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

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	1045	183321-74-6

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
0.15	g	O

ADMET properties:

Property	Value	Reference
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 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:

Date	Agency	Company	Orphan
Nov. 18, 2004	FDA	OSI PHARMS

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
Death	5758.85	19.10	2778	19551	322601	50260194
Disease progression	932.32	19.10	559	21770	95307	50487488
Rash	688.47	19.10	899	21430	436572	50146223
Diarrhoea	556.80	19.10	953	21376	587523	49995272
Malignant neoplasm progression	464.05	19.10	318	22011	67806	50514989
Dermatitis acneiform	365.78	19.10	115	22214	3942	50578853
Drug resistance	240.66	19.10	132	22197	18857	50563938
Dry skin	202.07	19.10	161	22168	43030	50539765
Metastases to central nervous system	196.23	19.10	97	22232	11185	50571610
Paronychia	169.92	19.10	67	22262	4497	50578298
Neoplasm malignant	154.77	19.10	108	22221	23607	50559188
Incorrect dose administered	152.48	19.10	144	22185	48270	50534525
Decreased appetite	118.97	19.10	269	22060	200654	50382141
EGFR gene mutation	104.83	19.10	24	22305	231	50582564
Acne	91.47	19.10	73	22256	19522	50563273
Pleural effusion	86.55	19.10	140	22189	81314	50501481
Lung cancer metastatic	86.51	19.10	34	22295	2261	50580534
Lung neoplasm malignant	86.09	19.10	64	22265	15420	50567375
Acquired gene mutation	85.18	19.10	26	22303	805	50581990
Metastasis	83.21	19.10	40	22289	4335	50578460
Dehydration	78.05	19.10	193	22136	152256	50430539
Drug hypersensitivity	76.94	19.10	10	22319	251000	50331795
Hair growth abnormal	76.14	19.10	32	22297	2529	50580266
Joint swelling	74.63	19.10	10	22319	245276	50337519
Arthralgia	71.07	19.10	54	22275	438648	50144147
Headache	61.78	19.10	80	22249	506455	50076340
Rash pustular	58.07	19.10	36	22293	6445	50576350
Skin fissures	57.75	19.10	40	22289	8628	50574167
Arthropathy	57.34	19.10	3	22326	157903	50424892
Condition aggravated	57.07	19.10	30	22299	297028	50285767
Non-small cell lung cancer metastatic	56.11	19.10	17	22312	513	50582282
Pancreatic carcinoma metastatic	55.69	19.10	24	22305	2018	50580777
Growth of eyelashes	52.73	19.10	13	22316	176	50582619
Malignant pleural effusion	52.65	19.10	24	22305	2306	50580489
Drug ineffective	52.61	19.10	186	22143	819147	49763648
Metastases to lung	51.31	19.10	41	22288	10979	50571816
Skin toxicity	48.98	19.10	27	22302	3886	50578909
Alopecia scarring	48.22	19.10	11	22318	104	50582691
Metastases to bone	48.15	19.10	49	22280	17946	50564849
Sinusitis	47.24	19.10	9	22320	170549	50412246
Pulmonary embolism	47.05	19.10	124	22205	101580	50481215
Metastases to liver	45.37	19.10	50	22279	20054	50562741
Multiple-drug resistance	44.63	19.10	24	22305	3290	50579505
Naevoid melanoma	44.59	19.10	7	22322	3	50582792
Non-small cell lung cancer	44.46	19.10	23	22306	2914	50579881
Haemoptysis	43.45	19.10	55	22274	25518	50557277
Trichiasis	42.63	19.10	9	22320	57	50582738
Weight increased	42.41	19.10	18	22311	201873	50380922
Nasopharyngitis	40.85	19.10	17	22312	192910	50389885
Skin exfoliation	38.73	19.10	60	22269	33552	50549243
Neoplasm progression	37.81	19.10	55	22274	29102	50553693
Injection site pain	37.66	19.10	3	22326	111021	50471774
Eye irritation	37.60	19.10	42	22287	17098	50565697
Hair texture abnormal	37.11	19.10	22	22307	3634	50579161
Interstitial lung disease	36.85	19.10	76	22253	53100	50529695
Nausea	35.53	19.10	470	21859	704928	49877867
Hypersensitivity	35.37	19.10	26	22303	215135	50367660
Product use issue	35.32	19.10	11	22318	149464	50433331
Swelling	34.70	19.10	23	22306	200849	50381946
Pain	34.04	19.10	136	22193	578767	50004028
Peripheral swelling	32.43	19.10	26	22303	205910	50376885
Dysphagia	32.32	19.10	91	22238	77427	50505368
Lung adenocarcinoma	32.15	19.10	21	22308	4113	50578682
Metastatic neoplasm	31.49	19.10	20	22309	3734	50579061
Erythema dyschromicum perstans	31.41	19.10	7	22322	59	50582736
Henoch-Schonlein purpura	31.33	19.10	13	22316	995	50581800
Metastases to spine	31.28	19.10	18	22311	2813	50579982
Metastases to meninges	31.23	19.10	16	22313	1986	50580809
Wound	30.55	19.10	5	22324	105789	50477006
Pain in extremity	30.26	19.10	46	22283	272819	50309976
Glossodynia	30.14	19.10	7	22322	115562	50467233
Pyogenic granuloma	29.56	19.10	9	22320	276	50582519
Treatment failure	29.33	19.10	12	22317	137625	50445170
Product dose omission issue	29.20	19.10	23	22306	183815	50398980
Therapeutic product effect decreased	28.76	19.10	12	22317	136038	50446757
Corneal perforation	28.72	19.10	10	22319	472	50582323
Stomatitis	28.58	19.10	104	22225	101240	50481555
Pneumatosis intestinalis	27.68	19.10	15	22314	2088	50580707
Malignant transformation	27.59	19.10	9	22320	347	50582448
Discomfort	27.41	19.10	7	22322	108373	50474422
Blood bilirubin increased	27.33	19.10	50	22279	31988	50550807
Onychalgia	27.25	19.10	11	22318	784	50582011
Vomiting	26.96	19.10	316	22013	460442	50122353
Ulcerative keratitis	26.22	19.10	15	22314	2318	50580477
Onychoclasis	25.62	19.10	20	22309	5176	50577619
Therapy partial responder	25.43	19.10	22	22307	6569	50576226
Metastases to neck	25.16	19.10	6	22323	70	50582725
Skin disorder	25.07	19.10	41	22288	23989	50558806
Hirsutism	24.79	19.10	11	22318	992	50581803
Abdominal discomfort	24.77	19.10	40	22289	231601	50351194
Blepharitis	24.37	19.10	14	22315	2181	50580614
Performance status decreased	24.28	19.10	16	22313	3179	50579616
Asthenia	23.87	19.10	230	22099	318812	50263983
Pneumothorax	23.54	19.10	30	22299	14004	50568791
Conjunctivitis	23.21	19.10	32	22297	16113	50566682
Lymphangiosis carcinomatosa	22.94	19.10	11	22318	1185	50581610
Corneal disorder	22.52	19.10	12	22317	1614	50581181
Xerosis	22.48	19.10	9	22320	628	50582167
Toxicity to various agents	22.43	19.10	37	22292	212462	50370333
Palpitations	22.24	19.10	7	22322	94499	50488296
Asthma	22.15	19.10	6	22323	89331	50493464
Weight decreased	22.04	19.10	170	22159	221075	50361720
Metastases to breast	21.31	19.10	7	22322	276	50582519
Migraine	20.77	19.10	4	22325	75276	50507519
Psoriasis	20.51	19.10	3	22326	68997	50513798
Osteoarthritis	20.35	19.10	3	22326	68603	50514192
Iridocele	20.18	19.10	3	22326	0	50582795
Dry eye	20.06	19.10	44	22285	32051	50550744
Drug intolerance	19.73	19.10	42	22287	219062	50363733
Feeling abnormal	19.54	19.10	16	22313	125476	50457319
Epistaxis	19.19	19.10	67	22262	63887	50518908

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
Death	5804.75	17.31	3309	17753	338775	29214690
Rash	907.56	17.31	875	20187	188944	29364521
Disease progression	759.52	17.31	555	20507	81361	29472104
Dermatitis acneiform	278.05	17.31	115	20947	5376	29548089
Malignant neoplasm progression	255.59	17.31	288	20774	73571	29479894
Diarrhoea	214.92	17.31	618	20444	332080	29221385
Neoplasm malignant	196.33	17.31	132	20930	16793	29536672
Dehydration	108.58	17.31	247	20815	114501	29438964
Metastases to central nervous system	98.29	17.31	62	21000	7069	29546396
Incorrect dose administered	89.76	17.31	114	20948	32870	29520595
Interstitial lung disease	81.70	17.31	147	20915	57571	29495894
Haemoptysis	77.51	17.31	102	20960	30448	29523017
Lung neoplasm malignant	76.90	17.31	71	20991	14286	29539179
Non-small cell lung cancer metastatic	76.41	17.31	24	21038	498	29552967
Drug resistance	67.56	17.31	80	20982	21460	29532005
Decreased appetite	66.64	17.31	241	20821	145101	29408364
Lung cancer metastatic	57.37	17.31	30	21032	2397	29551068
Non-small cell lung cancer	54.26	17.31	31	21031	2950	29550515
Acne	54.09	17.31	48	21014	9172	29544293
Pleural effusion	53.21	17.31	141	20921	71767	29481698
Paronychia	49.21	17.31	29	21033	2924	29550541
EGFR gene mutation	47.83	17.31	12	21050	104	29553361
Toxicity to various agents	47.27	17.31	33	21029	173628	29379837
Metastasis	45.22	17.31	29	21033	3400	29550065
Drug abuse	45.13	17.31	3	21059	79880	29473585
Product use in unapproved indication	41.94	17.31	6	21056	86869	29466596
Skin toxicity	40.34	17.31	28	21034	3743	29549722
Drug ineffective	40.31	17.31	129	20933	363041	29190424
Neoplasm progression	39.45	17.31	57	21005	18555	29534910
Malignant pleural effusion	39.09	17.31	19	21043	1299	29552166
Gastrointestinal perforation	37.58	17.31	26	21036	3457	29550008
Product dose omission issue	37.58	17.31	11	21051	96372	29457093
Bradycardia	35.55	17.31	3	21059	65626	29487839
Metastases to lung	34.79	17.31	35	21027	7820	29545645
Lymphangiosis carcinomatosa	34.42	17.31	15	21047	797	29552668
Pneumothorax	34.28	17.31	49	21013	15793	29537672
Vomiting	33.55	17.31	262	20800	211998	29341467
Weight increased	33.28	17.31	7	21055	76660	29476805
Pneumoperitoneum	33.11	17.31	18	21044	1555	29551910
Metastases to liver	32.26	17.31	41	21021	11815	29541650
Metastases to bone	31.42	17.31	37	21025	9861	29543604
Dizziness	30.82	17.31	55	21007	189629	29363836
Rash pustular	30.70	17.31	26	21036	4665	29548800
Drug hypersensitivity	30.19	17.31	6	21056	68400	29485065
Metastases to spine	30.18	17.31	19	21043	2157	29551308
Acute kidney injury	29.52	17.31	94	20968	265173	29288292
Arthralgia	29.05	17.31	34	21028	139583	29413882
Lung adenocarcinoma	26.44	17.31	22	21040	3853	29549612
Pancreatic carcinoma metastatic	26.32	17.31	19	21043	2702	29550763
Pneumonitis	26.01	17.31	60	21002	27984	29525481
Metastases to meninges	25.95	17.31	14	21048	1191	29552274
Stomatitis	25.64	17.31	71	20991	37042	29516423
Pulmonary embolism	25.46	17.31	115	20947	76419	29477046
Condition aggravated	24.12	17.31	42	21020	146253	29407212
Nausea	23.79	17.31	312	20750	288943	29264522
Overdose	23.27	17.31	14	21048	79805	29473660
Growth of eyelashes	23.05	17.31	6	21056	61	29553404
Hyperhidrosis	22.32	17.31	9	21053	64531	29488934
Oesophageal ulcer	21.88	17.31	18	21044	3102	29550363
Bronchial fistula	21.52	17.31	7	21055	163	29553302
Palmar-plantar erythrodysaesthesia syndrome	21.37	17.31	38	21024	14721	29538744
Tremor	21.29	17.31	13	21049	73525	29479940
Nasopharyngitis	21.16	17.31	8	21054	59657	29493808
Lung carcinoma cell type unspecified stage IV	20.31	17.31	9	21053	498	29552967
Blood pressure increased	20.08	17.31	14	21048	73789	29479676
Acquired gene mutation	20.04	17.31	12	21050	1246	29552219
Mucosal inflammation	19.45	17.31	58	21004	31537	29521928
Conjunctivitis	19.18	17.31	26	21036	7972	29545493
Therapy partial responder	19.16	17.31	21	21041	5178	29548287
Insomnia	19.11	17.31	21	21041	88740	29464725
Infusion related reaction	19.05	17.31	4	21058	43882	29509583
Rhabdomyolysis	18.68	17.31	10	21052	60798	29492667
Hypophagia	18.63	17.31	44	21018	20828	29532637
Skin reaction	18.32	17.31	19	21043	4398	29549067
Product use issue	18.07	17.31	7	21055	51437	29502028
Headache	17.72	17.31	64	20998	173943	29379522

FDA Adverse Event Reporting System (Geriatric)

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
Rash	808.73	16.16	939	24215	457610	64015968
Malignant neoplasm progression	683.52	16.16	467	24687	112404	64361174
Disease progression	550.05	16.16	449	24705	141231	64332347
Diarrhoea	526.64	16.16	975	24179	721729	63751849
Dermatitis acneiform	520.19	16.16	174	24980	8269	64465309
Drug resistance	345.35	16.16	198	24956	34904	64438674
Death	344.26	16.16	647	24507	482058	63991520
Metastases to central nervous system	197.01	16.16	100	25054	13812	64459766
EGFR gene mutation	174.58	16.16	38	25116	326	64473252
Dehydration	170.57	16.16	304	24850	216459	64257119
Paronychia	155.09	16.16	67	25087	6425	64467153
Dry skin	143.33	16.16	135	25019	51026	64422552
Interstitial lung disease	139.50	16.16	181	24973	97551	64376027
Decreased appetite	122.54	16.16	310	24844	280979	64192599
Pleural effusion	110.49	16.16	186	24968	126373	64347205
Acquired gene mutation	103.00	16.16	36	25118	1950	64471628
Haemoptysis	96.50	16.16	107	25047	48941	64424637
Non-small cell lung cancer metastatic	87.49	16.16	26	25128	833	64472745
Rash pustular	87.20	16.16	52	25102	9833	64463745
Skin toxicity	83.50	16.16	44	25110	6558	64467020
Acne	76.56	16.16	67	25087	23014	64450564
Non-small cell lung cancer	65.88	16.16	34	25120	4856	64468722
Arthralgia	64.69	16.16	47	25107	442213	64031365
Trichiasis	59.46	16.16	12	25142	68	64473510
Therapy partial responder	58.48	16.16	41	25113	10207	64463371
Nausea	57.57	16.16	511	24643	785289	63688289
Pulmonary embolism	57.12	16.16	155	24999	146201	64327377
Drug hypersensitivity	56.34	16.16	12	25142	237803	64235775
Lung adenocarcinoma	55.26	16.16	34	25120	6799	64466779
Pneumothorax	54.80	16.16	57	25097	24241	64449337
Lymphangiosis carcinomatosa	54.25	16.16	22	25132	1799	64471779
Neoplasm progression	52.44	16.16	72	25082	40892	64432686
Infusion related reaction	52.03	16.16	3	25151	164464	64309114
Metastases to meninges	51.14	16.16	24	25130	2791	64470787
Incorrect dose administered	49.92	16.16	87	25067	60678	64412900
Vomiting	49.74	16.16	376	24778	550741	63922837
Pneumonitis	49.28	16.16	78	25076	50287	64423291
Drug ineffective	47.96	16.16	168	24986	840079	63633499
Growth of eyelashes	47.19	16.16	11	25143	132	64473446
Skin fissures	46.97	16.16	36	25118	10270	64463308
Malignant pleural effusion	46.93	16.16	23	25131	2944	64470634
Gastrointestinal perforation	46.45	16.16	28	25126	5396	64468182
Weight increased	46.17	16.16	13	25141	213335	64260243
Blood bilirubin increased	45.47	16.16	81	25073	57472	64416106
Alopecia scarring	45.02	16.16	10	25144	95	64473483
Metastases to lung	44.10	16.16	41	25113	15223	64458355
Naevoid melanoma	43.62	16.16	7	25147	6	64473572
Erythema dyschromicum perstans	43.34	16.16	9	25145	60	64473518
Joint swelling	43.25	16.16	15	25139	215367	64258211
Ulcerative keratitis	43.07	16.16	22	25132	3075	64470503
Toxicity to various agents	43.06	16.16	47	25107	363466	64110112
Hair growth abnormal	42.57	16.16	20	25134	2332	64471246
Respiratory failure	41.74	16.16	148	25006	161035	64312543
Corneal perforation	41.72	16.16	14	25140	670	64472908
Headache	40.37	16.16	92	25062	529375	63944203
Metastases to liver	39.95	16.16	48	25106	23893	64449685
Conjunctivitis	39.32	16.16	44	25110	20310	64453268
Metastases to bone	39.17	16.16	44	25110	20391	64453187
Pneumatosis intestinalis	37.22	16.16	24	25130	5205	64468373
Eye irritation	37.20	16.16	38	25116	15818	64457760
Nasopharyngitis	37.11	16.16	15	25139	196058	64277520
Multiple-drug resistance	37.07	16.16	26	25128	6476	64467102
Condition aggravated	36.03	16.16	56	25098	372370	64101208
Pyogenic granuloma	34.48	16.16	11	25143	448	64473130
Pneumoperitoneum	34.09	16.16	18	25136	2693	64470885
Stomatitis	34.01	16.16	107	25047	109498	64364080
Skin exfoliation	33.95	16.16	62	25092	44823	64428755
Arthropathy	33.34	16.16	4	25150	120963	64352615
Bradycardia	32.36	16.16	4	25150	118215	64355363
Overdose	32.22	16.16	11	25143	159555	64314023
Embolism	31.80	16.16	31	25123	12204	64461374
Lung cancer metastatic	31.61	16.16	18	25136	3122	64470456
Neoplasm malignant	31	16.16	43	25111	24645	64448933
Hypophagia	30.35	16.16	55	25099	39532	64434046
Corneal disorder	29.94	16.16	15	25139	2012	64471566
Hair texture abnormal	29.65	16.16	17	25137	2987	64470591
Sinusitis	29.57	16.16	10	25144	145918	64327660
Henoch-Schonlein purpura	28.74	16.16	15	25139	2191	64471387
Skin disorder	28.64	16.16	44	25110	27636	64445942
Lung neoplasm malignant	27.90	16.16	38	25116	21410	64452168
Injection site pain	27.67	16.16	5	25149	111403	64362175
Xerosis	26.37	16.16	11	25143	966	64472612
Mucosal inflammation	26.12	16.16	68	25086	62516	64411062
Peripheral swelling	25.90	16.16	26	25128	209127	64264451
Product use in unapproved indication	25.46	16.16	19	25135	176599	64296979
Palpitations	25.29	16.16	5	25149	104483	64369095
Performance status decreased	25.02	16.16	19	25135	5345	64468233
Malignant transformation	24.73	16.16	11	25143	1130	64472448
Haemoglobin decreased	24.70	16.16	145	25009	194918	64278660
Pain	24.42	16.16	122	25032	553389	63920189
Metastasis	24.01	16.16	19	25135	5676	64467902
Anaemia	23.90	16.16	239	24915	378441	64095137
Metastases to pleura	23.65	16.16	11	25143	1253	64472325
Product use issue	23.62	16.16	15	25139	151700	64321878
Blood alkaline phosphatase increased	23.33	16.16	61	25093	56218	64417360
Therapeutic product effect decreased	23.20	16.16	8	25146	115343	64358235
Nail disorder	22.69	16.16	22	25132	8602	64464976
Carcinoembryonic antigen increased	22.32	16.16	12	25142	1861	64471717
Product dose omission issue	22.13	16.16	26	25128	194721	64278857
Aspartate aminotransferase increased	22.12	16.16	99	25055	119689	64353889
Pneumopericardium	21.88	16.16	6	25148	143	64473435
Proteinuria	21.86	16.16	39	25115	27684	64445894
Off label use	21.79	16.16	151	25003	632655	63840923
Hypersensitivity	21.50	16.16	27	25127	196425	64277153
Drug intolerance	21.47	16.16	25	25129	187967	64285611
Blepharitis	21.39	16.16	13	25141	2542	64471036
Lung infiltration	21.32	16.16	33	25121	20856	64452722
Blood albumin decreased	21.11	16.16	33	25121	21040	64452538
Sudden death	20.87	16.16	32	25122	20064	64453514
Weight decreased	20.83	16.16	186	24968	285553	64188025
Onychoclasis	20.83	16.16	16	25138	4576	64469002
Dermatitis	20.57	16.16	30	25124	17999	64455579
Asthenia	20.55	16.16	256	24898	427788	64045790
Pericardial effusion	19.94	16.16	46	25108	39208	64434370
Dizziness	19.42	16.16	94	25060	430069	64043509
Hepatotoxicity	19.39	16.16	46	25108	39916	64433662
Pain in extremity	18.98	16.16	58	25096	303027	64170551
Squamous cell carcinoma of lung	18.80	16.16	11	25143	2007	64471571
Epistaxis	18.80	16.16	82	25072	98049	64375529
Dysphagia	18.77	16.16	87	25067	106725	64366853
Sarcomatoid carcinoma	18.74	16.16	4	25150	31	64473547
Palmar-plantar erythrodysaesthesia syndrome	18.34	16.16	37	25117	28782	64444796
Onychalgia	18.30	16.16	8	25146	789	64472789
Laryngeal papilloma	18.01	16.16	3	25151	4	64473574
Pancreatic carcinoma metastatic	17.74	16.16	13	25141	3465	64470113
Corneal defect	17.61	16.16	3	25151	5	64473573
Failure to thrive	17.59	16.16	21	25133	10383	64463195
Alanine aminotransferase increased	17.36	16.16	103	25051	138928	64334650
Biliary cancer metastatic	17.26	16.16	3	25151	6	64473572
Feeling abnormal	17.24	16.16	16	25138	133586	64339992
Hypoxia	17.14	16.16	74	25080	88075	64385503
Non-small cell lung cancer stage IV	16.83	16.16	5	25149	160	64473418
Neoplasm	16.76	16.16	17	25137	7014	64466564
Cerebral ischaemia	16.66	16.16	20	25134	9942	64463636
Carbohydrate antigen 19-9 increased	16.37	16.16	6	25148	373	64473205

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
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|

Disease	Relation	SNOMED_ID	DOID
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 level	Dissociation constant	Type (acidic/basic)
pKa1	4.01	Basic

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])	Bioact source	MoA source
Epidermal growth factor receptor	Kinase	P00533	EGFR_HUMAN	INHIBITOR	IC50	9.22	WOMBAT-PK	CHEMBL
Tyrosine-protein kinase JAK3	Kinase	P52333	JAK3_HUMAN		Kd	6.15	CHEMBL
Platelet-derived growth factor receptor beta	Kinase	P09619	PGFRB_HUMAN		Kd	5.85	CHEMBL
Tyrosine-protein kinase ABL1	Kinase	P00519	ABL1_HUMAN		Kd	7.24	CHEMBL
Mast/stem cell growth factor receptor Kit	Kinase	P10721	KIT_HUMAN		Kd	5.89	CHEMBL
Breakpoint cluster region protein	Kinase	P11274	BCR_HUMAN		Kd	5.74	CHEMBL
Proto-oncogene tyrosine-protein kinase Src	Kinase	P12931	SRC_HUMAN		Kd	6.15	CHEMBL
Tyrosine-protein kinase Lck	Kinase	P06239	LCK_HUMAN		Kd	6.60	CHEMBL
Tyrosine-protein kinase Yes	Kinase	P07947	YES_HUMAN		Kd	5.66	CHEMBL
Serine/threonine-protein kinase B-raf	Kinase	P15056	BRAF_HUMAN		IC50	7.22	CHEMBL
Receptor-type tyrosine-protein kinase FLT3	Kinase	P36888	FLT3_HUMAN		Kd	6.89	CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret	Kinase	P07949	RET_HUMAN		Kd	6.48	CHEMBL
Vascular endothelial growth factor receptor 1	Kinase	P17948	VGFR1_HUMAN		Kd	5.36	CHEMBL
Vascular endothelial growth factor receptor 2	Kinase	P35968	VGFR2_HUMAN		Kd	5.24	CHEMBL
Vascular endothelial growth factor receptor 3	Kinase	P35916	VGFR3_HUMAN		Kd	5.68	CHEMBL
Platelet-derived growth factor receptor alpha	Kinase	P16234	PGFRA_HUMAN		Kd	5.74	CHEMBL
Receptor tyrosine-protein kinase erbB-2	Kinase	P04626	ERBB2_HUMAN		Kd	5.54	CHEMBL
Cyclin-dependent kinase 2	Kinase	P24941	CDK2_HUMAN		IC50	5.94	CHEMBL
Death-associated protein kinase 3	Kinase	O43293	DAPK3_HUMAN		Kd	5.22	CHEMBL
Focal adhesion kinase 1	Kinase	Q05397	FAK1_HUMAN		IC50	5.13	CHEMBL
Tyrosine-protein kinase HCK	Kinase	P08631	HCK_HUMAN		Kd	5.74	CHEMBL
Receptor tyrosine-protein kinase erbB-4	Kinase	Q15303	ERBB4_HUMAN		Kd	6.64	CHEMBL
Mitogen-activated protein kinase 10	Kinase	P53779	MK10_HUMAN		Kd	5.37	CHEMBL
Tyrosine-protein kinase JAK2	Kinase	O60674	JAK2_HUMAN		Kd	5.43	CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit delta	Kinase	Q13557	KCC2D_HUMAN		Kd	5.19	CHEMBL
Myosin light chain kinase 2, skeletal/cardiac muscle	Kinase	Q9H1R3	MYLK2_HUMAN		Kd	6.01	CHEMBL
Tyrosine-protein kinase CSK	Kinase	P41240	CSK_HUMAN		Kd	5.02	CHEMBL
Ephrin type-A receptor 8	Kinase	P29322	EPHA8_HUMAN		Kd	6.03	CHEMBL
AP2-associated protein kinase 1	Kinase	Q2M2I8	AAK1_HUMAN		Kd	5.92	CHEMBL
Hepatocyte growth factor receptor	Kinase	P08581	MET_HUMAN		Kd	5.96	CHEMBL
Tyrosine-protein kinase Lyn	Kinase	P07948	LYN_HUMAN		Kd	6.28	CHEMBL
Serine/threonine-protein kinase 17B	Kinase	O94768	ST17B_HUMAN		Kd	5.03	CHEMBL
Serine/threonine-protein kinase 10	Kinase	O94804	STK10_HUMAN		Kd	7.72	CHEMBL
Serine/threonine-protein kinase PLK4	Kinase	O00444	PLK4_HUMAN		Kd	5.72	CHEMBL
Aurora kinase C	Kinase	Q9UQB9	AURKC_HUMAN		Kd	6.22	CHEMBL
Dual specificity protein kinase TTK	Kinase	P33981	TTK_HUMAN		Kd	5.43	CHEMBL
Abelson tyrosine-protein kinase 2	Kinase	P42684	ABL2_HUMAN		Kd	6.70	CHEMBL
Ephrin type-A receptor 5	Kinase	P54756	EPHA5_HUMAN		Kd	6.15	CHEMBL
Fibroblast growth factor receptor 2	Kinase	P21802	FGFR2_HUMAN		Kd	5.72	CHEMBL
Serine/threonine-protein kinase 17A	Kinase	Q9UEE5	ST17A_HUMAN		Kd	5.20	CHEMBL
Ephrin type-A receptor 6	Kinase	Q9UF33	EPHA6_HUMAN		Kd	6.36	CHEMBL
TRAF2 and NCK-interacting protein kinase	Kinase	Q9UKE5	TNIK_HUMAN		Kd	5.35	CHEMBL
Casein kinase I isoform epsilon	Kinase	P49674	KC1E_HUMAN		Kd	6.30	CHEMBL
Tyrosine-protein kinase Fgr	Kinase	P09769	FGR_HUMAN		Kd	5.96	CHEMBL
Aurora kinase A	Kinase	O14965	AURKA_HUMAN		Kd	5.66	CHEMBL
ALK tyrosine kinase receptor	Kinase	Q9UM73	ALK_HUMAN		Kd	5.92	CHEMBL
Serine/threonine-protein kinase 36	Kinase	Q9NRP7	STK36_HUMAN		Kd	5.36	CHEMBL
Ephrin type-A receptor 3	Kinase	P29320	EPHA3_HUMAN		Kd	5.62	CHEMBL
BMP-2-inducible protein kinase	Kinase	Q9NSY1	BMP2K_HUMAN		Kd	5.92	CHEMBL
Tyrosine-protein kinase FRK	Kinase	P42685	FRK_HUMAN		Kd	5.70	CHEMBL
Cyclin-G-associated kinase	Kinase	O14976	GAK_HUMAN		Kd	8.51	CHEMBL
Receptor-interacting serine/threonine-protein kinase 2	Kinase	O43353	RIPK2_HUMAN		Kd	6.39	CHEMBL
Ephrin type-B receptor 1	Kinase	P54762	EPHB1_HUMAN		Kd	5.96	CHEMBL
Ephrin type-A receptor 7	Kinase	Q15375	EPHA7_HUMAN		Kd	5.85	CHEMBL
STE20-like serine/threonine-protein kinase	Kinase	Q9H2G2	SLK_HUMAN		Kd	7.59	CHEMBL
MAP kinase-interacting serine/threonine-protein kinase 2	Kinase	Q9HBH9	MKNK2_HUMAN		Kd	6	CHEMBL
Epithelial discoidin domain-containing receptor 1	Kinase	Q08345	DDR1_HUMAN		Kd	6.10	CHEMBL
Solute carrier family 22 member 1	Transporter	O15245	S22A1_HUMAN		IC50	4.79	CHEMBL
Ephrin type-B receptor 4	Kinase	P54760	EPHB4_HUMAN		Kd	5.66	CHEMBL
Tyrosine-protein kinase receptor UFO	Kinase	P30530	UFO_HUMAN		Kd	5.40	CHEMBL
Tyrosine-protein kinase receptor TYRO3	Kinase	Q06418	TYRO3_HUMAN		Kd	5.41	CHEMBL
Non-receptor tyrosine-protein kinase TNK1	Kinase	Q13470	TNK1_HUMAN		Kd	6.20	CHEMBL
Non-receptor tyrosine-protein kinase TYK2	Kinase	P29597	TYK2_HUMAN		Kd	5.62	CHEMBL
Casein kinase I isoform delta	Kinase	P48730	KC1D_HUMAN		Kd	5.46	CHEMBL
Tyrosine-protein kinase receptor Tie-1	Kinase	P35590	TIE1_HUMAN		Kd	6.07	CHEMBL
Tyrosine-protein kinase TXK	Kinase	P42681	TXK_HUMAN		Kd	5.42	CHEMBL
MAP kinase-interacting serine/threonine-protein kinase 1	Kinase	Q9BUB5	MKNK1_HUMAN		Kd	6.16	CHEMBL
Eukaryotic translation initiation factor 2-alpha kinase 4	Kinase	Q9P2K8	E2AK4_HUMAN		Kd	5.36	CHEMBL
Serine/threonine-protein kinase SIK2	Kinase	Q9H0K1	SIK2_HUMAN		Kd	5.59	CHEMBL
Serine/threonine-protein kinase TNNI3K	Kinase	Q59H18	TNI3K_HUMAN		Kd	6.24	CHEMBL
Myotonin-protein kinase	Kinase	Q09013	DMPK_HUMAN		Kd	5.54	CHEMBL
Chaperone activity of bc1 complex-like, mitochondrial	Kinase	Q8NI60	COQ8A_HUMAN		Kd	5.72	CHEMBL
Serine/threonine-protein kinase MRCK gamma	Kinase	Q6DT37	MRCKG_HUMAN		Kd	5.47	CHEMBL
Leukocyte tyrosine kinase receptor	Kinase	P29376	LTK_HUMAN		Kd	6.05	CHEMBL
Aurora kinase B	Kinase	Q96GD4	AURKB_HUMAN		Kd	5.85	CHEMBL
Tyrosine-protein kinase Blk	Kinase	P51451	BLK_HUMAN		Kd	6.72	CHEMBL
Tyrosine-protein kinase Mer	Kinase	Q12866	MERTK_HUMAN		Kd	6.01	CHEMBL
Citron Rho-interacting kinase	Kinase	O14578	CTRO_HUMAN		Kd	6.17	CHEMBL
AarF domain-containing protein kinase 4	Kinase	Q96D53	COQ8B_HUMAN		Kd	5.60	CHEMBL
Mitogen-activated protein kinase 4	Kinase	P31152	MK04_HUMAN		Kd	5.60	CHEMBL
Interferon-induced, double-stranded RNA-activated protein kinase	Kinase	P19525	E2AK2_HUMAN		Kd	5.89	CHEMBL
Ribosomal protein S6 kinase alpha-4	Kinase	O75676	KS6A4_HUMAN		Kd	5.15	CHEMBL
Misshapen-like kinase 1	Kinase	Q8N4C8	MINK1_HUMAN		Kd	5.89	CHEMBL
Serine/threonine-protein kinase TBK1	Kinase	Q9UHD2	TBK1_HUMAN		Kd	5.51	CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 2	Kinase	Q92630	DYRK2_HUMAN		Kd	5.89	CHEMBL
Ephrin type-B receptor 6	Kinase	O15197	EPHB6_HUMAN		Kd	5.77	CHEMBL
G protein-coupled receptor kinase 4	Kinase	P32298	GRK4_HUMAN		Kd	5.14	CHEMBL
Homeodomain-interacting protein kinase 4	Kinase	Q8NE63	HIPK4_HUMAN		Kd	6.02	CHEMBL
Mitogen-activated protein kinase kinase kinase 2	Kinase	Q9Y2U5	M3K2_HUMAN		Kd	5.60	CHEMBL
Mitogen-activated protein kinase kinase kinase 3	Kinase	Q99759	M3K3_HUMAN		Kd	5.64	CHEMBL
SRSF protein kinase 3	Kinase	Q9UPE1	SRPK3_HUMAN		Kd	5.08	CHEMBL
Serine/threonine-protein kinase ULK3	Kinase	Q6PHR2	ULK3_HUMAN		Kd	6.04	CHEMBL
Mitogen-activated protein kinase kinase kinase 19	Kinase	Q56UN5	M3K19_HUMAN		Kd	7.60	CHEMBL
Receptor-interacting serine/threonine-protein kinase 4	Kinase	P57078	RIPK4_HUMAN		Kd	5.31	CHEMBL
Receptor tyrosine-protein kinase erbB-3	Kinase	P21860	ERBB3_HUMAN		Kd	5.96	CHEMBL
Mitogen-activated protein kinase kinase kinase 1	Kinase	Q13233	M3K1_HUMAN		Kd	5.65	CHEMBL
Serine/threonine-protein kinase SBK1	Kinase	Q52WX2	SBK1_HUMAN		Kd	5.92	CHEMBL
Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma	Kinase	Q8TBX8	PI42C_HUMAN		Kd	6	CHEMBL
Dual specificity mitogen-activated protein kinase kinase 5	Kinase	Q13163	MP2K5_HUMAN		Kd	7.02	CHEMBL
Leucine-rich repeat serine/threonine-protein kinase 2	Kinase	Q5S007	LRRK2_HUMAN		Kd	5.54	CHEMBL
Solute carrier organic anion transporter family member 2B1	Transporter	O94956	SO2B1_HUMAN	INHIBITOR	Ki	6.28	IUPHAR
Ferrochelatase, mitochondrial	Enzyme	P22830	HEMH_HUMAN		Kd	5.16	CHEMBL
Mitotic checkpoint serine/threonine-protein kinase BUB1	Kinase	O43683	BUB1_HUMAN		Kd	6.95	CHEMBL
Acyl-CoA dehydrogenase family member 11	Enzyme	Q709F0	ACD11_HUMAN		Kd	5.38	CHEMBL
Mitogen-activated protein kinase 9	Kinase	P45984	MK09_HUMAN		Kd	5.70	CHEMBL
dCTP pyrophosphatase 1	Unclassified	Q9H773	DCTP1_HUMAN		Kd	5.51	CHEMBL
Serine/threonine-protein kinase ULK3	Kinase		ULK3_MOUSE		Kd	6.20	CHEMBL
Proto-oncogene tyrosine-protein kinase Src	Kinase		SRC_CHICK		IC50	6	CHEMBL
Tubulin alpha-1A chain	Structural		TBA1A_RAT		Kd	6.64	CHEMBL
Serine/threonine-protein kinase B-raf	Kinase		BRAF_MOUSE		IC50	7.40	CHEMBL

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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