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

Stem definition	Drug id	CAS RN
chimeric origin	4954	205923-56-4

Description:

Molecule	Description
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

Molecule

Description

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:

Date	Agency	Company
July 16, 2008	PMDA	Merck
Feb. 12, 2004	FDA	IMCLONE
June 29, 2004	EMA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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:

Source	Code	Description
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)

Disease	Relation	SNOMED_ID	DOID
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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Epidermal growth factor receptor	Kinase	P00533	EGFR_HUMAN	ANTIBODY BINDING	Kd	9.41		IUPHAR	DRUG LABEL

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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