erlotinib 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) 0.40 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0.30 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 5.45 ┬ÁM/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
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 5648.60 20.24 2780 19619 354452 52972215
Disease progression 915.96 20.24 555 21844 101365 53225302
Rash 705.03 20.24 896 21503 445295 52881372
Diarrhoea 543.50 20.24 949 21450 624597 52702070
Malignant neoplasm progression 452.44 20.24 313 22086 71228 53255439
Dermatitis acneiform 360.43 20.24 115 22284 4355 53322312
Lung neoplasm malignant 243.52 20.24 126 22273 16826 53309841
Drug resistance 229.63 20.24 128 22271 19834 53306833
Metastases to central nervous system 203.60 20.24 100 22299 11957 53314710
Dry skin 203.06 20.24 162 22237 45598 53281069
Paronychia 167.43 20.24 67 22332 4917 53321750
Neoplasm malignant 156.80 20.24 110 22289 25491 53301176
Incorrect dose administered 150.17 20.24 143 22256 50902 53275765
Non-small cell lung cancer 148.89 20.24 56 22343 3477 53323190
Lung adenocarcinoma 117.75 20.24 51 22348 4567 53322100
Decreased appetite 114.64 20.24 268 22131 214706 53111961
Lung cancer metastatic 95.66 20.24 37 22362 2479 53324188
EGFR gene mutation 90.98 20.24 21 22378 222 53326445
Acne 88.45 20.24 73 22326 21513 53305154
Pleural effusion 83.01 20.24 140 22259 88439 53238228
Drug hypersensitivity 79.96 20.24 9 22390 265233 53061434
Acquired gene mutation 79.50 20.24 24 22375 753 53325914
Metastasis 79.13 20.24 39 22360 4692 53321975
Hair growth abnormal 75.20 20.24 32 22367 2743 53323924
Dehydration 72.85 20.24 194 22205 168216 53158451
Pancreatic carcinoma metastatic 71.72 20.24 30 22369 2464 53324203
Arthralgia 65.88 20.24 53 22346 439730 52886937
Joint swelling 65.81 20.24 10 22389 234628 53092039
Headache 64.05 20.24 79 22320 536742 52789925
Skin fissures 59.23 20.24 40 22359 8705 53317962
Condition aggravated 58.20 20.24 26 22373 297108 53029559
Non-small cell lung cancer metastatic 57.82 20.24 18 22381 627 53326040
Growth of eyelashes 52.77 20.24 13 22386 185 53326482
Malignant pleural effusion 51.48 20.24 24 22375 2553 53324114
Metastases to lung 50.92 20.24 41 22358 11663 53315004
Skin toxicity 49.10 20.24 27 22372 4066 53322601
Alopecia scarring 49.06 20.24 11 22388 101 53326566
Arthropathy 47.51 20.24 3 22396 141450 53185217
Metastases to bone 47.26 20.24 49 22350 19279 53307388
Multiple-drug resistance 46.29 20.24 24 22375 3211 53323456
Naevoid melanoma 44.94 20.24 7 22392 3 53326664
Metastases to liver 44.66 20.24 50 22349 21446 53305221
Drug ineffective 44.41 20.24 185 22214 817060 52509607
Rash pustular 44.37 20.24 31 22368 7125 53319542
Trichiasis 42.05 20.24 9 22390 65 53326602
Haemoptysis 41.60 20.24 55 22344 27984 53298683
Sinusitis 41.29 20.24 10 22389 168554 53158113
Weight increased 39.86 20.24 18 22381 204549 53122118
Pulmonary embolism 39.85 20.24 122 22277 114320 53212347
Neoplasm progression 38.82 20.24 55 22344 29864 53296803
Skin exfoliation 37.78 20.24 60 22339 36023 53290644
Nasopharyngitis 37.34 20.24 17 22382 192278 53134389
Eye irritation 36.77 20.24 42 22357 18407 53308260
Hair texture abnormal 36.58 20.24 22 22377 3920 53322747
Injection site pain 36.36 20.24 3 22396 113388 53213279
Pancreatic carcinoma 35.99 20.24 27 22372 6927 53319740
Stomatitis 34.50 20.24 105 22294 98053 53228614
Metastatic neoplasm 34.02 20.24 21 22378 3921 53322746
Interstitial lung disease 33.24 20.24 75 22324 58547 53268120
Lung adenocarcinoma stage IV 32.11 20.24 9 22390 216 53326451
Erythema dyschromicum perstans 31.86 20.24 7 22392 58 53326609
Metastases to spine 31.20 20.24 18 22381 2972 53323695
Metastases to meninges 30.99 20.24 16 22383 2123 53324544
Henoch-Schonlein purpura 30.74 20.24 13 22386 1097 53325570
Nausea 30.44 20.24 465 21934 755626 52571041
Dysphagia 30.33 20.24 91 22308 84306 53242361
Pain 30.14 20.24 136 22263 588262 52738405
Pain in extremity 29.82 20.24 46 22353 285004 53041663
Hypersensitivity 29.50 20.24 27 22372 210638 53116029
Peripheral swelling 29.35 20.24 26 22373 206082 53120585
Pyogenic granuloma 29.26 20.24 9 22390 301 53326366
Product use issue 29.25 20.24 11 22388 139573 53187094
Product dose omission issue 28.73 20.24 23 22376 191597 53135070
Swelling 28.57 20.24 23 22376 191082 53135585
Malignant transformation 28.03 20.24 9 22390 347 53326320
Hirsutism 27.90 20.24 12 22387 1056 53325611
Therapy partial responder 27.68 20.24 22 22377 6141 53320526
Asthma 27.60 20.24 6 22393 108966 53217701
Metastases to neck 26.30 20.24 6 22393 60 53326607
Ulcerative keratitis 26.12 20.24 15 22384 2454 53324213
Psoriasis 26.09 20.24 3 22396 87086 53239581
Corneal perforation 24.79 20.24 9 22390 505 53326162
Pneumatosis intestinalis 24.72 20.24 14 22385 2232 53324435
Vomiting 24.46 20.24 317 22082 496822 52829845
Blepharitis 24.21 20.24 14 22385 2320 53324347
Skin disorder 24.08 20.24 40 22359 24918 53301749
Blood bilirubin increased 24.03 20.24 49 22350 35681 53290986
Treatment failure 23.92 20.24 12 22387 128391 53198276
Performance status decreased 23.92 20.24 16 22383 3427 53323240
Onychalgia 23.56 20.24 10 22389 851 53325816
Palpitations 23.30 20.24 7 22392 102341 53224326
Wound 23.27 20.24 5 22394 91552 53235115
Onychoclasis 23.26 20.24 19 22380 5514 53321153
Conjunctivitis 23.08 20.24 32 22367 17025 53309642
Therapeutic product effect decreased 23.03 20.24 12 22387 125643 53201024
Lymphangiosis carcinomatosa 22.95 20.24 11 22388 1245 53325422
Glossodynia 22.58 20.24 7 22392 100284 53226383
Laryngeal papilloma 22.39 20.24 4 22395 9 53326658
Pneumothorax 22.36 20.24 30 22369 15477 53311190
Xerosis 21.97 20.24 9 22390 701 53325966
Asthenia 21.71 20.24 230 22169 343360 52983307
Toxicity to various agents 21.49 20.24 37 22362 219561 53107106
Weight decreased 21.29 20.24 170 22229 234778 53091889
Migraine 21.25 20.24 4 22395 80413 53246254
Discomfort 20.89 20.24 7 22392 95465 53231202
Metastases to breast 20.72 20.24 7 22392 317 53326350
Feeling abnormal 20.57 20.24 16 22383 135285 53191382
Iridocele 20.33 20.24 3 22396 0 53326667

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 5721.70 18.22 3308 17929 379209 32113080
Rash 902.77 18.22 877 20360 208456 32283833
Disease progression 771.05 18.22 554 20683 86308 32405981
Dermatitis acneiform 280.36 18.22 116 21121 5929 32486360
Malignant neoplasm progression 251.28 18.22 282 20955 78214 32414075
Diarrhoea 214.66 18.22 620 20617 364182 32128107
Neoplasm malignant 198.33 18.22 134 21103 18751 32473538
Lung neoplasm malignant 191.27 18.22 123 21114 15840 32476449
Non-small cell lung cancer 167.27 18.22 71 21166 3866 32488423
Dehydration 107.95 18.22 251 20986 128707 32363582
Metastases to central nervous system 98.78 18.22 62 21175 7646 32484643
Incorrect dose administered 92.16 18.22 114 21123 34914 32457375
Non-small cell lung cancer metastatic 87.78 18.22 27 21210 571 32491718
Lung adenocarcinoma 85.17 18.22 47 21190 4567 32487722
Interstitial lung disease 78.28 18.22 147 21090 64854 32427435
Haemoptysis 75.45 18.22 101 21136 33424 32458865
Drug resistance 67.35 18.22 79 21158 22886 32469403
Pancreatic carcinoma 64.31 18.22 49 21188 8257 32484032
Decreased appetite 63.79 18.22 240 20997 160573 32331716
Lung cancer metastatic 59.78 18.22 31 21206 2657 32489632
EGFR gene mutation 53.42 18.22 13 21224 108 32492181
Acne 53.32 18.22 48 21189 10194 32482095
Pleural effusion 52.54 18.22 141 21096 78851 32413438
Paronychia 49.07 18.22 29 21208 3208 32489081
Metastasis 48.32 18.22 30 21207 3627 32488662
Skin toxicity 42.30 18.22 28 21209 3778 32488511
Neoplasm progression 40.84 18.22 57 21180 19601 32472688
Toxicity to various agents 39.42 18.22 35 21202 178006 32314283
Metastases to lung 39.06 18.22 37 21200 8380 32483909
Drug ineffective 37.58 18.22 127 21110 383350 32108939
Product use in unapproved indication 37.52 18.22 6 21231 87198 32405091
Gastrointestinal perforation 37.02 18.22 26 21211 3864 32488425
Malignant pleural effusion 36.50 18.22 18 21219 1387 32490902
Product dose omission issue 36.20 18.22 11 21226 102564 32389725
Pancreatic carcinoma metastatic 35.82 18.22 24 21213 3305 32488984
Bradycardia 35.55 18.22 3 21234 71559 32420730
Pneumothorax 35.10 18.22 50 21187 17520 32474769
Lymphangiosis carcinomatosa 33.42 18.22 15 21222 934 32491355
Weight increased 33.32 18.22 7 21230 83656 32408633
Acute kidney injury 32.39 18.22 92 21145 293376 32198913
Metastases to liver 32.24 18.22 41 21196 12891 32479398
Dizziness 31.91 18.22 55 21182 209563 32282726
Metastases to bone 31.65 18.22 37 21200 10673 32481616
Pneumoperitoneum 31.60 18.22 18 21219 1858 32490431
Vomiting 31.60 18.22 262 20975 235295 32256994
Metastases to spine 30.03 18.22 19 21218 2374 32489915
Rash pustular 29.99 18.22 26 21211 5253 32487036
Drug hypersensitivity 29.52 18.22 6 21231 73394 32418895
Pneumonitis 27.72 18.22 61 21176 30073 32462216
Arthralgia 27.43 18.22 34 21203 148414 32343875
Plasma cell myeloma 27.07 18.22 3 21234 57611 32434678
Metastases to meninges 25.91 18.22 14 21223 1304 32490985
Pulmonary embolism 25.30 18.22 115 21122 83544 32408745
Stomatitis 24.91 18.22 70 21167 40159 32452130
Overdose 23.29 18.22 14 21223 87063 32405226
Hyperhidrosis 22.74 18.22 9 21228 71159 32421130
Growth of eyelashes 22.66 18.22 6 21231 72 32492217
Condition aggravated 22.63 18.22 42 21195 155619 32336670
Nausea 22.38 18.22 313 20924 320536 32171753
Tremor 21.84 18.22 13 21224 81264 32411025
Bronchial fistula 21.69 18.22 7 21230 174 32492115
Lung carcinoma cell type unspecified stage IV 21.66 18.22 9 21228 464 32491825
Oesophageal ulcer 21.49 18.22 18 21219 3470 32488819
Acquired gene mutation 21.10 18.22 12 21225 1235 32491054
Insomnia 20.69 18.22 21 21216 100327 32391962
Mucosal inflammation 20.52 18.22 58 21179 33376 32458913
Nasopharyngitis 20.49 18.22 8 21229 63779 32428510
Headache 19.81 18.22 64 21173 196133 32296156
Therapy partial responder 19.75 18.22 20 21217 4910 32487379
Blood pressure increased 19.54 18.22 14 21223 79340 32412949
Conjunctivitis 19.17 18.22 26 21211 8700 32483589
Rhabdomyolysis 19.16 18.22 10 21227 67255 32425034
Hypophagia 18.62 18.22 45 21192 23578 32468711

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
FDA EPC N0000175605 Kinase Inhibitor
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D047428 Protein Kinase Inhibitors
CHEBI has role CHEBI:35610 cytostatic
CHEBI has role CHEBI:37699 protein kinase inhibitors
CHEBI has role CHEBI:74440 EGFR inhibitor

Drug Use (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

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
Ephrin type-A receptor 5 Kinase Kd 6.15 CHEMBL
Tyrosine-protein kinase JAK3 Kinase Kd 6.15 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
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
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
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
Abelson tyrosine-protein kinase 2 Kinase Kd 6.70 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
8133 INN_ID
DB00530 DRUGBANK_ID
J4T82NDH7E UNII
176870 PUBCHEM_CID
337525 RXNORM
19073 MMSL
248186 MMSL
63773 MMSL
d05412 MMSL
008759 NDDF
008760 NDDF
414122006 SNOMEDCT_US
414123001 SNOMEDCT_US
426686007 SNOMEDCT_US
D000069347 MESH_DESCRIPTOR_UI
C1533491 UMLSCUI

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 46708-566 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 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 51991-891 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
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 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
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