All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

erlotinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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

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)	0.00 mg/mL	Bocci G, Oprea TI, Benet LZ
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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
azlogd74	LogD at pH 7.4	3.294		Moderate	0.69
caco2-efflux	Caco-2 efflux ratio (BA/AB)	0.800		Moderate	0.69
caco2-intrinsic-papp	Caco-2 intrinsic apparent permeability	62.230	10^-6 cm/s	Moderate	0.69
dh-clint	Dog hepatocyte intrinsic clearance	8.110	uL/min/10^6 cells	Moderate	0.69
dppb	Dog plasma protein binding (% unbound)	10.890	%	Moderate	0.69
fcs-ppb	Fetal calf serum protein binding (% unbound)	31.470	%	Moderate	0.69
herg	hERG pIC50	4.974	pIC50	Moderate	0.69
hh-clint	Human hepatocyte intrinsic clearance	2.917	uL/min/10^6 cells	Moderate	0.69
hlm-clint	Human liver microsomal intrinsic clearance	25.942	uL/min/mg protein	Moderate	0.69
hppb	Human plasma protein binding (% unbound)	7.100	%	Moderate	0.69
kinase-safety-class	ABL1,ABL2,ACVR2A,ACVR2B,AKT2,AKT3,ALK,AURKA,AURKB,AXL,BLK,BMX,BRAF,CAMK2B,CAMK2D,CDK5,CDK9,CHEK1,CSF1R,CSK,DDR1,DYRK1B,EGFR,EIF2AK3,EPHA2,EPHB1,EPHB4,ERBB2,ERBB4,FGFR1,FLT1,FLT3,FLT4,FYN,GAK,GRK2,GSK3B,INSR,IRAK1,IRAK3,IRAK4,ITK,JAK1,JAK2,KDR,KIT,LCK,LYN,MAP2K1,MAP3K1,MAP3K10,MAP3K21,MAP3K7,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK10,MAPK11,MAPK12,MAPK14,MAPK7,MAPKAPK2,MARK4,MET,MKNK1,MKNK2,MTOR,NTRK1,NTRK2,PAK4,PDGFRB,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PRKCD,PRKDC,PTK6,RET,RIPK3,SIK2,SIK3,SRC,STK10,STK33,SYK,TEK,TNIK,TTK,TYRO3,ULK1,YES1	95
kinase-selectivity-class	ALK,AURKA,AXL,BRAF,CAMK2B,CAMK2D,CDK9,CSF1R,DDR1,DYRK1B,EGFR,EPHA2,EPHB4,ERBB2,ERBB4,FLT3,FYN,IRAK3,JAK1,KDR,KIT,LYN,MAP3K10,MAP3K21,MAP4K1,MAP4K3,MAPK7,MET,PDK4,PRKCD,RET,SIK2,SIK3,STK10,STK33,SYK,ULK1,YES1	38
mdck-mdr1-bcrp-efflux	MDCK-MDR1-BCRP efflux ratio	5.610		High	1
mdck-mdr1-efflux	MDCK-MDR1 efflux ratio	4.198		Moderate	0.69
mh-clint	Mouse hepatocyte intrinsic clearance	18.836		Moderate	0.69
mppb	Mouse plasma protein binding (% unbound)	6.050		Moderate	0.69
nih-mdck-mdr1-efflux	NIH MDCK-MDR1 efflux ratio	7.638		Moderate	0.69
pfas-class	PFAS structural alert (1 = True, 0 = False)	0
pld-class	Phospholipidosis risk class (1 = positive, 0 = negative)	1		High	1
pppb	Pig plasma protein binding (% unbound)	17.280	%	Moderate	0.69
rat-kpuu-brain	Rat brain Kpuu	0.144	%	High	1
rh-clint	Rat hepatocyte intrinsic clearance	8.995	uL/min/10^6 cells	Moderate	0.69
rh-fuinc	Rat hepatocyte fraction unbound in incubation	55.500	%	Moderate	0.69
rppb	Rat plasma protein binding (% unbound)	6.460	%	Moderate	0.69
solubility-dd	Solubility at pH 7.4 in DMSO	14.322	uM	Moderate	0.69

Approvals:

Date	Agency	Company	Orphan
Nov. 18, 2004	FDA	OSI PHARMS
Sept. 19, 2005	EMA	ROCHE REGISTRATION GMBH

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	784.93	22.28	620	13999	455931	90157897
Disease progression	718.28	22.28	394	14225	156221	90457607
Diarrhoea	519.32	22.28	691	13928	938499	89675329
Rash	483.38	22.28	614	14005	795486	89818342
Malignant neoplasm progression	467.51	22.28	261	14358	106609	90507219
Drug resistance	441.92	22.28	171	14448	30278	90583550
Dermatitis acneiform	410.46	22.28	111	14508	6243	90607585
Dry skin	181.41	22.28	134	14485	87939	90525889
Paronychia	171.73	22.28	60	14559	7946	90605882
Neoplasm malignant	151.20	22.28	84	14535	33796	90580032
Metastases to central nervous system	148.00	22.28	67	14552	17475	90596353
EGFR gene mutation	139.67	22.28	27	14592	323	90613505
Acquired gene mutation	124.62	22.28	31	14588	1248	90612580
Incorrect dose administered	104.88	22.28	93	14526	78837	90534991
Rash pustular	98.46	22.28	40	14579	8009	90605819
Acne	96.26	22.28	59	14560	28448	90585380
Dehydration	86.54	22.28	130	14489	194317	90419511
Malignant transformation	81.36	22.28	19	14600	583	90613245
Erythema dyschromicum perstans	76.60	22.28	13	14606	69	90613759
Pleural effusion	76.01	22.28	92	14527	111899	90501929
Decreased appetite	75.69	22.28	179	14440	376361	90237467
Metastases to lung	66.84	22.28	38	14581	15953	90597875
Growth of eyelashes	62.99	22.28	13	14606	221	90613607
Metastases to meninges	57.77	22.28	22	14597	3713	90610115
Neoplasm progression	54.30	22.28	50	14569	44436	90569392
Multiple-drug resistance	54.09	22.28	26	14593	7750	90606078
Joint swelling	52.57	22.28	9	14610	503291	90110537
Nausea	52.19	22.28	331	14288	1109985	89503843
Naevoid melanoma	51.63	22.28	7	14612	3	90613825
Malignant pleural effusion	51.45	22.28	19	14600	2945	90610883
Non-small cell lung cancer	50.95	22.28	21	14598	4360	90609468
Therapy partial responder	48.63	22.28	35	14584	22008	90591820
Lung cancer metastatic	48.11	22.28	18	14601	2893	90610935
Skin fissures	48.11	22.28	34	14585	20775	90593053
Hair growth abnormal	47.48	22.28	19	14600	3657	90610171
Drug hypersensitivity	46.88	22.28	9	14610	463600	90150228
Non-small cell lung cancer metastatic	46.81	22.28	13	14606	805	90613023
Hair texture abnormal	46.28	22.28	20	14599	4667	90609161
Metastases to bone	46.24	22.28	36	14583	25469	90588359
Pulmonary embolism	45.19	22.28	78	14541	130742	90483086
Skin toxicity	42.17	22.28	21	14598	6758	90607070
Alopecia scarring	41.54	22.28	9	14610	195	90613633
Pneumonitis	41.47	22.28	43	14576	44127	90569701
Anaemia	41.38	22.28	138	14481	352664	90261164
Arthralgia	41.23	22.28	39	14580	778483	89835345
Trichiasis	39.89	22.28	8	14611	117	90613711
Lung neoplasm malignant	39.17	22.28	32	14587	24241	90589587
Condition aggravated	38.96	22.28	24	14595	595521	90018307
Xerosis	38.95	22.28	13	14606	1498	90612330
Sinusitis	38.41	22.28	5	14614	343083	90270745
Glossodynia	37.73	22.28	4	14615	321775	90292053
Pancreatic carcinoma metastatic	36.69	22.28	14	14605	2374	90611454
Wound	34.93	22.28	4	14615	302976	90310852
Onychoclasis	34.79	22.28	19	14600	7380	90606448
Blepharitis	32.93	22.28	15	14604	3961	90609867
Vomiting	32.64	22.28	228	14391	788065	89825763
Skin exfoliation	32.45	22.28	47	14572	67866	90545962
Metastasis	32.34	22.28	17	14602	6120	90607708
Pyogenic granuloma	32.23	22.28	8	14611	319	90613509
Ulcerative keratitis	31.70	22.28	14	14605	3439	90610389
Corneal disorder	31.48	22.28	12	14607	2030	90611798
Discomfort	30.69	22.28	4	14615	274331	90339497
Metastases to liver	30.62	22.28	30	14589	28777	90585051
Fatigue	30.26	22.28	301	14318	1153722	89460106
Weight increased	29.97	22.28	15	14604	417912	90195916
Nasopharyngitis	28.61	22.28	15	14604	407089	90206739
Asthma	28.41	22.28	3	14616	242157	90371671
Corneal perforation	27.25	22.28	8	14611	605	90613223
Swelling	27.22	22.28	17	14602	419041	90194787
Non-small cell lung cancer stage IV	26.68	22.28	6	14613	155	90613673
Dysphagia	26.52	22.28	57	14562	112221	90501607
Asthenia	26.06	22.28	161	14458	533590	90080238
Epistaxis	25.85	22.28	48	14571	85077	90528751
Lung adenocarcinoma	25.36	22.28	14	14605	5551	90608277
Hypersensitivity	24.94	22.28	22	14597	454655	90159173
Henoch-Schonlein purpura	23.08	22.28	9	14610	1618	90612210
Performance status decreased	22.96	22.28	12	14607	4268	90609560
Headache	22.64	22.28	68	14551	862678	89751150
Sarcomatoid carcinoma	22.49	22.28	4	14615	29	90613799
Pneumatosis intestinalis	22.42	22.28	11	14608	3426	90610402
Pneumothorax	22.33	22.28	21	14598	19146	90594682

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	592.02	20.19	704	11829	470481	42138321
Disease progression	490.53	20.19	375	12158	143281	42465521
Rash	475.72	20.19	489	12044	276465	42332337
Dermatitis acneiform	232.56	20.19	87	12446	7652	42601150
Malignant neoplasm progression	211.50	20.19	206	12327	108194	42500608
Diarrhoea	176.86	20.19	405	12128	460444	42148358
Neoplasm malignant	166.76	20.19	96	12437	22647	42586155
Drug resistance	153.94	20.19	106	12427	34142	42574660
EGFR gene mutation	93.53	20.19	20	12513	214	42608588
Dehydration	90.75	20.19	155	12378	141612	42467190
Decreased appetite	68.24	20.19	165	12368	192972	42415830
Metastases to central nervous system	63.55	20.19	39	12494	10316	42598486
Incorrect dose administered	61.77	20.19	77	12456	52897	42555905
Acquired gene mutation	55.73	20.19	20	12513	1560	42607242
Non-small cell lung cancer metastatic	55.14	20.19	17	12516	826	42607976
Erythema dyschromicum perstans	54.51	20.19	8	12525	3	42608799
Pleural effusion	50.32	20.19	97	12436	97069	42511733
Vomiting	43.27	20.19	184	12349	289539	42319263
Paronychia	42.34	20.19	22	12511	4233	42604569
Interstitial lung disease	41.43	20.19	79	12454	78383	42530419
Skin toxicity	38.49	20.19	24	12509	6525	42602277
Neoplasm progression	36.78	20.19	44	12489	28956	42579846
Acne	36.43	20.19	31	12502	13613	42595189
Gastrointestinal perforation	35.71	20.19	20	12513	4466	42604336
Product use in unapproved indication	35.12	20.19	6	12527	184450	42424352
Pneumoperitoneum	34.79	20.19	16	12517	2362	42606440
Malignant pleural effusion	34.51	20.19	15	12518	1940	42606862
Metastases to meninges	34.46	20.19	15	12518	1946	42606856
Rash pustular	32.12	20.19	21	12512	6194	42602608
Pneumothorax	28.67	20.19	35	12498	23508	42585294
Metastases to lung	28.56	20.19	25	12508	11399	42597403
Metastases to liver	27.98	20.19	29	12504	16297	42592505
Nausea	27.53	20.19	205	12328	396594	42212208
Non-small cell lung cancer	26.17	20.19	17	12516	4957	42603845
Condition aggravated	26.10	20.19	23	12510	260731	42348071
Product dose omission issue	23.56	20.19	8	12525	154357	42454445
Metastases to bone	23.06	20.19	25	12508	14784	42594018
Lung adenocarcinoma	22.72	20.19	16	12517	5323	42603479
Failure to thrive	22.32	20.19	20	12513	9402	42599400
Pneumonitis	21.99	20.19	42	12491	41676	42567126
Toxicity to various agents	21.98	20.19	21	12512	229115	42379687
Anaemia	21.83	20.19	149	12384	280129	42328673
Blood bilirubin increased	21.62	20.19	42	12491	42210	42566592
Therapy partial responder	21.57	20.19	28	12505	19993	42588809
COVID-19	21.56	20.19	4	12529	115944	42492858
Growth of eyelashes	20.97	20.19	5	12528	90	42608712
Bronchial fistula	20.78	20.19	6	12527	232	42608570
Lung cancer metastatic	20.26	20.19	12	12521	2974	42605828

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
Disease progression	709.18	20.48	463	17946	243571	110327319
Malignant neoplasm progression	676.40	20.48	398	18011	174169	110396721
Drug resistance	624.75	20.48	263	18146	56111	110514779
Dermatitis acneiform	496.34	20.48	151	18258	12544	110558346
Rash	457.61	20.48	618	17791	820346	109750544
Diarrhoea	397.63	20.48	690	17719	1138815	109432075
Death	349.45	20.48	500	17909	698369	109872521
EGFR gene mutation	251.02	20.48	48	18361	522	110570368
Acquired gene mutation	175.77	20.48	48	18361	2706	110568184
Metastases to central nervous system	164.71	20.48	79	18330	22738	110548152
Dehydration	144.73	20.48	204	18205	279307	110291583
Paronychia	143.93	20.48	58	18351	11023	110559867
Erythema dyschromicum perstans	130.27	20.48	21	18388	73	110570817
Rash pustular	116.21	20.48	52	18357	12777	110558113
Metastases to meninges	99.59	20.48	36	18373	5092	110565798
Dry skin	95.24	20.48	103	18306	107550	110463340
Pleural effusion	89.35	20.48	128	18281	177581	110393309
Skin toxicity	85.64	20.48	41	18368	11742	110559148
Therapy partial responder	80.47	20.48	59	18350	37002	110533888
Decreased appetite	79.40	20.48	215	18194	475631	110095259
Malignant transformation	76.43	20.48	22	18387	1503	110569387
Metastases to lung	74.62	20.48	47	18362	23016	110547874
Interstitial lung disease	68.02	20.48	99	18310	139235	110431655
Neoplasm progression	64.59	20.48	66	18343	64529	110506361
Multiple-drug resistance	64.02	20.48	35	18374	13200	110557690
Non-small cell lung cancer metastatic	61.11	20.48	18	18391	1334	110569556
Acne	58.78	20.48	47	18362	33473	110537417
Pneumonitis	55.38	20.48	66	18343	76465	110494425
Metastases to bone	55.04	20.48	44	18365	31328	110539562
Growth of eyelashes	53.01	20.48	11	18398	186	110570704
Metastases to liver	50.41	20.48	44	18365	35342	110535548
Trichiasis	50.22	20.48	10	18399	136	110570754
Non-small cell lung cancer	49.85	20.48	25	18384	7910	110562980
Naevoid melanoma	49.58	20.48	7	18402	6	110570884
Infusion related reaction	48.49	20.48	4	18405	381158	110189732
Lung adenocarcinoma	48.31	20.48	26	18383	9505	110561385
Arthralgia	47.86	20.48	36	18373	779596	109791294
Pneumothorax	46.53	20.48	42	18367	35243	110535647
Anaemia	46.38	20.48	197	18212	546889	110024001
Gastrointestinal perforation	45.40	20.48	23	18386	7433	110563457
Malignant pleural effusion	44.93	20.48	19	18390	4074	110566816
Drug hypersensitivity	43.50	20.48	11	18398	454079	110116811
Ulcerative keratitis	42.15	20.48	19	18390	4747	110566143
Joint swelling	41.90	20.48	11	18398	442834	110128056
Xerosis	41.33	20.48	14	18395	1635	110569255
Nausea	39.65	20.48	345	18064	1235345	109335545
Condition aggravated	38.93	20.48	39	18370	734797	109836093
Pneumoperitoneum	38.82	20.48	17	18392	3967	110566923
Corneal disorder	38.64	20.48	15	18394	2582	110568308
Weight increased	38.62	20.48	11	18398	419633	110151257
Blood bilirubin increased	38.54	20.48	55	18354	75917	110494973
Metastases to pleura	38.26	20.48	14	18395	2049	110568841
Embolism	37.78	20.48	27	18382	16262	110554628
Pneumatosis intestinalis	37.01	20.48	21	18388	8508	110562382
Nasopharyngitis	36.91	20.48	10	18399	394351	110176539
Hepatotoxicity	36.83	20.48	49	18360	63351	110507539
Proteinuria	36.61	20.48	39	18370	39979	110530911
Arthropathy	36.61	20.48	3	18406	287519	110283371
Alopecia scarring	36.01	20.48	8	18401	189	110570701
Pulmonary embolism	34.76	20.48	96	18313	214378	110356512
Gene mutation	34.61	20.48	15	18394	3414	110567476
Skin fissures	34.01	20.48	30	18379	24428	110546462
Blepharitis	33.56	20.48	16	18393	4536	110566354
Aspartate aminotransferase increased	32.54	20.48	78	18331	159858	110411032
Pyogenic granuloma	32.50	20.48	9	18400	534	110570356
Vomiting	32.18	20.48	260	18149	910415	109660475
Performance status decreased	31.82	20.48	18	18391	7248	110563642
Corneal perforation	31.57	20.48	10	18399	946	110569944
Asthma	30.81	20.48	3	18406	250288	110320602
Sinusitis	30.79	20.48	6	18403	296682	110274208
Metastasis	29.66	20.48	18	18391	8249	110562641
Skin disorder	29.39	20.48	36	18373	42877	110528013
Non-small cell lung cancer stage IV	28.98	20.48	7	18402	241	110570649
Wound	28.36	20.48	3	18406	234434	110336456
Drug eruption	27.44	20.48	39	18370	53620	110517270
Laryngeal papilloma	26.76	20.48	4	18405	7	110570883
Hair texture abnormal	26.44	20.48	13	18396	3941	110566949
Squamous cell carcinoma	26.38	20.48	23	18386	18440	110552450
Alanine aminotransferase increased	25.66	20.48	78	18331	183695	110387195
COVID-19	25.33	20.48	5	18404	245055	110325835
Hair growth abnormal	24.77	20.48	12	18397	3525	110567365
Respiratory failure	24.30	20.48	85	18324	215247	110355643
Mobility decreased	24.22	20.48	5	18404	237417	110333473
Pneumopericardium	23.80	20.48	6	18403	247	110570643
Overdose	23.69	20.48	5	18404	233789	110337101
Product use in unapproved indication	23.36	20.48	24	18385	447353	110123537
Blood alkaline phosphatase increased	23.13	20.48	42	18367	70893	110499997
Lymphangiosis carcinomatosa	22.28	20.48	10	18399	2472	110568418
Toxicity to various agents	21.64	20.48	29	18380	480526	110090364
Failure to thrive	21.62	20.48	18	18391	13556	110557334
Haemoglobin decreased	21.35	20.48	90	18319	248637	110322253
Hyponatraemia	21.27	20.48	82	18327	217571	110353319
Wheezing	21.16	20.48	8	18401	255222	110315668
Carcinoembryonic antigen increased	21.05	20.48	10	18399	2814	110568076
Conjunctivitis	20.99	20.48	27	18382	33765	110537125
Sarcomatoid carcinoma	20.79	20.48	4	18405	45	110570845
Hypersensitivity	20.72	20.48	22	18387	403976	110166914
Abdominal discomfort	20.71	20.48	21	18388	393837	110177053
Neoplasm malignant	20.49	20.48	28	18381	37115	110533775

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	D000092004	Tyrosine 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 agent
CHEBI has role	CHEBI:37699	protein kinase inhibitor
CHEBI has role	CHEBI:22587	antiviral agent
CHEBI has role	CHEBI:50748	antipsoriatic
CHEBI has role	CHEBI:74440	epidermal growth factor receptor antagonist

Related Drugs by ATC class:

L01EB Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors 8 drugs

afatinibdacomitinibgefitinibicotiniblazertinibmobocertinibolmutinibosimertinib

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])	Mechanism action	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
ATP-binding cassette sub-family G member 2	Transporter	Q9UNQ0	ABCG2_HUMAN		IC50	6.89		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
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
Mitogen-activated protein kinase 9	Kinase	P45984	MK09_HUMAN		Kd	5.70		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
Lysine-specific histone demethylase 1A	Enzyme	O60341	KDM1A_HUMAN		IC50	4.45		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
Integrin-linked protein kinase	Kinase	Q13418	ILK_HUMAN		Kd	6.37		CHEMBL
Acyl-CoA dehydrogenase family member 11	Enzyme	Q709F0	ACD11_HUMAN		Kd	5.38		CHEMBL
Tyrosine-protein kinase CSK	Kinase	P41240	CSK_HUMAN		Kd	5.02		CHEMBL
dCTP pyrophosphatase 1	Enzyme	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
Epidermal growth factor receptor	Kinase		EGFR_MOUSE		IC50	7.71		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
DB00530	DRUGBANK_ID
337525	RXNORM
19073	MMSL
248186	MMSL
63773	MMSL
d05412	MMSL
008759	NDDF
008760	NDDF
414122006	SNOMEDCT_US
414123001	SNOMEDCT_US
426686007	SNOMEDCT_US
C1533491	UMLSCUI
D000069347	MESH_DESCRIPTOR_UI
8133	INN_ID
176870	PUBCHEM_CID
J4T82NDH7E	UNII
J4T82NDH7E	INXIGHT DRUGS

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	HUMAN PRESCRIPTION DRUG LABEL	1	31722-263	TABLET, FILM COATED	25 mg	ORAL	ANDA	25 sections
ERLOTINIB	HUMAN PRESCRIPTION DRUG LABEL	1	31722-264	TABLET, FILM COATED	100 mg	ORAL	ANDA	25 sections
ERLOTINIB	HUMAN PRESCRIPTION DRUG LABEL	1	31722-265	TABLET, FILM COATED	150 mg	ORAL	ANDA	25 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	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	59651-530	TABLET, FILM COATED	25 mg	ORAL	ANDA	25 sections
Erlotinib	Human Prescription Drug Label	1	59651-531	TABLET, FILM COATED	100 mg	ORAL	ANDA	25 sections
Erlotinib	Human Prescription Drug Label	1	59651-532	TABLET, FILM COATED	150 mg	ORAL	ANDA	25 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
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 Hydrochloride	Human Prescription Drug Label	1	72205-080	TABLET, FILM COATED	25 mg	ORAL	ANDA	24 sections
Erlotinib Hydrochloride	Human Prescription Drug Label	1	72205-081	TABLET, FILM COATED	100 mg	ORAL	ANDA	24 sections
Erlotinib Hydrochloride	Human Prescription Drug Label	1	72205-082	TABLET, FILM COATED	150 mg	ORAL	ANDA	24 sections