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

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 640.57 26.46 192 6313 19906 50578713
Malignant neoplasm progression 547.51 26.46 234 6271 67890 50530729
Diarrhoea 263.03 26.46 347 6158 588129 50010490
Decreased appetite 162.73 26.46 162 6343 200761 50397858
Stomatitis 113.34 26.46 98 6407 101246 50497373
Hypertension 96.86 26.46 127 6378 211076 50387543
Hypothyroidism 96.36 26.46 58 6447 34067 50564552
Hepatic function abnormal 96.06 26.46 57 6448 32624 50565995
Off label use 94.05 26.46 195 6310 474231 50124388
Hair colour changes 86.40 26.46 26 6479 2698 50595921
Taste disorder 77.88 26.46 32 6473 8292 50590327
Mucosal inflammation 71.16 26.46 51 6454 40091 50558528
Fatigue 71.15 26.46 225 6280 707376 49891243
Drug ineffective 52.66 26.46 20 6485 819313 49779306
Nausea 45.06 26.46 194 6311 705204 49893415
Oral pain 44.79 26.46 32 6473 25001 50573618
Proteinuria 43.71 26.46 27 6478 16570 50582049
Hyperthyroidism 43.13 26.46 24 6481 12151 50586468
Blood thyroid stimulating hormone increased 42.40 26.46 19 6486 6073 50592546
Inappropriate schedule of product administration 40.47 26.46 48 6457 71783 50526836
Dysphonia 36.24 26.46 34 6471 38858 50559761
Death 34.72 26.46 106 6399 325273 50273346
Disease progression 33.88 26.46 51 6454 95815 50502804
Drug intolerance 30.84 26.46 79 6426 219025 50379594
Asthenia 30.41 26.46 100 6405 318942 50279677
Hyperkeratosis 29.70 26.46 14 6491 5021 50593598
Embolism 28.18 26.46 15 6490 6953 50591666
Alanine aminotransferase increased 27.03 26.46 44 6461 88315 50510304

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 1494.61 21.88 477 15331 14282 29544437
Malignant neoplasm progression 1022.03 21.88 578 15230 73281 29485438
Diarrhoea 538.67 21.88 764 15044 331934 29226785
Hypothyroidism 363.67 21.88 175 15633 15731 29542988
Decreased appetite 321.69 21.88 391 15417 144951 29413768
Hepatic function abnormal 288.89 21.88 207 15601 39052 29519667
Hypertension 264.63 21.88 318 15490 116296 29442423
Stomatitis 262.33 21.88 191 15617 36922 29521797
Hair colour changes 199.86 21.88 61 15747 1550 29557169
Proteinuria 191.47 21.88 114 15694 15690 29543029
Taste disorder 181.24 21.88 75 15733 4701 29554018
Malaise 175.61 21.88 309 15499 159293 29399426
Dysphonia 168.69 21.88 113 15695 19083 29539636
Fatigue 133.78 21.88 421 15387 316400 29242319
Drug intolerance 129.57 21.88 144 15664 48235 29510484
Blister 96.25 21.88 82 15726 19824 29538895
Disease progression 92.86 21.88 161 15647 81755 29476964
Oral pain 87.07 21.88 57 15751 9250 29549469
Dysgeusia 77.63 21.88 77 15731 22597 29536122
Drug ineffective 74.27 21.88 52 15756 363118 29195601
Inappropriate schedule of product administration 66.19 21.88 99 15709 44373 29514346
Off label use 62.54 21.88 321 15487 300479 29258240
Mucosal inflammation 61.45 21.88 80 15728 31515 29527204
Immune-mediated hepatitis 61.38 21.88 25 15783 1502 29557217
Asthenia 58.09 21.88 248 15560 215002 29343717
Nausea 56.87 21.88 304 15504 288951 29269768
Skin toxicity 55.77 21.88 31 15777 3740 29554979
Liver function test increased 53.47 21.88 47 15761 11838 29546881
Drug interaction 52.48 21.88 20 15788 197365 29361354
Blood thyroid stimulating hormone increased 47.22 21.88 26 15782 3079 29555640
Product selection error 46.07 21.88 10 15798 59 29558660
Skin ulcer 45.15 21.88 53 15755 18787 29539932
Hyperthyroidism 44.77 21.88 37 15771 8571 29550148
Adrenal insufficiency 42.26 21.88 40 15768 11074 29547645
Metastases to bone 42.25 21.88 38 15770 9860 29548859
Pulmonary embolism 41.87 21.88 112 15696 76422 29482297
Weight decreased 41.49 21.88 175 15633 150730 29407989
Death 40.85 21.88 317 15491 341767 29216952
Ageusia 37.53 21.88 34 15774 8904 29549815
Skin disorder 37.08 21.88 38 15770 11580 29547139
Liver disorder 35.98 21.88 58 15750 27691 29531028
Aspartate aminotransferase increased 34.28 21.88 89 15719 59636 29499083
Osteonecrosis of jaw 33.96 21.88 43 15765 16467 29542252
Alanine aminotransferase increased 32.14 21.88 97 15711 70847 29487872
Vomiting 30.60 21.88 206 15602 212054 29346665
Hepatic encephalopathy 30.12 21.88 36 15772 12999 29545720
Dry skin 29.24 21.88 48 15760 23259 29535460
Blood pressure increased 28.04 21.88 95 15713 73708 29485011
Hypoproteinaemia 27.55 21.88 15 15793 1737 29556982
Overdose 26.99 21.88 5 15803 79814 29478905
Tumour pain 26.88 21.88 12 15796 904 29557815
Pneumothorax 26.06 21.88 37 15771 15805 29542914
Amylase increased 26.01 21.88 22 15786 5258 29553461
Glossodynia 25.87 21.88 18 15790 3225 29555494
Glossitis 25.12 21.88 12 15796 1056 29557663
Dry mouth 24.85 21.88 43 15765 21741 29536978
Acute kidney injury 23.99 21.88 68 15740 265199 29293520
Weight increased 23.49 21.88 6 15802 76661 29482058
Dehydration 21.98 21.88 120 15688 114628 29444091

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 1873.23 20.87 574 18049 28245 64451864
Malignant neoplasm progression 789.93 20.87 458 18165 112413 64367696
Diarrhoea 626.82 20.87 893 17730 721811 63758298
Hypothyroidism 429.87 20.87 217 18406 40240 64439869
Decreased appetite 415.80 20.87 456 18167 280833 64199276
Hepatic function abnormal 394.08 20.87 240 18383 64073 64416036
Hypertension 327.94 20.87 388 18235 258873 64221236
Stomatitis 260.90 20.87 231 18392 109374 64370735
Taste disorder 231.24 20.87 91 18532 9342 64470767
Proteinuria 221.42 20.87 123 18500 27600 64452509
Hair colour changes 186.46 20.87 61 18562 3666 64476443
Dysphonia 170.18 20.87 126 18497 46256 64433853
Disease progression 152.65 20.87 196 18427 141484 64338625
Fatigue 141.92 20.87 505 18118 748225 63731884
Malaise 132.04 20.87 327 18296 395920 64084189
Drug ineffective 131.62 20.87 40 18583 840207 63639902
Mucosal inflammation 119.88 20.87 117 18506 62467 64417642
Dysgeusia 92.03 20.87 89 18534 46958 64433151
Death 87.92 20.87 322 18301 482383 63997726
Hyperthyroidism 86.66 20.87 58 18565 18121 64461988
Immune-mediated hepatitis 86.44 20.87 31 18592 2458 64477651
Asthenia 77.42 20.87 285 18338 427759 64052350
Inappropriate schedule of product administration 72.80 20.87 110 18513 92176 64387933
Blood thyroid stimulating hormone increased 72.34 20.87 38 18585 7616 64472493
Oral pain 69.37 20.87 60 18563 27433 64452676
Off label use 67.72 20.87 360 18263 632446 63847663
Alanine aminotransferase increased 66.70 20.87 133 18490 138898 64341211
Aspartate aminotransferase increased 66.58 20.87 122 18501 119666 64360443
Pneumothorax 63.28 20.87 54 18569 24244 64455865
Adrenal insufficiency 62.74 20.87 52 18571 22435 64457674
Pulmonary embolism 61.97 20.87 133 18490 146223 64333886
Product selection error 58.49 20.87 13 18610 172 64479937
Nausea 58.01 20.87 406 18217 785394 63694715
Weight decreased 55.58 20.87 195 18428 285544 64194565
Drug interaction 55.08 20.87 18 18605 362065 64118044
Amylase increased 51.27 20.87 33 18590 9652 64470457
Drug hypersensitivity 50.68 20.87 5 18618 237810 64242299
Metastases to bone 48.34 20.87 43 18580 20392 64459717
Lipase increased 48.06 20.87 37 18586 14365 64465744
Ageusia 47.22 20.87 36 18587 13777 64466332
Liver function test increased 45.05 20.87 50 18573 30920 64449189
Skin toxicity 43.86 20.87 26 18597 6576 64473533
Blood bilirubin increased 41.71 20.87 66 18557 57487 64422622
Pleural effusion 41.44 20.87 104 18519 126455 64353654
Osteonecrosis of jaw 41.07 20.87 54 18569 39771 64440338
Hypersensitivity 39.65 20.87 5 18618 196447 64283662
Hepatic encephalopathy 39.58 20.87 39 18584 21027 64459082
Blister 38.24 20.87 77 18546 80890 64399219
Weight increased 37.35 20.87 8 18615 213340 64266769
Dehydration 37.09 20.87 142 18481 216621 64263488
Toxicity to various agents 36.30 20.87 31 18592 363482 64116627
Infusion related reaction 36.26 20.87 3 18620 164464 64315645
Anal abscess 35.89 20.87 24 18599 7484 64472625
Tumour pain 34.93 20.87 15 18608 1918 64478191
Transaminases increased 34.91 20.87 53 18570 44541 64435568
Liver disorder 34.35 20.87 58 18565 53293 64426816
Joint swelling 33.99 20.87 10 18613 215372 64264737
Vomiting 33.84 20.87 273 18350 550844 63929265
Rheumatoid arthritis 33.60 20.87 4 18619 164290 64315819
Hypocalcaemia 33.22 20.87 50 18573 41703 64438406
Pain 33.09 20.87 69 18554 553442 63926667
Skin ulcer 31.27 20.87 50 18573 43924 64436185
Constipation 31.18 20.87 140 18483 229197 64250912
Nasopharyngitis 31.12 20.87 9 18614 196064 64284045
Dry skin 29.52 20.87 53 18570 51108 64429001
Colitis 29.14 20.87 57 18566 58617 64421492
Hyperkeratosis 28.71 20.87 20 18603 6661 64473448
Blood pressure increased 28.65 20.87 112 18511 172440 64307669
Skin disorder 27.72 20.87 37 18586 27643 64452466
Fall 26.57 20.87 50 18573 416776 64063333
Intestinal perforation 26.29 20.87 27 18596 15286 64464823
General physical health deterioration 25.71 20.87 122 18501 204303 64275806
Urticaria 24.82 20.87 6 18617 147311 64332798
Glossitis 24.79 20.87 14 18609 3233 64476876
Cell death 24.44 20.87 15 18608 4039 64476070
Hypoproteinaemia 24.26 20.87 14 18609 3368 64476741
Product dose omission issue 24.24 20.87 13 18610 194734 64285375
Cholecystitis 24.02 20.87 29 18594 19607 64460502
Bradycardia 23.87 20.87 3 18620 118216 64361893
Depression 23.16 20.87 12 18611 183279 64296830
Large intestine perforation 23.06 20.87 23 18600 12581 64467528
Performance status decreased 22.92 20.87 16 18607 5348 64474761
Microangiopathic haemolytic anaemia 22.76 20.87 10 18613 1352 64478757
Overdose 22.41 20.87 9 18614 159557 64320552
Injection site pain 22.07 20.87 3 18620 111405 64368704
Embolism 21.78 20.87 22 18601 12213 64467896
Pneumonitis 21.54 20.87 46 18577 50319 64429790
Scrotal dermatitis 21.45 20.87 3 18620 0 64480109
Cancer pain 21.29 20.87 14 18609 4243 64475866
Swelling 20.98 20.87 10 18613 160208 64319901

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:35610 antineoplastic agents
CHEBI has role CHEBI:38637 tyrosine kinase inhibitors
CHEBI has role CHEBI:50266 Prodrugs

Drug Use (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 CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 8497284 Sept. 24, 2024 TREATMENT OF ADVANCED RENAL CELL CARCINOMA
EQ 20MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 8497284 Sept. 24, 2024 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 8497284 Sept. 24, 2024 TREATMENT OF RENAL CELL CARCINOMA
EQ 40MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 8497284 Sept. 24, 2024 TREATMENT OF ADVANCED RENAL CELL CARCINOMA
EQ 40MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 8497284 Sept. 24, 2024 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 8497284 Sept. 24, 2024 TREATMENT OF RENAL CELL CARCINOMA
EQ 60MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 8497284 Sept. 24, 2024 TREATMENT OF ADVANCED RENAL CELL CARCINOMA
EQ 60MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 8497284 Sept. 24, 2024 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 8497284 Sept. 24, 2024 TREATMENT OF RENAL CELL CARCINOMA
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 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 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 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 CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 11141413 April 17, 2037 TREATMENT OF ADVANCED RENAL CELL CARCINOMA (RCC) IN PATIENTS WHO HAVE RECEIVED PRIOR ANTI-ANGIOGENIC THERAPY
EQ 40MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 11141413 April 17, 2037 TREATMENT OF ADVANCED RENAL CELL CARCINOMA (RCC) IN PATIENTS WHO HAVE RECEIVED PRIOR ANTI-ANGIOGENIC THERAPY
EQ 60MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL 11141413 April 17, 2037 TREATMENT OF ADVANCED RENAL CELL CARCINOMA (RCC) IN PATIENTS WHO HAVE RECEIVED PRIOR ANTI-ANGIOGENIC THERAPY

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, 2022 TREATMENT OF PATIENTS WITH HEPATOCELLULAR CARCINOMA WHO HAVE BEEN PREVIOUSLY TREATED WITH SORAFENIB
EQ 40MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL Jan. 14, 2022 TREATMENT OF PATIENTS WITH HEPATOCELLULAR CARCINOMA WHO HAVE BEEN PREVIOUSLY TREATED WITH SORAFENIB
EQ 60MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL Jan. 14, 2022 TREATMENT OF PATIENTS WITH HEPATOCELLULAR CARCINOMA WHO HAVE BEEN PREVIOUSLY TREATED WITH SORAFENIB
EQ 20MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL Jan. 22, 2024 FOR THE TREATMENT OF PATIENTS WITH ADVANCED RENAL CELL CARCINOMA, AS A FIRST-LINE TREATMENT IN COMBINATION WITH NIVOLUMAB
EQ 40MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL Jan. 22, 2024 FOR THE TREATMENT OF PATIENTS WITH ADVANCED RENAL CELL CARCINOMA, AS A FIRST-LINE TREATMENT IN COMBINATION WITH NIVOLUMAB
EQ 60MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL Jan. 22, 2024 FOR THE TREATMENT OF PATIENTS WITH ADVANCED RENAL CELL CARCINOMA, AS A FIRST-LINE TREATMENT IN COMBINATION WITH NIVOLUMAB
EQ 20MG BASE CABOMETYX EXELIXIS INC N208692 April 25, 2016 RX TABLET ORAL Sept. 17, 2024 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, 2024 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, 2024 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 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

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
Macrophage-stimulating protein receptor Kinase INHIBITOR IC50 6.91 WOMBAT-PK
Receptor-interacting serine/threonine-protein kinase 2 Kinase Kd 6.12 CHEMBL
Epithelial discoidin domain-containing receptor 1 Kinase Kd 6.68 CHEMBL
Protein-tyrosine kinase 6 Kinase Kd 5.75 CHEMBL
Tyrosine-protein kinase receptor UFO Kinase IC50 8.47 CHEMBL
Discoidin domain-containing receptor 2 Kinase Kd 6.30 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
Tyrosine-protein kinase FRK Kinase Kd 6.25 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
1140909-48-3 SECONDARY_CAS_RN
4032025 VANDF
C3181682 UMLSCUI
CHEBI:72319 CHEBI
CHEMBL2105717 ChEMBL_ID
25102847 PUBCHEM_CID
DB08875 DRUGBANK_ID
CHEMBL2103868 ChEMBL_ID
9297 INN_ID
C558660 MESH_SUPPLEMENTAL_RECORD_UI
5887 IUPHAR_LIGAND_ID
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

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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 42388-024 TABLET 20 mg ORAL NDA 27 sections
CABOMETYX HUMAN PRESCRIPTION DRUG LABEL 1 42388-025 TABLET 40 mg ORAL NDA 27 sections