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

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 4225 319460-85-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • axitinib
  • inlyta
  • AG 013736
  • AG-013736
A benzamide and indazole derivative that acts as a TYROSINE KINASE inhibitor of the VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR. It is used in the treatment of advanced RENAL CELL CARCINOMA.
  • Molecular weight: 386.47
  • Formula: C22H18N4OS
  • CLOGP: 3.19
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 2
  • TPSA: 70.67
  • ALOGS: -5.85
  • ROTB: 5
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
10 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Hosey CM, Chan R, Benet LZ
CL (Clearance) 5 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.00 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 4.30 hours Lombardo F, Berellini G, Obach RS
S (Water solubility) 0.00 mg/mL Bocci G, Oprea TI, Benet LZ
BA (Bioavailability) 58 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class AAK1,ABL1,ABL2,ACVR1B,ACVR2A,ACVR2B,ACVRL1,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,BTK,CAMK2A,CAMK2B,CAMK2D,CAMK2G,CDK1,CDK14,CDK16,CDK19,CDK2,CDK3,CDK4,CDK5,CDK6,CDK7,CDK9,CHEK1,CLK2,CLK4,CSF1R,DDR1,DYRK1A,DYRK1B,EGFR,EIF2AK3,EPHA2,EPHB4,ERBB2,ERBB4,FGFR1,FLT1,FLT3,FLT4,FYN,GAK,GRK1,GRK2,GRK3,GSK3A,GSK3B,IGF1R,IKBKB,INSR,IRAK1,IRAK3,ITK,JAK1,JAK2,JAK3,KDR,KIT,LCK,LYN,MAP2K1,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K21,MAP3K7,MAP3K9,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK1,MAPK10,MAPK12,MAPK3,MAPK7,MAPK8,MAPK9,MAPKAPK2,MARK1,MARK2,MARK4,MELK,MET,MINK1,MST1R,MTOR,NTRK1,NTRK2,NUAK1,PAK4,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PIM2,PRKAA1,PRKAA2,PRKCD,PRKCZ,PRKDC,RIPK3,ROCK1,RPS6KA1,SGK1,SIK2,SIK3,SRC,STK10,STK17A,STK33,SYK,TEK,TGFBR1,TNIK,TTK,TYRO3,UHMK1,ULK1,ULK2,YES1,ZAP70 137
kinase-selectivity-class AAK1,ABL2,ACVR1B,ACVR2A,ACVR2B,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,CAMK2A,CAMK2B,CAMK2D,CDK1,CDK16,CDK2,CDK3,CDK4,CDK6,CDK7,CDK9,CHEK1,CLK2,CLK4,CSF1R,CSK,DDR1,DYRK1A,DYRK1B,DYRK2,DYRK3,EGFR,EIF2AK3,EPHA2,EPHB3,EPHB4,ERBB2,FGFR1,FGFR4,FLT1,FLT3,FLT4,FYN,GAK,GRK2,GSK3A,GSK3B,HASPIN,INSR,IRAK1,IRAK3,IRAK4,JAK1,JAK2,JAK3,KDR,KIT,LCK,LRRK2,LYN,MAP2K1,MAP2K3,MAP2K4,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K19,MAP3K2,MAP3K21,MAP3K7,MAP3K9,MAP4K1,MAP4K3,MAP4K4,MAP4K5,MAPK1,MAPK10,MAPK12,MAPK7,MAPK8,MARK1,MARK2,MARK3,MARK4,MELK,MET,MINK1,MKNK2,MST1R,NTRK1,NTRK3,NUAK1,PAK4,PDGFRB,PDK1,PDPK1,PIK3CA,PIM3,PLK4,PRKAA1,PRKAA2,PRKCD,PRKCZ,PTK2,RET,RIPK1,RIPK3,ROCK1,ROCK2,SGK1,SIK2,SIK3,SRC,STK10,STK16,STK17A,STK33,STK4,SYK,TEK,TGFBR1,TNIK,TNK1,TTK,TYRO3,ULK1,ULK2,YES1,ZAP70 134
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
Jan. 27, 2012 FDA PFIZER

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
Neoplasm progression 749.10 22.74 256 10363 44230 90573598
Diarrhoea 474.31 22.74 562 10057 938628 89679200
Death 397.96 22.74 367 10252 456184 90161644
Disease progression 309.74 22.74 205 10414 156410 90461418
Hypertension 276.62 22.74 302 10317 457230 90160598
Palmar-plantar erythrodysaesthesia syndrome 262.60 22.74 105 10514 27918 90589910
Dysphonia 253.72 22.74 131 10488 62953 90554875
Blood pressure increased 209.65 22.74 178 10441 197039 90420789
Fatigue 206.87 22.74 430 10189 1153593 89464235
Decreased appetite 197.21 22.74 231 10388 376309 90241519
Hypothyroidism 151.63 22.74 88 10531 53039 90564789
Stomatitis 136.06 22.74 164 10455 274534 90343294
Oral pain 117.42 22.74 63 10556 32620 90585208
Nausea 89.06 22.74 308 10311 1110008 89507820
Off label use 83.39 22.74 300 10319 1101952 89515876
Drug ineffective 75.86 22.74 34 10585 1384264 89233564
Weight decreased 70.04 22.74 144 10475 379766 90238062
Dehydration 66.57 22.74 97 10522 194350 90423478
Malignant neoplasm progression 63.15 22.74 70 10549 106800 90511028
Posterior reversible encephalopathy syndrome 58.43 22.74 35 10584 22304 90595524
Constipation 51.27 22.74 106 10513 280289 90337539
Proteinuria 49.55 22.74 32 10587 23259 90594569
Thyroid disorder 49.48 22.74 29 10590 17756 90600072
Asthenia 48.63 22.74 155 10464 533596 90084232
Immune-mediated hepatic disorder 40.85 22.74 13 10606 1779 90616049
Second primary malignancy 40.06 22.74 21 10598 10357 90607471
Oral discomfort 39.86 22.74 21 10598 10462 90607366
Polycythaemia 36.90 22.74 11 10608 1212 90616616
Aphonia 36.69 22.74 21 10598 12298 90605530
Infusion related reaction 34.92 22.74 4 10615 416776 90201052
Joint swelling 33.17 22.74 9 10610 503291 90114537
Nephrectomy 31.68 22.74 11 10608 1970 90615858
Drug hypersensitivity 31.10 22.74 8 10611 463601 90154227
Thyroiditis 28.49 22.74 12 10607 3625 90614203
Oligodipsia 28.46 22.74 5 10614 48 90617780
Feeding disorder 27.61 22.74 20 10599 17492 90600336
Sinusitis 27.03 22.74 4 10615 343084 90274744
Rheumatoid arthritis 26.86 22.74 5 10614 362609 90255219
Hyperkeratosis 26.69 22.74 14 10605 6914 90610914
Hepatotoxicity 25.30 22.74 29 10590 45813 90572015
Hypersensitivity 23.47 22.74 12 10607 454665 90163163
Hepatic function abnormal 23.41 22.74 28 10591 46260 90571568
Renal cancer 22.86 22.74 12 10607 5933 90611895

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
Neoplasm progression 1475.15 19.27 578 24781 28422 42567554
Dysphonia 1418.71 19.27 559 24800 27891 42568085
Diarrhoea 919.57 19.27 1237 24122 459612 42136364
Fatigue 705.05 19.27 1060 24299 434581 42161395
Hypertension 666.09 19.27 645 24714 166559 42429417
Disease progression 652.12 19.27 596 24763 143060 42452916
Death 503.78 19.27 954 24405 470231 42125745
Palmar-plantar erythrodysaesthesia syndrome 434.36 19.27 222 25137 20360 42575616
Decreased appetite 400.10 19.27 531 24828 192606 42403370
Blood pressure increased 393.02 19.27 387 24972 101541 42494435
Stomatitis 275.80 19.27 233 25126 50096 42545880
Oral pain 226.12 19.27 122 25237 12474 42583502
Aphonia 221.17 19.27 86 25273 4103 42591873
Drug ineffective 201.53 19.27 63 25296 630134 41965842
Hypothyroidism 178.65 19.27 150 25209 31934 42564042
Glossodynia 166.65 19.27 70 25289 4082 42591894
Weight decreased 141.86 19.27 353 25006 207595 42388381
Nausea 105.91 19.27 491 24868 396308 42199668
Proteinuria 101.01 19.27 94 25265 22889 42573087
Blister 97.55 19.27 100 25259 27390 42568586
Dry skin 84.68 19.27 123 25236 48215 42547761
Immune-mediated hepatic disorder 83.23 19.27 37 25322 2477 42593499
Febrile neutropenia 81.69 19.27 8 25351 185695 42410281
Neutropenia 79.39 19.27 12 25347 199419 42396557
Product dose omission in error 70.44 19.27 50 25309 8304 42587672
Drug interaction 69.72 19.27 36 25323 266963 42329013
Constipation 68.29 19.27 232 25127 162059 42433917
Second primary malignancy 66.52 19.27 51 25308 9524 42586452
Dry mouth 66.26 19.27 99 25260 39780 42556196
Asthenia 65.70 19.27 335 25024 280458 42315518
Oral discomfort 65.31 19.27 33 25326 2944 42593032
Thyroid disorder 64.62 19.27 36 25323 3914 42592062
Taste disorder 63.64 19.27 51 25308 10156 42585820
Blood pressure abnormal 58.21 19.27 48 25311 9950 42586026
Malignant neoplasm progression 57.54 19.27 168 25191 108232 42487744
Pain in extremity 57.04 19.27 208 25151 150396 42445580
Immune-mediated myocarditis 56.82 19.27 27 25332 2107 42593869
Toxicity to various agents 53.94 19.27 35 25324 229101 42366875
Overdose 50.59 19.27 3 25356 105261 42490715
Anaemia 48.81 19.27 57 25302 280221 42315755
Nephrectomy 45.68 19.27 18 25341 889 42595087
Product dose omission issue 44.63 19.27 196 25163 154169 42441807
Off label use 43.61 19.27 574 24785 637761 41958215
Pancytopenia 42.66 19.27 9 25350 117734 42478242
Headache 42.27 19.27 265 25094 239104 42356872
Pneumonia 40.68 19.27 123 25236 422026 42173950
Tongue discomfort 38.87 19.27 15 25344 700 42595276
Adrenal insufficiency 38.85 19.27 52 25307 18872 42577104
Body surface area decreased 38.79 19.27 7 25352 10 42595966
Blood thyroid stimulating hormone increased 38.55 19.27 29 25330 5263 42590713
Thrombocytopenia 36.08 19.27 36 25323 190243 42405733
Dehydration 35.78 19.27 173 25186 141594 42454382
Hyperkeratosis 33.25 19.27 25 25334 4533 42591443
Oropharyngeal pain 32.96 19.27 76 25283 42434 42553542
Thyroid function test abnormal 32.22 19.27 13 25346 683 42595293
Thyroiditis 31.11 19.27 21 25338 3215 42592761
Abdominal discomfort 31.07 19.27 107 25252 75148 42520828
Hepatic function abnormal 29.34 19.27 82 25277 51485 42544491
Arthralgia 28.91 19.27 215 25144 205023 42390953
Abdominal pain upper 28.65 19.27 111 25248 82498 42513478
Oral mucosal blistering 28.37 19.27 18 25341 2483 42593493
Nephritis 28.13 19.27 21 25338 3768 42592208
Cardiac arrest 28.09 19.27 15 25344 109305 42486671
Agitation 27.65 19.27 3 25356 64311 42531665
Ageusia 27.12 19.27 34 25325 11571 42584405
Therapy interrupted 27.09 19.27 48 25311 22202 42573774
Osteonecrosis of jaw 27.04 19.27 44 25315 19005 42576971
Multiple organ dysfunction syndrome 25.39 19.27 13 25346 97022 42498954
Condition aggravated 25.03 19.27 76 25283 260678 42335298
Drug hypersensitivity 25.00 19.27 14 25345 99375 42496601
Sepsis 24.65 19.27 51 25308 199283 42396693
Respiratory failure 24.55 19.27 24 25335 128108 42467868
Tachycardia 24.36 19.27 15 25344 101072 42494904
Asthma 24.19 19.27 4 25355 62310 42533666
Protein urine present 24.08 19.27 23 25336 5778 42590198
Pyrexia 24.03 19.27 137 25222 393905 42202071
Hepatic enzyme increased 22.40 19.27 69 25290 45715 42550261
Illness 22.06 19.27 47 25312 24883 42571093
Hyperaesthesia 21.73 19.27 22 25337 5930 42590046
Skin exfoliation 21.63 19.27 64 25295 41489 42554487
Tremor 21.19 19.27 16 25343 96913 42499063
Hypoxia 20.37 19.27 8 25351 69778 42526198
Hyperthyroidism 20.18 19.27 33 25326 14308 42581668
Renal impairment 20.00 19.27 123 25236 110105 42485871
Coronary artery disease 19.67 19.27 4 25355 53716 42542260
Rhabdomyolysis 19.61 19.27 11 25348 78008 42517968
Hepatotoxicity 19.51 19.27 45 25314 25122 42570854
Therapy non-responder 19.48 19.27 4 25355 53355 42542621
Incorrect dose administered 19.28 19.27 4 25355 52970 42543006

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
Neoplasm progression 2185.06 20.25 802 33544 63793 110491160
Dysphonia 1561.80 20.25 658 33688 75271 110479682
Diarrhoea 1311.98 20.25 1677 32669 1137828 109417125
Death 1038.36 20.25 1174 33172 697695 109857258
Disease progression 942.17 20.25 702 33644 243332 110311621
Fatigue 857.25 20.25 1422 32924 1214536 109340417
Hypertension 784.61 20.25 874 33472 509210 110045743
Palmar-plantar erythrodysaesthesia syndrome 671.15 20.25 303 34043 40722 110514231
Decreased appetite 587.18 20.25 729 33617 475117 110079836
Blood pressure increased 574.77 20.25 541 33805 257832 110297121
Oral pain 325.14 20.25 180 34166 37264 110517689
Hypothyroidism 317.22 20.25 226 34120 72673 110482280
Stomatitis 264.03 20.25 370 33976 269872 110285081
Drug ineffective 256.06 20.25 78 34268 1520462 109034491
Aphonia 232.63 20.25 102 34244 12758 110542195
Weight decreased 230.82 20.25 472 33874 467585 110087368
Proteinuria 149.01 20.25 113 34233 39905 110515048
Nausea 146.54 20.25 762 33584 1234928 109320025
Constipation 135.59 20.25 325 34021 357461 110197492
Immune-mediated hepatic disorder 134.44 20.25 51 34295 4399 110550554
Dry skin 119.48 20.25 157 34189 107496 110447457
Malignant neoplasm progression 118.23 20.25 202 34144 174365 110380588
Asthenia 116.35 20.25 472 33874 688527 109866426
Second primary malignancy 102.35 20.25 66 34280 18002 110536951
Off label use 101.16 20.25 802 33544 1499383 109055570
Thyroid disorder 98.63 20.25 63 34283 16906 110538047
Product dose omission issue 93.76 20.25 265 34081 321517 110233436
Drug hypersensitivity 92.65 20.25 15 34331 454075 110100878
Dehydration 92.24 20.25 241 34105 279270 110275683
Product dose omission in error 91.09 20.25 68 34278 23444 110531509
Oral discomfort 88.99 20.25 51 34295 11260 110543693
Blood pressure abnormal 76.22 20.25 60 34286 22364 110532589
Immune-mediated myocarditis 73.99 20.25 31 34315 3467 110551486
Nephrectomy 71.69 20.25 28 34318 2612 110552341
Febrile neutropenia 70.42 20.25 8 34338 316759 110238194
Hepatic function abnormal 63.95 20.25 106 34240 89189 110465764
Wheezing 63.40 20.25 4 34342 255226 110299727
Hyperkeratosis 63.06 20.25 38 34308 9201 110545752
Joint swelling 62.02 20.25 30 34316 442815 110112138
Blood thyroid stimulating hormone increased 60.14 20.25 41 34305 12260 110542693
Arthropathy 59.74 20.25 9 34337 287513 110267440
Treatment failure 56.86 20.25 9 34337 277225 110277728
Thyroiditis 55.39 20.25 31 34315 6542 110548411
Asthma 53.96 20.25 7 34339 250284 110304669
Sinusitis 53.78 20.25 13 34333 296675 110258278
Adrenal insufficiency 53.60 20.25 66 34280 42324 110512629
Drug interaction 53.54 20.25 46 34300 500137 110054816
Neutropenia 51.51 20.25 26 34320 374594 110180359
Body surface area decreased 51.48 20.25 10 34336 59 110554894
Renal impairment 49.82 20.25 150 34196 188295 110366658
Overdose 49.30 20.25 7 34339 233787 110321166
Toxicity to various agents 49.26 20.25 46 34300 480509 110074444
Condition aggravated 48.48 20.25 97 34249 734739 109820214
Rheumatoid arthritis 47.24 20.25 17 34329 299596 110255357
Feeding disorder 45.90 20.25 44 34302 21318 110533635
Pain in extremity 45.78 20.25 283 34063 486835 110068118
Oral mucosal blistering 44.97 20.25 29 34317 7905 110547048
Posterior reversible encephalopathy syndrome 44.89 20.25 54 34292 33807 110521146
Hypersensitivity 44.64 20.25 36 34310 403962 110150991
Tongue discomfort 42.99 20.25 20 34326 2868 110552085
Pancytopenia 42.54 20.25 7 34339 209606 110345347
Osteoarthritis 42.15 20.25 4 34342 182619 110372334
Myocarditis 41.61 20.25 49 34297 30006 110524947
Skin exfoliation 41.36 20.25 87 34259 87564 110467389
Pericarditis 40.89 20.25 9 34337 219105 110335848
Dry mouth 39.31 20.25 144 34202 199804 110355149
Drug intolerance 38.13 20.25 42 34304 406470 110148483
Lower respiratory tract infection 37.97 20.25 14 34332 243092 110311861
Hyperthyroidism 37.71 20.25 46 34300 29215 110525738
Polycythaemia 37.64 20.25 19 34327 3256 110551697
Ageusia 37.62 20.25 38 34308 19607 110535346
Therapy non-responder 37.52 20.25 3 34343 157304 110397649
Protein urine present 37.46 20.25 30 34316 11454 110543499
Infusion related reaction 37.29 20.25 38 34308 381124 110173829
Irritable bowel syndrome 36.85 20.25 4 34342 164211 110390742
Weight increased 35.50 20.25 47 34299 419597 110135356
Pneumonia 34.90 20.25 147 34199 876567 109678386
Urticaria 34.49 20.25 29 34317 318828 110236125
Osteonecrosis of jaw 34.37 20.25 57 34289 47960 110506993
Renal cancer 34.15 20.25 30 34316 13004 110541949
Discomfort 34.15 20.25 12 34334 214695 110340258
Nasopharyngitis 33.52 20.25 44 34302 394317 110160636
Nephrotic syndrome 32.61 20.25 30 34316 13801 110541152
Leukopenia 32.45 20.25 4 34342 148787 110406166
Renal cell carcinoma 31.92 20.25 23 34323 7507 110547446
Myalgia 31.69 20.25 145 34201 222236 110332717
Thyroid function test abnormal 31.45 20.25 17 34329 3350 110551603
Hospice care 31.27 20.25 28 34318 12445 110542508
Taste disorder 30.96 20.25 65 34281 65322 110489631
Blister 30.02 20.25 145 34201 227231 110327722
Wound 29.70 20.25 18 34328 234419 110320534
Eating disorder 29.66 20.25 42 34304 30816 110524137
Depression 29.51 20.25 33 34313 317302 110237651
Dysgeusia 29.07 20.25 66 34280 69919 110485034
Swelling 28.99 20.25 40 34306 351001 110203952
Intentional product use issue 28.76 20.25 21 34325 247885 110307068
Oropharyngeal pain 27.92 20.25 99 34247 135177 110419776
Speech disorder 27.76 20.25 60 34286 61509 110493444
Blood corticotrophin increased 27.43 20.25 8 34338 303 110554650
Cancer pain 27.15 20.25 20 34326 6752 110548201
Blood cholesterol increased 26.64 20.25 12 34334 184773 110370180
Musculoskeletal stiffness 26.13 20.25 29 34317 279793 110275160
Type 1 diabetes mellitus 26.09 20.25 22 34324 9025 110545928
Hyperaesthesia 25.52 20.25 27 34319 14700 110540253
Immune-mediated hepatitis 25.08 20.25 19 34327 6692 110548261
Injury 24.80 20.25 12 34334 177253 110377700
Metastatic renal cell carcinoma 24.51 20.25 13 34333 2467 110552486
Pyrexia 24.45 20.25 171 34175 898094 109656859
Oligodipsia 24.41 20.25 5 34341 40 110554913
Oedema 24.07 20.25 18 34328 209958 110344995
Illness 23.22 20.25 67 34279 82104 110472849
Bronchitis 22.95 20.25 10 34336 157022 110397931
Ill-defined disorder 22.90 20.25 10 34336 156843 110398110
Tachycardia 22.84 20.25 22 34324 226623 110328330
Anaphylactic reaction 22.78 20.25 4 34342 114296 110440657
Immune-mediated hypothyroidism 22.71 20.25 13 34333 2862 110552091
Medication error 22.57 20.25 3 34343 105363 110449590
Agitation 22.44 20.25 4 34342 113047 110441906
Nephritis 22.14 20.25 17 34329 6109 110548844
Glossitis 22.00 20.25 15 34331 4486 110550467
Cardiac dysfunction 21.90 20.25 17 34329 6206 110548747
Hepatic cytolysis 21.85 20.25 51 34295 55002 110499951
Mobility decreased 21.73 20.25 25 34321 237397 110317556
Liver injury 21.32 20.25 10 34336 150403 110404550
Gastrointestinal perforation 21.23 20.25 18 34328 7438 110547515
Cardiac arrest 21.13 20.25 18 34328 196735 110358218
Dental care 20.87 20.25 9 34337 1080 110553873
Alopecia 20.85 20.25 52 34294 364701 110190252
Angioedema 20.64 20.25 3 34343 98497 110456456
Immune-mediated renal disorder 20.56 20.25 8 34338 739 110554214
Inflammation 20.36 20.25 18 34328 193220 110361733

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EK01 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitors
FDA MoA N0000020000 Receptor Tyrosine Kinase Inhibitors
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D047428 Protein Kinase Inhibitors
FDA EPC N0000175605 Kinase Inhibitor
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:38637 tyrosine kinase inhibitor
CHEBI has role CHEBI:65207 vascular endothelial growth factor receptor antagonist

Related Drugs by ATC class:

L01EK Vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitors 3 drugs
apatinibfruquintinibtivozanib

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

DiseaseRelationSNOMED_IDDOID
Renal cell carcinoma indication 702391001 DOID:4450




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.57 acidic
pKa2 12.18 acidic
pKa3 4.85 Basic
pKa4 1.98 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
1MG INLYTA PF PRISM CV N202324 Jan. 27, 2012 RX TABLET ORAL 10570202 Feb. 3, 2035 IN COMBINATION WITH PEMBROLIZUMAB FOR THE FIRST-LINE TREATMENT OF PATIENTS WITH ADVANCED RENAL CELL CARCINOMA
1MG INLYTA PF PRISM CV N202324 Jan. 27, 2012 RX TABLET ORAL 12534530 Feb. 3, 2035 A FIRST-LINE METHOD OF TREATING ADVANCED RENAL CELL CARCINOMA IN AN INDIVIDUAL BY ADMINISTERING AXITINIB AT A STARTING DOSE OF 5 MG TWICE DAILY IN COMBINATION WITH PEMBROLIZUMAB, WHERE THE AXITINIB DOSE IS INCREASED AS CLAIMED
1MG INLYTA PF PRISM CV N202324 Jan. 27, 2012 RX TABLET ORAL 12534530 Feb. 3, 2035 A FIRST-LINE METHOD OF TREATING ADVANCED RENAL CELL CARCINOMA IN AN INDIVIDUAL BY ADMINISTERING AXITINIB AT A STARTING DOSE OF 5 MG TWICE DAILY IN COMBINATION WITH PEMBROLIZUMAB, WHERE THE AXITINIB DOSE IS REDUCED AS CLAIMED
5MG INLYTA PF PRISM CV N202324 Jan. 27, 2012 RX TABLET ORAL 10570202 Feb. 3, 2035 IN COMBINATION WITH PEMBROLIZUMAB FOR THE FIRST-LINE TREATMENT OF PATIENTS WITH ADVANCED RENAL CELL CARCINOMA
5MG INLYTA PF PRISM CV N202324 Jan. 27, 2012 RX TABLET ORAL 12534530 Feb. 3, 2035 A FIRST-LINE METHOD OF TREATING ADVANCED RENAL CELL CARCINOMA IN AN INDIVIDUAL BY ADMINISTERING AXITINIB AT A STARTING DOSE OF 5 MG TWICE DAILY IN COMBINATION WITH PEMBROLIZUMAB, WHERE THE AXITINIB DOSE IS INCREASED AS CLAIMED
5MG INLYTA PF PRISM CV N202324 Jan. 27, 2012 RX TABLET ORAL 12534530 Feb. 3, 2035 A FIRST-LINE METHOD OF TREATING ADVANCED RENAL CELL CARCINOMA IN AN INDIVIDUAL BY ADMINISTERING AXITINIB AT A STARTING DOSE OF 5 MG TWICE DAILY IN COMBINATION WITH PEMBROLIZUMAB, WHERE THE AXITINIB DOSE IS REDUCED AS CLAIMED
1MG INLYTA PF PRISM CV N202324 Jan. 27, 2012 RX TABLET ORAL 10869924 Jan. 12, 2037 AXITINIB IN COMBINATION WITH AVELUMAB FOR THE FIRST-LINE TREATMENT OF PATIENTS WITH ADVANCED RENAL CELL CARCINOMA
5MG INLYTA PF PRISM CV N202324 Jan. 27, 2012 RX TABLET ORAL 10869924 Jan. 12, 2037 AXITINIB IN COMBINATION WITH AVELUMAB FOR THE FIRST-LINE TREATMENT OF PATIENTS WITH ADVANCED RENAL CELL CARCINOMA

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Vascular endothelial growth factor receptor 2 Kinase INHIBITOR Kd 8.23 CHEMBL CHEMBL
Vascular endothelial growth factor receptor 3 Kinase INHIBITOR Kd 6.77 CHEMBL CHEMBL
Vascular endothelial growth factor receptor 1 Kinase INHIBITOR Kd 8.24 CHEMBL CHEMBL
Mast/stem cell growth factor receptor Kit Kinase Kd 9.31 CHEMBL
Epidermal growth factor receptor Kinase Kd 5.64 CHEMBL
Breakpoint cluster region protein Kinase Kd 6.73 CHEMBL
Tyrosine-protein kinase Lck Kinase Kd 5.57 CHEMBL
Tyrosine-protein kinase Yes Kinase Kd 5.57 CHEMBL
Receptor-type tyrosine-protein kinase FLT3 Kinase Kd 7.51 CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret Kinase Kd 7 CHEMBL
Macrophage colony-stimulating factor 1 receptor Kinase Kd 7.68 CHEMBL
Platelet-derived growth factor receptor alpha Kinase Kd 9.29 CHEMBL
Histone deacetylase 6 Enzyme IC50 6.39 CHEMBL
Mitogen-activated protein kinase 8 Kinase Kd 5.41 CHEMBL
Fibroblast growth factor receptor 3 Kinase Kd 6.68 CHEMBL
Mitogen-activated protein kinase 10 Kinase Kd 5.96 CHEMBL
High affinity nerve growth factor receptor Kinase Kd 5.74 CHEMBL
Tyrosine-protein kinase JAK2 Kinase Kd 5.48 CHEMBL
Myosin light chain kinase 2, skeletal/cardiac muscle Kinase Kd 5.89 CHEMBL
Tyrosine-protein kinase CSK Kinase Kd 5.96 CHEMBL
Angiopoietin-1 receptor Kinase Kd 6.51 CHEMBL
AP2-associated protein kinase 1 Kinase Kd 5.92 CHEMBL
Hepatocyte growth factor receptor Kinase Kd 6.09 CHEMBL
Fibroblast growth factor receptor 1 Kinase Kd 6.42 CHEMBL
Serine/threonine-protein kinase 10 Kinase Kd 5.92 CHEMBL
Serine/threonine-protein kinase PLK4 Kinase Ki 8.38 CHEMBL
Aurora kinase C Kinase Kd 8.89 CHEMBL
Serine/threonine-protein kinase 16 Kinase Kd 6.43 CHEMBL
Dual specificity protein kinase TTK Kinase Kd 5.41 CHEMBL
Abelson tyrosine-protein kinase 2 Kinase Kd 7.15 CHEMBL
Fibroblast growth factor receptor 2 Kinase Kd 6.96 CHEMBL
TRAF2 and NCK-interacting protein kinase Kinase Kd 6.74 CHEMBL
Tyrosine-protein kinase Fgr Kinase Kd 5.74 CHEMBL
Aurora kinase A Kinase Kd 7.14 CHEMBL
BMP-2-inducible protein kinase Kinase Kd 6 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 5 Kinase Kd 6.26 CHEMBL
Mitogen-activated protein kinase kinase kinase 4 Kinase Kd 5.25 CHEMBL
Cyclin-G-associated kinase Kinase Kd 5.57 CHEMBL
Receptor-interacting serine/threonine-protein kinase 2 Kinase Kd 5 CHEMBL
Cyclin-dependent kinase 16 Kinase Kd 5.28 CHEMBL
Serine/threonine-protein kinase 4 Kinase Kd 5.85 CHEMBL
Activated CDC42 kinase 1 Kinase Kd 5.22 CHEMBL
STE20-like serine/threonine-protein kinase Kinase Kd 6 CHEMBL
Calcium/calmodulin-dependent protein kinase kinase 2 Kinase Kd 5.82 CHEMBL
Calcium/calmodulin-dependent protein kinase kinase 1 Kinase Kd 5.85 CHEMBL
Epithelial discoidin domain-containing receptor 1 Kinase Kd 6.47 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 1 Kinase Kd 5.57 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 2 Kinase Kd 5.59 CHEMBL
Tyrosine-protein kinase ITK/TSK Kinase Kd 5.92 CHEMBL
Tyrosine-protein kinase receptor UFO Kinase Kd 6.38 CHEMBL
Serine/threonine-protein kinase N2 Kinase Kd 5.57 CHEMBL
Serine/threonine-protein kinase 3 Kinase Kd 5.66 CHEMBL
NUAK family SNF1-like kinase 2 Kinase Kd 5.89 CHEMBL
Non-receptor tyrosine-protein kinase TNK1 Kinase Kd 6.80 CHEMBL
Non-receptor tyrosine-protein kinase TYK2 Kinase Kd 5.44 CHEMBL
Mitogen-activated protein kinase kinase kinase MLT Kinase Kd 5.59 CHEMBL
Serine/threonine-protein kinase RIO1 Kinase Kd 5.92 CHEMBL
Tyrosine-protein kinase receptor Tie-1 Kinase Kd 7.01 CHEMBL
Tyrosine-protein kinase TXK Kinase Kd 5.62 CHEMBL
Casein kinase II subunit alpha' Kinase Kd 5.55 CHEMBL
Serine/threonine-protein kinase RIO3 Kinase Kd 6 CHEMBL
SRSF protein kinase 1 Kinase Kd 5.74 CHEMBL
Activin receptor type-2B Kinase Kd 5.28 CHEMBL
Ankyrin repeat and protein kinase domain-containing protein 1 Kinase Kd 5.44 CHEMBL
Discoidin domain-containing receptor 2 Kinase Kd 5.28 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 1 Kinase Kd 6.48 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 3 Kinase Kd 5.92 CHEMBL
Aurora kinase B Kinase Kd 7.96 CHEMBL
Tyrosine-protein kinase Blk Kinase Kd 5.51 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 4 Kinase Kd 6.46 CHEMBL
Tyrosine-protein kinase Mer Kinase Kd 5.49 CHEMBL
Mitogen-activated protein kinase kinase kinase 9 Kinase Kd 5.52 CHEMBL
Serine/threonine-protein kinase MRCK beta Kinase Kd 5.32 CHEMBL
Myosin-IIIa Kinase Kd 5.72 CHEMBL
Serine/threonine-protein kinase PAK 4 Kinase Kd 5.35 CHEMBL
Serine/threonine-protein kinase SIK1 Kinase Kd 5.68 CHEMBL
Dual specificity testis-specific protein kinase 1 Kinase Kd 5.37 CHEMBL
Interferon-induced, double-stranded RNA-activated protein kinase Kinase Kd 5.13 CHEMBL
Receptor-interacting serine/threonine-protein kinase 1 Kinase Kd 5.60 CHEMBL
Proto-oncogene tyrosine-protein kinase ROS Kinase Kd 5.49 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 2 Kinase Kd 5.89 CHEMBL
Misshapen-like kinase 1 Kinase Kd 6.25 CHEMBL
Cyclin-dependent kinase-like 2 Kinase Kd 6.28 CHEMBL
Protein delta homolog 1 Membrane other Kd 5.77 CHEMBL
Ephrin type-B receptor 6 Kinase Kd 6.44 CHEMBL
G protein-coupled receptor kinase 4 Kinase Kd 5.64 CHEMBL
Hormonally up-regulated neu tumor-associated kinase Kinase Kd 5.82 CHEMBL
Interleukin-1 receptor-associated kinase 1 Kinase Kd 5.51 CHEMBL
Mitogen-activated protein kinase kinase kinase 3 Kinase Kd 5.55 CHEMBL
SRSF protein kinase 3 Kinase Kd 5.64 CHEMBL
Serine/threonine-protein kinase ULK2 Kinase Kd 5 CHEMBL
Serine/threonine-protein kinase ULK3 Kinase Kd 6.17 CHEMBL
Mitogen-activated protein kinase kinase kinase 19 Kinase Kd 6.57 CHEMBL
Receptor-interacting serine/threonine-protein kinase 4 Kinase Kd 5.85 CHEMBL
Bone morphogenetic protein receptor type-1B Kinase Kd 5.54 CHEMBL
Mitogen-activated protein kinase kinase kinase 12 Kinase Kd 5.77 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 5 Kinase Kd 6.85 CHEMBL
Myosin light chain kinase 3 Kinase Kd 5.77 CHEMBL
Leucine-rich repeat serine/threonine-protein kinase 2 Kinase Kd 6.04 CHEMBL
Ferrochelatase, mitochondrial Enzyme Kd 5.17 CHEMBL
Tyrosine-protein kinase JAK3 Kinase Kd 5.51 CHEMBL
Uncharacterized protein FLJ45252 Unclassified Kd 5.64 CHEMBL
Platelet-derived growth factor receptor beta Kinase Kd 9.24 CHEMBL
Tyrosine-protein kinase ABL1 Kinase Kd 8.82 CHEMBL

External reference:

IDSource
4031332 VUID
N0000184323 NUI
D03218 KEGG_DRUG
4031332 VANDF
C1700874 UMLSCUI
CHEBI:66910 CHEBI
AXI PDB_CHEM_ID
CHEMBL1289926 ChEMBL_ID
D000077784 MESH_DESCRIPTOR_UI
DB06626 DRUGBANK_ID
5659 IUPHAR_LIGAND_ID
8720 INN_ID
C9LVQ0YUXG UNII
6450551 PUBCHEM_CID
1242999 RXNORM
187097 MMSL
28294 MMSL
d07823 MMSL
014143 NDDF
427882000 SNOMEDCT_US
429507005 SNOMEDCT_US
C9LVQ0YUXG INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
INLYTA HUMAN PRESCRIPTION DRUG LABEL 1 0069-0145 TABLET, FILM COATED 1 mg ORAL NDA 29 sections
INLYTA HUMAN PRESCRIPTION DRUG LABEL 1 0069-0151 TABLET, FILM COATED 5 mg ORAL NDA 29 sections
INLYTA HUMAN PRESCRIPTION DRUG LABEL 1 63539-026 TABLET, FILM COATED 1 mg ORAL NDA 29 sections
INLYTA HUMAN PRESCRIPTION DRUG LABEL 1 63539-044 TABLET, FILM COATED 5 mg ORAL NDA 29 sections