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

Approvals:

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

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 5963.47 20.84 2794 20140 371587 63094501
Disease progression 982.69 20.84 588 22346 122170 63343918
Rash 679.95 20.84 916 22018 559955 62906133
Diarrhoea 576 20.84 965 21969 714401 62751687
Malignant neoplasm progression 533.34 20.84 345 22589 81776 63384312
Dermatitis acneiform 381.56 20.84 119 22815 4877 63461211
Drug resistance 313.65 20.84 157 22777 22776 63443312
Metastases to central nervous system 222.27 20.84 104 22830 13001 63453087
Dry skin 203.91 20.84 167 22767 56720 63409368
Paronychia 170.03 20.84 67 22867 5498 63460590
Neoplasm malignant 154.12 20.84 109 22825 29752 63436336
Incorrect dose administered 152.66 20.84 145 22789 59823 63406265
Decreased appetite 117.07 20.84 271 22663 250781 63215307
EGFR gene mutation 116.87 20.84 26 22908 271 63465817
Acquired gene mutation 112.41 20.84 32 22902 951 63465137
Pleural effusion 97.74 20.84 143 22791 93067 63373021
Metastasis 96.71 20.84 44 22890 5153 63460935
Acne 93.23 20.84 73 22861 23220 63442868
Lung cancer metastatic 92.86 20.84 35 22899 2545 63463543
Lung neoplasm malignant 88.39 20.84 66 22868 19567 63446521
Dehydration 88.37 20.84 194 22740 173160 63292928
Joint swelling 81.48 20.84 11 22923 327655 63138433
Arthralgia 78.72 20.84 55 22879 569655 62896433
Hair growth abnormal 77.63 20.84 32 22902 2949 63463139
Drug hypersensitivity 75.90 20.84 11 22923 310676 63155412
Arthropathy 71.93 20.84 3 22931 234789 63231299
Growth of eyelashes 63.56 20.84 15 22919 207 63465881
Rash pustular 63.48 20.84 37 22897 7245 63458843
Headache 63.10 20.84 82 22852 633159 62832929
Condition aggravated 62.18 20.84 34 22900 402183 63063905
Pancreatic carcinoma metastatic 58.83 20.84 24 22910 2154 63463934
Non-small cell lung cancer metastatic 56.38 20.84 17 22917 620 63465468
Skin fissures 55.12 20.84 40 22894 11348 63454740
Malignant pleural effusion 54.68 20.84 24 22910 2582 63463506
Pulmonary embolism 54.28 20.84 126 22808 116558 63349530
Metastases to bone 53.77 20.84 51 22883 20968 63445120
Metastases to lung 53.27 20.84 41 22893 12709 63453379
Sinusitis 53.12 20.84 9 22925 226644 63239444
Metastases to liver 52.34 20.84 53 22881 23586 63442502
Skin toxicity 52.12 20.84 28 22906 4686 63461402
Alopecia scarring 50.41 20.84 11 22923 104 63465984
Haemoptysis 48.83 20.84 56 22878 28670 63437418
Non-small cell lung cancer 47.31 20.84 24 22910 3571 63462517
Drug ineffective 46.72 20.84 207 22727 1044558 62421530
Weight increased 46.54 20.84 18 22916 260774 63205314
Nasopharyngitis 46.29 20.84 17 22917 254240 63211848
Naevoid melanoma 45.99 20.84 7 22927 3 63466085
Metastases to meninges 45.19 20.84 21 22913 2581 63463507
Multiple-drug resistance 44.35 20.84 26 22908 5144 63460944
Hypersensitivity 43.39 20.84 26 22908 292659 63173429
Product use issue 43.19 20.84 13 22921 220507 63245581
Trichiasis 43.16 20.84 9 22925 67 63466021
Swelling 42.92 20.84 23 22911 275355 63190733
Neoplasm progression 42.73 20.84 59 22875 36369 63429719
Glossodynia 42.13 20.84 7 22927 178869 63287219
Wound 41.70 20.84 5 22929 163258 63302830
Ulcerative keratitis 41.33 20.84 20 22914 2690 63463398
Nausea 40.36 20.84 478 22456 853993 62612095
Pain 39.90 20.84 136 22798 740492 62725596
Interstitial lung disease 39.40 20.84 76 22858 61832 63404256
Treatment failure 38.49 20.84 12 22922 199031 63267057
Discomfort 38.43 20.84 7 22927 167367 63298721
Dysphagia 38.30 20.84 93 22841 88492 63377596
Hair texture abnormal 38.15 20.84 22 22912 4221 63461867
Skin exfoliation 37.91 20.84 61 22873 43041 63423047
Corneal perforation 37.46 20.84 12 22922 536 63465552
Therapeutic product effect decreased 36.73 20.84 12 22922 193175 63272913
Lung adenocarcinoma 36.52 20.84 22 22912 4575 63461513
Peripheral swelling 36.19 20.84 26 22908 265916 63200172
Eye irritation 35.94 20.84 42 22892 21929 63444159
Injection site pain 35.68 20.84 3 22931 129797 63336291
Erythema dyschromicum perstans 32.80 20.84 7 22927 59 63466029
Metastatic neoplasm 32.69 20.84 20 22914 4275 63461813
Abdominal discomfort 32.43 20.84 41 22893 320844 63145244
Metastases to spine 32.33 20.84 18 22916 3231 63462857
Malignant transformation 32.11 20.84 10 22924 407 63465681
Henoch-Schonlein purpura 32.04 20.84 13 22921 1150 63464938
Product dose omission issue 31.76 20.84 23 22911 234290 63231798
Pneumatosis intestinalis 31.44 20.84 16 22918 2397 63463691
Therapy partial responder 31.42 20.84 28 22906 10630 63455458
Pyogenic granuloma 30.48 20.84 9 22925 305 63465783
COVID-19 30.05 20.84 3 22931 113100 63352988
Pain in extremity 29.85 20.84 46 22888 331440 63134648
Blood bilirubin increased 29.22 20.84 50 22884 37090 63428998
Vomiting 28.51 20.84 318 22616 559299 62906789
Asthma 27.88 20.84 6 22928 127555 63338533
Iridocele 27.71 20.84 4 22930 0 63466088
Onychalgia 27.26 20.84 11 22923 960 63465128
Blepharitis 26.85 20.84 15 22919 2710 63463378
Drug intolerance 26.69 20.84 44 22890 308617 63157471
Hirsutism 26.55 20.84 12 22922 1383 63464705
Corneal disorder 26.50 20.84 13 22921 1801 63464287
Product use in unapproved indication 26.39 20.84 16 22918 179064 63287024
Asthenia 26.33 20.84 232 22702 383372 63082716
Metastases to neck 26.12 20.84 6 22928 73 63466015
Onychoclasis 25.97 20.84 20 22914 6202 63459886
Mobility decreased 25.88 20.84 6 22928 121153 63344935
Performance status decreased 25.15 20.84 16 22918 3662 63462426
Skin disorder 24.91 20.84 41 22893 29466 63436622
Pneumothorax 24.81 20.84 30 22904 16231 63449857
Migraine 24.42 20.84 4 22930 103342 63362746
Osteoarthritis 24.14 20.84 3 22931 95340 63370748
Lymphangiosis carcinomatosa 23.05 20.84 11 22923 1434 63464654
Epistaxis 22.98 20.84 68 22866 72657 63393431
Stomatitis 22.85 20.84 105 22829 138620 63327468
Respiratory failure 22.18 20.84 84 22850 101774 63364314
Eyelash thickening 22.17 20.84 4 22930 12 63466076
Metastases to breast 22.11 20.84 7 22927 301 63465787
Anaemia 21.97 20.84 181 22753 293249 63172839
Conjunctivitis 21.90 20.84 32 22902 20764 63445324
Psoriasis 21.38 20.84 3 22931 86954 63379134
Weight decreased 20.86 20.84 171 22763 276627 63189461

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 5821.52 17.39 3320 18137 394729 34540745
Rash 914.03 17.39 883 20574 221869 34713605
Disease progression 752.34 17.39 581 20876 107496 34827978
Dermatitis acneiform 281.26 17.39 115 21342 6074 34929400
Malignant neoplasm progression 280.07 17.39 306 21151 87740 34847734
Diarrhoea 218.77 17.39 626 20831 389286 34546188
Neoplasm malignant 204.30 17.39 136 21321 19769 34915705
Dehydration 117.17 17.39 251 21206 129718 34805756
Metastases to central nervous system 111.52 17.39 67 21390 8138 34927336
Drug resistance 103.58 17.39 102 21355 25825 34909649
Interstitial lung disease 85.71 17.39 148 21309 65134 34870340
Incorrect dose administered 84.63 17.39 114 21343 40401 34895073
Haemoptysis 80.07 17.39 103 21354 34903 34900571
Lung neoplasm malignant 76.18 17.39 72 21385 17323 34918151
Non-small cell lung cancer metastatic 74.74 17.39 24 21433 626 34934848
Decreased appetite 70.23 17.39 243 21214 166149 34769325
EGFR gene mutation 63.99 17.39 16 21441 161 34935313
Pleural effusion 59.49 17.39 145 21312 81401 34854073
Lung cancer metastatic 57.66 17.39 30 21427 2757 34932717
Acne 52.69 17.39 48 21409 11018 34924456
Product use in unapproved indication 51.31 17.39 6 21451 117493 34817981
Non-small cell lung cancer 50.52 17.39 31 21426 3909 34931565
Paronychia 49.38 17.39 29 21428 3376 34932098
Drug abuse 48.88 17.39 3 21454 99093 34836381
Toxicity to various agents 46.76 17.39 33 21424 200329 34735145
Metastases to liver 44.16 17.39 48 21409 13615 34921859
Metastasis 44.14 17.39 29 21428 4115 34931359
Malignant pleural effusion 42.04 17.39 20 21437 1516 34933958
Neoplasm progression 41.83 17.39 61 21396 23239 34912235
Product dose omission issue 41.68 17.39 11 21446 119700 34815774
Skin toxicity 40.37 17.39 29 21428 4755 34930719
Gastrointestinal perforation 38.65 17.39 26 21431 3837 34931637
Acquired gene mutation 38.18 17.39 18 21439 1337 34934137
Lymphangiosis carcinomatosa 37.88 17.39 16 21441 916 34934558
Metastases to lung 37.82 17.39 37 21420 9283 34926191
Drug ineffective 37.58 17.39 149 21308 456602 34478872
COVID-19 36.36 17.39 3 21454 77547 34857927
Pneumothorax 35.76 17.39 51 21406 19041 34916433
Weight increased 35.47 17.39 7 21450 93026 34842448
Vomiting 35.17 17.39 266 21191 247355 34688119
Bradycardia 35.13 17.39 3 21454 75415 34860059
Rash pustular 35.04 17.39 28 21429 5380 34930094
Pneumoperitoneum 33.44 17.39 18 21439 1772 34933702
Condition aggravated 31.71 17.39 43 21414 192153 34743321
Arthralgia 31.24 17.39 35 21422 170006 34765468
Metastases to bone 30.18 17.39 37 21420 11933 34923541
Metastases to spine 29.77 17.39 19 21438 2565 34932909
Drug hypersensitivity 28.79 17.39 7 21450 80522 34854952
Dizziness 28.49 17.39 57 21400 218464 34717010
Acute kidney injury 27.96 17.39 95 21362 304893 34630581
Lung adenocarcinoma 27.77 17.39 23 21434 4648 34930826
Pancreatic carcinoma metastatic 27.54 17.39 19 21438 2921 34932553
Stomatitis 26.21 17.39 71 21386 42443 34893031
Palmar-plantar erythrodysaesthesia syndrome 25.93 17.39 41 21416 16754 34918720
Pulmonary embolism 25.56 17.39 116 21341 89630 34845844
Metastases to meninges 25.44 17.39 14 21443 1440 34934034
Nausea 24.94 17.39 318 21139 339590 34595884
Pneumonitis 24.41 17.39 60 21397 33818 34901656
Oesophageal ulcer 22.97 17.39 18 21439 3363 34932111
Hyperhidrosis 22.72 17.39 9 21448 75683 34859791
Overdose 22.55 17.39 14 21443 91045 34844429
Bronchial fistula 21.82 17.39 7 21450 182 34935292
Respiratory failure 21.62 17.39 127 21330 108445 34827029
Nasopharyngitis 21.53 17.39 8 21449 69960 34865514
Growth of eyelashes 21.38 17.39 6 21451 97 34935377
Blood pressure increased 21.20 17.39 14 21443 88088 34847386
Infusion related reaction 20.20 17.39 4 21453 53053 34882421
Tremor 20.04 17.39 13 21444 82574 34852900
Hypophagia 19.98 17.39 45 21412 23977 34911497
Conjunctivitis 19.77 17.39 27 21430 9678 34925796
Insomnia 19.49 17.39 21 21436 103886 34831588
Mucosal inflammation 18.53 17.39 59 21398 38563 34896911
Product use issue 18.19 17.39 8 21449 63208 34872266
Intentional product use issue 18.14 17.39 7 21450 59809 34875665
Skin reaction 18 17.39 19 21438 5211 34930263
Rhabdomyolysis 17.55 17.39 10 21447 68153 34867321
Rash follicular 17.41 17.39 4 21453 27 34935447

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
Rash 802.18 16.46 961 25107 577397 79140923
Malignant neoplasm progression 770.75 16.46 505 25563 135485 79582835
Disease progression 630.47 16.46 504 25564 183858 79534462
Diarrhoea 535.53 16.46 994 25074 879495 78838825
Dermatitis acneiform 533.50 16.46 177 25891 9816 79708504
Drug resistance 480.39 16.46 247 25821 41966 79676354
Death 376.10 16.46 666 25402 565848 79152472
Metastases to central nervous system 231.11 16.46 111 25957 16264 79702056
EGFR gene mutation 200.02 16.46 43 26025 421 79717899
Dehydration 185.01 16.46 308 25760 247879 79470441
Paronychia 154.57 16.46 67 26001 7741 79710579
Acquired gene mutation 149.52 16.46 47 26021 2186 79716134
Interstitial lung disease 146.10 16.46 182 25886 112418 79605902
Dry skin 141.99 16.46 141 25927 67854 79650466
Pleural effusion 124.13 16.46 192 25876 145070 79573250
Decreased appetite 122.61 16.46 314 25754 342104 79376216
Haemoptysis 103.93 16.46 109 25959 55890 79662430
Rash pustular 97.23 16.46 55 26013 11256 79707064
Non-small cell lung cancer metastatic 86.97 16.46 26 26042 1020 79717300
Skin toxicity 86.88 16.46 46 26022 8268 79710052
Acne 77.29 16.46 67 26001 27123 79691197
Arthralgia 74.04 16.46 48 26020 571755 79146565
Therapy partial responder 66.60 16.46 51 26017 17346 79700974
Metastases to meninges 65.11 16.46 29 26039 3572 79714748
Non-small cell lung cancer 63.11 16.46 34 26034 6326 79711994
Infusion related reaction 62.70 16.46 3 26065 230234 79488086
Pulmonary embolism 61.88 16.46 158 25910 171496 79546824
Drug hypersensitivity 60.69 16.46 12 26056 298904 79419416
Nausea 59.95 16.46 524 25544 956672 78761648
Metastases to liver 59.59 16.46 59 26009 28255 79690065
Pneumothorax 59.57 16.46 59 26009 28264 79690056
Lung adenocarcinoma 58.98 16.46 35 26033 7829 79710491
Trichiasis 58.78 16.46 12 26056 89 79718231
Ulcerative keratitis 58.15 16.46 27 26041 3662 79714658
Lymphangiosis carcinomatosa 57.90 16.46 23 26045 2131 79716189
Neoplasm progression 56.76 16.46 77 25991 51605 79666715
Growth of eyelashes 56.00 16.46 13 26055 185 79718135
Multiple-drug resistance 55.32 16.46 35 26033 8773 79709547
Respiratory failure 54.64 16.46 156 25912 180755 79537565
Weight increased 52.54 16.46 13 26055 277373 79440947
Metastases to lung 52.11 16.46 45 26023 18118 79700202
Joint swelling 51.89 16.46 15 26053 288631 79429689
Malignant pleural effusion 50.99 16.46 24 26044 3356 79714964
Corneal perforation 50.83 16.46 16 26052 747 79717573
Vomiting 50.49 16.46 381 25687 665447 79052873
Pneumonitis 48.53 16.46 78 25990 60782 79657538
Gastrointestinal perforation 47.83 16.46 28 26040 6109 79712211
Blood bilirubin increased 47.59 16.46 81 25987 66151 79652169
Alopecia scarring 46.78 16.46 10 26058 95 79718225
Incorrect dose administered 46.44 16.46 87 25981 76543 79641777
Skin fissures 45.01 16.46 36 26032 13037 79705283
Erythema dyschromicum perstans 44.93 16.46 9 26059 60 79718260
Naevoid melanoma 44.85 16.46 7 26061 6 79718314
Arthropathy 43.26 16.46 4 26064 177107 79541213
Condition aggravated 42.76 16.46 61 26007 501063 79217257
Hair growth abnormal 42.72 16.46 20 26048 2764 79715556
Nasopharyngitis 42.42 16.46 15 26053 253866 79464454
Headache 41.96 16.46 95 25973 653677 79064643
Metastases to bone 40.82 16.46 45 26023 24382 79693938
Toxicity to various agents 40.40 16.46 47 26021 421493 79296827
Conjunctivitis 38.93 16.46 45 26023 25670 79692650
Drug ineffective 38.27 16.46 203 25865 1080710 78637610
COVID-19 37.36 16.46 4 26064 157670 79560650
Pneumatosis intestinalis 36.67 16.46 24 26044 6373 79711947
Sinusitis 35.42 16.46 10 26058 195491 79522829
Pyogenic granuloma 35.15 16.46 11 26057 504 79717816
Pneumoperitoneum 34.76 16.46 18 26050 3090 79715230
Lung cancer metastatic 34.55 16.46 19 26049 3680 79714640
Eye irritation 34.39 16.46 38 26030 20643 79697677
Off label use 33.99 16.46 167 25901 907048 78811272
Skin exfoliation 33.93 16.46 63 26005 55037 79663283
Corneal disorder 33.74 16.46 16 26052 2275 79716045
Hypophagia 33.27 16.46 56 26012 45311 79673009
Embolism 32.93 16.46 31 26037 13951 79704369
Product use in unapproved indication 32.35 16.46 21 26047 250338 79467982
Neoplasm malignant 31.35 16.46 45 26023 31765 79686555
Bradycardia 30.72 16.46 4 26064 135553 79582767
Overdose 30.56 16.46 11 26057 184195 79534125
Peripheral swelling 30.47 16.46 26 26042 269591 79448729
Metastasis 30.43 16.46 22 26046 6858 79711462
Therapeutic product effect decreased 30.39 16.46 8 26060 163855 79554465
Haemoglobin decreased 30.11 16.46 148 25920 221971 79496349
Hair texture abnormal 29.87 16.46 17 26051 3517 79714803
Metastases to pleura 29.66 16.46 13 26055 1541 79716779
Pain 29.64 16.46 124 25944 703678 79014642
Product use issue 29.35 16.46 16 26052 209806 79508514
Malignant transformation 29.27 16.46 12 26056 1206 79717114
Henoch-Schonlein purpura 28.33 16.46 15 26053 2695 79715625
Drug intolerance 28.02 16.46 27 26041 264092 79454228
Aspartate aminotransferase increased 27.77 16.46 104 25964 138537 79579783
Skin disorder 27.73 16.46 44 26024 33899 79684421
Stomatitis 27.68 16.46 108 25960 146649 79571671
Hypersensitivity 27.60 16.46 27 26041 262212 79456108
Lung neoplasm malignant 26.92 16.46 39 26029 27753 79690567
Injection site pain 26.78 16.46 5 26063 129833 79588487
Mucosal inflammation 26.61 16.46 69 25999 75511 79642809
Xerosis 26.01 16.46 11 26057 1195 79717125
Hepatotoxicity 25.91 16.46 54 26014 51298 79667022
Anaemia 25.80 16.46 240 25828 444775 79273545
Performance status decreased 25.79 16.46 19 26049 6094 79712226
Product dose omission issue 25.46 16.46 26 26042 247511 79470809
Blood alkaline phosphatase increased 25.44 16.46 61 26007 63603 79654717
Carcinoembryonic antigen increased 25.30 16.46 13 26055 2196 79716124
Eyelash thickening 24.06 16.46 4 26064 7 79718313
Palpitations 23.83 16.46 6 26062 126604 79591716
Pericarditis 23.80 16.46 3 26065 104233 79614087
Blepharitis 23.68 16.46 14 26054 3110 79715210
Glossodynia 23.54 16.46 3 26065 103334 79614986
Blood albumin decreased 23.45 16.46 34 26034 24209 79694111
Lung infiltration 23.44 16.46 33 26035 22879 79695441
Palmar-plantar erythrodysaesthesia syndrome 23.11 16.46 40 26028 33094 79685226
Wound 22.86 16.46 5 26063 116174 79602146
Sudden death 22.41 16.46 32 26036 22479 79695841
Proteinuria 22.36 16.46 39 26029 32463 79685857
Dysphagia 22.32 16.46 89 25979 122047 79596273
Asthenia 22.12 16.46 260 25808 511429 79206891
Squamous cell carcinoma of lung 21.93 16.46 12 26056 2302 79716018
Abdominal discomfort 21.86 16.46 30 26038 250697 79467623
Epistaxis 21.79 16.46 83 25985 111432 79606888
Pneumopericardium 21.18 16.46 6 26062 194 79718126
Asthma 20.87 16.46 9 26059 135086 79583234
Dermatitis 20.77 16.46 30 26038 21291 79697029
Onychoclasis 20.58 16.46 16 26052 5562 79712758
Alanine aminotransferase increased 20.38 16.46 106 25962 162464 79555856
Pericardial effusion 20.33 16.46 46 26022 46191 79672129
Gene mutation 20.26 16.46 12 26056 2674 79715646
Nail disorder 20.09 16.46 22 26046 11830 79706490
Dizziness 19.59 16.46 97 25971 526344 79191976
Pain in extremity 19.47 16.46 58 26010 364480 79353840
Mobility decreased 19.10 16.46 8 26060 122167 79596153
Pancreatic carcinoma metastatic 18.92 16.46 13 26055 3740 79714580
Weight decreased 18.81 16.46 188 25880 355010 79363310
Laryngeal papilloma 18.54 16.46 3 26065 4 79718316
Disseminated intravascular coagulation 18.44 16.46 38 26030 35804 79682516
Discomfort 18.42 16.46 9 26059 125608 79592712
Failure to thrive 18.39 16.46 21 26047 11823 79706497
Gastrointestinal haemorrhage 18.30 16.46 96 25972 147623 79570697
Onychalgia 18.29 16.46 8 26060 944 79717376
Sarcomatoid carcinoma 18.26 16.46 4 26064 43 79718277
Hypoxia 17.88 16.46 74 25994 103169 79615151
Biliary cancer metastatic 17.79 16.46 3 26065 6 79718314
Cerebral ischaemia 17.63 16.46 20 26048 11175 79707145
Iridocele 17.23 16.46 4 26064 57 79718263
Arthritis 17.20 16.46 8 26060 114872 79603448
Pneumonia 17.16 16.46 307 25761 659939 79058381
Purpura 16.91 16.46 26 26042 19501 79698819
Non-small cell lung cancer stage IV 16.80 16.46 5 26063 193 79718127
Migraine 16.74 16.46 4 26064 87489 79630831
Oesophagitis 16.52 16.46 29 26039 24260 79694060
Corneal defect 16.46 16.46 3 26065 11 79718309

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 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 agents
CHEBI has role CHEBI:37699 protein kinase inhibitors
CHEBI has role CHEBI:74440 EGFR antagonoists

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
Aurora kinase C Kinase Kd 6.22 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
Tyrosine-protein kinase CSK Kinase Kd 5.02 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
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
Acyl-CoA dehydrogenase family member 11 Enzyme Kd 5.38 CHEMBL
Serine/threonine-protein kinase PLK4 Kinase Kd 5.72 CHEMBL
dCTP pyrophosphatase 1 Unclassified 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

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

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 Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0378-7131 TABLET, FILM COATED 25 mg ORAL ANDA 26 sections
Erlotinib Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0378-7132 TABLET, FILM COATED 100 mg ORAL ANDA 26 sections
Erlotinib Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0378-7133 TABLET, FILM COATED 150 mg ORAL ANDA 26 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 46708-565 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 46708-566 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
ERLOTINIB HYDROCHLORIDE Human Prescription Drug Label 1 46708-567 TABLET, FILM COATED 150 mg ORAL ANDA 25 sections
TARCEVA HUMAN PRESCRIPTION DRUG LABEL 1 50242-062 TABLET 25 mg ORAL NDA 24 sections
TARCEVA HUMAN PRESCRIPTION DRUG LABEL 1 50242-063 TABLET 100 mg ORAL NDA 24 sections
TARCEVA HUMAN PRESCRIPTION DRUG LABEL 1 50242-064 TABLET 150 mg ORAL NDA 24 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 51991-890 TABLET, FILM COATED 25 mg ORAL ANDA 28 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 51991-890 TABLET, FILM COATED 25 mg ORAL ANDA 28 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 51991-891 TABLET, FILM COATED 100 mg ORAL ANDA 28 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 51991-891 TABLET, FILM COATED 100 mg ORAL ANDA 28 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 51991-892 TABLET, FILM COATED 150 mg ORAL ANDA 28 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 51991-892 TABLET, FILM COATED 150 mg ORAL ANDA 28 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 HUMAN PRESCRIPTION DRUG LABEL 1 59923-725 TABLET, FILM COATED 25 mg ORAL ANDA 28 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 59923-726 TABLET, FILM COATED 100 mg ORAL ANDA 28 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 59923-727 TABLET, FILM COATED 150 mg ORAL ANDA 28 sections