cetuximab Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
chimeric origin 4954 205923-56-4

Description:

MoleculeDescription

Synonyms:

  • cetuximab
  • cetuximab (genetical recombination)
  • erbitux
  • C-225
  • IMC-C225
A chimeric monoclonal antibody that functions as an ANTINEOPLASTIC AGENT through its binding to the EPIDERMAL GROWTH FACTOR RECEPTOR, where it prevents the binding and signaling action of cell growth and survival factors.
  • Molecular weight:
  • Formula:
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA:
  • ALOGS:
  • ROTB: None

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
July 16, 2008 PMDA Merck
Feb. 12, 2004 FDA IMCLONE
June 29, 2004 EMA

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
Dermatitis acneiform 386.71 22.00 104 10697 3966 46671295
Diarrhoea 176.13 22.00 393 10408 559209 46116052
Mucosal inflammation 174.64 22.00 110 10691 38866 46636395
Dehydration 152.76 22.00 186 10615 159354 46515907
Neutropenia 152.01 22.00 176 10625 143028 46532233
Malignant neoplasm progression 142.82 22.00 119 10682 64807 46610454
Hypomagnesaemia 136.82 22.00 77 10724 22133 46653128
Rash 135.52 22.00 271 10530 356241 46319020
Infusion related reaction 116.79 22.00 130 10671 101078 46574183
Stomatitis 93.31 22.00 96 10705 68201 46607060
Paronychia 85.14 22.00 34 10767 4532 46670729
Drug ineffective 84.90 22.00 26 10775 677812 45997449
Vomiting 83.17 22.00 261 10540 452533 46222728
Disease progression 76.90 22.00 100 10701 91200 46584061
Radiation skin injury 72.49 22.00 20 10781 837 46674424
Hypokalaemia 64.33 22.00 90 10711 87934 46587327
Skin toxicity 63.95 22.00 26 10775 3628 46671633
Pulmonary embolism 60.77 22.00 98 10703 108487 46566774
Skin fissures 56.61 22.00 30 10771 7650 46667611
Nausea 56.33 22.00 309 10492 687145 45988116
Dermatitis 51.12 22.00 35 10766 14173 46661088
Pyrexia 48.03 22.00 183 10618 348619 46326642
Arthralgia 47.28 22.00 13 10788 364590 46310671
Metastases to lung 42.44 22.00 28 10773 10668 46664593
Febrile neutropenia 41.87 22.00 77 10724 94550 46580711
Palmar-plantar erythrodysaesthesia syndrome 37.82 22.00 34 10767 20417 46654844
Colorectal cancer metastatic 35.26 22.00 11 10790 709 46674552
Deep vein thrombosis 32.90 22.00 63 10738 79710 46595551
Trichomegaly 32.71 22.00 6 10795 35 46675226
Hypertrichosis 32.38 22.00 11 10790 929 46674332
Chills 31.51 22.00 69 10732 95963 46579298
Haematotoxicity 29.59 22.00 19 10782 6914 46668347
Renal tubular disorder 28.22 22.00 13 10788 2452 46672809
Thrombocytopenia 27.81 22.00 78 10723 126503 46548758
Multiple-drug resistance 27.73 22.00 13 10788 2552 46672709
Stress cardiomyopathy 27.58 22.00 19 10782 7765 46667496
Nail disorder 27.34 22.00 19 10782 7877 46667384
Rash pustular 27.15 22.00 18 10783 6911 46668350
Anastomotic leak 27.09 22.00 8 10793 428 46674833
Dyspnoea 26.75 22.00 207 10594 515341 46159920
Drug interaction 26.73 22.00 7 10794 203087 46472174
Skin reaction 25.97 22.00 21 10780 10925 46664336
Colon cancer metastatic 25.96 22.00 10 10791 1210 46674051
Drug hypersensitivity 25.93 22.00 12 10789 243813 46431448
Ileus 25.25 22.00 23 10778 14041 46661220
Hypocalcaemia 25.13 22.00 31 10770 26754 46648507
Weight increased 25.10 22.00 4 10797 164469 46510792
Anaemia 24.90 22.00 121 10680 255658 46419603
Dysphagia 24.73 22.00 55 10746 77257 46598004
Dry skin 24.25 22.00 38 10763 40978 46634283
Neutrophil count decreased 23.98 22.00 39 10762 43387 46631874
Abdominal pain 23.97 22.00 111 10690 229920 46445341
Interstitial lung disease 23.97 22.00 44 10757 53905 46621356
Anaphylactic reaction 23.19 22.00 43 10758 53069 46622192
Bone marrow failure 22.63 22.00 31 10770 29638 46645623
Leukopenia 22.29 22.00 49 10752 68294 46606967
Steatohepatitis 22.18 22.00 7 10794 469 46674792

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
Dermatitis acneiform 805.11 18.59 257 21929 5432 29924860
Infusion related reaction 466.56 18.59 319 21867 40245 29890047
Mucosal inflammation 433.85 18.59 274 21912 30220 29900072
Anaphylactic reaction 283.98 18.59 204 21982 27778 29902514
Hypomagnesaemia 273.70 18.59 164 22022 16434 29913858
Radiation skin injury 250.57 18.59 65 22121 625 29929667
Dehydration 248.70 18.59 376 21810 123163 29807129
Rash 245.22 18.59 477 21709 191412 29738880
Skin toxicity 231.30 18.59 88 22098 3161 29927131
Paronychia 194.53 18.59 76 22110 2935 29927357
Stomatitis 193.15 18.59 184 22002 37095 29893197
Malignant neoplasm progression 152.22 18.59 225 21961 72062 29858230
Drug ineffective 132.30 18.59 44 22142 340343 29589949
Dysphagia 115.73 18.59 174 22012 56524 29873768
Neutropenia 112.63 18.59 275 21911 128265 29802027
Acne 107.71 18.59 74 22112 9362 29920930
Chills 105.78 18.59 191 21995 72147 29858145
Hypotension 103.78 18.59 355 21831 200210 29730082
Hypersensitivity 97.93 18.59 157 22029 53871 29876421
Pharyngeal inflammation 94.98 18.59 26 22160 312 29929980
Diarrhoea 90.10 18.59 485 21701 333618 29596674
Drug interaction 80.54 18.59 24 22162 199544 29730748
Flushing 77.17 18.59 102 22084 29390 29900902
Skin fissures 75.50 18.59 41 22145 3398 29926894
Dermatitis 70.46 18.59 54 22132 8088 29922204
Vomiting 69.46 18.59 334 21852 219484 29710808
Radiation mucositis 63.05 18.59 15 22171 97 29930195
Erythema 61.72 18.59 160 22026 77291 29853001
Conjunctivitis 60.48 18.59 49 22137 7951 29922341
Nausea 59.91 18.59 400 21786 296557 29633735
Rash pustular 56.67 18.59 39 22147 4944 29925348
Arthralgia 55.33 18.59 16 22170 135775 29794517
Oxygen saturation decreased 53.87 18.59 107 22079 43333 29886959
Hypocalcaemia 52.95 18.59 72 22114 21304 29908988
Skin reaction 52.84 18.59 36 22150 4489 29925803
Palmar-plantar erythrodysaesthesia syndrome 52.78 18.59 60 22126 14810 29915482
Dyspnoea 52.37 18.59 423 21763 332872 29597420
Toxicity to various agents 51.53 18.59 34 22152 177149 29753143
Pulmonary embolism 50.92 18.59 150 22036 77985 29852307
Folliculitis 49.88 18.59 32 22154 3608 29926684
Fall 47.58 18.59 39 22147 181833 29748459
Pain in extremity 46.74 18.59 12 22174 110209 29820083
Pulse absent 46.70 18.59 36 22150 5437 29924855
Pyrexia 46.33 18.59 374 21812 294115 29636177
Decreased appetite 45.95 18.59 226 21960 149684 29780608
Anaphylactic shock 45.54 18.59 54 22132 13939 29916353
Pruritus 45.00 18.59 190 21996 118014 29812278
Device related infection 44.72 18.59 59 22127 16956 29913336
Febrile neutropenia 43.36 18.59 175 22011 106518 29823774
Dry skin 43.05 18.59 67 22119 22387 29907905
Product dose omission issue 42.85 18.59 8 22178 91623 29838669
Proteus infection 42.03 18.59 17 22169 719 29929573
Insomnia 41.87 18.59 9 22177 93327 29836965
Disease progression 41.64 18.59 142 22044 79732 29850560
Leukopenia 40.64 18.59 112 22074 56047 29874245
Alopecia 37.62 18.59 58 22128 19217 29911075
Gastrointestinal toxicity 36.09 18.59 21 22165 1987 29928305
Blood pressure immeasurable 35.34 18.59 16 22170 895 29929397
Pneumatosis intestinalis 35.26 18.59 23 22163 2667 29927625
Blood magnesium decreased 34.07 18.59 30 22156 5453 29924839
Urticaria 33.81 18.59 103 22083 54503 29875789
Ileus 33.49 18.59 49 22137 15506 29914786
Clostridial infection 33.48 18.59 25 22161 3600 29926692
Nail disorder 33.17 18.59 19 22167 1746 29928546
Condition aggravated 33.10 18.59 32 22154 137834 29792458
Neutrophil count decreased 33.05 18.59 87 22099 42367 29887925
Gait disturbance 31.96 18.59 8 22178 74769 29855523
Oesophagitis 31.33 18.59 40 22146 11131 29919161
Cardiac failure congestive 30.77 18.59 12 22174 84395 29845897
Interstitial lung disease 30.47 18.59 106 22080 60091 29870201
Myalgia 29.47 18.59 10 22176 76657 29853635
Rhabdomyolysis 28.77 18.59 6 22180 63574 29866718
Necrotising oesophagitis 28.43 18.59 11 22175 413 29929879
Colorectal cancer metastatic 27.87 18.59 14 22172 988 29929304
Nasopharyngitis 27.80 18.59 5 22181 58844 29871448
Blood pressure decreased 27.48 18.59 87 22099 46988 29883304
Cardio-respiratory arrest 27.36 18.59 99 22087 57207 29873085
Headache 27.31 18.59 59 22127 182247 29748045
Induration 26.91 18.59 13 22173 843 29929449
Weight increased 26.73 18.59 11 22175 74902 29855390
Coronary artery disease 26.33 18.59 3 22183 49709 29880583
Colon cancer metastatic 26.07 18.59 16 22170 1669 29928623
Thrombocytopenia 25.92 18.59 182 22004 136862 29793430
Neuropathy peripheral 25.78 18.59 112 22074 70363 29859929
Prothrombin level decreased 25.69 18.59 14 22172 1168 29929124
Pneumonitis 25.29 18.59 60 22126 27394 29902898
White blood cell count decreased 25.26 18.59 126 22060 83821 29846471
Peripheral swelling 25.21 18.59 7 22179 61067 29869225
Monocytopenia 24.64 18.59 7 22179 97 29930195
Laryngeal oedema 24.42 18.59 20 22166 3294 29926998
Embolism 24.39 18.59 28 22158 6981 29923311
Aspiration 23.82 18.59 34 22152 10517 29919775
Anxiety 23.80 18.59 19 22167 89852 29840440
Metastases to lung 23.30 18.59 29 22157 7866 29922426
Neoplasm progression 23.06 18.59 45 22141 17978 29912314
Depression 22.86 18.59 20 22166 90417 29839875
Hospitalisation 22.67 18.59 3 22183 44316 29885976
Anaphylactoid reaction 22.28 18.59 16 22170 2170 29928122
Influenza 22.05 18.59 3 22183 43395 29886897
Hypophagia 22.02 18.59 50 22136 22186 29908106
Hypokalaemia 21.70 18.59 84 22102 50108 29880184
Squamous cell carcinoma of head and neck 21.63 18.59 7 22179 154 29930138
Somnolence 21.47 18.59 24 22162 96739 29833553
Unresponsive to stimuli 21.43 18.59 55 22131 26364 29903928
Abdominal discomfort 21.27 18.59 5 22181 48786 29881506
Abdominal compartment syndrome 20.73 18.59 11 22175 870 29929422
Metastases to liver 20.59 18.59 34 22152 11931 29918361
Butterfly rash 20.56 18.59 6 22180 92 29930200
Cerebral ischaemia 20.29 18.59 24 22162 6176 29924116
Bronchospasm 20.02 18.59 31 22155 10307 29919985
Neutrophilia 19.89 18.59 18 22168 3389 29926903
Overdose 19.73 18.59 20 22166 84317 29845975
Cardiac disorder 19.70 18.59 3 22183 39890 29890402
Ileal perforation 19.63 18.59 10 22176 727 29929565
Death 19.61 18.59 170 22016 357113 29573179
Neurotoxicity 19.46 18.59 35 22151 13147 29917145
Odynophagia 19.08 18.59 20 22166 4507 29925785
Diabetes mellitus 18.83 18.59 4 22182 41861 29888431
Mucosal infection 18.83 18.59 7 22179 235 29930057
Pelvic sepsis 18.83 18.59 4 22182 14 29930278
Staphylococcal infection 18.68 18.59 57 22129 30167 29900125

Pharmacologic Action:

SourceCodeDescription
ATC L01XC06 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Monoclonal antibodies
FDA MoA N0000020010 HER1 Antagonists
FDA EPC N0000175664 Epidermal Growth Factor Receptor Antagonist
MeSH PA D000970 Antineoplastic Agents
MeSH PA D000074322 Antineoplastic Agents, Immunological

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Squamous cell carcinoma of mouth indication 307502000
Malignant tumor of colon indication 363406005 DOID:219
Squamous cell carcinoma of larynx indication 405822008
Squamous cell carcinoma of pharynx indication 408649007
Squamous cell carcinoma of nose indication 448930008

Acid dissociation constants calculated using MoKa v3.0.0

None

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 ANTIBODY BINDING Kd 9.41 IUPHAR DRUG LABEL

External reference:

IDSource
D03455 KEGG_DRUG
4021419 VUID
N0000148833 NUI
4021419 VANDF
C0995188 UMLSCUI
CHEMBL1201577 ChEMBL_ID
DB00002 DRUGBANK_ID
D000068818 MESH_DESCRIPTOR_UI
6882 IUPHAR_LIGAND_ID
7906 INN_ID
PQX0D8J21J UNII
318341 RXNORM
17947 MMSL
48970 MMSL
d05101 MMSL
008568 NDDF
409400001 SNOMEDCT_US
409401002 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
ERBITUX HUMAN PRESCRIPTION DRUG LABEL 1 66733-948 SOLUTION 2 mg INTRAVENOUS BLA 29 sections
ERBITUX HUMAN PRESCRIPTION DRUG LABEL 1 66733-958 SOLUTION 2 mg INTRAVENOUS BLA 29 sections