Stem definition | Drug id | CAS RN |
---|---|---|
Raf (Rapidely Accelerated Fibrosarcoma) kinase inhibitors | 4654 | 755037-03-7 |
Dose | Unit | Route |
---|---|---|
0.12 | g | O |
None
Date | Agency | Company | Orphan |
---|---|---|---|
Aug. 26, 2013 | EMA | ||
Sept. 27, 2012 | FDA | BAYER HLTHCARE |
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 | 1133.27 | 26.32 | 340 | 11216 | 19758 | 50573810 |
Dysphonia | 417.76 | 26.32 | 195 | 11361 | 38697 | 50554871 |
Decreased appetite | 245.93 | 26.32 | 264 | 11292 | 200659 | 50392909 |
Off label use | 241.26 | 26.32 | 405 | 11151 | 474021 | 50119547 |
Metastases to lung | 158.87 | 26.32 | 68 | 11488 | 10952 | 50582616 |
Fatigue | 153.64 | 26.32 | 428 | 11128 | 707173 | 49886395 |
Blister | 107.16 | 26.32 | 114 | 11442 | 85304 | 50508264 |
Hyperkeratosis | 106.75 | 26.32 | 41 | 11515 | 4994 | 50588574 |
Skin exfoliation | 106.12 | 26.32 | 76 | 11480 | 33536 | 50560032 |
Asthenia | 102.58 | 26.32 | 225 | 11331 | 318817 | 50274751 |
Diarrhoea | 101.63 | 26.32 | 329 | 11227 | 588147 | 50005421 |
Pyrexia | 98.13 | 26.32 | 246 | 11310 | 379957 | 50213611 |
Metastases to liver | 96.37 | 26.32 | 59 | 11497 | 20045 | 50573523 |
Carcinoembryonic antigen increased | 96.16 | 26.32 | 28 | 11528 | 1446 | 50592122 |
Hypertension | 91.78 | 26.32 | 169 | 11387 | 211034 | 50382534 |
Blood bilirubin increased | 91.08 | 26.32 | 68 | 11488 | 31970 | 50561598 |
Pain in extremity | 90.55 | 26.32 | 195 | 11361 | 272670 | 50320898 |
Neuropathy peripheral | 89.00 | 26.32 | 110 | 11446 | 96647 | 50496921 |
Stomatitis | 75.71 | 26.32 | 104 | 11452 | 101240 | 50492328 |
Oral pain | 75.34 | 26.32 | 55 | 11501 | 24978 | 50568590 |
Dehydration | 73.85 | 26.32 | 128 | 11428 | 152321 | 50441247 |
Weight decreased | 70.89 | 26.32 | 156 | 11400 | 221089 | 50372479 |
Dry skin | 65.68 | 26.32 | 64 | 11492 | 43127 | 50550441 |
Rash | 65.00 | 26.32 | 233 | 11323 | 437238 | 50156330 |
Blood pressure increased | 64.74 | 26.32 | 112 | 11444 | 133020 | 50460548 |
Platelet count decreased | 62.97 | 26.32 | 95 | 11461 | 100631 | 50492937 |
Hepatic function abnormal | 54.56 | 26.32 | 51 | 11505 | 32630 | 50560938 |
Hospitalisation | 51.12 | 26.32 | 70 | 11486 | 67867 | 50525701 |
Drug ineffective | 50.90 | 26.32 | 68 | 11488 | 819265 | 49774303 |
Disseminated intravascular coagulation | 50.09 | 26.32 | 37 | 11519 | 17098 | 50576470 |
Condition aggravated | 47.45 | 26.32 | 6 | 11550 | 297052 | 50296516 |
Skin fissures | 45.56 | 26.32 | 27 | 11529 | 8641 | 50584927 |
Erythema | 45.41 | 26.32 | 102 | 11454 | 146312 | 50447256 |
Mucosal inflammation | 44.06 | 26.32 | 50 | 11506 | 40092 | 50553476 |
Skin toxicity | 43.08 | 26.32 | 20 | 11536 | 3893 | 50589675 |
Plantar erythema | 42.86 | 26.32 | 10 | 11546 | 213 | 50593355 |
Abdominal pain | 42.15 | 26.32 | 134 | 11422 | 236094 | 50357474 |
Gait inability | 42.14 | 26.32 | 47 | 11509 | 36980 | 50556588 |
Tumour marker increased | 40.33 | 26.32 | 19 | 11537 | 3821 | 50589747 |
Dry mouth | 39.44 | 26.32 | 56 | 11500 | 56122 | 50537446 |
Colorectal cancer metastatic | 39.04 | 26.32 | 11 | 11545 | 504 | 50593064 |
Exercise tolerance decreased | 38.90 | 26.32 | 20 | 11536 | 4854 | 50588714 |
Palmoplantar keratoderma | 37.92 | 26.32 | 8 | 11548 | 105 | 50593463 |
Hepatic encephalopathy | 35.57 | 26.32 | 24 | 11532 | 9612 | 50583956 |
Colon cancer | 35.36 | 26.32 | 23 | 11533 | 8668 | 50584900 |
Jaundice | 30.85 | 26.32 | 34 | 11522 | 26395 | 50567173 |
Constipation | 29.20 | 26.32 | 101 | 11455 | 185607 | 50407961 |
Feeding disorder | 28.97 | 26.32 | 22 | 11534 | 10591 | 50582977 |
Drug hypersensitivity | 28.26 | 26.32 | 11 | 11545 | 250999 | 50342569 |
Joint swelling | 27.20 | 26.32 | 11 | 11545 | 245275 | 50348293 |
Ascites | 27.03 | 26.32 | 37 | 11519 | 35824 | 50557744 |
Hepatic failure | 26.92 | 26.32 | 35 | 11521 | 32248 | 50561320 |
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 | 1889.48 | 23.25 | 564 | 14492 | 14195 | 29545276 |
Dysphonia | 719.25 | 23.25 | 294 | 14762 | 18902 | 29540569 |
Decreased appetite | 335.60 | 23.25 | 390 | 14666 | 144952 | 29414519 |
Metastases to lung | 309.77 | 23.25 | 125 | 14931 | 7730 | 29551741 |
Off label use | 300.03 | 23.25 | 541 | 14515 | 300259 | 29259212 |
Fatigue | 273.74 | 23.25 | 536 | 14520 | 316285 | 29243186 |
Diarrhoea | 201.22 | 23.25 | 488 | 14568 | 332210 | 29227261 |
Blister | 199.63 | 23.25 | 125 | 14931 | 19781 | 29539690 |
Metastases to liver | 175.90 | 23.25 | 96 | 14960 | 11760 | 29547711 |
Hypertension | 155.72 | 23.25 | 240 | 14816 | 116374 | 29443097 |
Carcinoembryonic antigen increased | 153.80 | 23.25 | 40 | 15016 | 584 | 29558887 |
Pain in extremity | 134.53 | 23.25 | 218 | 14838 | 110215 | 29449256 |
Skin exfoliation | 121.37 | 23.25 | 97 | 14959 | 22548 | 29536923 |
Blood bilirubin increased | 118.81 | 23.25 | 114 | 14942 | 33779 | 29525692 |
Asthenia | 106.88 | 23.25 | 294 | 14762 | 214956 | 29344515 |
Skin fissures | 100.41 | 23.25 | 46 | 15010 | 3873 | 29555598 |
Neuropathy peripheral | 98.57 | 23.25 | 149 | 14907 | 70878 | 29488593 |
Dry skin | 96.39 | 23.25 | 86 | 14970 | 23221 | 29536250 |
Weight decreased | 92.18 | 23.25 | 223 | 14833 | 150682 | 29408789 |
Stomatitis | 85.75 | 23.25 | 100 | 14956 | 37013 | 29522458 |
Hyperkeratosis | 85.73 | 23.25 | 39 | 15017 | 3230 | 29556241 |
Alpha 1 foetoprotein increased | 84.20 | 23.25 | 25 | 15031 | 606 | 29558865 |
Tumour marker increased | 78.94 | 23.25 | 23 | 15033 | 521 | 29558950 |
Ascites | 76.91 | 23.25 | 94 | 14962 | 36525 | 29522946 |
Blood pressure increased | 71.73 | 23.25 | 132 | 14924 | 73671 | 29485800 |
Hospitalisation | 64.48 | 23.25 | 97 | 14959 | 45891 | 29513580 |
Hepatic function abnormal | 64.08 | 23.25 | 89 | 14967 | 39170 | 29520301 |
Oral pain | 58.85 | 23.25 | 44 | 15012 | 9263 | 29550208 |
Hepatic encephalopathy | 57.68 | 23.25 | 50 | 15006 | 12985 | 29546486 |
Dehydration | 52.06 | 23.25 | 152 | 14904 | 114596 | 29444875 |
Toxicity to various agents | 50.68 | 23.25 | 13 | 15043 | 173648 | 29385823 |
Abdominal pain | 48.29 | 23.25 | 165 | 14891 | 135192 | 29424279 |
Abdominal pain upper | 48.16 | 23.25 | 100 | 14956 | 60893 | 29498578 |
Metastases to lymph nodes | 47.34 | 23.25 | 28 | 15028 | 3989 | 29555482 |
Glossodynia | 44.61 | 23.25 | 25 | 15031 | 3218 | 29556253 |
Aphonia | 44.15 | 23.25 | 24 | 15032 | 2910 | 29556561 |
Drug interaction | 40.90 | 23.25 | 25 | 15031 | 197360 | 29362111 |
Colorectal cancer metastatic | 40.78 | 23.25 | 14 | 15042 | 547 | 29558924 |
Metastases to peritoneum | 39.43 | 23.25 | 18 | 15038 | 1502 | 29557969 |
Dry mouth | 37.96 | 23.25 | 51 | 15005 | 21733 | 29537738 |
Febrile neutropenia | 37.71 | 23.25 | 6 | 15050 | 112234 | 29447237 |
Gastrointestinal stromal tumour | 36.28 | 23.25 | 14 | 15042 | 766 | 29558705 |
Malaise | 36.28 | 23.25 | 169 | 14887 | 159433 | 29400038 |
Drug ineffective | 34.17 | 23.25 | 85 | 14971 | 363085 | 29196386 |
Colon cancer | 33.12 | 23.25 | 29 | 15027 | 7626 | 29551845 |
Acute kidney injury | 32.70 | 23.25 | 53 | 15003 | 265214 | 29294257 |
Condition aggravated | 32.47 | 23.25 | 17 | 15039 | 146278 | 29413193 |
Constipation | 30.56 | 23.25 | 127 | 14929 | 114033 | 29445438 |
Colon cancer metastatic | 30.52 | 23.25 | 15 | 15041 | 1476 | 29557995 |
Proteinuria | 29.07 | 23.25 | 38 | 15018 | 15766 | 29543705 |
Biliary obstruction | 28.90 | 23.25 | 17 | 15039 | 2397 | 29557074 |
Hypotension | 28.77 | 23.25 | 34 | 15022 | 194320 | 29365151 |
Angular cheilitis | 28.49 | 23.25 | 8 | 15048 | 158 | 29559313 |
Cardiac arrest | 27.80 | 23.25 | 5 | 15051 | 85586 | 29473885 |
Overdose | 27.41 | 23.25 | 4 | 15052 | 79815 | 29479656 |
Colorectal cancer | 27.34 | 23.25 | 15 | 15041 | 1852 | 29557619 |
Plantar erythema | 26.34 | 23.25 | 6 | 15050 | 48 | 29559423 |
Gait inability | 26.06 | 23.25 | 39 | 15017 | 18336 | 29541135 |
Protein induced by vitamin K absence or antagonist II increased | 25.30 | 23.25 | 5 | 15051 | 18 | 29559453 |
Metastases to central nervous system | 24.97 | 23.25 | 24 | 15032 | 7107 | 29552364 |
General physical health deterioration | 24.88 | 23.25 | 111 | 14945 | 102746 | 29456725 |
Metastases to adrenals | 24.25 | 23.25 | 11 | 15045 | 904 | 29558567 |
Adverse drug reaction | 23.33 | 23.25 | 43 | 15013 | 23977 | 29535494 |
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 | 2704.01 | 21.41 | 817 | 24495 | 28002 | 64445418 |
Dysphonia | 1038.01 | 21.41 | 457 | 24855 | 45925 | 64427495 |
Decreased appetite | 532.64 | 21.41 | 601 | 24711 | 280688 | 64192732 |
Metastases to lung | 470.01 | 21.41 | 189 | 25123 | 15075 | 64458345 |
Off label use | 454.01 | 21.41 | 852 | 24460 | 631954 | 63841466 |
Fatigue | 366.06 | 21.41 | 862 | 24450 | 747868 | 63725552 |
Diarrhoea | 284.37 | 21.41 | 767 | 24545 | 721937 | 63751483 |
Metastases to liver | 253.36 | 21.41 | 142 | 25170 | 23799 | 64449621 |
Blister | 240.11 | 21.41 | 221 | 25091 | 80746 | 64392674 |
Asthenia | 222.22 | 21.41 | 506 | 24806 | 427538 | 64045882 |
Neuropathy peripheral | 214.41 | 21.41 | 247 | 25065 | 117278 | 64356142 |
Skin exfoliation | 211.05 | 21.41 | 160 | 25152 | 44725 | 64428695 |
Hypertension | 210.86 | 21.41 | 370 | 24942 | 258891 | 64214529 |
Carcinoembryonic antigen increased | 200.54 | 21.41 | 59 | 25253 | 1814 | 64471606 |
Pain in extremity | 198.35 | 21.41 | 394 | 24918 | 302691 | 64170729 |
Blood bilirubin increased | 194.13 | 21.41 | 169 | 25143 | 57384 | 64416036 |
Hyperkeratosis | 156.09 | 21.41 | 68 | 25244 | 6613 | 64466807 |
Weight decreased | 154.81 | 21.41 | 344 | 24968 | 285395 | 64188025 |
Dry skin | 150.30 | 21.41 | 139 | 25173 | 51022 | 64422398 |
Stomatitis | 143.21 | 21.41 | 195 | 25117 | 109410 | 64364010 |
Skin fissures | 142.34 | 21.41 | 73 | 25239 | 10233 | 64463187 |
Oral pain | 122.58 | 21.41 | 95 | 25217 | 27398 | 64446022 |
Blood pressure increased | 119.47 | 21.41 | 230 | 25082 | 172322 | 64301098 |
Dehydration | 116.16 | 21.41 | 260 | 25052 | 216503 | 64256917 |
Hepatic function abnormal | 113.51 | 21.41 | 133 | 25179 | 64180 | 64409240 |
Hospitalisation | 99.99 | 21.41 | 135 | 25177 | 75072 | 64398348 |
Pyrexia | 86.73 | 21.41 | 440 | 24872 | 558204 | 63915216 |
Alpha 1 foetoprotein increased | 86.69 | 21.41 | 25 | 25287 | 715 | 64472705 |
Ascites | 85.01 | 21.41 | 113 | 25199 | 61888 | 64411532 |
Toxicity to various agents | 83.66 | 21.41 | 20 | 25292 | 363493 | 64109927 |
Tumour marker increased | 83.48 | 21.41 | 36 | 25276 | 3414 | 64470006 |
Condition aggravated | 82.80 | 21.41 | 22 | 25290 | 372404 | 64101016 |
Abdominal pain | 80.26 | 21.41 | 287 | 25025 | 312088 | 64161332 |
Drug ineffective | 77.68 | 21.41 | 132 | 25180 | 840115 | 63633305 |
Colon cancer | 72.49 | 21.41 | 51 | 25261 | 12688 | 64460732 |
Dry mouth | 67.75 | 21.41 | 100 | 25212 | 60318 | 64413102 |
Hepatic encephalopathy | 67.24 | 21.41 | 60 | 25252 | 21006 | 64452414 |
Gait inability | 65.56 | 21.41 | 82 | 25230 | 42286 | 64431134 |
Drug interaction | 61.15 | 21.41 | 33 | 25279 | 362050 | 64111370 |
Abdominal pain upper | 60.42 | 21.41 | 178 | 25134 | 174852 | 64298568 |
Colorectal cancer metastatic | 59.82 | 21.41 | 20 | 25292 | 940 | 64472480 |
Rash | 59.38 | 21.41 | 344 | 24968 | 458205 | 64015215 |
Platelet count decreased | 59.27 | 21.41 | 172 | 25140 | 167539 | 64305881 |
Metastases to peritoneum | 57.45 | 21.41 | 28 | 25284 | 3519 | 64469901 |
Mucosal inflammation | 56.82 | 21.41 | 94 | 25218 | 62490 | 64410930 |
Colon cancer metastatic | 56.36 | 21.41 | 23 | 25289 | 1900 | 64471520 |
Constipation | 54.85 | 21.41 | 206 | 25106 | 229131 | 64244289 |
Plantar erythema | 53.25 | 21.41 | 14 | 25298 | 281 | 64473139 |
Metastases to lymph nodes | 49.83 | 21.41 | 35 | 25277 | 8682 | 64464738 |
Jaundice | 46.93 | 21.41 | 75 | 25237 | 48437 | 64424983 |
Exercise tolerance decreased | 46.52 | 21.41 | 32 | 25280 | 7678 | 64465742 |
Drug hypersensitivity | 45.82 | 21.41 | 18 | 25294 | 237797 | 64235623 |
Erythema | 44.67 | 21.41 | 168 | 25144 | 186902 | 64286518 |
Disseminated intravascular coagulation | 42.85 | 21.41 | 58 | 25254 | 32290 | 64441130 |
Overdose | 42.61 | 21.41 | 6 | 25306 | 159560 | 64313860 |
Hepatic failure | 42.18 | 21.41 | 77 | 25235 | 55317 | 64418103 |
Infusion related reaction | 42.06 | 21.41 | 7 | 25305 | 164460 | 64308960 |
Proteinuria | 41.84 | 21.41 | 53 | 25259 | 27670 | 64445750 |
Acute kidney injury | 40.04 | 21.41 | 72 | 25240 | 449168 | 64024252 |
Aspartate aminotransferase increased | 39.57 | 21.41 | 120 | 25192 | 119668 | 64353752 |
Cardiac arrest | 38.43 | 21.41 | 7 | 25305 | 154057 | 64319363 |
Gastrointestinal stromal tumour | 38.38 | 21.41 | 16 | 25296 | 1395 | 64472025 |
Biliary obstruction | 38.37 | 21.41 | 22 | 25290 | 3842 | 64469578 |
Hypotension | 36.76 | 21.41 | 58 | 25254 | 380916 | 64092504 |
Weight increased | 36.63 | 21.41 | 19 | 25293 | 213329 | 64260091 |
Skin toxicity | 36.56 | 21.41 | 26 | 25286 | 6576 | 64466844 |
Colorectal cancer | 36.50 | 21.41 | 20 | 25292 | 3201 | 64470219 |
Feeding disorder | 35.72 | 21.41 | 34 | 25278 | 12915 | 64460505 |
Sinusitis | 35.61 | 21.41 | 7 | 25305 | 145921 | 64327499 |
Palmoplantar keratoderma | 35.22 | 21.41 | 11 | 25301 | 415 | 64473005 |
Febrile neutropenia | 34.85 | 21.41 | 15 | 25297 | 187642 | 64285778 |
Fall | 34.34 | 21.41 | 70 | 25242 | 416756 | 64056664 |
Pre-existing condition improved | 34.12 | 21.41 | 22 | 25290 | 4740 | 64468680 |
Metastases to adrenals | 34.09 | 21.41 | 14 | 25298 | 1175 | 64472245 |
Gastrointestinal perforation | 33.88 | 21.41 | 23 | 25289 | 5401 | 64468019 |
Rectal cancer | 33.40 | 21.41 | 18 | 25294 | 2788 | 64470632 |
Ammonia increased | 33.04 | 21.41 | 25 | 25287 | 6952 | 64466468 |
Decreased activity | 32.40 | 21.41 | 25 | 25287 | 7155 | 64466265 |
Protein induced by vitamin K absence or antagonist II increased | 32.27 | 21.41 | 6 | 25306 | 20 | 64473400 |
Pain of skin | 32.08 | 21.41 | 28 | 25284 | 9519 | 64463901 |
Arthropathy | 31.26 | 21.41 | 5 | 25307 | 120962 | 64352458 |
Therapeutic product ineffective | 30.84 | 21.41 | 14 | 25298 | 1499 | 64471921 |
Adverse drug reaction | 30.65 | 21.41 | 60 | 25252 | 45404 | 64428016 |
Food refusal | 30.44 | 21.41 | 10 | 25302 | 445 | 64472975 |
Joint swelling | 30.38 | 21.41 | 24 | 25288 | 215358 | 64258062 |
Hypersomnia | 30.23 | 21.41 | 38 | 25274 | 19679 | 64453741 |
Nasopharyngitis | 30.06 | 21.41 | 20 | 25292 | 196053 | 64277367 |
Gait disturbance | 29.67 | 21.41 | 140 | 25172 | 172015 | 64301405 |
Death | 28.54 | 21.41 | 302 | 25010 | 482403 | 63991017 |
Aphonia | 28.20 | 21.41 | 25 | 25287 | 8672 | 64464748 |
Oral hyperaesthesia | 27.37 | 21.41 | 4 | 25308 | 0 | 64473420 |
Pancytopenia | 27.33 | 21.41 | 11 | 25301 | 143298 | 64330122 |
Intestinal obstruction | 27.06 | 21.41 | 50 | 25262 | 36236 | 64437184 |
Hyperbilirubinaemia | 26.54 | 21.41 | 37 | 25275 | 21168 | 64452252 |
Liver disorder | 26.28 | 21.41 | 62 | 25250 | 53289 | 64420131 |
Metastasis | 26.07 | 21.41 | 20 | 25292 | 5675 | 64467745 |
Tumour rupture | 24.41 | 21.41 | 8 | 25304 | 353 | 64473067 |
Malaise | 24.38 | 21.41 | 250 | 25062 | 395997 | 64077423 |
Pneumonia | 24.34 | 21.41 | 125 | 25187 | 559451 | 63913969 |
Syncope | 24.27 | 21.41 | 16 | 25296 | 157619 | 64315801 |
Cancer pain | 24.12 | 21.41 | 17 | 25295 | 4240 | 64469180 |
Treatment failure | 23.91 | 21.41 | 8 | 25304 | 116808 | 64356612 |
Protein urine present | 23.73 | 21.41 | 23 | 25289 | 8933 | 64464487 |
Hepatic lesion | 23.53 | 21.41 | 19 | 25293 | 5805 | 64467615 |
Abnormal loss of weight | 23.46 | 21.41 | 21 | 25291 | 7379 | 64466041 |
Anxiety | 23.42 | 21.41 | 27 | 25285 | 202622 | 64270798 |
Depression | 22.75 | 21.41 | 23 | 25289 | 183268 | 64290152 |
Intestinal metastasis | 22.57 | 21.41 | 7 | 25305 | 258 | 64473162 |
Asthma | 22.33 | 21.41 | 5 | 25307 | 95220 | 64378200 |
Hepatic pain | 22.21 | 21.41 | 15 | 25297 | 3493 | 64469927 |
Osteosarcoma metastatic | 22.16 | 21.41 | 5 | 25307 | 51 | 64473369 |
Cardiac failure congestive | 21.86 | 21.41 | 12 | 25300 | 130568 | 64342852 |
Metastases to abdominal cavity | 21.85 | 21.41 | 8 | 25304 | 493 | 64472927 |
Hypersensitivity | 21.82 | 21.41 | 27 | 25285 | 196425 | 64276995 |
Angular cheilitis | 21.80 | 21.41 | 8 | 25304 | 496 | 64472924 |
Skin disorder | 21.73 | 21.41 | 39 | 25273 | 27641 | 64445779 |
None
Source | Code | Description |
---|---|---|
ATC | L01EX05 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Other protein kinase inhibitors |
FDA MoA | N0000175076 | Protein Kinase Inhibitors |
FDA EPC | N0000175605 | Kinase Inhibitor |
FDA MoA | N0000185504 | Cytochrome P450 2C9 Inhibitors |
CHEBI has role | CHEBI:35610 | antineoplastic agents |
CHEBI has role | CHEBI:38637 | tyrosine kinase inhibitors |
CHEBI has role | CHEBI:50908 | agente hepatotoxico |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Liver cell carcinoma | indication | 109841003 | DOID:684 |
Metastasis from malignant tumor of colon | indication | 314998002 | |
Gastrointestinal stromal tumor | indication | 420120006 | DOID:9253 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 11.41 | acidic |
pKa2 | 11.83 | acidic |
pKa3 | 12.52 | acidic |
pKa4 | 2.76 | Basic |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
---|---|---|---|---|---|---|---|---|---|---|
40MG | STIVARGA | BAYER HLTHCARE | N203085 | Sept. 27, 2012 | RX | TABLET | ORAL | 8680124 | June 2, 2030 | TREATMENT OF PATIENTS WITH GASTROINTESTINAL STROMAL TUMOR (GIST), INCLUDING BUT NOT LIMITED TO PATIENTS PREVIOUSLY TREATED WITH IMATINIB AND PATIENTS WITH GIST HAVING RESISTANCE TO A KIT TYROSINE KINASE INHIBITOR |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
---|---|---|---|---|---|---|---|---|---|
40MG | STIVARGA | BAYER HLTHCARE | N203085 | Sept. 27, 2012 | RX | TABLET | ORAL | April 27, 2024 | TREATMENT OF PATIENTS WITH HEPATOCELLULAR CARCINOMA (HCC OR LIVER CANCER) WHO HAVE BEEN PREVIOUSLY TREATED WITH THE DRUG SORAFENIB. |
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Serine/threonine-protein kinase B-raf | Kinase | INHIBITOR | IC50 | 7.55 | CHEMBL | CHEMBL | |||
Vascular endothelial growth factor receptor 2 | Kinase | INHIBITOR | IC50 | 7.90 | IUPHAR | CHEMBL | |||
Tyrosine-protein kinase ABL1 | Kinase | Kd | 6.12 | CHEMBL | |||||
Mast/stem cell growth factor receptor Kit | Kinase | IC50 | 8.21 | CHEMBL | |||||
Breakpoint cluster region protein | Kinase | Kd | 6.13 | CHEMBL | |||||
Ephrin type-A receptor 2 | Kinase | Kd | 6.08 | CHEMBL | |||||
RAF proto-oncogene serine/threonine-protein kinase | Kinase | IC50 | 8.82 | CHEMBL | |||||
Receptor-type tyrosine-protein kinase FLT3 | Kinase | IC50 | 7.09 | CHEMBL | |||||
Proto-oncogene tyrosine-protein kinase receptor Ret | Kinase | Kd | 6.90 | CHEMBL | |||||
Vascular endothelial growth factor receptor 1 | Kinase | IC50 | 8.82 | CHEMBL | |||||
Angiopoietin-1 receptor | Kinase | IC50 | 8.82 | CHEMBL | |||||
LIM domain kinase 1 | Kinase | Kd | 6.21 | CHEMBL | |||||
Fibroblast growth factor receptor 1 | Kinase | IC50 | 8.82 | CHEMBL | |||||
Dual specificity protein kinase TTK | Kinase | Kd | 5.41 | CHEMBL | |||||
Mitogen-activated protein kinase 11 | Kinase | Kd | 5.72 | CHEMBL | |||||
Ephrin type-A receptor 5 | Kinase | Kd | 5.95 | CHEMBL | |||||
Mitogen-activated protein kinase 14 | Kinase | Kd | 6.15 | CHEMBL | |||||
Dual specificity protein kinase CLK1 | Kinase | Kd | 5.68 | CHEMBL | |||||
Receptor-interacting serine/threonine-protein kinase 2 | Kinase | Kd | 6.12 | CHEMBL | |||||
Epithelial discoidin domain-containing receptor 1 | Kinase | Kd | 6.45 | CHEMBL | |||||
Bifunctional epoxide hydrolase 2 | Enzyme | INHIBITOR | IC50 | 9.30 | CHEMBL | ||||
MAP kinase-activated protein kinase 2 | Kinase | Kd | 6.17 | CHEMBL | |||||
Cyclin-dependent kinase 17 | Kinase | Kd | 6.14 | CHEMBL | |||||
Mitogen-activated protein kinase kinase kinase MLT | Kinase | Kd | 6.56 | CHEMBL | |||||
Discoidin domain-containing receptor 2 | Kinase | Kd | 6.38 | CHEMBL | |||||
Ephrin type-A receptor 1 | Kinase | Kd | 8.15 | CHEMBL | |||||
Mitogen-activated protein kinase kinase kinase 1 | Kinase | Kd | 6.33 | CHEMBL | |||||
Glycine receptor subunit alpha-1 | Ion channel | EC50 | 5.74 | CHEMBL | |||||
Receptor-interacting serine/threonine-protein kinase 3 | Kinase | Kd | 6.43 | CHEMBL | |||||
Platelet-derived growth factor receptor beta | Kinase | IC50 | 8.82 | CHEMBL | |||||
Vascular endothelial growth factor receptor 2 | Kinase | IC50 | 8.82 | CHEMBL | |||||
Vascular endothelial growth factor receptor 3 | Kinase | IC50 | 8.82 | CHEMBL |
ID | Source |
---|---|
D10137 | KEGG_DRUG |
4031721 | VANDF |
CHEBI:68647 | CHEBI |
CHEMBL1946170 | ChEMBL_ID |
C559147 | MESH_SUPPLEMENTAL_RECORD_UI |
5891 | IUPHAR_LIGAND_ID |
DB08896 | DRUGBANK_ID |
MGN125FS9D | UNII |
11167602 | PUBCHEM_CID |
1312397 | RXNORM |
193440 | MMSL |
28887 | MMSL |
d07913 | MMSL |
014656 | NDDF |
702804006 | SNOMEDCT_US |
703808002 | SNOMEDCT_US |
C2980094 | UMLSCUI |
1019206-88-2 | SECONDARY_CAS_RN |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Stivarga | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50419-171 | TABLET, FILM COATED | 40 mg | ORAL | NDA | 29 sections |