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:

None

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 9542.99 42.97 2664 4488 78804 2272129
Rash 2080.17 42.97 810 6342 58748 2292185
Diarrhoea 1966.14 42.97 856 6296 82708 2268225
Disease progression 1700.36 42.97 512 6640 16583 2334350
Malignant neoplasm progression 757.43 42.97 256 6896 11872 2339061
Nausea 555.24 42.97 419 6733 111770 2239163
Decreased appetite 508.26 42.97 245 6907 28646 2322287
Fatigue 481.93 42.97 345 6807 84528 2266405
Neoplasm malignant 445.25 42.97 139 7013 4954 2345979
Dry skin 432.48 42.97 145 7007 6507 2344426
Vomiting 414.80 42.97 295 6857 71307 2279626
Lung neoplasm malignant 405.17 42.97 115 7037 2927 2348006
Dehydration 391.34 42.97 189 6963 22106 2328827
Dermatitis acneiform 385.59 42.97 85 7067 724 2350209
Incorrect dose administered 343.50 42.97 135 7017 9560 2341373
Metastases to central nervous system 326.09 42.97 90 7062 2058 2348875
Dyspnoea 303.42 42.97 255 6897 78478 2272455
Asthenia 283.89 42.97 199 6953 46727 2304206
Pleural effusion 279.80 42.97 123 7029 11545 2339388
Anaemia 264.15 42.97 170 6982 34622 2316311
Pneumonia 259.13 42.97 192 6960 49104 2301829
Weight decreased 254.05 42.97 154 6998 28217 2322716
Non-small cell lung cancer 233.58 42.97 53 7099 520 2350413
Drug resistance 222.32 42.97 70 7082 2554 2348379
Stomatitis 218.68 42.97 98 7054 9612 2341321
Acne 185.61 42.97 64 7088 3112 2347821
Pulmonary embolism 174.20 42.97 103 7049 17980 2332953
Alopecia 170.36 42.97 109 7043 21892 2329041
Paronychia 160.30 42.97 42 7110 780 2350153
Lung adenocarcinoma 151.26 42.97 39 7113 678 2350255
Dysphagia 150.27 42.97 83 7069 12722 2338211
Respiratory failure 148.71 42.97 84 7068 13444 2337489
Haemoptysis 142.09 42.97 54 7098 3473 2347460
Interstitial lung disease 141.99 42.97 68 7084 7744 2343189
Cough 140.86 42.97 114 7038 33003 2317930
Lung cancer metastatic 138.46 42.97 34 7118 480 2350453
Skin exfoliation 135.26 42.97 60 7092 5730 2345203
Metastasis 127.64 42.97 36 7116 890 2350043
Haemoglobin decreased 125.93 42.97 84 7068 18067 2332866
Pancreatic carcinoma metastatic 125.69 42.97 31 7121 446 2350487
Metastases to liver 125.61 42.97 47 7105 2894 2348039
Skin fissures 125.47 42.97 38 7114 1213 2349720
Constipation 121.69 42.97 88 7064 21541 2329392
Pyrexia 119.76 42.97 129 7023 53579 2297354
Hair growth abnormal 114.23 42.97 30 7122 562 2350371
Epistaxis 113.62 42.97 63 7089 9716 2341217
Metastases to bone 106.98 42.97 39 7113 2230 2348703
Abdominal pain 106.91 42.97 99 7053 34275 2316658
Malaise 104.20 42.97 122 7030 55463 2295470
Non-small cell lung cancer metastatic 103.54 42.97 21 7131 113 2350820
Pain 103.28 42.97 128 7024 61729 2289204
Eye irritation 100.42 42.97 42 7110 3470 2347463
Pruritus 99.88 42.97 106 7046 43234 2307699
Off label use 96.14 42.97 135 7017 73463 2277470
Dry eye 95.61 42.97 42 7110 3914 2347019
Malignant pleural effusion 94.63 42.97 24 7128 389 2350544
Drug ineffective 92.92 42.97 158 6994 101466 2249467
Blood bilirubin increased 92.47 42.97 45 7107 5300 2345633
Neoplasm progression 92.04 42.97 43 7109 4625 2346308
Hypoxia 85.96 42.97 45 7107 6182 2344751
Confusional state 79.30 42.97 72 7080 24272 2326661
Skin ulcer 78.81 42.97 37 7115 4022 2346911
Multiple-drug resistance 75.46 42.97 18 7134 223 2350710
Mental status changes 73.25 42.97 39 7113 5543 2345390
Mucosal inflammation 72.81 42.97 38 7114 5186 2345747
Acute kidney injury 72.30 42.97 73 7079 28049 2322884
General physical health deterioration 71.52 42.97 54 7098 14085 2336848
Urinary tract infection 70.26 42.97 74 7078 29868 2321065
Skin disorder 70.19 42.97 33 7119 3598 2347335
Hypophagia 70.15 42.97 34 7118 3966 2346967
Pneumonitis 69.84 42.97 34 7118 4005 2346928
Conjunctivitis 69.69 42.97 29 7123 2364 2348569
Metastatic neoplasm 68.44 42.97 21 7131 700 2350233
Metastases to lung 67.88 42.97 26 7126 1705 2349228
Hypokalaemia 65.96 42.97 46 7106 10608 2340325
Pancreatic carcinoma 65.27 42.97 24 7128 1405 2349528
Platelet count decreased 64.07 42.97 53 7099 15760 2335173
Sepsis 62.78 42.97 56 7096 18432 2332501
Dyspepsia 59.77 42.97 42 7110 9802 2341131
Thrombocytopenia 59.19 42.97 55 7097 19076 2331857
Skin toxicity 58.34 42.97 19 7133 771 2350162
Gastrooesophageal reflux disease 58.01 42.97 40 7112 9055 2341878
Onychoclasis 57.11 42.97 19 7133 825 2350108
Erythema 56.91 42.97 61 7091 25098 2325835
Dermatitis 56.63 42.97 25 7127 2355 2348578
Infection 56.09 42.97 52 7100 17977 2332956
Pericardial effusion 55.40 42.97 29 7123 3980 2346953
Metastases to meninges 52.85 42.97 15 7137 379 2350554
Rash pustular 52.50 42.97 21 7131 1546 2349387
Hair texture abnormal 52.24 42.97 16 7136 530 2350403
Deep vein thrombosis 51.66 42.97 43 7109 12889 2338044
Growth of eyelashes 51.50 42.97 11 7141 79 2350854
Pulmonary oedema 50.80 42.97 34 7118 7329 2343604
Chronic obstructive pulmonary disease 49.60 42.97 33 7119 7044 2343889
Hyponatraemia 48.50 42.97 42 7110 13283 2337650
Oesophagitis 47.49 42.97 21 7131 1985 2348948
Hypotension 47.48 42.97 63 7089 32373 2318560
Blood alkaline phosphatase increased 47.03 42.97 31 7121 6514 2344419
Gastrointestinal haemorrhage 46.89 42.97 40 7112 12395 2338538
Aspartate aminotransferase increased 46.40 42.97 40 7112 12572 2338361
Blister 46.08 42.97 31 7121 6740 2344193
Acquired gene mutation 45.91 42.97 11 7141 139 2350794
Performance status decreased 45.88 42.97 15 7137 616 2350317
Eye pruritus 45.84 42.97 22 7130 2509 2348424
Sudden death 45.74 42.97 20 7132 1840 2349093
Back pain 45.59 42.97 61 7091 31598 2319335
Hypomagnesaemia 45.57 42.97 22 7130 2542 2348391
Fall 45.19 42.97 75 7077 47024 2303909
Cholangitis 44.81 42.97 16 7136 860 2350073
Pneumothorax 44.64 42.97 21 7131 2291 2348642
Neutrophil count decreased 44.53 42.97 30 7122 6537 2344396
Metastases to spine 44.36 42.97 13 7139 369 2350564
Dysgeusia 44.29 42.97 33 7119 8426 2342507
Neoplasm 44.21 42.97 17 7135 1126 2349807
Rash pruritic 43.08 42.97 31 7121 7504 2343429
Hirsutism 42.98 42.97 12 7140 285 2350648

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 10141.86 46.66 3170 4179 84273 1655159
Rash 2001.26 46.66 810 6539 37883 1701549
Disease progression 1367.68 46.66 496 6853 16767 1722665
Diarrhoea 983.59 46.66 554 6795 53298 1686134
Neoplasm malignant 480.64 46.66 161 7188 4178 1735254
Malignant neoplasm progression 462.50 46.66 217 7132 13941 1725491
Dehydration 446.00 46.66 227 7122 17431 1722001
Dermatitis acneiform 376.37 46.66 97 7252 955 1738477
Decreased appetite 363.61 46.66 220 7129 23651 1715781
Lung neoplasm malignant 332.22 46.66 113 7236 3066 1736366
Nausea 305.28 46.66 267 7082 50929 1688503
Pneumonia 291.68 46.66 249 7100 45933 1693499
Fatigue 285.04 46.66 256 7093 50525 1688907
Dyspnoea 279.56 46.66 256 7093 51803 1687629
Non-small cell lung cancer 271.00 46.66 68 7281 594 1738838
Interstitial lung disease 250.99 46.66 127 7222 9569 1729863
Vomiting 250.64 46.66 211 7138 38104 1701328
Haemoptysis 223.62 46.66 95 7254 4781 1734651
Pleural effusion 223.58 46.66 123 7226 10987 1728445
Incorrect dose administered 212.21 46.66 104 7245 7305 1732127
Asthenia 206.30 46.66 181 7168 34489 1704943
Anaemia 185.65 46.66 159 7190 29298 1710134
Off label use 180.24 46.66 176 7173 38395 1701037
Pulmonary embolism 176.97 46.66 112 7237 12947 1726485
Pyrexia 173.92 46.66 188 7161 46212 1693220
Respiratory failure 173.46 46.66 115 7234 14390 1725042
Weight decreased 149.72 46.66 126 7223 22627 1716805
General physical health deterioration 142.43 46.66 98 7251 13020 1726412
Metastases to central nervous system 142.20 46.66 50 7299 1495 1737937
Constipation 137.35 46.66 101 7248 14899 1724533
Abdominal pain 131.12 46.66 114 7235 21376 1718056
Haemoglobin decreased 123.39 46.66 100 7249 17014 1722418
Stomatitis 122.98 46.66 65 7284 5339 1734093
Lung adenocarcinoma 117.74 46.66 36 7313 684 1738748
Lung cancer metastatic 117.23 46.66 34 7315 534 1738898
Non-small cell lung cancer metastatic 116.54 46.66 25 7324 98 1739334
Acne 116.45 46.66 45 7304 1763 1737669
Drug resistance 115.87 46.66 53 7296 3177 1736255
Cough 113.37 46.66 100 7249 19097 1720335
Neoplasm progression 112.17 46.66 52 7297 3215 1736217
Pneumonitis 103.21 46.66 52 7297 3863 1735569
Mucosal inflammation 103.01 46.66 53 7296 4116 1735316
Pancreatic carcinoma 93.73 46.66 38 7311 1691 1737741
Hypoxia 87.85 46.66 54 7295 5909 1733523
Metastases to liver 87.00 46.66 39 7310 2228 1737204
Dry skin 85.42 46.66 45 7304 3667 1735765
Pneumothorax 83.35 46.66 40 7309 2672 1736760
Epistaxis 82.93 46.66 59 7290 8247 1731185
Pancreatic carcinoma metastatic 80.93 46.66 26 7323 584 1738848
Hypophagia 79.35 46.66 42 7307 3455 1735977
Blood bilirubin increased 78.38 46.66 51 7298 6159 1733273
Pain 77.54 46.66 95 7254 26562 1712870
Malaise 77.47 46.66 100 7249 29465 1709967
Metastasis 76.63 46.66 27 7322 811 1738621
Dysphagia 74.43 46.66 60 7289 10108 1729324
Hyponatraemia 74.26 46.66 57 7292 8943 1730489
Paronychia 74.00 46.66 24 7325 556 1738876
Gastrointestinal haemorrhage 73.71 46.66 69 7280 14198 1725234
Metastases to lung 70.58 46.66 30 7319 1505 1737927
Metastases to bone 70.21 46.66 31 7318 1707 1737725
Skin toxicity 69.23 46.66 23 7326 576 1738856
Metastases to spine 66.56 46.66 20 7329 357 1739075
Thrombocytopenia 58.96 46.66 74 7275 21175 1718257
Malignant pleural effusion 57.96 46.66 17 7332 278 1739154
Platelet count decreased 56.47 46.66 64 7285 16459 1722973
Oedema peripheral 56.17 46.66 62 7287 15488 1723944
Lung disorder 54.88 46.66 38 7311 5081 1734351
Ascites 54.17 46.66 39 7310 5547 1733885
Confusional state 54.15 46.66 71 7278 21207 1718225
Rash pustular 53.97 46.66 23 7326 1161 1738271
Deep vein thrombosis 53.18 46.66 49 7300 9871 1729561
Intestinal obstruction 52.24 46.66 32 7317 3475 1735957
International normalised ratio increased 50.43 46.66 44 7305 8255 1731177
Conjunctivitis 49.96 46.66 24 7325 1605 1737827
Lymphangiosis carcinomatosa 48.60 46.66 14 7335 214 1739218
Aspartate aminotransferase increased 47.96 46.66 48 7301 10708 1728724
Skin exfoliation 47.06 46.66 33 7316 4502 1734930
Hypotension 46.71 46.66 79 7270 29575 1709857

Pharmacologic Action:

SourceCodeDescription
ATC L01XE03 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
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 antineoplastic agent

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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 100MG BASE TARCEVA OSI PHARMS N021743 Nov. 18, 2004 RX TABLET ORAL 6900221 Nov. 9, 2020 FIRST-LINE TREATMENT OF LOCALLY ADVANCED UNRESECTABLE OR METASTATIC PANCREATIC CANCER, IN COMBINATION WITH GEMCITABINE
EQ 100MG BASE TARCEVA OSI PHARMS N021743 Nov. 18, 2004 RX TABLET ORAL 6900221 Nov. 9, 2020 FIRST-LINE TREATMENT OF METASTATIC NON SMALL-CELL LUNG CANCER (NSCLC) WITH EGFR EXON 19 DELETIONS OR EXON 21 (L858R) SUBSTITUTION MUTATIONS AS DETECTED BY AN FDA-APPROVED TEST
EQ 100MG BASE TARCEVA OSI PHARMS N021743 Nov. 18, 2004 RX TABLET ORAL 6900221 Nov. 9, 2020 MAINTENANCE TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC NSCLC WHOSE DISEASE HAS NOT PROGRESSED AFTER FOUR CYCLES PLATINUM-BASED CHEMOTHERAPY
EQ 100MG BASE TARCEVA OSI PHARMS N021743 Nov. 18, 2004 RX TABLET ORAL 6900221 Nov. 9, 2020 TREATMENT OF LOCALLY ADVANCED OR METASTATIC NON SMALL-CELL LUNG CANCER (NSCLC) AFTER FAILURE OF AT LEAST ONE PRIOR CHEMOTHERAPY REGIMEN
EQ 100MG BASE TARCEVA OSI PHARMS N021743 Nov. 18, 2004 RX TABLET ORAL 7087613 Nov. 9, 2020 FIRST-LINE TREATMENT OF METASTATIC NON SMALL-CELL LUNG CANCER (NSCLC) WITH EGFR EXON 19 DELETIONS OR EXON 21 (L858R) SUBSTITUTION MUTATIONS AS DETECTED BY AN FDA-APPROVED TEST
EQ 100MG BASE TARCEVA OSI PHARMS N021743 Nov. 18, 2004 RX TABLET ORAL 7087613 Nov. 9, 2020 MAINTENANCE TREATMENT IN PATIENTS WITH LOCALLY ADVANCED OR METASTATIC NSCLC WHO HAVE NOT PROGRESSED ON 1ST-LINE TREATMENT WTH PLATINUM-BASED CHEMOTHERAPY
EQ 100MG BASE TARCEVA OSI PHARMS N021743 Nov. 18, 2004 RX TABLET ORAL 7087613 Nov. 9, 2020 TREATMENT OF LOCALLY ADVANCED OR METASTATIC NON SMALL-CELL LUNG CANCER (NSCLC) AFTER FAILURE OF AT LEAST ONE PRIOR CHEMOTHERAPY REGIMEN
EQ 150MG BASE TARCEVA OSI PHARMS N021743 Nov. 18, 2004 RX TABLET ORAL 6900221 Nov. 9, 2020 FIRST-LINE TREATMENT OF LOCALLY ADVANCED UNRESECTABLE OR METASTATIC PANCREATIC CANCER, IN COMBINATION WITH GEMCITABINE
EQ 150MG BASE TARCEVA OSI PHARMS N021743 Nov. 18, 2004 RX TABLET ORAL 6900221 Nov. 9, 2020 FIRST-LINE TREATMENT OF METASTATIC NON SMALL-CELL LUNG CANCER (NSCLC) WITH EGFR EXON 19 DELETIONS OR EXON 21 (L858R) SUBSTITUTION MUTATIONS AS DETECTED BY AN FDA-APPROVED TEST
EQ 150MG BASE TARCEVA OSI PHARMS N021743 Nov. 18, 2004 RX TABLET ORAL 6900221 Nov. 9, 2020 MAINTENANCE TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC NSCLC WHOSE DISEASE HAS NOT PROGRESSED AFTER FOUR CYCLES PLATINUM-BASED CHEMOTHERAPY
EQ 150MG BASE TARCEVA OSI PHARMS N021743 Nov. 18, 2004 RX TABLET ORAL 6900221 Nov. 9, 2020 TREATMENT OF LOCALLY ADVANCED OR METASTATIC NON SMALL-CELL LUNG CANCER (NSCLC) AFTER FAILURE OF AT LEAST ONE PRIOR CHEMOTHERAPY REGIMEN
EQ 150MG BASE TARCEVA OSI PHARMS N021743 Nov. 18, 2004 RX TABLET ORAL 7087613 Nov. 9, 2020 FIRST-LINE TREATMENT OF METASTATIC NON SMALL-CELL LUNG CANCER (NSCLC) WITH EGFR EXON 19 DELETIONS OR EXON 21 (L858R) SUBSTITUTION MUTATIONS AS DETECTED BY AN FDA-APPROVED TEST
EQ 150MG BASE TARCEVA OSI PHARMS N021743 Nov. 18, 2004 RX TABLET ORAL 7087613 Nov. 9, 2020 MAINTENANCE TREATMENT IN PATIENTS WITH LOCALLY ADVANCED OR METASTATIC NSCLC WHO HAVE NOT PROGRESSED ON 1ST-LINE TREATMENT WTH PLATINUM-BASED CHEMOTHERAPY
EQ 150MG BASE TARCEVA OSI PHARMS N021743 Nov. 18, 2004 RX TABLET ORAL 7087613 Nov. 9, 2020 TREATMENT OF LOCALLY ADVANCED OR METASTATIC NON SMALL-CELL LUNG CANCER (NSCLC) AFTER FAILURE OF AT LEAST ONE PRIOR CHEMOTHERAPY REGIMEN
EQ 25MG BASE TARCEVA OSI PHARMS N021743 Nov. 18, 2004 RX TABLET ORAL 6900221 Nov. 9, 2020 FIRST-LINE TREATMENT OF LOCALLY ADVANCED UNRESECTABLE OR METASTATIC PANCREATIC CANCER, IN COMBINATION WITH GEMCITABINE
EQ 25MG BASE TARCEVA OSI PHARMS N021743 Nov. 18, 2004 RX TABLET ORAL 6900221 Nov. 9, 2020 FIRST-LINE TREATMENT OF METASTATIC NON SMALL-CELL LUNG CANCER (NSCLC) WITH EGFR EXON 19 DELETIONS OR EXON 21 (L858R) SUBSTITUTION MUTATIONS AS DETECTED BY AN FDA-APPROVED TEST
EQ 25MG BASE TARCEVA OSI PHARMS N021743 Nov. 18, 2004 RX TABLET ORAL 6900221 Nov. 9, 2020 MAINTENANCE TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC NSCLC WHOSE DISEASE HAS NOT PROGRESSED AFTER FOUR CYCLES PLATINUM-BASED CHEMOTHERAPY
EQ 25MG BASE TARCEVA OSI PHARMS N021743 Nov. 18, 2004 RX TABLET ORAL 6900221 Nov. 9, 2020 TREATMENT OF LOCALLY ADVANCED OR METASTATIC NON SMALL-CELL LUNG CANCER (NSCLC) AFTER FAILURE OF AT LEAST ONE PRIOR CHEMOTHERAPY REGIMEN
EQ 25MG BASE TARCEVA OSI PHARMS N021743 Nov. 18, 2004 RX TABLET ORAL 7087613 Nov. 9, 2020 FIRST-LINE TREATMENT OF METASTATIC NON SMALL-CELL LUNG CANCER (NSCLC) WITH EGFR EXON 19 DELETIONS OR EXON 21 (L858R) SUBSTITUTION MUTATIONS AS DETECTED BY AN FDA-APPROVED TEST
EQ 25MG BASE TARCEVA OSI PHARMS N021743 Nov. 18, 2004 RX TABLET ORAL 7087613 Nov. 9, 2020 MAINTENANCE TREATMENT IN PATIENTS WITH LOCALLY ADVANCED OR METASTATIC NSCLC WHO HAVE NOT PROGRESSED ON 1ST-LINE TREATMENT WTH PLATINUM-BASED CHEMOTHERAPY
EQ 25MG BASE TARCEVA OSI PHARMS N021743 Nov. 18, 2004 RX TABLET ORAL 7087613 Nov. 9, 2020 TREATMENT OF LOCALLY ADVANCED OR METASTATIC NON SMALL-CELL LUNG CANCER (NSCLC) AFTER FAILURE OF AT LEAST ONE PRIOR CHEMOTHERAPY REGIMEN

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
Mitogen-activated protein kinase 10 Kinase Kd 5.37 CHEMBL
Receptor-type tyrosine-protein kinase FLT3 Kinase Kd 6.89 CHEMBL
Tyrosine-protein kinase ABL1 Kinase Kd 7.24 CHEMBL
Serine/threonine-protein kinase MRCK gamma Kinase Kd 5.47 CHEMBL
Vascular endothelial growth factor receptor 1 Kinase Kd 5.36 CHEMBL
Mitogen-activated protein kinase 9 Kinase Kd 5.70 CHEMBL
G protein-coupled receptor kinase 4 Kinase Kd 5.14 CHEMBL
Vascular endothelial growth factor receptor 2 Kinase Kd 5.24 CHEMBL
Proto-oncogene tyrosine-protein kinase Src Kinase Kd 6.15 CHEMBL
Mitogen-activated protein kinase kinase kinase 2 Kinase Kd 5.60 CHEMBL
Serine/threonine-protein kinase ULK3 Kinase Kd 6.04 CHEMBL
Abelson tyrosine-protein kinase 2 Kinase Kd 6.70 CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 2 Kinase Kd 5.89 CHEMBL
Platelet-derived growth factor receptor alpha Kinase Kd 5.74 CHEMBL
Tyrosine-protein kinase Blk Kinase Kd 6.72 CHEMBL
Hepatocyte growth factor receptor Kinase Kd 5.96 CHEMBL
Casein kinase I isoform epsilon Kinase Kd 6.30 CHEMBL
Receptor tyrosine-protein kinase erbB-3 Kinase Kd 5.96 CHEMBL
Ephrin type-B receptor 6 Kinase Kd 5.77 CHEMBL
Receptor-interacting serine/threonine-protein kinase 2 Kinase Kd 6.39 CHEMBL
Ephrin type-B receptor 4 Kinase Kd 5.66 CHEMBL
Tyrosine-protein kinase JAK2 Kinase Kd 5.43 CHEMBL
Serine/threonine-protein kinase SIK2 Kinase Kd 5.59 CHEMBL
Cyclin-G-associated kinase Kinase Kd 8.51 CHEMBL
Serine/threonine-protein kinase SBK1 Kinase Kd 5.92 CHEMBL
Aurora kinase A Kinase Kd 5.66 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 5 Kinase Kd 7.02 CHEMBL
Casein kinase I isoform delta Kinase Kd 5.46 CHEMBL
Interferon-induced, double-stranded RNA-activated protein kinase Kinase Kd 5.89 CHEMBL
Mitogen-activated protein kinase 4 Kinase Kd 5.60 CHEMBL
Serine/threonine-protein kinase TBK1 Kinase Kd 5.51 CHEMBL
Vascular endothelial growth factor receptor 3 Kinase Kd 5.68 CHEMBL
AarF domain-containing protein kinase 4 Kinase Kd 5.60 CHEMBL
MAP kinase-interacting serine/threonine-protein kinase 1 Kinase Kd 6.16 CHEMBL
Tyrosine-protein kinase Fgr Kinase Kd 5.96 CHEMBL
Death-associated protein kinase 3 Kinase Kd 5.22 CHEMBL
Tyrosine-protein kinase FRK Kinase Kd 5.70 CHEMBL
Ephrin type-A receptor 8 Kinase Kd 6.03 CHEMBL
Dual specificity protein kinase TTK Kinase Kd 5.43 CHEMBL
Tyrosine-protein kinase receptor Tie-1 Kinase Kd 6.07 CHEMBL
Ephrin type-A receptor 3 Kinase Kd 5.62 CHEMBL
Serine/threonine-protein kinase 10 Kinase Kd 7.72 CHEMBL
Serine/threonine-protein kinase 17B Kinase Kd 5.03 CHEMBL
Serine/threonine-protein kinase PLK4 Kinase Kd 5.72 CHEMBL
AP2-associated protein kinase 1 Kinase Kd 5.92 CHEMBL
Tyrosine-protein kinase JAK3 Kinase Kd 6.15 CHEMBL
Eukaryotic translation initiation factor 2-alpha kinase 4 Kinase Kd 5.36 CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret Kinase Kd 6.48 CHEMBL
Myotonin-protein kinase Kinase Kd 5.54 CHEMBL
Epithelial discoidin domain-containing receptor 1 Kinase Kd 6.10 CHEMBL
Tyrosine-protein kinase receptor TYRO3 Kinase Kd 5.41 CHEMBL
Tyrosine-protein kinase Yes Kinase Kd 5.66 CHEMBL
Tyrosine-protein kinase Lck Kinase Kd 6.60 CHEMBL
Myosin light chain kinase 2, skeletal/cardiac muscle Kinase Kd 6.01 CHEMBL
Leukocyte tyrosine kinase receptor Kinase Kd 6.05 CHEMBL
Mitogen-activated protein kinase kinase kinase 19 Kinase Kd 7.60 CHEMBL
Tyrosine-protein kinase CSK Kinase Kd 5.02 CHEMBL
Tyrosine-protein kinase receptor UFO Kinase Kd 5.40 CHEMBL
Serine/threonine-protein kinase TNNI3K Kinase Kd 6.24 CHEMBL
Receptor tyrosine-protein kinase erbB-2 Kinase Kd 5.54 CHEMBL
Tyrosine-protein kinase HCK Kinase Kd 5.74 CHEMBL
Aurora kinase C Kinase Kd 6.22 CHEMBL
SRSF protein kinase 3 Kinase Kd 5.08 CHEMBL
Tyrosine-protein kinase TXK Kinase Kd 5.42 CHEMBL
Platelet-derived growth factor receptor beta Kinase Kd 5.85 CHEMBL
Fibroblast growth factor receptor 2 Kinase Kd 5.72 CHEMBL
ALK tyrosine kinase receptor Kinase Kd 5.92 CHEMBL
Citron Rho-interacting kinase Kinase Kd 6.17 CHEMBL
Homeodomain-interacting protein kinase 4 Kinase Kd 6.02 CHEMBL
Chaperone activity of bc1 complex-like, mitochondrial Kinase Kd 5.72 CHEMBL
Mitogen-activated protein kinase kinase kinase 3 Kinase Kd 5.64 CHEMBL
Misshapen-like kinase 1 Kinase Kd 5.89 CHEMBL
Leucine-rich repeat serine/threonine-protein kinase 2 Kinase Kd 5.54 CHEMBL
Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma Kinase Kd 6 CHEMBL
Serine/threonine-protein kinase 36 Kinase Kd 5.36 CHEMBL
Mast/stem cell growth factor receptor Kit Kinase Kd 5.89 CHEMBL
Receptor tyrosine-protein kinase erbB-4 Kinase Kd 6.64 CHEMBL
BMP-2-inducible protein kinase Kinase Kd 5.92 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
Calcium/calmodulin-dependent protein kinase type II subunit delta Kinase Kd 5.19 CHEMBL
Ribosomal protein S6 kinase alpha-4 Kinase Kd 5.15 CHEMBL
Aurora kinase B 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
Non-receptor tyrosine-protein kinase TYK2 Kinase Kd 5.62 CHEMBL
Ephrin type-A receptor 7 Kinase Kd 5.85 CHEMBL
Receptor-interacting serine/threonine-protein kinase 4 Kinase Kd 5.31 CHEMBL
Tyrosine-protein kinase Lyn Kinase Kd 6.28 CHEMBL
Ephrin type-A receptor 5 Kinase Kd 6.15 CHEMBL
Tyrosine-protein kinase Mer Kinase Kd 6.01 CHEMBL
Ephrin type-B receptor 1 Kinase Kd 5.96 CHEMBL
Non-receptor tyrosine-protein kinase TNK1 Kinase Kd 6.20 CHEMBL
Solute carrier organic anion transporter family member 2B1 Unclassified INHIBITOR Ki 6.28 IUPHAR
Tubulin alpha-1A chain Structural Kd 6.64 CHEMBL
Serine/threonine-protein kinase ULK3 Kinase Kd 6.20 CHEMBL

External reference:

IDSource
D000069347 MESH_DESCRIPTOR_UI
C1533491 UMLSCUI
D04023 KEGG_DRUG
414122006 SNOMEDCT_US
248186 MMSL
414123001 SNOMEDCT_US
4021511 VANDF
337525 RXNORM
19073 MMSL
d05412 MMSL
008759 NDDF
DA87705X9K UNII
183319-69-9 SECONDARY_CAS_RN
CHEMBL553 ChEMBL_ID
DB00530 DRUGBANK_ID
CHEMBL1079742 ChEMBL_ID
8133 INN_ID
AQ4 PDB_CHEM_ID
CHEBI:114785 CHEBI
176870 PUBCHEM_CID
4920 IUPHAR_LIGAND_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 0093-7663 TABLET, FILM COATED 100 mg ORAL ANDA 16 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 0093-7664 TABLET, FILM COATED 150 mg ORAL ANDA 16 sections
Erlotinib Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0378-7131 TABLET, FILM COATED 25 mg ORAL ANDA 16 sections
Erlotinib Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0378-7132 TABLET, FILM COATED 100 mg ORAL ANDA 16 sections
Erlotinib Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0378-7133 TABLET, FILM COATED 150 mg ORAL ANDA 16 sections
Erlotinib Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42292-051 TABLET, FILM COATED 25 mg ORAL ANDA 16 sections
Erlotinib Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42292-052 TABLET, FILM COATED 100 mg ORAL ANDA 16 sections
Erlotinib Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42292-053 TABLET, FILM COATED 150 mg ORAL ANDA 16 sections
TARCEVA HUMAN PRESCRIPTION DRUG LABEL 1 50242-062 TABLET 25 mg ORAL NDA 17 sections
TARCEVA HUMAN PRESCRIPTION DRUG LABEL 1 50242-063 TABLET 100 mg ORAL NDA 17 sections
TARCEVA HUMAN PRESCRIPTION DRUG LABEL 1 50242-064 TABLET 150 mg ORAL NDA 17 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 51991-890 TABLET, FILM COATED 25 mg ORAL ANDA 18 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 51991-891 TABLET, FILM COATED 100 mg ORAL ANDA 18 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 51991-892 TABLET, FILM COATED 150 mg ORAL ANDA 18 sections
Tarceva HUMAN PRESCRIPTION DRUG LABEL 1 54868-5290 TABLET 25 mg ORAL NDA 18 sections
Tarceva HUMAN PRESCRIPTION DRUG LABEL 1 54868-5447 TABLET 150 mg ORAL NDA 18 sections
Tarceva HUMAN PRESCRIPTION DRUG LABEL 1 54868-5474 TABLET 100 mg ORAL NDA 18 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 59923-725 TABLET, FILM COATED 25 mg ORAL ANDA 15 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 59923-726 TABLET, FILM COATED 100 mg ORAL ANDA 15 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 59923-727 TABLET, FILM COATED 150 mg ORAL ANDA 15 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 63304-095 TABLET, FILM COATED 25 mg ORAL ANDA 17 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 63304-096 TABLET, FILM COATED 100 mg ORAL ANDA 17 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 63304-135 TABLET, FILM COATED 150 mg ORAL ANDA 17 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 68382-913 TABLET 25 mg ORAL ANDA 17 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 68382-914 TABLET 100 mg ORAL ANDA 17 sections
Erlotinib HUMAN PRESCRIPTION DRUG LABEL 1 68382-915 TABLET 150 mg ORAL ANDA 17 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 HUMAN PRESCRIPTION DRUG LABEL 1 72485-217 TABLET, FILM COATED 25 mg ORAL ANDA 16 sections