Stem definition | Drug id | CAS RN |
---|---|---|
tyrosine kinase inhibitors | 4715 | 849217-68-1 |
Dose | Unit | Route |
---|---|---|
60 | mg | O |
None
Date | Agency | Company | Orphan |
---|---|---|---|
March 25, 2020 | PMDA | Takeda Pharmaceutical Company Limited | |
March 21, 2014 | EMA | TMC Pharma Services Ltd | |
Nov. 29, 2012 | FDA | EXELIXIS |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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 |
None
Source | Code | Description |
---|---|---|
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 |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
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 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 11.15 | acidic |
pKa2 | 11.76 | acidic |
pKa3 | 4.95 | Basic |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent 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 |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
---|---|---|---|---|---|---|---|---|---|
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 |
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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 |
ID | Source |
---|---|
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 |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
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 |