tyrosine-protein kinase HCK Kinase Kd 5.96 CHEMBL
High affinity nerve growth factor receptor Kinase Kd 5.39 CHEMBL
Tyrosine-protein kinase Lyn Kinase Kd 5.88 CHEMBL
Fibroblast growth factor receptor 1 Kinase IC50 7.95 CHEMBL
Abelson tyrosine-protein kinase 2 Kinase Kd 6.04 CHEMBL
Aurora kinase A Kinase Kd 5.47 CHEMBL
Tyrosine-protein kinase FRK Kinase Kd 6.25 CHEMBL
Receptor-interacting serine/threonine-protein kinase 2 Kinase Kd 6.12 CHEMBL
Macrophage-stimulating protein receptor Kinase INHIBITOR IC50 6.91 WOMBAT-PK
Protein-tyrosine kinase 6 Kinase Kd 5.75 CHEMBL
Tyrosine-protein kinase receptor UFO Kinase IC50 8.47 CHEMBL
Tyrosine-protein kinase receptor TYRO3 Kinase IC50 8.54 CHEMBL
Discoidin domain-containing receptor 2 Kinase Kd 6.30 CHEMBL
Tyrosine-protein kinase Mer Kinase IC50 9.30 CHEMBL
Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma Kinase Kd 5.54 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 5 Kinase Kd 5.62 CHEMBL
Ferrochelatase, mitochondrial Enzyme Kd 5.58 CHEMBL
Receptor-interacting serine/threonine-protein kinase 3 Kinase Kd 5.61 CHEMBL
SAFB-like transcription modulator Transcription factor IC50 8.89 CHEMBL
Epithelial discoidin domain-containing receptor 1 Kinase Kd 6.68 CHEMBL
Tyrosine-protein kinase ABL1 Kinase Kd 5.96 CHEMBL
Epidermal growth factor receptor Kinase IC50 6.65 CHEMBL
Breakpoint cluster region protein Kinase Kd 6.47 CHEMBL
Proto-oncogene tyrosine-protein kinase Src Kinase IC50 6.75 CHEMBL
Tyrosine-protein kinase Lck Kinase Kd 5.98 CHEMBL

External reference:

IDSource
1C39JW444G UNII
D10062 KEGG_DRUG
4032025 VUID
N0000186139 NUI
4032025 VANDF
C3181682 UMLSCUI
CHEMBL2105717 ChEMBL_ID
25102847 PUBCHEM_CID
DB08875 DRUGBANK_ID
CHEMBL2103868 ChEMBL_ID
9297 INN_ID
C558660 MESH_SUPPLEMENTAL_RECORD_UI
5887 IUPHAR_LIGAND_ID
1140909-48-3 SECONDARY_CAS_RN
1363267 RXNORM
194795 MMSL
240294 MMSL
28993 MMSL
31609 MMSL
d07931 MMSL
014768 NDDF
014782 NDDF
718844003 SNOMEDCT_US
763605009 SNOMEDCT_US
864011003 SNOMEDCT_US
CHEBI:72319 CHEBI
A1JS8 PDB_CHEM_ID
1C39JW444G INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
COMETRIQ HUMAN PRESCRIPTION DRUG LABEL 1 42388-013 CAPSULE 20 mg ORAL NDA 27 sections
COMETRIQ HUMAN PRESCRIPTION DRUG LABEL 1 42388-013 CAPSULE 20 mg ORAL NDA 27 sections
CABOMETYX HUMAN PRESCRIPTION DRUG LABEL 1 42388-023 TABLET 60 mg ORAL NDA 27 sections
CABOMETYX HUMAN PRESCRIPTION DRUG LABEL 1 42388-023 TABLET 60 mg ORAL NDA 27 sections
CABOMETYX HUMAN PRESCRIPTION DRUG LABEL 1 42388-024 TABLET 20 mg ORAL NDA 27 sections
CABOMETYX HUMAN PRESCRIPTION DRUG LABEL 1 42388-024 TABLET 20 mg ORAL NDA 27 sections
CABOMETYX HUMAN PRESCRIPTION DRUG LABEL 1 42388-025 TABLET 40 mg ORAL NDA 27 sections
CABOMETYX HUMAN PRESCRIPTION DRUG LABEL 1 42388-025 TABLET 40 mg ORAL NDA 27 sections