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

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 1045 183321-74-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • erlotinib hydrochloride
  • tarceva
  • erlotinib
  • CP-358,774-01
  • OSI-774
  • erlotinib HCl
A quinazoline derivative and ANTINEOPLASTIC AGENT that functions as a PROTEIN KINASE INHIBITOR for EGFR associated tyrosine kinase. It is used in the treatment of NON-SMALL CELL LUNG CANCER.
  • Molecular weight: 393.44
  • Formula: C22H23N3O4
  • CLOGP: 4.19
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 1
  • TPSA: 74.73
  • ALOGS: -4.64
  • ROTB: 10
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.15 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.00 mg/mL Bocci G, Oprea TI, Benet LZ
EoM (Fraction excreted unchanged in urine) 0.30 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 5.45 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 59 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.77 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 1.69 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.07 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 6.50 hours Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 3.294 Moderate 0.69
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.800 Moderate 0.69
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 62.230 10^-6 cm/s Moderate 0.69
dh-clint Dog hepatocyte intrinsic clearance 8.110 uL/min/10^6 cells Moderate 0.69
dppb Dog plasma protein binding (% unbound) 10.890 % Moderate 0.69
fcs-ppb Fetal calf serum protein binding (% unbound) 31.470 % Moderate 0.69
herg hERG pIC50 4.974 pIC50 Moderate 0.69
hh-clint Human hepatocyte intrinsic clearance 2.917 uL/min/10^6 cells Moderate 0.69
hlm-clint Human liver microsomal intrinsic clearance 25.942 uL/min/mg protein Moderate 0.69
hppb Human plasma protein binding (% unbound) 7.100 % Moderate 0.69
kinase-safety-class ABL1,ABL2,ACVR2A,ACVR2B,AKT2,AKT3,ALK,AURKA,AURKB,AXL,BLK,BMX,BRAF,CAMK2B,CAMK2D,CDK5,CDK9,CHEK1,CSF1R,CSK,DDR1,DYRK1B,EGFR,EIF2AK3,EPHA2,EPHB1,EPHB4,ERBB2,ERBB4,FGFR1,FLT1,FLT3,FLT4,FYN,GAK,GRK2,GSK3B,INSR,IRAK1,IRAK3,IRAK4,ITK,JAK1,JAK2,KDR,KIT,LCK,LYN,MAP2K1,MAP3K1,MAP3K10,MAP3K21,MAP3K7,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK10,MAPK11,MAPK12,MAPK14,MAPK7,MAPKAPK2,MARK4,MET,MKNK1,MKNK2,MTOR,NTRK1,NTRK2,PAK4,PDGFRB,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PRKCD,PRKDC,PTK6,RET,RIPK3,SIK2,SIK3,SRC,STK10,STK33,SYK,TEK,TNIK,TTK,TYRO3,ULK1,YES1 95
kinase-selectivity-class ALK,AURKA,AXL,BRAF,CAMK2B,CAMK2D,CDK9,CSF1R,DDR1,DYRK1B,EGFR,EPHA2,EPHB4,ERBB2,ERBB4,FLT3,FYN,IRAK3,JAK1,KDR,KIT,LYN,MAP3K10,MAP3K21,MAP4K1,MAP4K3,MAPK7,MET,PDK4,PRKCD,RET,SIK2,SIK3,STK10,STK33,SYK,ULK1,YES1 38
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 5.610 High 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 4.198 Moderate 0.69
mh-clint Mouse hepatocyte intrinsic clearance 18.836 Moderate 0.69
mppb Mouse plasma protein binding (% unbound) 6.050 Moderate 0.69
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 7.638 Moderate 0.69
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 1 High 1
pppb Pig plasma protein binding (% unbound) 17.280 % Moderate 0.69
rat-kpuu-brain Rat brain Kpuu 0.144 % High 1
rh-clint Rat hepatocyte intrinsic clearance 8.995 uL/min/10^6 cells Moderate 0.69
rh-fuinc Rat hepatocyte fraction unbound in incubation 55.500 % Moderate 0.69
rppb Rat plasma protein binding (% unbound) 6.460 % Moderate 0.69
solubility-dd Solubility at pH 7.4 in DMSO 14.322 uM Moderate 0.69

Approvals:

DateAgencyCompanyOrphan
Nov. 18, 2004 FDA OSI PHARMS
Sept. 19, 2005 EMA ROCHE REGISTRATION GMBH

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
Death 784.93 22.28 620 13999 455931 90157897
Disease progression 718.28 22.28 394 14225 156221 90457607
Diarrhoea 519.32 22.28 691 13928 938499 89675329
Rash 483.38 22.28 614 14005 795486 89818342
Malignant neoplasm progression 467.51 22.28 261 14358 106609 90507219
Drug resistance 441.92 22.28 171 14448 30278 90583550
Dermatitis acneiform 410.46 22.28 111 14508 6243 90607585
Dry skin 181.41 22.28 134 14485 87939 90525889
Paronychia 171.73 22.28 60 14559 7946 90605882
Neoplasm malignant 151.20 22.28 84 14535 33796 90580032
Metastases to central nervous system 148.00 22.28 67 14552 17475 90596353
EGFR gene mutation 139.67 22.28 27 14592 323 90613505
Acquired gene mutation 124.62 22.28 31 14588 1248 90612580
Incorrect dose administered 104.88 22.28 93 14526 78837 90534991
Rash pustular 98.46 22.28 40 14579 8009 90605819
Acne 96.26 22.28 59 14560 28448 90585380
Dehydration 86.54 22.28 130 14489 194317 90419511
Malignant transformation 81.36 22.28 19 14600 583 90613245
Erythema dyschromicum perstans 76.60 22.28 13 14606 69 90613759
Pleural effusion 76.01 22.28 92 14527 111899 90501929
Decreased appetite 75.69 22.28 179 14440 376361 90237467
Metastases to lung 66.84 22.28 38 14581 15953 90597875
Growth of eyelashes 62.99 22.28 13 14606 221 90613607
Metastases to meninges 57.77 22.28 22 14597 3713 90610115
Neoplasm progression 54.30 22.28 50 14569 44436 90569392
Multiple-drug resistance 54.09 22.28 26 14593 7750 90606078
Joint swelling 52.57 22.28 9 14610 503291 90110537
Nausea 52.19 22.28 331 14288 1109985 89503843
Naevoid melanoma 51.63 22.28 7 14612 3 90613825
Malignant pleural effusion 51.45 22.28 19 14600 2945 90610883
Non-small cell lung cancer 50.95 22.28 21 14598 4360 90609468
Therapy partial responder 48.63 22.28 35 14584 22008 90591820
Lung cancer metastatic 48.11 22.28 18 14601 2893 90610935
Skin fissures 48.11 22.28 34 14585 20775 90593053
Hair growth abnormal 47.48 22.28 19 14600 3657 90610171
Drug hypersensitivity 46.88 22.28 9 14610 463600 90150228
Non-small cell lung cancer metastatic 46.81 22.28 13 14606 805 90613023
Hair texture abnormal 46.28 22.28 20 14599 4667 90609161
Metastases to bone 46.24 22.28 36 14583 25469 90588359
Pulmonary embolism 45.19 22.28 78 14541 130742 90483086
Skin toxicity 42.17 22.28 21 14598 6758 90607070
Alopecia scarring 41.54 22.28 9 14610 195 90613633
Pneumonitis 41.47 22.28 43 14576 44127 90569701
Anaemia 41.38 22.28 138 14481 352664 90261164
Arthralgia 41.23 22.28 39 14580 778483 89835345
Trichiasis 39.89 22.28 8 14611 117 90613711
Lung neoplasm malignant 39.17 22.28 32 14587 24241 90589587
Condition aggravated 38.96 22.28 24 14595 595521 90018307
Xerosis 38.95 22.28 13 14606 1498 90612330
Sinusitis 38.41 22.28 5 14614 343083 90270745
Glossodynia 37.73 22.28 4 14615 321775 90292053
Pancreatic carcinoma metastatic 36.69 22.28 14 14605 2374 90611454
Wound 34.93 22.28 4 14615 302976 90310852
Onychoclasis 34.79 22.28 19 14600 7380 90606448
Blepharitis 32.93 22.28 15 14604 3961 90609867
Vomiting 32.64 22.28 228 14391 788065 89825763
Skin exfoliation 32.45 22.28 47 14572 67866 90545962
Metastasis 32.34 22.28 17 14602 6120 90607708
Pyogenic granuloma 32.23 22.28 8 14611 319 90613509
Ulcerative keratitis 31.70 22.28 14 14605 3439 90610389
Corneal disorder 31.48 22.28 12 14607 2030 90611798
Discomfort 30.69 22.28 4 14615 274331 90339497
Metastases to liver 30.62 22.28 30 14589 28777 90585051
Fatigue 30.26 22.28 301 14318 1153722 89460106
Weight increased 29.97 22.28 15 14604 417912 90195916
Nasopharyngitis 28.61 22.28 15 14604 407089 90206739
Asthma 28.41 22.28 3 14616 242157 90371671
Corneal perforation 27.25 22.28 8 14611 605 90613223
Swelling 27.22 22.28 17 14602 419041 90194787
Non-small cell lung cancer stage IV 26.68 22.28 6 14613 155 90613673
Dysphagia 26.52 22.28 57 14562 112221 90501607
Asthenia 26.06 22.28 161 14458 533590 90080238
Epistaxis 25.85 22.28 48 14571 85077 90528751
Lung adenocarcinoma 25.36 22.28 14 14605 5551 90608277
Hypersensitivity 24.94 22.28 22 14597 454655 90159173
Henoch-Schonlein purpura 23.08 22.28 9 14610 1618 90612210
Performance status decreased 22.96 22.28 12 14607 4268 90609560
Headache 22.64 22.28 68 14551 862678 89751150
Sarcomatoid carcinoma 22.49 22.28 4 14615 29 90613799
Pneumatosis intestinalis 22.42 22.28 11 14608 3426 90610402
Pneumothorax 22.33 22.28 21 14598 19146 90594682

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
Death 592.02 20.19 704 11829 470481 42138321
Disease progression 490.53 20.19 375 12158 143281 42465521
Rash 475.72 20.19 489 12044 276465 42332337
Dermatitis acneiform 232.56 20.19 87 12446 7652 42601150
Malignant neoplasm progression 211.50 20.19 206 12327 108194 42500608
Diarrhoea 176.86 20.19 405 12128 460444 42148358
Neoplasm malignant 166.76 20.19 96 12437 22647 42586155
Drug resistance 153.94 20.19 106 12427 34142 42574660
EGFR gene mutation 93.53 20.19 20 12513 214 42608588
Dehydration 90.75 20.19 155 12378 141612 42467190
Decreased appetite 68.24 20.19 165 12368 192972 42415830
Metastases to central nervous system 63.55 20.19 39 12494 10316 42598486
Incorrect dose administered 61.77 20.19 77 12456 52897 42555905
Acquired gene mutation 55.73 20.19 20 12513 1560 42607242
Non-small cell lung cancer metastatic 55.14 20.19 17 12516 826 42607976
Erythema dyschromicum perstans 54.51 20.19 8 12525 3 42608799
Pleural effusion 50.32 20.19 97 12436 97069 42511733
Vomiting 43.27 20.19 184 12349 289539 42319263
Paronychia 42.34 20.19 22 12511 4233 42604569
Interstitial lung disease 41.43 20.19 79 12454 78383 42530419
Skin toxicity 38.49 20.19 24 12509 6525 42602277
Neoplasm progression 36.78 20.19 44 12489 28956 42579846
Acne 36.43 20.19 31 12502 13613 42595189
Gastrointestinal perforation 35.71 20.19 20 12513 4466 42604336
Product use in unapproved indication 35.12 20.19 6 12527 184450 42424352
Pneumoperitoneum 34.79 20.19 16 12517 2362 42606440
Malignant pleural effusion 34.51 20.19 15 12518 1940 42606862
Metastases to meninges 34.46 20.19 15 12518 1946 42606856
Rash pustular 32.12 20.19 21 12512 6194 42602608
Pneumothorax 28.67 20.19 35 12498 23508 42585294
Metastases to lung 28.56 20.19 25 12508 11399 42597403
Metastases to liver 27.98 20.19 29 12504 16297 42592505
Nausea 27.53 20.19 205 12328 396594 42212208
Non-small cell lung cancer 26.17 20.19 17 12516 4957 42603845
Condition aggravated 26.10 20.19 23 12510 260731 42348071
Product dose omission issue 23.56 20.19 8 12525 154357 42454445
Metastases to bone 23.06 20.19 25 12508 14784 42594018
Lung adenocarcinoma 22.72 20.19 16 12517 5323 42603479
Failure to thrive 22.32 20.19 20 12513 9402 42599400
Pneumonitis 21.99 20.19 42 12491 41676 42567126
Toxicity to various agents 21.98 20.19 21 12512 229115 42379687
Anaemia 21.83 20.19 149 12384 280129 42328673
Blood bilirubin increased 21.62 20.19 42 12491 42210 42566592
Therapy partial responder 21.57 20.19 28 12505 19993 42588809
COVID-19 21.56 20.19 4 12529 115944 42492858
Growth of eyelashes 20.97 20.19 5 12528 90 42608712
Bronchial fistula 20.78 20.19 6 12527 232 42608570
Lung cancer metastatic 20.26 20.19 12 12521 2974 42605828

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
Disease progression 709.18 20.48 463 17946 243571 110327319
Malignant neoplasm progression 676.40 20.48 398 18011 174169 110396721
Drug resistance 624.75 20.48 263 18146 56111 110514779
Dermatitis acneiform 496.34 20.48 151 18258 12544 110558346
Rash 457.61 20.48 618 17791 820346 109750544
Diarrhoea 397.63 20.48 690 17719 1138815 109432075
Death 349.45 20.48 500 17909 698369 109872521
EGFR gene mutation 251.02 20.48 48 18361 522 110570368
Acquired gene mutation 175.77 20.48 48 18361 2706 110568184
Metastases to central nervous system 164.71 20.48 79 18330 22738 110548152
Dehydration 144.73 20.48 204 18205 279307 110291583
Paronychia 143.93 20.48 58 18351 11023 110559867
Erythema dyschromicum perstans 130.27 20.48 21 18388 73 110570817
Rash pustular 116.21 20.48 52 18357 12777 110558113
Metastases to meninges 99.59 20.48 36 18373 5092 110565798
Dry skin 95.24 20.48 103 18306 107550 110463340
Pleural effusion 89.35 20.48 128 18281 177581 110393309
Skin toxicity 85.64 20.48 41 18368 11742 110559148
Therapy partial responder 80.47 20.48 59 18350 37002 110533888
Decreased appetite 79.40 20.48 215 18194 475631 110095259
Malignant transformation 76.43 20.48 22 18387 1503 110569387
Metastases to lung 74.62 20.48 47 18362 23016 110547874
Interstitial lung disease 68.02 20.48 99 18310 139235 110431655
Neoplasm progression 64.59 20.48 66 18343 64529 110506361
Multiple-drug resistance 64.02 20.48 35 18374 13200 110557690
Non-small cell lung cancer metastatic 61.11 20.48 18 18391 1334 110569556
Acne 58.78 20.48 47 18362 33473 110537417
Pneumonitis 55.38 20.48 66 18343 76465 110494425
Metastases to bone 55.04 20.48 44 18365 31328 110539562
Growth of eyelashes 53.01 20.48 11 18398 186 110570704
Metastases to liver 50.41 20.48 44 18365 35342 110535548
Trichiasis 50.22 20.48 10 18399 136 110570754
Non-small cell lung cancer 49.85 20.48 25 18384 7910 110562980
Naevoid melanoma 49.58 20.48 7 18402 6 110570884
Infusion related reaction 48.49 20.48 4 18405 381158 110189732
Lung adenocarcinoma 48.31 20.48 26 18383 9505 110561385
Arthralgia 47.86 20.48 36 18373 779596 109791294
Pneumothorax 46.53 20.48 42 18367 35243 110535647
Anaemia 46.38 20.48 197 18212 546889 110024001
Gastrointestinal perforation 45.40 20.48 23 18386 7433 110563457
Malignant pleural effusion 44.93 20.48 19 18390 4074 110566816
Drug hypersensitivity 43.50 20.48 11 18398 454079 110116811
Ulcerative keratitis 42.15 20.48 19 18390 4747 110566143
Joint swelling 41.90 20.48 11 18398 442834 110128056
Xerosis 41.33 20.48 14 18395 1635 110569255
Nausea 39.65 20.48 345 18064 1235345 109335545
Condition aggravated 38.93 20.48 39 18370 734797 109836093
Pneumoperitoneum 38.82 20.48 17 18392 3967 110566923
Corneal disorder 38.64 20.48 15 18394 2582 110568308
Weight increased 38.62 20.48 11 18398 419633 110151257
Blood bilirubin increased 38.54 20.48 55 18354 75917 110494973
Metastases to pleura 38.26 20.48 14 18395 2049 110568841
Embolism 37.78 20.48 27 18382 16262 110554628
Pneumatosis intestinalis 37.01 20.48 21 18388 8508 110562382
Nasopharyngitis 36.91 20.48 10 18399 394351 110176539
Hepatotoxicity 36.83 20.48 49 18360 63351 110507539
Proteinuria 36.61 20.48 39 18370 39979 110530911
Arthropathy 36.61 20.48 3 18406 287519 110283371
Alopecia scarring 36.01 20.48 8 18401 189 110570701
Pulmonary embolism 34.76 20.48 96 18313 214378 110356512
Gene mutation 34.61 20.48 15 18394 3414 110567476
Skin fissures 34.01 20.48 30 18379 24428 110546462
Blepharitis 33.56 20.48 16 18393 4536 110566354
Aspartate aminotransferase increased 32.54 20.48 78 18331 159858 110411032
Pyogenic granuloma 32.50 20.48 9 18400 534 110570356
Vomiting 32.18 20.48 260 18149 910415 109660475
Performance status decreased 31.82 20.48 18 18391 7248 110563642
Corneal perforation 31.57 20.48 10 18399 946 110569944
Asthma 30.81 20.48 3 18406 250288 110320602
Sinusitis 30.79 20.48 6 18403 296682 110274208
Metastasis 29.66 20.48 18 18391 8249 110562641
Skin disorder 29.39 20.48 36 18373 42877 110528013
Non-small cell lung cancer stage IV 28.98 20.48 7 18402 241 110570649
Wound 28.36 20.48 3 18406 234434 110336456
Drug eruption 27.44 20.48 39 18370 53620 110517270
Laryngeal papilloma 26.76 20.48 4 18405 7 110570883
Hair texture abnormal 26.44 20.48 13 18396 3941 110566949
Squamous cell carcinoma 26.38 20.48 23 18386 18440 110552450
Alanine aminotransferase increased 25.66 20.48 78 18331 183695 110387195
COVID-19 25.33 20.48 5 18404 245055 110325835
Hair growth abnormal 24.77 20.48 12 18397 3525 110567365
Respiratory failure 24.30 20.48 85 18324 215247 110355643
Mobility decreased 24.22 20.48 5 18404 237417 110333473
Pneumopericardium 23.80 20.48 6 18403 247 110570643
Overdose 23.69 20.48 5 18404 233789 110337101
Product use in unapproved indication 23.36 20.48 24 18385 447353 110123537
Blood alkaline phosphatase increased 23.13 20.48 42 18367 70893 110499997
Lymphangiosis carcinomatosa 22.28 20.48 10 18399 2472 110568418
Toxicity to various agents 21.64 20.48 29 18380 480526 110090364
Failure to thrive 21.62 20.48 18 18391 13556 110557334
Haemoglobin decreased 21.35 20.48 90 18319 248637 110322253
Hyponatraemia 21.27 20.48 82 18327 217571 110353319
Wheezing 21.16 20.48 8 18401 255222 110315668
Carcinoembryonic antigen increased 21.05 20.48 10 18399 2814 110568076
Conjunctivitis 20.99 20.48 27 18382 33765 110537125
Sarcomatoid carcinoma 20.79 20.48 4 18405 45 110570845
Hypersensitivity 20.72 20.48 22 18387 403976 110166914
Abdominal discomfort 20.71 20.48 21 18388 393837 110177053
Neoplasm malignant 20.49 20.48 28 18381 37115 110533775

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EB02 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors
FDA MoA N0000175076 Protein Kinase Inhibitors
MeSH PA D000092004 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:37699 protein kinase inhibitor
CHEBI has role CHEBI:22587 antiviral agent
CHEBI has role CHEBI:50748 antipsoriatic
CHEBI has role CHEBI:74440 epidermal growth factor receptor antagonist

Related Drugs by ATC class:

L01EB Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors 8 drugs
afatinibdacomitinibgefitinibicotiniblazertinibmobocertinibolmutinibosimertinib

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

DiseaseRelationSNOMED_IDDOID
Non-small cell lung cancer indication 254637007 DOID:3908
Adenocarcinoma of pancreas indication 700423003 DOID:4074
Hyperbilirubinemia contraindication 14783006 DOID:2741
Myocardial infarction contraindication 22298006 DOID:5844
Dehydration contraindication 34095006
Hypokalemia contraindication 43339004
Hepatorenal syndrome contraindication 51292008 DOID:11823
Fibrosis of lung contraindication 51615001 DOID:3770
Gastrointestinal perforation contraindication 51875005
Hemolytic anemia contraindication 61261009 DOID:583
Interstitial pneumonia contraindication 64667001
Blood coagulation disorder contraindication 64779008 DOID:1247
Adult respiratory distress syndrome contraindication 67782005 DOID:11394
Thrombotic thrombocytopenic purpura contraindication 78129009 DOID:10772
Kidney disease contraindication 90708001 DOID:557
Corneal ulcer contraindication 91514001 DOID:8463
Malignant neoplasm of liver contraindication 93870000 DOID:3571
Bleeding contraindication 131148009
Liver function tests abnormal contraindication 166603001
Cerebrovascular accident contraindication 230690007
Interstitial lung disease contraindication 233703007 DOID:3082
Disease of liver contraindication 235856003 DOID:409
Pregnancy, function contraindication 289908002
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Breastfeeding (mother) contraindication 413712001
Myocardial ischemia contraindication 414795007 DOID:3393
Smokes tobacco daily contraindication 449868002
Obstructive Bronchiolitis contraindication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 4.01 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Epidermal growth factor receptor Kinase INHIBITOR IC50 9.22 WOMBAT-PK CHEMBL
Tyrosine-protein kinase JAK3 Kinase Kd 6.15 CHEMBL
ATP-binding cassette sub-family G member 2 Transporter IC50 6.89 CHEMBL
Platelet-derived growth factor receptor beta Kinase Kd 5.85 CHEMBL
Tyrosine-protein kinase ABL1 Kinase Kd 7.24 CHEMBL
Mast/stem cell growth factor receptor Kit Kinase Kd 5.89 CHEMBL
Breakpoint cluster region protein Kinase Kd 5.74 CHEMBL
Proto-oncogene tyrosine-protein kinase Src Kinase Kd 6.15 CHEMBL
Tyrosine-protein kinase Lck Kinase Kd 6.60 CHEMBL
Tyrosine-protein kinase Yes Kinase Kd 5.66 CHEMBL
Serine/threonine-protein kinase B-raf Kinase IC50 7.22 CHEMBL
Receptor-type tyrosine-protein kinase FLT3 Kinase Kd 6.89 CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret Kinase Kd 6.48 CHEMBL
Vascular endothelial growth factor receptor 1 Kinase Kd 5.36 CHEMBL
Vascular endothelial growth factor receptor 2 Kinase Kd 5.24 CHEMBL
Vascular endothelial growth factor receptor 3 Kinase Kd 5.68 CHEMBL
Platelet-derived growth factor receptor alpha Kinase Kd 5.74 CHEMBL
Receptor tyrosine-protein kinase erbB-2 Kinase Kd 5.54 CHEMBL
Cyclin-dependent kinase 2 Kinase IC50 5.94 CHEMBL
Death-associated protein kinase 3 Kinase Kd 5.22 CHEMBL
Focal adhesion kinase 1 Kinase IC50 5.13 CHEMBL
Tyrosine-protein kinase HCK Kinase Kd 5.74 CHEMBL
Receptor tyrosine-protein kinase erbB-4 Kinase Kd 6.64 CHEMBL
Mitogen-activated protein kinase 10 Kinase Kd 5.37 CHEMBL
Tyrosine-protein kinase JAK2 Kinase Kd 5.43 CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit delta Kinase Kd 5.19 CHEMBL
Myosin light chain kinase 2, skeletal/cardiac muscle Kinase Kd 6.01 CHEMBL
Ephrin type-A receptor 8 Kinase Kd 6.03 CHEMBL
AP2-associated protein kinase 1 Kinase Kd 5.92 CHEMBL
Hepatocyte growth factor receptor Kinase Kd 5.96 CHEMBL
Tyrosine-protein kinase Lyn Kinase Kd 6.28 CHEMBL
Serine/threonine-protein kinase 17B Kinase Kd 5.03 CHEMBL
Serine/threonine-protein kinase 10 Kinase Kd 7.72 CHEMBL
Serine/threonine-protein kinase PLK4 Kinase Kd 5.72 CHEMBL
Aurora kinase C Kinase Kd 6.22 CHEMBL
Dual specificity protein kinase TTK Kinase Kd 5.43 CHEMBL
Abelson tyrosine-protein kinase 2 Kinase Kd 6.70 CHEMBL
Ephrin type-A receptor 5 Kinase Kd 6.15 CHEMBL
Fibroblast growth factor receptor 2 Kinase Kd 5.72 CHEMBL
Serine/threonine-protein kinase 17A Kinase Kd 5.20 CHEMBL
Ephrin type-A receptor 6 Kinase Kd 6.36 CHEMBL
TRAF2 and NCK-interacting protein kinase Kinase Kd 5.35 CHEMBL
Casein kinase I isoform epsilon Kinase Kd 6.30 CHEMBL
Tyrosine-protein kinase Fgr Kinase Kd 5.96 CHEMBL
Aurora kinase A Kinase Kd 5.66 CHEMBL
ALK tyrosine kinase receptor Kinase Kd 5.92 CHEMBL
Serine/threonine-protein kinase 36 Kinase Kd 5.36 CHEMBL
Ephrin type-A receptor 3 Kinase Kd 5.62 CHEMBL
BMP-2-inducible protein kinase Kinase Kd 5.92 CHEMBL
Tyrosine-protein kinase FRK Kinase Kd 5.70 CHEMBL
Cyclin-G-associated kinase Kinase Kd 8.51 CHEMBL
Receptor-interacting serine/threonine-protein kinase 2 Kinase Kd 6.39 CHEMBL
Ephrin type-B receptor 1 Kinase Kd 5.96 CHEMBL
Ephrin type-A receptor 7 Kinase Kd 5.85 CHEMBL
STE20-like serine/threonine-protein kinase Kinase Kd 7.59 CHEMBL
MAP kinase-interacting serine/threonine-protein kinase 2 Kinase Kd 6 CHEMBL
Mitogen-activated protein kinase 9 Kinase Kd 5.70 CHEMBL
Epithelial discoidin domain-containing receptor 1 Kinase Kd 6.10 CHEMBL
Solute carrier family 22 member 1 Transporter IC50 4.79 CHEMBL
Ephrin type-B receptor 4 Kinase Kd 5.66 CHEMBL
Tyrosine-protein kinase receptor UFO Kinase Kd 5.40 CHEMBL
Tyrosine-protein kinase receptor TYRO3 Kinase Kd 5.41 CHEMBL
Non-receptor tyrosine-protein kinase TNK1 Kinase Kd 6.20 CHEMBL
Non-receptor tyrosine-protein kinase TYK2 Kinase Kd 5.62 CHEMBL
Casein kinase I isoform delta Kinase Kd 5.46 CHEMBL
Tyrosine-protein kinase receptor Tie-1 Kinase Kd 6.07 CHEMBL
Tyrosine-protein kinase TXK Kinase Kd 5.42 CHEMBL
MAP kinase-interacting serine/threonine-protein kinase 1 Kinase Kd 6.16 CHEMBL
Eukaryotic translation initiation factor 2-alpha kinase 4 Kinase Kd 5.36 CHEMBL
Serine/threonine-protein kinase SIK2 Kinase Kd 5.59 CHEMBL
Serine/threonine-protein kinase TNNI3K Kinase Kd 6.24 CHEMBL
Myotonin-protein kinase Kinase Kd 5.54 CHEMBL
Chaperone activity of bc1 complex-like, mitochondrial Kinase Kd 5.72 CHEMBL
Serine/threonine-protein kinase MRCK gamma Kinase Kd 5.47 CHEMBL
Leukocyte tyrosine kinase receptor Kinase Kd 6.05 CHEMBL
Aurora kinase B Kinase Kd 5.85 CHEMBL
Tyrosine-protein kinase Blk Kinase Kd 6.72 CHEMBL
Tyrosine-protein kinase Mer Kinase Kd 6.01 CHEMBL
Citron Rho-interacting kinase Kinase Kd 6.17 CHEMBL
AarF domain-containing protein kinase 4 Kinase Kd 5.60 CHEMBL
Mitogen-activated protein kinase 4 Kinase Kd 5.60 CHEMBL
Interferon-induced, double-stranded RNA-activated protein kinase Kinase Kd 5.89 CHEMBL
Ribosomal protein S6 kinase alpha-4 Kinase Kd 5.15 CHEMBL
Misshapen-like kinase 1 Kinase Kd 5.89 CHEMBL
Serine/threonine-protein kinase TBK1 Kinase Kd 5.51 CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 2 Kinase Kd 5.89 CHEMBL
Ephrin type-B receptor 6 Kinase Kd 5.77 CHEMBL
G protein-coupled receptor kinase 4 Kinase Kd 5.14 CHEMBL
Homeodomain-interacting protein kinase 4 Kinase Kd 6.02 CHEMBL
Mitogen-activated protein kinase kinase kinase 2 Kinase Kd 5.60 CHEMBL
Mitogen-activated protein kinase kinase kinase 3 Kinase Kd 5.64 CHEMBL
SRSF protein kinase 3 Kinase Kd 5.08 CHEMBL
Serine/threonine-protein kinase ULK3 Kinase Kd 6.04 CHEMBL
Mitogen-activated protein kinase kinase kinase 19 Kinase Kd 7.60 CHEMBL
Receptor-interacting serine/threonine-protein kinase 4 Kinase Kd 5.31 CHEMBL
Receptor tyrosine-protein kinase erbB-3 Kinase Kd 5.96 CHEMBL
Mitogen-activated protein kinase kinase kinase 1 Kinase Kd 5.65 CHEMBL
Serine/threonine-protein kinase SBK1 Kinase Kd 5.92 CHEMBL
Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma Kinase Kd 6 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 5 Kinase Kd 7.02 CHEMBL
Leucine-rich repeat serine/threonine-protein kinase 2 Kinase Kd 5.54 CHEMBL
Lysine-specific histone demethylase 1A Enzyme IC50 4.45 CHEMBL
Solute carrier organic anion transporter family member 2B1 Transporter INHIBITOR Ki 6.28 IUPHAR
Ferrochelatase, mitochondrial Enzyme Kd 5.16 CHEMBL
Mitotic checkpoint serine/threonine-protein kinase BUB1 Kinase Kd 6.95 CHEMBL
Integrin-linked protein kinase Kinase Kd 6.37 CHEMBL
Acyl-CoA dehydrogenase family member 11 Enzyme Kd 5.38 CHEMBL
Tyrosine-protein kinase CSK Kinase Kd 5.02 CHEMBL
dCTP pyrophosphatase 1 Enzyme Kd 5.51 CHEMBL
Serine/threonine-protein kinase ULK3 Kinase Kd 6.20 CHEMBL
Proto-oncogene tyrosine-protein kinase Src Kinase IC50 6 CHEMBL
Tubulin alpha-1A chain Structural Kd 6.64 CHEMBL
Serine/threonine-protein kinase B-raf Kinase IC50 7.40 CHEMBL
Epidermal growth factor receptor Kinase IC50 7.71 CHEMBL

External reference:

IDSource
D04023 KEGG_DRUG
183319-69-9 SECONDARY_CAS_RN
4021511 VANDF
CHEBI:114785 CHEBI
AQ4 PDB_CHEM_ID
CHEMBL553 ChEMBL_ID
CHEMBL1079742 ChEMBL_ID
4920 IUPHAR_LIGAND_ID
DB00530 DRUGBANK_ID
337525 RXNORM
19073 MMSL
248186 MMSL
63773 MMSL
d05412 MMSL
008759 NDDF
008760 NDDF
414122006 SNOMEDCT_US
414123001 SNOMEDCT_US
426686007 SNOMEDCT_US
C1533491 UMLSCUI
D000069347 MESH_DESCRIPTOR_UI
8133 INN_ID
176870 PUBCHEM_CID
J4T82NDH7E UNII
J4T82NDH7E INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 0093-7662 TABLET, FILM COATED 25 mg ORAL ANDA 24 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 0093-7663 TABLET, FILM COATED 100 mg ORAL ANDA 24 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 0093-7664 TABLET, FILM COATED 150 mg ORAL ANDA 24 sections
ERLOTINIB HUMAN PRESCRIPTION DRUG LABEL 1 31722-263 TABLET, FILM COATED 25 mg ORAL ANDA 25 sections
ERLOTINIB HUMAN PRESCRIPTION DRUG LABEL 1 31722-264 TABLET, FILM COATED 100 mg ORAL ANDA 25 sections
ERLOTINIB HUMAN PRESCRIPTION DRUG LABEL 1 31722-265 TABLET, FILM COATED 150 mg ORAL ANDA 25 sections
ERLOTINIB HYDROCHLORIDE Human Prescription Drug Label 1 46708-565 TABLET, FILM COATED 25 mg ORAL ANDA 25 sections
ERLOTINIB HYDROCHLORIDE Human Prescription Drug Label 1 46708-566 TABLET, FILM COATED 100 mg ORAL ANDA 25 sections
ERLOTINIB HYDROCHLORIDE Human Prescription Drug Label 1 46708-567 TABLET, FILM COATED 150 mg ORAL ANDA 25 sections
Tarceva HUMAN PRESCRIPTION DRUG LABEL 1 54868-5290 TABLET 25 mg ORAL NDA 20 sections
Tarceva HUMAN PRESCRIPTION DRUG LABEL 1 54868-5447 TABLET 150 mg ORAL NDA 20 sections
Tarceva HUMAN PRESCRIPTION DRUG LABEL 1 54868-5474 TABLET 100 mg ORAL NDA 20 sections
Erlotinib Human Prescription Drug Label 1 59651-530 TABLET, FILM COATED 25 mg ORAL ANDA 25 sections
Erlotinib Human Prescription Drug Label 1 59651-531 TABLET, FILM COATED 100 mg ORAL ANDA 25 sections
Erlotinib Human Prescription Drug Label 1 59651-532 TABLET, FILM COATED 150 mg ORAL ANDA 25 sections
ERLOTINIB HYDROCHLORIDE Human Prescription Drug Label 1 62332-565 TABLET, FILM COATED 25 mg ORAL ANDA 25 sections
ERLOTINIB HYDROCHLORIDE Human Prescription Drug Label 1 62332-566 TABLET, FILM COATED 100 mg ORAL ANDA 25 sections
ERLOTINIB HYDROCHLORIDE Human Prescription Drug Label 1 62332-567 TABLET, FILM COATED 150 mg ORAL ANDA 25 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 63304-095 TABLET, FILM COATED 25 mg ORAL ANDA 26 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 63304-096 TABLET, FILM COATED 100 mg ORAL ANDA 26 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 63304-135 TABLET, FILM COATED 150 mg ORAL ANDA 26 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 68382-913 TABLET 25 mg ORAL ANDA 23 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 68382-914 TABLET 100 mg ORAL ANDA 23 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 68382-915 TABLET 150 mg ORAL ANDA 23 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 70771-1521 TABLET, FILM COATED 25 mg ORAL ANDA 1 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 70771-1522 TABLET, FILM COATED 100 mg ORAL ANDA 1 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 70771-1523 TABLET, FILM COATED 150 mg ORAL ANDA 1 sections
Erlotinib Hydrochloride Human Prescription Drug Label 1 72205-080 TABLET, FILM COATED 25 mg ORAL ANDA 24 sections
Erlotinib Hydrochloride Human Prescription Drug Label 1 72205-081 TABLET, FILM COATED 100 mg ORAL ANDA 24 sections
Erlotinib Hydrochloride Human Prescription Drug Label 1 72205-082 TABLET, FILM COATED 150 mg ORAL ANDA 24 sections